Advances in Pharmacological Sciences The latest articles from Hindawi Publishing Corporation © 2015 , Hindawi Publishing Corporation . All rights reserved. Anti-Inflammatory Effects of Heparin and Its Derivatives: A Systematic Review Tue, 12 May 2015 09:26:47 +0000 Background. Heparin, used clinically as an anticoagulant, also has anti-inflammatory properties. The purpose of this systematic review was to provide a comprehensive review regarding the efficacy and safety of heparin and its derivatives as anti-inflammatory agents. Methods. We searched the following databases up to March 2012: Pub Med, Scopus, Web of Science, Ovid, Elsevier, and Google Scholar using combination of Mesh terms. Randomized Clinical Trials (RCTs) and trials with quasi-experimental design in clinical setting published in English were included. Quality assessments of RCTs were performed using Jadad score and Consolidated Standards of Reporting Trials (CONSORT) checklist. Results. A total of 280 relevant studies were reviewed and 57 studies met the inclusion criteria. Among them 48 studies were RCTs. About 65% of articles had score of 3 and higher according to Jadad score. Twelve studies had a quality score > 40% according to CONSORT items. Asthma (), inflammatory bowel disease (), cardiopulmonary bypass (), and cataract surgery () were the most studied disease condition. Forty studies use unfractionated heparin (UFH) for intervention; the remaining studies use low molecular weight heparin (LMWH). Conclusion. Despite the conflicting results, heparin seems to be a safe and effective anti-inflammatory agent; although it is shown that heparin can decrease the level of inflammatory biomarkers and improves patient conditions, still more data from larger rigorously designed studies are needed to support use of heparin as an anti-inflammatory agent in clinical setting. However, because of the association between inflammation, atherogenesis, thrombogenesis, and cell proliferation, heparin and related compounds with pleiotropic effects may have greater therapeutic efficacy than compounds acting against a single target. Sarah Mousavi, Mandana Moradi, Tina Khorshidahmad, and Maryam Motamedi Copyright © 2015 Sarah Mousavi et al. All rights reserved. Antileishmanial Effect of 5,3′-Hydroxy-7,4′-dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo Studies Thu, 30 Apr 2015 17:28:05 +0000 Species of Picramnia genus are used in folk medicine to treat or prevent skin disorders, but only few species have been studied for biological activity and chemical composition. P. gracilis Tul. is a native species from Central and South America and although its fruits are edible, phytochemical analysis or medicinal uses of this species are not known. In the search of candidates to antileishmanial drugs, this work aimed to evaluate the antileishmanial activity of P. gracilis Tul. in in vitro and in vivo studies. Only ethanolic extract of fruits showed leishmanicidal activity. The majoritarian metabolite was 5,3′-hydroxy-7,4′-dimethoxyflavanone ether that exhibited high activity against L. (V.) panamensis (EC50 17.0 + 2.8 mg/mL, 53.7 μM) and low toxicity on mammalian U-937 cells, with an index of selectivity >11.8. In vivo studies showed that the flavanone administered in solution (2 mg/kg/day) or cream (2%) induces clinical improvement and no toxicity in hamsters with CL. In conclusion, this is the first report about isolation of 5,3′-hydroxy-7,4′-dimethoxyflavanone of P. gracilis Tul. The leishmanicidal activity attributed to this flavanone is also reported for the first time. Finally, the in vitro and in vivo leishmanicidal activity reported here for 5,3′-hydroxy-7,4′-dimethoxyflavanone offers a greater prospect towards antileishmanial drug discovery and development. Sara M. Robledo, Wilson Cardona, Karen Ligardo, Jéssica Henao, Natalia Arbeláez, Andrés Montoya, Fernando Alzate, Juan M. Pérez, Victor Arango, Iván D. Vélez, and Jairo Sáez Copyright © 2015 Sara M. Robledo et al. All rights reserved. Pandanus odoratissimus (Kewda): A Review on Ethnopharmacology, Phytochemistry, and Nutritional Aspects Mon, 22 Dec 2014 07:24:22 +0000 Pandanus odoratissimus Linn. (family: Pandanaceae) is traditionally recommended by the Indian Ayurvedic medicines for treatment of headache, rheumatism, spasm, cold/flu, epilepsy, wounds, boils, scabies, leucoderma, ulcers, colic, hepatitis, smallpox, leprosy, syphilis, and cancer and as a cardiotonic, antioxidant, dysuric, and aphrodisiac. It contains phytochemicals, namely, lignans and isoflavones, coumestrol, alkaloids, steroids, carbohydrates, phenolic compounds, glycosides, proteins, amino acids as well as vitamins and nutrients, and so forth. It is having immense importance in nutrition. A 100 g edible Pandanus pericarp is mainly comprised of water and carbohydrates (80 and 17 g, resp.) and protein (1.3 mg), fat (0.7 mg), and fiber (3.5 g). Pandanus fruits paste provides 321 kilocalories, protein (2.2 g), calcium (134 mg), phosphorus (108 mg), iron (5.7 mg), thiamin (0.04 mg), vitamin C (5 mg), and beta-carotene (19 to 19,000 μg) (a carotenoid that is a precursor to vitamin A). Pandanus fruit is an important source of vitamins C, B1, B2, B3, and so forth, usually prepared as a Pandanus floured drink. Traditional claims were scientifically evaluated by the various authors and the phytochemical profile of plant parts was well established. The methods for analytical estimations were developed. However, there is paucity of systematic compilation of scientifically important information about this plant. In the present review we have systematically reviewed and compiled information of pharmacognostic, ethnopharmacology, phytochemistry, pharmacology, nutritional aspects, and analytical methods. This review will enrich knowledge leading the way into the discovery of new therapeutic agents with improved and intriguing pharmacological properties. Prafulla P. Adkar and V. H. Bhaskar Copyright © 2014 Prafulla P. Adkar and V. H. Bhaskar. All