Research Breakdown on Kaempferia parviflora
Kaempferia parviflora (of the family Zingiberaceae) is a medicinal herb from Thailand that has purported usage as an aphrodisiac as well as general health promotion and stimulation. Other usages touted towards this herb include anti-depressive, anti-peptic ulcer, anti-inflammatory, anti-mutagenic and anti-allergic; it is sometimes referred to as Kra chai Dum or just as a Thai Ginseng (although taxonomically unrelated to Panax Ginseng). It is also sometimes referred to as 'Black Turmeric' due to sharing similar morphology to Curcuma Longa (source of dietary Turmeric), but these two compounds do not have similar bioactives and Kaempferia Parviflora does not have a curcumin content. It should be noted that sources of confusion here is Curcuma Parviflora, another herb with a similar name to both and Kra chai (rather than Kra Chai Dum) being used to refer to Boesenbergia rotunda.
Kaempferia parviflora is Thai Ginseng, and commonly called Black Turmeric (since the root is purplish-black underneath the outer layer) although not related to the common spice Turmeric
The three 'main' methoxyflavonoids 5,7-dimethoxyflavone (DMF) at 0.289%, 5,7,4'-trimethoxyflavone (TMF) at 0.0101% and 3,5,7,3',4'-pentamethoxyflavone (PMF) and a variety of other polymethoxyflavonoids
5-hydroxy-3,7-dimethoxyflavone at 0.0252%; a methoxyflavone that appears to be well reseached but is not one of the 'primary' three
Tetramethylluteolin at 0.0312% (derivative of Luteolin)
Tilianine (Methanolic fragment)
Ayanin at 0.0111%
Retusine at 0.0215%
Sesquiterpenoids 4αα-acetoxycadina-2,9-diene-1,8-dione and 1αα,3αα,4ββ-trihydroxy-9-cadinen-8-one
(2R,3R)-(−)-aromadendrin trimethyl ether (ethanol acetate fragment)
Tamarixetin 3-O-rutinoside (Methanolic fragment)
Syringetin 3-O-rutinoside (Methanolic fragment)
A thermostable lectin (sugar-binding protein) in the rhizome at 0.45%
In general, the 'Kaempferosides' appear to be unique to Kaempferia Parviflora but are not seen as the active ingredients. The methoxyflavones (flavones with methoxy groups attached to them) are seen as the main compounds, with the three known as DMF, TMF, and PMF being most commonly researched. This plant also appears to take standard bioflavonoid compounds and add either methoxy or methyl groups to their structures 5,7-dimethoxyflavone (DMF) had a Cmax of 0.78+/-0.11ug/mL at a Tmax of 0.76+/-0.4 hours with an AUC of 7.01+/-1.37h/ug/mL and a half-life of 5.85+/-1.72 hours; the overall bioavailability was determined to be 2.1%. 5,7,4'-trimethoxyflavone (TMF) had a Cmax of 0.88+/-0.11ug/mL at a Tmax of 0.85+/-0.40 hours with an AUC of 6.96+/-1.11h/ug/mL and a half-life of 5.04+/-1.10 hours; the bioavailability was 1.75%. 3,5,7,3',4'-pentamethoxyflavone (PMF) had a Cmax of 0.55+/-0.05ug/mL at a Tmax of 1.71+/-0.36 hours with an AUC of 3.65+/-0.63h/ug/mL and a half-life of 3.12+/-1.34 hours; the bioavailability was 3.32%.
The methoxyflavanoids appear to be poorly yet quickly absorbed with a relatively long half-life The rhizome extract appears to also inhibit the Xanthine Oxidase enzyme to a degree of 38% at 500mcg/mL concentration (underperforming the active control of Allopurinol at 10uM inhibiting 44%). Isolated methoxyflavones were tested on Xanthine Oxidase, and most showed weak inhibitory potential aside from 3',4',5,7-tetramethoxyﬂavone (36% at 400uM) and PMF (54% at 400uM), both still underperforming Allopurinol. TMF reached the brain with a Cmax of 1.43+/-0.58ug/g and a Tmax of 3.43+/-0.98 hours giving an overall neural AUC of 2.50+/-0.37ug/g/h, and DMF reached the brain with a Cmax of 0.96+/-0.37ug/g and a Tmax of 3.14+/-1.07 hours giving an overall neural AUC of 1.91+/-0.56ug/g/h.
