Advances in Pharmacological and Pharmaceutical Sciences

Proliferation is a cellular process strongly linked to the genesis of cancer. Natural substances with antiproliferative activities are currently potential alternatives in the treatment of cancers. Dacryodes edulis, for instance, is a medicinal plant traditionally used in the treatment of cancer. Scientific studies have reported the antioxidant activity of this plant. In addition, the presence of prostate cancer chemopreventive polyphenols was reported in D. edulis extracts. Therefore, this study was aimed to evaluate the effects of the aqueous extract of D. edulis leaves on cell proliferation induced by estradiol in ovariectomized female Wistar rats. In this regard, ovariectomized (OVX) rats were cotreated with estradiol valerate (E₂V) (0.75 mg/kg) and the aqueous extract of D. edulis leaves. Control groups received either the vehicle (sham-operated animals and the OVX control), E₂V (0.75 mg/kg) only, or E₂V (0.75 mg/kg) and tamoxifen (10 mg/kg). Treatments were administered orally for 3 consecutive days, and animals were sacrificed thereafter. Epithelial heights of the uterus and vagina were assessed. Uterine levels of total cholesterol and estradiol were determined as well. Results showed that the aqueous extract of D. edulis leaves reversed the effects of estradiol as it reduced uterine weight (), uterine (), and vaginal () epithelium heights. This antiproliferative effect of D. edulis was associated with reduced tissue (uterine) levels of estradiol (). These results suggest that the aqueous extract of D. edulis leaves could be a potential alternative treatment for proliferation-related diseases.

The study aimed to determine the phytochemicals and to assess the antibacterial activities of crude extracts of different parts of Calpurnia aurea against Staphylococcus aureus, Streptococcus pyogenes, Listeria monocytogenes, Escherichia coli O157 H:7, Salmonella typhi, and Campylobacter jejuni. The fresh and healthy leaves, barks, stems, and roots of the plant parts were collected, herbarium, dried, and grounded, and bioactive compounds were extracted by ethanol (99%) and water. Mass of crude extracts was determined by using the Whatman No. 1 filter paper and rotary evaporator. Major secondary metabolites were also screened using phytochemical screening tests. Antibacterial activities (inhibition zones, mm) and minimum inhibition concentrations (MIC) were evaluated using agar-well diffused methods and agar dilution methods, respectively. The antibiotics ciprofloxacin, amoxicillin, penicillin, and tetracycline were used as positive controls at concentrations of 0.1 mg/ml and 0.2 mg/ml, while distilled water was used as the negative control. All the crude extracts were tested triplet (3x) for antibacterial activities against selected bacterial strains with two different concentrations 25 and 50 mg/ml and analyzed to compare the mean ± standard deviation between triplets. The results revealed that ethanol extracts showed high crude mass extracts, antibacterial activities, and major secondary metabolites such as alkaloids, tennis, flavonoids, saponins, steroids, and phlobatannins compared with aqueous extracts. Among antibiotics used, penicillin showed resistance to S. aureus and E. coli O157 H:7. C. jejuni was found to be the most susceptible bacterium to ethanol extracts’ leaves, barks, and stems with MIC 3.125 mg/ml, whereas S. aureus was the least susceptible to all crude extracts. The study provided the traditional and scientific basis of Calpurnia aurea used against some bacterial diseases.

Introduction. Researchers usually use herbal combinations to explore and develop traditional medicine to obtain additional benefits in the treatment of diseases, including diabetes. This study aims to evaluate the hypoglycemic effect of the combination of Andrographis paniculata (Burm. f.) Wall ex Nees and Caesalpinia sappan Linn extract (APCSE) on diabetes-induced rats. There has not been sufficient research on this combination; however, single extract studies of these plants have been widely conducted. Materials and Methods. Male Sprague Dawley rats (160–200 g) were induced by injecting a low dose of streptozotocin (35 mg/kg BW) twice and fed with a high-fat diet containing 25% fat, whereas control animals received only standard feed. Rats were treated with APCSE at doses of 100 mg and 200 mg/kg BW for seven days and compared to the APE and CSE groups treated with the extract at 100 mg, respectively. For the control group, rats were treated with metformin with a dose of 250 mg/kg. The antihyperglycemic and antihyperlipidemic effects were determined by measuring blood glucose levels and lipid profiles (cholesterol, triglycerides, HDL, and LDL). To assess the impact of the extract on pancreatic and adipose tissue, the number of pancreatic beta cells and adipocytes was evaluated through histopathological and immunohistochemical study. Results and Discussion. In a nonfasting state, the blood glucose change in APCSE 200 mg was 18.65% and was significantly lower from the DM group. However, a single extract of APE and CSE showed lower fasting blood glucose levels compared to the combined extract. Lipid profiles show no significant differences in cholesterol levels between groups; however, all treatment groups, including metformin, showed higher triglyceride levels. The APE-treated group showed significantly lower HDL and LDL, whereas CSE only showed lower LDL. The β-cell number was significantly higher after treatment with single extract CSE. The CSE and the combined extract groups showed hyperplasia adipocytes. Conclusion. The combined extract of APCSE has a moderate antihyperglycemic effect; however, a single extract may have better potential than the combined extract.