rights reserved. Liver Fibrosis and Protection Mechanisms Action of Medicinal Plants Targeting Apoptosis of Hepatocytes and Hepatic Stellate Cells Thu, 20 Nov 2014 07:49:00 +0000 Following chronic liver injury, hepatocytes undergo apoptosis leading to activation of hepatic stellate cells (HSC). Consequently, activated HSC proliferate and produce excessive extracellular matrix, responsible for the scar formation. The pandemic trend of obesity, combined with the high incidence of alcohol intake and viral hepatitis infections, highlights the urgent need to find accessible antifibrotic therapies. Treatment strategies should take into account the versatility of its pathogenesis and act on all the cell lines involved to reduce liver fibrosis. Medicinal plants are achieving popularity as antifibrotic agents, supported by their safety, cost-effectiveness, and versatility. This review will describe the role of hepatocytes and HSC in the pathogenesis of liver fibrosis and detail the mechanisms of modulation of apoptosis of both cell lines by twelve known hepatoprotective plants in order to reduce liver fibrosis. Florent Duval, Jorge E. Moreno-Cuevas, Maria Teresa González-Garza, Carlos Rodríguez-Montalvo, and Delia Elva Cruz-Vega Copyright © 2014 Florent Duval et al. All rights reserved. Comparative Evaluation of Cytotoxic and Apoptogenic Effects of Several Coumarins on Human Cancer Cell Lines: Osthole Induces Apoptosis in p53-Deficient H1299 Cells Wed, 03 Sep 2014 09:24:59 +0000 Natural products are excellent resources for finding lead structures for the development of chemotherapeutic agents. Coumarins are a class of natural compounds found in a variety of plants. In this study, we evaluated the cytotoxic potential of coumarins isolated from Prangos ferulacea (L.) Lindl. in PC3, SKNMC, and H1299 (p53 null) human carcinoma cell lines. Osthole proved to be an outstanding potent cytotoxic agent especially against PC3 cells. Isoimperatorin exhibited moderate inhibitory effect against SKNMC and PC3 cell lines. Oxypeucedanin and braylin did not display any cytotoxic activity. In the next set of experiments, the apoptotic potentials of osthole and isoimperatorin were investigated. Induction of apoptosis by isoimperatorin was accompanied by an increase in activation of caspase-3, -8, and -9 in SKNMC cells and caspase-3 and -9 in PC3 cells. Moreover, isoimperatorin induced apoptosis by upregulating Bax and Smac/DIABLO genes in PC3 and SKNMC cells. Osthole induced apoptosis by downregulating antiapoptotic Bcl-2 in only PC3 cells and upregulating the proapoptotic genes Bax and Smac/DIABLO in PC3, SKNMC, and H1299 cells. The effects of osthole on H1299 cells are important because the loss of p53 has been associated with poor clinical prognosis in cancer treatment. Yalda Shokoohinia, Leila Hosseinzadeh, Maryam Alipour, Ali Mostafaie, and Hamid-Reza Mohammadi-Motlagh Copyright © 2014 Yalda Shokoohinia et al. All rights reserved. Development of an Antioxidant Phytoextract of Lantana grisebachii with Lymphoprotective Activity against In Vitro Arsenic Toxicity Thu, 05 Jun 2014 11:46:32 +0000 Phytochemicals have been presumed to possess prophylactic and curative properties in several pathologies, such as arsenic- (As-) induced immunosuppression. Our aim was to discover a lymphoprotective extract from Lantana grisebachii Stuck. (Verbenaceae) (LG). We assessed its bioactivity and chemical composition using cell-based assays. Fractions produced from a hexane extract acutely induced nitrite formation in T-activated cell cultures . Water extraction released a fraction lacking nitrite inducing activity in both lymphocyte types. Aqueous LG was found to be safe in proliferated and proliferating cells. The infusion-derived extract presented better antioxidant capacity in proportion to phenolic amount in lymphocytes (infusive LG-1i at 100 μg/mL), which protected them against in vitro As-induced lymphotoxicity . This infusive LG phytoextract contained  mg/g of phenolics, with 58.46% being flavonoids. Among the phenolics, the only predominant compound was 0.723 mg of chlorogenic acid per gram of dry plant, in addition to 10 unknown minor compounds. A fatty acid profile was assessed. It contained one-third of saturated fatty acids, one-third of ω9, followed by ω6 (~24%) and ω3 (~4%), and scarce ω7. Summing up, L. grisebachii was a source of bioactive and lymphoprotective compounds, which could counteract As-toxicity. This supports its phytomedical use and research in order to reduce As-related dysfunctions. Elio A. Soria, Patricia L. Quiroga, Claudia Albrecht, Sabina I. Ramos Elizagaray, Juan J. Cantero, and Guillermina A. Bongiovanni Copyright © 2014 Elio A. Soria et al. All rights reserved. Evaluation of the Potential Nephroprotective and Antimicrobial Effect of Camellia sinensis Leaves versus Hibiscus sabdariffa (In Vivo and In Vitro Studies) Wed, 14 May 2014 12:48:17 +0000 Green tea and hibiscus are widely consumed as traditional beverages in Yemen and some regional countries. They are relatively cheap and the belief is that they improve health state and cure many diseases. The aim of this study was to evaluate the potential protective and antibacterial activity of these two famous plants in vitro through measuring their antibacterial activity and in vivo through measuring nonenzymatic kidney markers dysfunction after induction of nephrotoxicity by gentamicin. Gram positive bacteria like MRSA (methicillin resistant Staphylococcus aureus) were isolated from hospitalized patients’ different sources (pus and wound) and Gram negative bacteria including E. coli and P. aeruginosa were used in vitro study. In addition, the efficacy of these plants was assessed in vivo through measuring nonenzymatic kidney markers including S. creatinine and S. urea. Green tea was shown antimicrobial activity against MRSA with inhibition zone 19.67 ± 0.33 mm and MIC 1.25 ± 0.00 mg/mL compared with standard reference (vancomycin) 18.00 ± 0.00 mg/mL. Hibiscus