Evidence-Based Complementary and Alternative Medicine / 2018 / Article / Tab 1

Review Article

Kaempferia parviflora and Its Methoxyflavones: Chemistry and Biological Activities

Table 1

The biological activities of KP and its methoxyflavones.

ActivitiesExtracts/compoundsModelsDosesBiological activitiesRef.

Metabolism regulationEthanol KP extract: modified starch (3:7) for powder.
600 mg KP powder suspended in 40 mL water
Male ddY mice,
C2C12
45mg/kg/day,
10 μg/mL
Improve physical fitness performance and muscular endurance, increase PGC-1α and GS expression.[2]
Methanol KP extract dissolved in DMSO3T3-L13, 10, and 30 μg/mLActivate ATGL/HSL/PPARγ; increase lipolysis; decrease hypertrophy. [4]
Compound-1, -4 dissolved in DMSO3T3-L15, 15, and 30 μg/mL
50% ethanol extract was freeze-dried for powderC57BL6J miceHFD containing 0.5% or 1% KP extract for 7 weeksIncrease UCP1 expression, activate BAT.[18]
KP rhizome was pulverized with a Wonder Blender for KP powderTSOD mice1% and 3% KP powder in powder feed MFSuppress body weight increase, visceral fat accumulation, hypertension, hyperinsulinemia, glucose intolerance, peripheral neuropathy, lipid metabolism abnormalities, and insulin resistance.[19]
Ethyl acetate KP extract dissolved in DMSO3T3-L11 and 3 μg/mLUpregulate and PPARγ expression and downregulate GATA-2 expression. [20]
Compound-1, -4 dissolved in DMSO3T3-L13, 10, and 30 μM
Ethyl acetate KP extract was pulverized for KP powderTSOD mice,0.3% and 1% KP mix with MF for 8 weeksUpregulate PPARγ, UCP-1, and β3AR expression, accumulate triacylglycerol. [21]
Ethyl acetate KP extractBrown adipocytes1, 3, 10, and 30 μg/mL
70% ethanol KP extract dissolved in DMSOpC2C12 dC2C121, 3, and 10 μg/mLUpregulate the expression of GLUT4, MCT1, and PGC-1α [22]
Compound-6,-12,-15 dissolved in DMSO1 and 10μM
95% ethanol KP extractC57BL/6J200 mg/kg/day + HFD for 10 weeksIncrease PGC-1α, NRF-1, NRF-1, and Tfam expression [23]
L6 myotubes1 and 10 μg/mLUpregulate Sirt1/AMPK/PPARδ/
PGC-1α
95% ethanol KP extract was prepared by lyophilizationMale mice250 mg/kg KP extract in carboxymethyl cellulose for 7, 14, 21 daysIncrease CYP1A1, CYP1A2, CYP2B, and CYP2E1 activities, but CYP3A not change.[10]
60% ethanol KP extract mixed with dextrin for dried powdervolunteers100 mg in a pullulan capsuleIncrease whole-body energy expenditure.[24]

Anti-cancer95% ethanol KP extract was prepared for freeze-dried powder dissolved in DMSOU93720, 40, 60, 80, and 100 μg/mLInhibit proliferation and viability, increase apoptosis[25]
Methanol extract was partitioned into EtOAc-soluble fraction and methanol fractionB16 melanoma 4A51, 2.5, 5, and 10 μg/mLInhibit melanogenesis with IC50 = 9.6 and 4.9 μg/mL for methanol extract and EtOAc-soluble fraction[8]
Compound-3, -7, -10, and -11B16 melanoma 4A53,10, and 30 μMInhibit melanogenesis, suppress tyrosinase, TRP-1, and TRP-2 expression. [8, 26]
95% ethanol KP extract was prepared by lyophilization and dissolved in DMSOHeLa10, 50, and 100 μg/mLSuppress PI3K/AKT and MAPK signaling, inhibit migration and invasion, inhibit MMP-2 expression
Tincture, ethanol, or aqueous extract and Compound-1 dissolved in DMSOLLC-GA5-
COL 150
1, 5, 10, 50, and 100 μg/mLIncrease the accumulation of rhodamine 123 and daunorubicin[27]
Tincture, ethanol, or aqueous extract and Compound-1 dissolved in DMSOA5490.3-100 μg/mLAccumulate calcein and doxorubicin[28]
Ethanol extract (no details in preparation)aortic ring10 and 100 μg/mLAntagonize PE- or ACH-induced contraction.[29]