ESKAPE pathogens, namely, Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter species, are responsible for a majority of all healthcare-acquired infections (HAI). The bacteria cause nosocomial infections in immunocompromised patients. Extracts from Callistemon viminalis have been shown to have antibacterial, antifungal, and anti-inflammatory activities. Tormentic acid congener, a pentacyclic triterpene saponin, was isolated from C. viminalis leaves. This study aimed to investigate the antibacterial effects of tormentic acid congener and leaf extracts on biofilm formation by A. baumannii, S. aureus, S. pyogenes, and P. aeruginosa. The antibacterial effects were determined by the microbroth dilution method, and ciprofloxacin was used as the standard antibacterial drug. Biofilm formation and detachment assays were performed using crystal violet staining. Production of extracellular polymeric DNA and polysaccharides from biofilms was also determined. Tormentic acid congener showed time-dependent antibacterial activity against P. aeruginosa with a MIC of 100 µg/ml and caused significant protein leakage. Antibacterial activity was found when tormentic acid congener was tested against both S. aureus and P. aeruginosa. The MICs were found to be 25 µg/ml and 12.5 µg/ml for P. aeruginosa and S. aureus cells, respectively. S. pyogenes was found to be susceptible to tormentic acid congener and the hydroethanolic extract with an MIC of 100 µg/ml and 25 µg/ml, respectively. A. baumannii was found not to be susceptible to the compound or the extracts. The compound and the extracts caused a significant decrease in the biofilm extracellular polysaccharide content of S. pyogenes. The extracts and tormentic acid congener caused detachment of biofilms and decreased the release of extracellular DNA and capsular polysaccharides from biofilms of P. aeruginosa and S. aureus. Tormentic acid congener and extracts, thus, have significant antibacterial and antibiofilm activities on these selected ESKAPE bacteria and can act as source lead compounds for the development of antibacterial triterpenoids.

This study examined the effectiveness of niosomes loaded with levofloxacin in treating Pseudomonas aeruginosa (American Type Culture Collection—ATCC 27853) infections in Sprague Dawley rats since these infections are becoming more common and resistant to treatment. Levofloxacin entrapped in niosomes was prepared using the thin-film hydration method and was assessed for in vitro release and stability. Three groups of six (6) animals were infected with a lethal dose of Pseudomonas aeruginosa via the intraperitoneal (Ip) route. At six (6) hours postinfection, the animals were treated with either drug-free niosomes (control), free levofloxacin (conventional), or levofloxacin trapped in niosomes (Ip) at a dose of 7.5 mg/kg/once daily. Blood was collected via tail snips on days 0, 1, 3, 5, 7, and 10 for complete blood counts and viable bacterial counts (CFU/μl). At day 10, the animals were sacrificed, and the kidney, liver, and spleen were harvested for bacterial counts. The niosomes showed a sustained drug release profile and were most stable at 4°C. All animals in the control group succumbed to the infection; one animal from the conventional group died, and all niosome treated animals survived at day 10. The mean lymphocyte count (×10⁹) was lower for the niosome (7.258 ± 1.773) versus conventional group (17.684 ± 10.008) () at day ten (10). Neutrophil counts (×10⁹) were lower for the niosome (2.563 ± 1.609) versus conventional (6.2 ± 6.548) () groups. Though CFUs in the bloodstream were comparable for both treatment groups, the niosome treated group showed a significant reduction of CFUs in the liver, kidney, and spleen versus the conventional group (1.33 ± 2.074) vs (5.8 ± 3.74) (), (1.5 ± 2.35) vs (9.6 ± 8.65) () and (3.8 4.71) vs (25.6 14.66) (), respectively. These findings indicate that niosome is promising as a drug delivery system in treating systemic infections, but further work using niosomes with surface modification is recommended.

Picralima nitida is a therapeutic herb used in ethnomedicine for the management of several disease conditions including diabetes. This study examined the potential palliative effect of aqueous seed extract of Picralima nitida (APN) on dyslipidemia, hyperglycemia, oxidative stress, insulin resistance, and the expression of some metabolic genes in high-fat high-fructose-fed rats. Experimental rats (2 months old) were fed a control diet or a high-fat diet with 25% fructose (HFHF diet) in their drinking water for nine weeks. APN was administered orally during the last four weeks. Anthropometric and antioxidant parameters, lipid profile, plasma glucose, and insulin levels and the relative expression of some metabolic genes were assessed. APN caused a significant decrease () in weight gained, body mass index, insulin resistance, plasma glucose, and insulin levels. High-density lipoprotein cholesterol level was significantly increased (), while triacylglycerol, cholesterol, low-density lipoprotein, cardiac index, atherogenic index, coronary artery index, and malondialdehyde levels in plasma and liver samples were also significantly decreased () by APN at all experimental doses when compared to the group fed with an HFHF diet only. APN also significantly () upregulated the relative expression of glucokinase, carnitine palmitoyltransferase-1 (CPT-1), and leptin at 400 mg/kg body weight when compared to the group fed with an HFHF diet only. This study showed that APN alleviated dyslipidemia, hyperglycemia, and oxidant effect associated with the intake of a high-fat high-fructose diet.