did not exhibit a similar effect. Both Hibiscus- and green tea-treated groups had nephroprotective effects as they reduced the elevation in nonenzymatic kidney markers. We conclude that green tea has dual effects: antimicrobial and nephroprotective. Doa’a Anwar Ibrahim and Rowida Noman Albadani Copyright © 2014 Doa’a Anwar Ibrahim and Rowida Noman Albadani. All rights reserved. Attenuation of Carcinogenesis and the Mechanism Underlying by the Influence of Indole-3-carbinol and Its Metabolite 3,3′-Diindolylmethane: A Therapeutic Marvel Thu, 08 May 2014 15:35:09 +0000 Rising evidence provides credible support towards the potential role of bioactive products derived from cruciferous vegetables such as broccoli, cauliflower, kale, cabbage, brussels sprouts, turnips, kohlrabi, bok choy, and radishes. Many epidemiological studies point out that Brassica vegetable protects humans against cancer since they are rich sources of glucosinolates in addition to possessing a high content of flavonoids, vitamins, and mineral nutrients. Indole-3-carbinol (I3C) belongs to the class of compounds called indole glucosinolate, obtained from cruciferous vegetables, and is well-known for tits anticancer properties. In particular, I3C and its dimeric product, 3,3′-diindolylmethane (DIM), have been generally investigated for their value against a number of human cancers in vitro as well as in vivo. This paper reviews an in-depth study of the anticancer activity and the miscellaneous mechanisms underlying the anticarcinogenicity thereby broadening its therapeutic marvel. V. L. Maruthanila, J. Poornima, and S. Mirunalini Copyright © 2014 V. L. Maruthanila et al. All rights reserved. Influence of Flunixin on the Disposition Kinetic of Cefepime in Goats Mon, 05 May 2014 14:00:43 +0000 The pharmacokinetic profile of cefepime (10 mg/kg b.w.) was studied following intravenous and intramuscular administration of cefepime alone and coadministered with flunixin (2.2 mg/kg b.w.) in goats. Cefepime concentrations in serum were determined by microbiological assay technique using Escherichia coli (MTCC 443) as test organism. Following intravenous injection of cefepime alone and in combination with flunixin, there are no significant changes in the pharmacokinetic parameters. Following intramuscular injection of cefepime alone and in combination with flunixin, the maximum serum concentration was significantly increased in flunixin coadministered group compared with cefepime alone. However, no significant changes were reported in other pharmacokinetic parameters. The result of in vitro protein binding study indicated that 15.62% of cefepime was bound to goat’s serum protein. The mean bioavailability was 92.66% and 95.27% in cefepime alone and coadministered with flunixin, respectively. The results generated from the present study suggest that cefepime may be coadministered with flunixin without change in dose regimen. Cefepime may be given intramuscularly at 12 h intervals to combat susceptible bacterial infections. Mohamed El-Hewaity Copyright © 2014 Mohamed El-Hewaity. All rights reserved. Response of Bone Resorption Markers to Aristolochia longa Intake by Algerian Breast Cancer Postmenopausal Women Wed, 30 Apr 2014 14:06:01 +0000 Aristolochia longa is widely used in traditional medicine in Algeria to treat breast cancer. The aim of the present study was to investigate the response of bone resorption markers to A. longa intake by Algerian breast cancer postmenopausal women. According to the A. longa intake, breast cancer patients were grouped into A. longa group (Al) and non-A. longa group (non-Al) . 32 women constituted the control group. Bone resorption markers (from urine) pyridinoline (PYD) and deoxypyridinoline (DPD) were determined by HPLC. Serum and urinary creatinine, uric acid, and urea were measured. 1 g of A. longa intake resulted in significant rise of renal serum markers and a pronounced increase of bone resorption markers. The intake of A. longa roots is detrimental for kidney function and resulted in high bone resorption, maybe due to the reduction in renal function caused by the aristolochic acids contained in the roots. Bachir Benarba, Boumedienne Meddah, and Aicha Tir Touil Copyright © 2014 Bachir Benarba et al. All rights reserved. Simple and Robust Analysis of Cefuroxime in Human Plasma by LC-MS/MS: Application to a Bioequivalence Study Thu, 24 Apr 2014 13:13:39 +0000 A simple, robust LC-MS/MS assay for quantifying cefuroxime in human plasma was developed. Cefuroxime and tazobactam, as internal standard (IS), were extracted from human plasma by methanol to precipitate protein. Separation was achieved on a Zorbax SB-Aq ( mm, 5 μm) column under isocratic conditions. The calibration curve was linear in the concentration range of 0.0525–21.0 μg/mL (). The accuracy was higher than 90.92%, while the intra- and interday precision were less than 6.26%. The extraction procedure provides recovery ranged from 89.44% to 92.32%, for both analyte and IS. Finally, the method was successfully applied to a bioequivalence study of a single 500 mg dose of cefuroxime axetil in 22 healthy Chinese male subjects under fasting condition. Bioequivalence was determined by calculating 90% Cls for the ratios of , AU, and AU values for the test and reference products, using logarithmic transformed data. The 90% Cls for the ratios of (91.4%104.2%), AU (97.4%110.9%), and AU (97.6%111.1%) values were within the predetermined range. It was concluded that the two formulations (test for capsule, reference for tablet) analyzed were bioequivalent in terms of rate and extent of absorption and the method met the principle of quick and easy clinical analysis. Xingjiang Hu, Mingzhu Huang, Jian Liu, Junchun Chen, and Jianzhong Shentu Copyright © 2014 Xingjiang Hu et al. All rights reserved. Susceptibility of Porphyromonas gingivalis and Streptococcus mutans to Antibacterial Effect from Mammea americana Thu, 24 Apr 2014 12:22:47 +0000 The development of