Vascular relaxation and cardioprotection95% ethanol KP extract dried under vacuum was dissolved in DMSOHUVEC1 and 10 μg/mLUpregulate the expression of eNOS and NO[30]
Dichloromethane fraction of KP ethanol extractmiddle-aged male rats100 mg/kg twice a day for 6 weeksDecrease contraction to phenylephrine, increase vasorelaxation to acetylcholine.[31]
95% ethanol KP extract was prepared by lyophilization suspended in 15% Tween-20aortic ring1, 10, and 100 μg/mLReduce superoxide anion[32]
95% ethanol KP extract was prepared by lyophilization suspended in 15% Tween-20
Compound-1 suspended in mixture (Tween 80: carboxy-methylcellulose sodium
salt: distilled water = 0.2: 0.2: 10)
aortic ring
middle-aged male rats
1, 10, and 100 μg/mL
22 mg/kg twice a day for 6 weeks
Upregulate cGMP-NO signaling, inhibit Ca2+ influx, and reduce ROS[33]
Upregulate eNOS and CSE expression and downregulate NO and H2S production. Low down plasma glucose and elevate HDLC levels.[34]
70% methanol extract was lyophilized to dried extract and was suspended in 50 % propylene glycol aqueous solutionDIC rats200 and 500 mg/kg for 7 successive daysprolong euglobulin lysis time, activate fibrinolysis[35]
Saline extract was filtered with Whatman filtered paper NO.1Swine heart12.5, 25, 50 and 100 mg/kgIncrease DFT and ULV, attenuate diastolic and systolic blood pressures.[36]
Saline extract was filtered with Whatman filtered paper NO.1normal rat heart12.5 and 100 mg/kgUpregulate cGMP-NO signaling and downregulate Ca2+ transient.[37]
Compound-6 dissolved in DMSOaortic ring10, 30, and 100 μMInduce vasorelaxation, activate NO-eGMP, increase K+ efflux, and attenuate Ca2+ influx.[38]
The water-soluble powder of KP suspended in Tween 80 (no details in preparation for dried powder)STZ-induced diabetic rats140, 280, and 420 mg/kgIncrease serum testosterone levels, sperm concentration, teste weight, and improve sexual performance.[39]

Sexual enhancementEthanol, hexane, and water extract prepared with polyvinylpyrrolidone (PVP)SD rats10, 20, and 40 mg/kg for 5 weeksOnly ethanol extract increases the blood flow to the testis.[40]
Ethanol extract was evaporated under reduced pressure until dried dissolved in DMSOPDE-5 from mouse lung50 μg/mLShow 62.63% inhibitory effect (IC50=12.24μg/mL)[7]
Compound-6 dissolved in DMSOPDE-5 from mouse lung10 μMIC50 = 10.64±2.09 μM[7]
Compound-1Isolated human cavernosum0.1 and 0.3 mMInhibit L-type Ca2+ channel, induce immobilization of Ca2+.[41]
Compound-4, -6AChE, BChE0.1 mg/mLInhibit the activity of AChE and BChE[6]