Oral administration of Thai Ginseng is able to increase methoxyflavone concentrations in the brain, but slightly due to poor bioavailability Other compounds were either less effective or wholly ineffective. butyrylcholinesterase is inhibited most potently by DMF (84.6+/-1.3%) which neared the inhibitory potential of Galantamine as active control (95.5+/-1.4%); other notable inhibitions were TMF (46.2+/-1.4%) and 5-hydroxy-7,4'-dimethoxyﬂavone (22.8+/-0.1%).
Possesses cholinergic properties, but is unlikely to be practically significant due to the concentrations required (unless bioavailability is otherwise enhanced) The only human study to assess pain was a human study measuring the Rate of Perceived Exertion (RPE) on an exercise test, and found no effect with an acute bolus of 1.35g. This has been replciated elsewhere, but the hexane and aqueous extracts were ineffective at decreasing mounting and ejaculatory latency. Interestingly, one study using a higher dose (240mg/kg) noted inhibitory effects on aphrodisia in rats and one using 1g/kg noted no significant differences between groups.
Some evidence that 70mg/kg in rats (human dose of 11.2mg/kg ethanolic extract) is an aphrodisiac, while higher doses may be adverse; the increase in sexuality does not appear to be too remarkable in magnitude This was less protective than the active controls of CNQX and MK‐801, but of similar potency to Amino‐5‐phosphonovaleric acid (APV). Other methoxyflavones were either ineffective (TMF and 5‐Hydroxy‐3,7‐dimethoxyflavone) or less protective.
Moderate neuroprotection from one compound; practical relevance of oral supplementation unknown Concentrations of 100mcg/mL have been found to protect cardiac contracility after Ischemic injury, possibly secondary to anti-oxidant effects. which may be due to the DMF content which works via the endothelium and work via multiple pathways (NO-cGMP and COX) but mostly calcium influx inhibition and facilitating potassium efflux. Antioxidant effects are also attributed to methoxyflavones which have shown benefit in diabetic rats (high oxidant stress in endothelium) at an oral intake of 100mg/kg bodyweight; in this study which confirmed a DMF content, the supplemental Kaempferia almost normalized superoxide production (and indirectly preserved nitric oxide levels) in diabetic mice without influencing control mice. One other study in obese mice using 1% and 3% failed to note these effects, however.In vitro, Kaempferia Parviflora appears to have pancreatic lipase inhibitory properties with an IC50 of 487μg/mL in regards to the whole plant; isolated constituents with inhibitory potential include 5-hydroxy-3,7-dimethoxyflavone (IC50 291μg/mL), 5-hydroxy-3,7,4′-tri-methoxyflavone (IC50 536μg/mL), 5-hydroxy-7,4′-dimethoxyflavone (IC50 220μg/mL), and 5-hydroxy-7-methoxyflavone (IC50 291μg/mL). This appeared to mostly be due to 3,5,7,4′-tetramethoxyﬂavone and 3,5,7,3′,4′-pentamethoxyﬂavone, and despite not being a PPARγ agonist they induced activity of C/EBPβ and C/EBPδ. Dose dependent benefits to weight loss have been noted with 1% and 3% in another study using the same mouse model (TSOD) and again showed no significant effect in lean control mice.
Slight unremarkable anti-obese effects Improvements did not occur in the grip tests or tandem (gait) tests, and the benefits were attributed to an improvement in oxidative markers. When compared to the reference compound of Parthenolide (active component of Feverfew with an IC50 of 0.31μg/mL and 1.1μM) they underperformed. The mechanism of these three anti-inflammatory methoxyflavones appears to be mixed on ERK and JNK (inhibition) with tetramethylluteolin being a SYK inhibitor. This suppression of iNOS has been noted elsewhere, alongside a small suppression of COX-2 mRNA, where PGE2 production can be inhibited with an IC50 value of 9.2μg/mL (ethanolic extract) mostly due to 5-hydroxy-3,7,3',4'-tetramethoxyflavone.
General anti-inflammatory effects against macrophage activation from inflammatory stimuliSome methoxyflavones appear to be anti-allergic, as one in vitro study in RBL-2H3 Mast Cells noted that degranulation (a hallmark of allergic responses) was attenuated most potently by 5-hydroxy-3,7,3',4'-tetramethoxyﬂavone with an IC50 of 8uM followed by 5-hydroxy-7-methoxyﬂavone (20.6uM) and 5-hydroxy-7,4'-dimethoxyﬂavone (26uM). The overall rhizome ethanolic extract (concentrated methoxyflavones) had an IC50 of 10.9ug/mL, and it appears to be the most anti-allergic of the Zingiberaceae family according to one study.