periodontal disease and dental caries is influenced by several factors, such as microorganisms of bacterial biofilm or commensal bacteria in the mouth. These microorganisms trigger inflammatory and immune responses in the host. Currently, medicinal plants are treatment options for these oral diseases. Mammea americana extracts have reported antimicrobial effects against several microorganisms. Nevertheless, this effect is unknown against oral bacteria. Therefore, the aim of this study was to evaluate the antibacterial effect of M. americana extract against Porphyromonas gingivalis and Streptococcus mutans. For this, an experimental study was conducted. Ethanolic extract was obtained from seeds of M. americana (one oil phase and one ethanolic phase). The strains of Porphyromonas gingivalis ATCC 33277 and Streptococcus mutans ATCC 25175 were exposed to this extract to evaluate its antibacterial effect. Antibacterial activity was observed with the two phases of M. americana extract on P. gingivalis and S. mutans with lower MICs (minimum inhibitory concentration). Also, bactericidal and bacteriostatic activity was detected against S. mutans, depending on the concentration of the extract, while on M. americana extract presented only bacteriostatic activity against P. gingivalis. These findings provide important and promising information allowing for further exploration in the future. Alejandra Herrera Herrera, Luis Franco Ospina, Luis Fang, and Antonio Díaz Caballero Copyright © 2014 Alejandra Herrera Herrera et al. All rights reserved. The Therapeutic Potential of Medicinal Foods Thu, 17 Apr 2014 00:00:00 +0000 Pharmaceutical and nutritional sciences have recently witnessed a bloom in the scientific literature geared towards the use of food plants for their diversified health benefits and potential clinical applications. Health professionals now recognize that a synergism of drug therapy and nutrition might confer optimum outcomes in the fight against diseases. The prophylactic benefits of food plants are being investigated for potential use as novel medicinal remedies due to the presence of pharmacologically active compounds. Although the availability of scientific data is rapidly growing, there is still a paucity of updated compilation of data and concerns about the rationale of these health-foods still persist in the literature. This paper attempts to congregate the nutritional value, phytochemical composition, traditional uses, in vitro and in vivo studies of 10 common medicinal food plants used against chronic noncommunicable and infectious diseases. Food plants included were based on the criteria that they are consumed as a common food in a typical diet as either fruit or vegetable for their nutritive value but have also other parts which are in common use in folk medicine. The potential challenges of incorporating these medicinal foods in the diet which offers prospective opportunities for future drug development are also discussed. Nelvana Ramalingum and M. Fawzi Mahomoodally Copyright © 2014 Nelvana Ramalingum and M. Fawzi Mahomoodally. All rights reserved. Beneficial Effect of Cissus quadrangularis Linn. on Osteopenia Associated with Streptozotocin-Induced Type 1 Diabetes Mellitus in Male Wistar Rats Mon, 07 Apr 2014 13:57:14 +0000 Petroleum ether fraction of Cissus quadrangularis (PECQ) impact on the development of osteopenia in type 1 diabetic rat model has been evaluated. Diabetic rats were treated orally with two doses of PECQ. Another group of diabetic rats were treated with subcutaneous injection of synthetic human insulin. The cortical and trabecular bone thickness and bone strength were significantly decreased in diabetic rats. Treatment with two doses of PECQ significantly prevented these changes in diabetic rats. However, PECQ treatment (two doses) did not alter the glycemic levels in these diabetic rats. Increased levels of serum alkaline phosphatase (ALP), tartrate-resistant acid phosphatase (TRAP), and hydroxyproline were noted in diabetic rats when compared to normal control rats. The two doses of PECQ treatment further improved the serum ALP levels and significantly decreased the serum levels of TRAP and hydroxyproline. The effects of PECQ treatment on histological, biomechanical, and biochemical parameters are comparable to those of insulin. Since PECQ improves the bone health in hyperglycemic conditions by enhancing the cortical and trabecular bone growth and altering the circulating bone markers, it could be used as an effective therapy against diabetes-associated bone disorders. Srinivasa Rao Sirasanagandla, Sreedhara Ranganath Pai Karkala, Bhagath Kumar Potu, and Kumar M.R. Bhat Copyright © 2014 Srinivasa Rao Sirasanagandla et al. All rights reserved. Effects of Melatonin and Epiphyseal Proteins on Fluoride-Induced Adverse Changes in Antioxidant Status of Heart, Liver, and Kidney of Rats Wed, 26 Mar 2014 07:25:25 +0000 Several experimental and clinical reports indicated the oxidative stress-mediated adverse changes in vital organs of human and animal in fluoride (F) toxicity. Therefore, the present study was undertaken to evaluate the therapeutic effect of buffalo (Bubalus bubalis) epiphyseal (pineal) proteins (BEP) and melatonin (MEL) against F-induced oxidative stress in heart, liver, and kidney of experimental adult female rats. To accomplish this experimental objective, twenty-four adult female Wistar rats (123–143 g body weights) were divided into four groups, namely, control, F, F + BEP, and F + MEL and were administered sodium fluoride (NaF, 150 ppm elemental F in drinking water), MEL (10 mg/kg BW, i.p.), and BEP (100 µg/kg BW, i.p.) for 28 days. There were significantly high levels of lipid peroxidation and catalase and low levels of reduced glutathione, superoxide dismutase, glutathione reductase, and glutathione peroxidase in cardiac, hepatic, and renal tissues of F-treated rats. Administration of BEP and MEL in F-treated rats, however, significantly attenuated these