NeuroprotectionEthanol extract was dissolved in 2% Tween 80SD rats200 mg/kgIncrease NE, 5-HT, and DA production, increase GFAP and DPYSL2 expression.[42]
Compound-1, -4, -6Recombinant human BACE13, 30, 50, and 100 μg/mLinhibit BACE1 activity (IC50= 5.98×10-5M, 3.69×10-5M, and 4.95×10-5M, respectively)[43]
95% ethanol KP extract dissolved in 0.5% carboxymethycelluloseRats100 mg/kgImprove spatial memory and cells proliferation damaged by VPA.[44]
n-hexane extract was dried by nitrogen gas and dissolved in DMSORBL-2H3125, 250, 500 μg/mLInhibit degranulation; Inhibit the productions of TNFα, IL-4, and MCP-1.[45]

anti-allergy
anti-inflammation
anti-oxidation
Compound-6, -10 was dissolved in 50% ethanolRBL-2H350μMInhibit degranulation; Inhibit the productions of TNFα, IL-4, and MCP-1.
Inhibit PGE2 expression with IC50 value of 9.2 μg/mL.
[45, 46]
Ethanol extract was partitioned by hexane, chloroform, ethyl acetate, and water fractions and evaporated to dryness in vacuoRAW264.73, 10, 30, and 100 μg/mL
Compound-10RAW264.73, 10, 30, and 100 μMInhibit PGE2 and iNOS expression.[46]
Compound-10 dissolved in DMSORAW264.73, 10, 30, and 100 μg/mLInhibit the release of NO (IC50=16.1μM) and PGE2 (IC50=16.3μM), but inactive on TNFα release.[47]
Chloroform fraction and ethanol extract were evaporated to dryness in vacuoRAW264.71,3, 10, 30, and 100 μg/mLInhibit NO release with IC50 value of 8.4 and 8.1 μg/mL, respectively.[48]
Compound-3,-4,-6RAW264.73, 10, and 30 μg/mLInhibit NO release with IC50 value of 5.1, 4.6, and 8.7 μg/mL, respectively. Suppress iNOS and TNFα expression through SYK pathway, but not ERK and JNK pathways.[48]
50% ethanol extractRAW264.7, THP-1250, 500, and 1000 μg/mLDecrease NO levels, inhibit THP-1 adhesive activity and CAMs and inflammatory cytokines expression, and ameliorate oxidative stress.[49]
Compound-3Rat chondrocytes5, 10, and 20 μg/mLDecrease IL-1β, TNFα, and PGE2 levels, inhibit EP/cAMP/PKA signaling and β-catenin signaling, downregulate PERK-CHOP signaling, IRE1-JNK signaling, and GSK-3β expression, upregulate GRP78 and XBP1 expression.[5053]

Anti-osteoarthritisEthanol extractTSOD mice1% KP mix with MF for 12 weeksDecrease the thickness of subcutaneous fat layer and the infiltration of adipocytes into the dermis. Prevent against UVB-induced denaturation of collagenous fibers.[54]

Transdermal permeationEthanol extractEpididymis, BPH rat model100, 200, 500 μg/mLInhibit 5αR activity, decrease the weights of seminal vesicles and prostate.[55]

Miscellaneous sectionCompound-1, -4Epididymis50 μMInhibit 5αR activity with IC50 values of 46.6 μM and 48.7 μM, respectively. [55, 56]
70% methanol KP extract was prepared by lyophilization and dissolved in propylene glycolRat30, 60, and 100 mg/kgInhibit gastric ulcer induction, preserve gastric wall mucus, and exhibit no effects on gastric volume, acidity, and pH output.
95% ethanol extract was concentrated under reduced pressure5-week-old female hairless mice100 and 200 mg/kgSuppress UVB-induced MMP-2, -3, -9, -13 IL-1β, COX-2, NF-κB and c-Jun/c-Fos signaling.[57]
95% ethanol extract was concentrated under reduced pressure8-week-old female hairless mice200mg/kg/day for 24 weeks;Increase PGC-1α, ERRα, NRF-1, Tfam, E2F1, E2F2, FoxO3a, and mTOR expression; inhibit β-galactosidase, p16, p21, p53, pRb, and PI3K/AKT expression.[58]
95% ethanol extract was concentrated under reduced pressureHs68 cells1, 5, and 10 μg/mLIncrease PGC-1α, ERRα, NRF-1, Tfam, E2F1, E2F2, FoxO3a, and mTOR expression; inhibit β-galactosidase, p16, p21, p53, pRb, and PI3K/AKT expression. [58]