adverse changes in all the target components of antioxidant defense system of cardiac, hepatic, and renal tissues. The present data suggest that F can induce oxidative stress in liver, heart, and kidney of female rats which may be a mechanism in F toxicity and these adverse effects can be ameliorated by buffalo (Bubalus bubalis) epiphyseal proteins and melatonin by upregulation of antioxidant defense system of heart, liver, and kidney of rats. Vijay K. Bharti, R. S. Srivastava, H. Kumar, S. Bag, A. C. Majumdar, G. Singh, S. R. Pandi-Perumal, and Gregory M. Brown Copyright © 2014 Vijay K. Bharti et al. All rights reserved. Evaluation of GABAergic Transmission Modulation as a Novel Functional Target for Management of Multiple Sclerosis: Exploring Inhibitory Effect of GABA on Glutamate-Mediated Excitotoxicity Thu, 20 Mar 2014 17:56:24 +0000 Multiple sclerosis (MS) is an autoimmune inflammatory disease of the central nervous system (CNS) where the communication ability of nerve cells in the brain and spinal cord with each other gets impaired. Some current findings suggest the role of glutamate excitotoxicity in the development and progression of MS. An excess release of glutamate leads to the activation of ionotropic and metabotropic receptors, thus resulting in accumulation of toxic cytoplasmic Ca2+ and cell death. However, it has been observed that gamma-aminobutyric acid-A (GABAA) receptors located in the nerve terminals activate presynaptic Ca2+/calmodulin-dependent signaling to inhibit depolarization-evoked Ca2+ influx and glutamate release from isolated nerve terminals, which suggest a potential implication of GABAA receptor in management of MS. With this proof of concept, we tried to explore the potential of selective GABAA receptor agonists or positive allosteric modulators (diazepam and phenobarbitone sodium) and GABAA level enhancer (sodium valproate) for management of MS by screening them for their activity in experimental autoimmune encephalomyelitis (EAE) model in rats and cuprizone-induced demyelination model in mice. In this study, sodium valproate was found to show the best activity in the animal models whereas phenobarbitone sodium showed moderate activity. However, diazepam was found to be ineffective. Ankit A. Gilani, Ranjeet Prasad Dash, Mehul N. Jivrajani, Sandeep Kumar Thakur, and Manish Nivsarkar Copyright © 2014 Ankit A. Gilani et al. All rights reserved. Evaluation of Cytotoxicity and Antifertility Effect of Artemisia kopetdaghensis Mon, 10 Mar 2014 09:51:26 +0000 To date, there is no report on safety of Artemisia Kopetdaghensis. This study aimed to determine the possible undesirable effects of A. Kopetdaghensis on reproduction of female rats. The pregnant rats were treated (i.p.) with vehicle or 200 and 400 mg/kg of A. Kopetdaghensis hydroalcoholic extract from the 2nd to 8th day of pregnancy. Then, number and weight of neonates, duration of pregnancy, and percent of dead fetuses were determined. Also, cytotoxicity of this plant was tested using fibroblast (L929) and ovary (Cho) cell lines. The A. Kopetdaghensis had no significant effect on duration of pregnancy, average number of neonates, and weight of neonates. However, administration of 200 and 400 mg/kg of the extract led to 30 and 44% abortion in animals, respectively. The extract at concentrations ≥200 g/mL significantly () inhibited the proliferation of L929 fibroblast cells. Regarding the Cho cells, the extract induced toxicity only at concentration of 800 g/mL (). Our results showed that continuous consumption of A. Kopetdaghensis in pregnancy may increase the risk of abortion and also may have toxic effect on some cells. Davood Oliaee, Mohammad Taher Boroushaki, Naiime Oliaee, and Ahmad Ghorbani Copyright © 2014 Davood Oliaee et al. All rights reserved. Inhibitory Potential of Five Traditionally Used Native Antidiabetic Medicinal Plants on α-Amylase, α-Glucosidase, Glucose Entrapment, and Amylolysis Kinetics In Vitro Sun, 02 Mar 2014 12:58:02 +0000 Five traditionally used antidiabetic native medicinal plants of Mauritius, namely, Stillingia lineata (SL), Faujasiopsis flexuosa (FF), Erythroxylum laurifolium (EL), Elaeodendron orientale (EO), and Antidesma madagascariensis (AM), were studied for possible α-amylase and α-glucosidase inhibitory property, glucose entrapment, and amylolysis kinetics in vitro. Only methanolic extracts of EL, EO, and AM (, , and  μg/mL, resp.) were found to significantly () inhibit α-amylase and were comparable to acarbose. EL, EO, AM, and SL extracts (5000 μg/mL) were found to significantly () inhibit α-glucosidase (between and % inhibition). Enzyme kinetic studies showed an uncompetitive and mixed type of inhibition. Extracts showed significant () glucose entrapment capacities (8 to 29% glucose diffusion retardation index (GDRI)), with SL being more active (29% GDRI) and showing concentration-dependent activity (29, 26, 21, 14, and 5%, resp.). Amylolysis kinetic studies showed that methanolic extracts were more potent inhibitors of α-amylase compared to aqueous extracts and possessed glucose entrapment properties. Our findings tend to provide justification for the hypoglycaemic action of these medicinal plants which has opened novel avenues for the development of new phytopharmaceuticals geared towards diabetes management. Carene M. N. Picot, A. Hussein Subratty, and M. Fawzi Mahomoodally Copyright © 2014 Carene M. N. Picot et al. All rights reserved. Antihyperglycemic Activity of Houttuynia cordata Thunb. in Streptozotocin-Induced Diabetic Rats Mon, 24 Feb 2014 08:59:53 +0000 Present study is an attempt to investigate plausible mechanism involved behind antidiabetic activity of standardized Houttuynia cordata Thunb. extract in streptozotocin-induced diabetic rats. The plant is used as a medicinal salad for lowering blood sugar level in North-Eastern parts of India. Oral administration of extract at 200 and 400 mg/kg dose level daily for 21 days showed a significant () decrease in fasting plasma glucose and also elevated insulin level in streptozotocin-induced diabetic rats. It also significantly reversed all the alterations in biochemical parameters, that is, total lipid profile, blood urea, creatinine, protein, and antioxidant enzymes in liver, pancreas, and adipose tissue of diabetic rats. Furthermore, we have demonstrated that the extract significantly reversed the expression patterns of various glucose homeostatic enzyme genes like GLUT-2, GLUT-4, and caspase-3 levels but did not show any significant effect on PPAR-γ protein expressions. Additionally, the extract positively regulated mitochondrial membrane potential and succinate dehydrogenase (SDH) activity in diabetic rats. The findings justified the antidiabetic effect of H. cordata which is attributed to an upregulation of GLUT-4 and potential antioxidant activity, which may play beneficial role in resolving complication associated with diabetes. Manish Kumar, Satyendra K. Prasad, Sairam Krishnamurthy, and Siva Hemalatha Copyright © 2014 Manish Kumar et al. All rights reserved. Antisecretory Action of the Extract of the Aerial Parts of Eremomastax speciosa (Acanthaceae) Occurs through Antihistaminic and Anticholinergic Pathways Thu, 20 Feb 2014 09:13:54 +0000 Objective. The objective of this study was to find out the possible antiulcer mechanism of action of Eremomastax speciosa. Method. Carbachol- and histamine-induced hypersecretion, associated with the pylorus ligation technique, were used in rats. Gastric mucosal ulceration, mucus production, pH, gastric volume, and acidity were measured. Results. Histamine and carbachol raised gastric acidity to 86.50 and 84.80 mEq/L, respectively, in the control rats, and the extracts (200 mg/kg) reduced gastric acidity to 34.60 and 39.00 mEq/L, respectively. Intraduodenal aqueous extract (400 mg/kg) in histamine- and carbachol-treated rats produced significant () decreases in acid secretion to 28.50 and 28.80 mEq/L, respectively, and 100 percent inhibition of gastric ulceration. Augmented histamine-induced gastric acid secretion (90.20 mEq/L) was significantly reduced to 52.60 and 27.50 mEq/L by the 200 and 400 mg/kg doses of the aqueous extract, respectively. The extract significantly reduced () the volume of gastric secretion and significantly increased mucus production. The ulcer inhibition potential of the extract significantly dropped to 25–44% (oral extract) and to 29–37% (duodenal extract) in carbachol/indomethacin-treated rats. Conclusion. The aqueous extract of E. speciosa has both cytoprotective and antisecretory effects. The antisecretory effect may involve a mechanism common to both cholinergic and histaminergic pathways. Amang André Perfusion, Paul V. Tan, Nkwengoua Ernestine, and Nyasse Barthélemy Copyright © 2014 Amang André Perfusion et al. All rights reserved. Effects of Resveratrol and Nebivolol on Isolated Vascular and Cardiac Tissues from Young Rats Thu, 20 Feb 2014 07:31:10 +0000 The mechanisms by which resveratrol and nebivolol induce vasodilation are not clearly understood. It has been postulated that both agents stimulate the production of nitric oxide; however, this remains to be conclusively established. The major aim of this study was to examine the vasodilatory and antiarrhythmic effects of both resveratrol and nebivolol and to provide further insight into possible mechanisms of action. Cardiac and vascular tissues were isolated from healthy male rodents. Results indicate that resveratrol and nebivolol decrease the action potential duration and induce mild vasorelaxation in aortic and mesenteric segments. Relaxation induced by resveratrol was prevented by the addition of verapamil, Nω-nitro-L-arginine-methyl ester, and 4-aminopyridine. This suggests that nebivolol and resveratrol act as putative antiarrhythmic and vasodilatory agents in vitro through possible indirect nitric oxide mechanisms. Candice Pullen, Fiona R. Coulson, and Andrew Fenning Copyright © 2014 Candice Pullen et al. All rights reserved. Development of Mass Spectrometry Selected Reaction Monitoring Method for Quantitation and Pharmacokinetic Study of Stepharine in Rabbit Plasma Thu, 20 Feb 2014 06:45:09 +0000 Highly sensitive liquid chromatography mass spectrometry method on triple quadrupole (QQQ) mass spectrometer was successfully applied for pharmacokinetic study of stepharine in rabbit plasma. Specific ion transitions of stepharine protonated precursor ion were selected and recorded in the certain retention time employing dynamic selected reaction monitoring mode. The developed method facilitated quantitative measurements of stepharine in plasma samples in linear range of five orders of magnitude with high accuracy and low standard deviation coefficient and pharmacokinetics parameters were calculated. The apparent volume of stepharine distribution (estimated as ratio of clearance to elimination rate constant, data not shown) allows us to assume that stepharine was extensively distributed throughout the body. Arthur T. Kopylov, Ksenia G. Kuznetsova, Olga M. Mikhailova, Andrey G. Moshkin, Vladimir V. Turkin, and Andrei A. Alimov Copyright © 2014 Arthur T. Kopylov et al. All rights reserved. Prophylactic Role of Averrhoa carambola (Star Fruit) Extract against Chemically Induced Hepatocellular Carcinoma in Swiss Albino Mice Wed, 19 Feb 2014 11:39:22 +0000 Liver cancer remains one of the severe lethal malignancies worldwide and hepatocellular carcinoma (HCC) is the most common form. The current study was designed to evaluate the prophylactic role of the fruit of Averrhoa carambola (star fruit or Kamrak) on diethylnitrosamine- (DENA-) induced (15 mg/kg b.wt.; single i.p. injection) and CCl4-promoted (1.6 g/kg b.wt. in corn oil thrice a week for 24 weeks) liver cancer in Swiss albino mice. Administration of ACE was made orally at a dose of 25 mg/kg b.wt/day for 5 consecutive days and it was withdrawn 48 hrs before the first administration of DENA (preinitiational stage). CCl4 was given after 2 weeks of DENA administration. A cent percent tumor incidence was noted in carcinogen treated animals while ACE administration resulted in a considerable reduction in tumor incidence, tumor yield, and tumor burden. Further, ACE treatment brings out a significant reduction in lipid peroxidation () along with an elevation in the activities of enzymatic antioxidants (superoxide dismutase, , and catalase, ), nonenzymatic antioxidant (reduced glutathione, ), and total proteins () when compared to the carcinogen treated control. These results demonstrate that ACE prevents the DENA/CCl4 induced adverse physical and biochemical alterations during hepatic carcinogenesis in mice. This study suggests the prophylactic role of Averrhoa carambola against hepatocellular carcinoma in mice; therefore, it could be employed for the further screening as a good chemopreventive natural supplement against cancer. Ritu Singh, Jyoti Sharma, and P. K. Goyal Copyright © 2014 Ritu Singh et al. All rights reserved. Trapa bispinosa Roxb.: A Review on Nutritional and Pharmacological Aspects Mon, 10 Feb 2014 12:29:59 +0000 Trapa bispinosa Roxb. which belongs to the family Trapaceae is a small herb well known for its medicinal properties and is widely used worldwide. Trapa bispinosa or Trapa natans is an important plant of Indian Ayurvedic system of medicine which is used in the problems of stomach, genitourinary system, liver, kidney, and spleen. It is bitter, astringent, stomachic, diuretic, febrifuge, and antiseptic. The whole plant is used in gonorrhea, menorrhagia, and other genital affections. It is useful in diarrhea, dysentery, ophthalmopathy, ulcers, and wounds. These are used in the validated conditions in pitta, burning sensation, dipsia, dyspepsia, hemorrhage, hemoptysis, diarrhea, dysentery, strangely, intermittent fever, leprosy, fatigue, inflammation, urethrorrhea, fractures, erysipelas, lumbago, pharyngitis, bronchitis and general debility, and suppressing stomach and heart burning. Maybe it is due to photochemical content of Trapa bispinosa having high quantity of minerals, ions, namely, Ca, K, Na, Zn, and vitamins; saponins, phenols, alkaloids, H-donation, flavonoids are reported in the plants. Nutritional and biochemical analyses of fruits of Trapa bispinosa in 100 g showed 22.30 and 71.55% carbohydrate, protein contents were 4.40% and 10.80%, a percentage of moisture, fiber, ash, and fat contents were 70.35 and 7.30, 2.05 and 6.35, 2.30 and 8.50, and 0.65 and 1.85, mineral contents of the seeds were 32 mg and 102.85 mg calcium, 1.4 and 3.8 mg Iron, and 121 and 325 mg phosphorus in 100 g, and seeds of Trapa bispinosa produced 115.52 and 354.85 Kcal of energy, in fresh and dry fruits, respectively. Chemical analysis of the fruit and fresh nuts having considerable water content citric acid and fresh fruit which substantiates its importance as dietary food also reported low crude lipid, and major mineral present with confirming good amount of minerals as an iron and manganese potassium were contained in the fruit. Crude fiber, total protein content of the water chestnut kernel, Trapa bispinosa are reported. In this paper, the recent reports on nutritional, phytochemical, and pharmacological aspects of Trapa bispinosa Roxb, as a medicinal and nutritional food, are reviewed. Prafulla Adkar, Amita Dongare, Shirishkumar Ambavade, and V. H. Bhaskar Copyright © 2014 Prafulla Adkar et al. All rights reserved. Hemozoin Inhibition and Control of Clinical Malaria Sun, 09 Feb 2014 13:16:00 +0000 Malaria has a negative impact on health and social and economic life of residents of endemic countries. The ultimate goals of designing new treatment for malaria are to prevent clinical infection, reduce morbidity, and decrease mortality. There are great advances in the understanding of the parasite-host interaction through studies by various scientists. In some of these studies, attempts were made to evaluate the roles of malaria pigment or toxins in the pathogenesis of malaria. Hemozoin is a key metabolite associated with severe malaria anemia (SMA), immunosuppression, and cytokine dysfunction. Targeting of this pigment may be necessary in the design of new therapeutic products against malaria. In this review, the roles of hemozoin in the morbidity and mortality of malaria are highlighted as an essential target in the quest for effective control of clinical malaria. Chibueze Peter Ihekwereme, Charles Okechukwu Esimone, and Edward Chieke Nwanegbo Copyright © 2014 Chibueze Peter Ihekwereme et al. All rights reserved. Effect of Hydroalcoholic Extract of Cydonia oblonga Miller (Quince) on Sexual Behaviour of Wistar Rats Tue, 04 Feb 2014 09:39:17 +0000 Cydonia oblonga Miller (quince) is regarded as a potent libido invigorator in Tib-e-Nabvi and Unani System of Medicine. This study was carried out to evaluate the aphrodisiac activity of the hydroalcoholic extract of the fruits of Cydonia oblonga Miller (quince) in Wistar rats. The extract was administered orally by gavage in the dose of 500 mg/kg and 800 mg/kg body weight per day as a single dose for 28 days. The observed parameters were mounting frequency, assessment of mating performance, and orientation activities towards females, towards the environment, and towards self. The results showed that after administration of the extract mounting frequency and the mating performance of the rats increased highly significantly . The extract also influenced the behaviour of treated animals in comparison to nontreated rats in a remarkable manner, making them more attracted to females. These effects were observed in sexually active male Wistar rats. Muhammad Aslam and Ali Akbar Sial Copyright © 2014 Muhammad Aslam and Ali Akbar Sial. All rights reserved. Embryotoxic and Teratogenic Effects of Norfloxacin in Pregnant Female Albino Rats Mon, 03 Feb 2014 13:12:59 +0000 This study was designed to investigate the possible developmental teratogenicity of norfloxacin in rats. Forty pregnant female rats were divided into four equal groups. Group A received norfloxacin in a dose of 500 mg/kgbwt/day orally from 6th to 15th day of gestation. Groups B and C received 1000 and 2000 mg/kgbwt/day orally for the same period, respectively; Group D behaved as control and received 0.5 mL distilled water orally for the same period. The dams were killed on 20th day of gestation and their fetuses were subjected to morphological, visceral, and skeletal examinations. Norfloxacin significantly decreased the number of viable fetuses, increased the number of resorbed fetuses, and induced retardation in growth of viable fetuses; some visceral and skeletal defects in these fetuses were seen and these effects were dose dependant. Conclusively, norfloxacin caused some fetal defects and abnormalities, so it is advisable to avoid using this drug during pregnancy. Mohamed Aboubakr, Mohamed Elbadawy, Ahmed Soliman, and Mohamed El-Hewaity Copyright © 2014 Mohamed Aboubakr et al. All rights reserved. Effects of Methanol Extract of Breadfruit (Artocarpus altilis) on Atherogenic Indices and Redox Status of Cellular System of Hypercholesterolemic Male Rats Thu, 30 Jan 2014 17:05:04 +0000 We investigated the effects of methanol extract of Artocarpus altilis (AA) on atherogenic indices and redox status of cellular system of rats fed with dietary cholesterol while Questran (QUE) served as standard. Biochemical indices such as total cholesterol (TC), triglycerides (TG), low- and high-density lipoproteins-cholesterol (LDL-C and HDL-C), aspartate and alanine aminotransferases (AST and ALT), lactate dehydrogenase (LDH), reduced glutathione, glutathione-s-transferase, glutathione peroxidase (GPx), catalase (CAT), superoxide dismutase (SOD), and lipid peroxidation (LPO) were assessed. Hypercholesterolemic (HC) rats had significantly increased relative weight of liver and heart. Dietary cholesterol caused a significant increase () in the levels of serum, hepatic, and cardiac TC by 110%, 70%, and 85%, LDL-C by 79%, 82%, and 176%, and TG by 68%, 96%, and 62%, respectively. Treatment with AA significantly reduced the relative weight of the organs and lipid parameters. There were beneficial increases in serum and cardiac HDL-C levels in HC rats treated with AA. In HC rats, serum LDH, ALT, and AST activities and levels of LPO were increased, whereas hepatic and cardiac SOD, CAT, and GPx were reduced. All biochemical and histological alterations were ameliorated upon treatment with AA. Extract of AA had protective effects against dietary cholesterol-induced hypercholesterolemia. Oluwatosin Adekunle Adaramoye and Olubukola Oyebimpe Akanni Copyright © 2014 Oluwatosin Adekunle Adaramoye and Olubukola Oyebimpe Akanni. All rights reserved. Teratogenic Effects of Coadministration of Fluoxetine and Olanzapine on Rat Fetuses Thu, 16 Jan 2014 11:21:23 +0000 Objective. Depression during pregnancy is a relatively common problem. Since little is known about the teratogenic effects of concomitant administration of fluoxetine and olanzapine during the organogenesis period, the aim of the present study was to evaluate the teratogenic effects of coadministration of fluoxetine and olanzapine on rat fetuses. Method. Forty-two pregnant rats were divided into seven groups, randomly. The first group received 0.5 mL of normal saline as the control. The second and third groups received fluoxetine at doses of 9 mg/kg and 18 mg/kg, respectively. Olanzapine was injected at 3 mg/kg and 6 mg/kg to the fourth and fifth groups, respectively. The sixth group received 9 mg/kg fluoxetine and 3 mg/kg olanzapine. Finally, the seventh group was administrated with fluoxetine and olanzapine at 18 mg/kg and 6 mg/kg, respectively. Drugs were injected intraperitoneally between day eight and day 15 of the pregnancy. On the 17th day of pregnancy, the fetuses were removed and micro-/macroscopically studied. Results. Fetuses of rats receiving high doses of these drugs showed a significant rate of cleft palate development, premature eyelid opening and torsion anomalies, compared to the control group (). It is concluded that these drugs can lead to teratogenicity, so their concomitant use during pregnancy should be avoided, or if necessary their doses must be decreased. Azam Bakhtiarian, Nasrin Takzare, Mehdi Sheykhi, Narges Sistany, Farahnaz Jazaeri, Mario Giorgi, and Vahid Nikoui Copyright © 2014 Azam Bakhtiarian et al. All rights reserved. The Genus Spilanthes Ethnopharmacology, Phytochemistry, and Pharmacological Properties: A Review Thu, 26 Dec 2013 09:43:41 +0000 Spilanthes spp. are popular, over-the-counter remedies; they are sold over the internet under various names and are widely used in traditional medicine in various cultures. This review will summarize the important reports on the ethnopharmacology, botany, phytochemistry, and pharmacological properties as described in the literature from recent years (1920 to 2013). Spilanthes spp. are used for more than 60 types of disorders. They are reported to contain a number of biologically active phytochemicals, although a large number of ethnopharmacological uses have been documented; only a few of these species have been investigated for their chemical and biological activities. The studies are carried out mainly on Spilanthes extracts and a few metabolites substantiate the uses of these plants in traditional medicine. Well-conducted pharmacological studies are still needed for several traditional indications, and the mechanisms of action by which the plant extracts and the active compounds exert their pharmacological effects remain to be studied. They are predominantly used as extracts in personal care products, traditional medicines, and the pharmaceutical and culinary areas. Suggestions are made regarding some of the possible mechanisms of action as to how the known compounds may exert their biological activity. Jayaraj Paulraj, Raghavan Govindarajan, and Pushpangadan Palpu Copyright © 2013 Jayaraj Paulraj et al. All rights reserved.