Possible anti-allergic effects of unknown practical potency Another study in adult male rats (not castrated) also failed to note significant changes to LH and FSH, while testosterone trended to be nonsignificantly reduced; oddly, this study noted an increase in the weight of the prostate but not levator ani (mixed results on androgenicity indpendent of serum testosterone). A later study in sexually mature rats measuring the weight of the levator ani muscle (hypertrophy of this muscle correlated with overall androgenicity) found no significant improvemenet with supplementation at 70mg/kg, while exercise increased the weight slightly; this latter study did not measure serum testosterone. A lack of influence on the levator ani has been noted elsewhere at 70mg/kg. In a test of PDE5 inhibition, PMF failed to augment glyceryl trinitrate-induced relaxation while Viagra was effective. These results suggest the relaxing effects of PMF on the penis tissue are not mediated by NO, cGMP, nor potassium channels (common mechanisms of action for other drugs) and is unlikely to be a Rho-Kinase inhibitor, but appears to be a calcium channel inhibitor but may act by other (currently unknown) mechanisms. Other constituents of Kaempferia parviflora appear to be PDE5 inhibitors (similar to Viagra and Horny Goat Weed's Icariin). When the extract was tested by itself at 50ug/mL, Kaempferia parviflora rhizome was able to inhibit 62.63+/-7.17% of PDE5 inhibitory value (out of 41 tested herbs, only Caesalpinia sappan stem (60.23+/-1.81%), Senna surattensis leaf (65.08+/-0.78%), Acacia auriculaeformis leaf (73.66+/-4.87%) and Boesenbergia rotunda rhizome (40.86+/-3.94%) were similar); K.Parviflora had an IC50 of 12.24+/-0.99ug/mL with the ethanolic extract. Isolated compounds and their individual PDE5 IC50 values are 10.64+/-2.09ug/mL (DMF), 37.38+/-1.15ug/mL (2,7,4'-trimethoxyflavone), 16.32+/-1.93ug/mL (3,5,7-trimethoxyflavone), and 30.41+/-2.34ug/mL (PMF); all underperforming relative to Viagra.
Has a variety of mechanisms which indicate that Thai Ginseng is pro-erectile, but the practical significance of these pro-erectile effects have not been recorded in vivo (the one aphrodisiac study did not measure effects on the Penile Erection Index; PEI) DMF reached with a Cmax of 0.91+/-0.44ug/g at a Tmax of 2.86+/-1.07 hours giving an AUC of 1.90+/-0.62ug/g/h, and TMF reached with a Cmax of 1.10+/-0.43ug/g at a Tmax of 3.14+/-1.07 hours giving an AUC of 1.96+/-0.67ug/g/h. One study in rats given 70mg/kg bodyweight of the herb noted an increase in the weight of the seminal vesicles, epididymus, and levator ani muscles when paired with exercise; these results were more likely induced by exercise, as changes in the supplementation only group were minimal. This same oral dose was found to not significantly increase testicular weight when ethanolic, hexane, and water extracts were all tested despite the ethanolic group conferring aphrodisiac properties. An increase in blood flow through the spermatic artery was noted with this extract independent of changes in blood pressure or heart rate, which was deemed an acute effect. DMF reached with a Cmax of 3.85+/-1.45ug/g at a Tmax of 2.57+/-1.10 hours giving an AUC of 8.60+/-1.97ug/g/h, and TMF reached with a Cmax of 3.01+/-1.49ug/g at a Tmax of 2.64+/-1.38 hours giving an AUC of 7.83+/-0.33ug/g/h.
The three main methoxyflavones have been detected in the rat liver following oral administrationIn a preliminary test of protection of liver cells against D-GalN-induced toxicity, 5,3′-dihydroxy-3,7,4'-trimethoxyﬂavone appeared to be more effective than Silybin (a constituent of Milk Thistle) in protecting the cells, with an IC50 of 18.4μM relative to Silybin's 38.8μM. DMF reached with a Cmax of 1.33+/-0.49ug/g at a Tmax of 3.43+/-0.98 hours giving an AUC of 2.51+/-0.68ug/g/h, and TMF reached with a Cmax of 1.64+/-0.59ug/g at a Tmax of 3.43+/-0.98 hours giving an AUC of 3.01+/-0.85ug/g/h. DMF reached with a Cmax of 2.00+/-1.20ug/g at a Tmax of 1.20+/-0.19 hours giving an AUC of 2.17+/-0.31ug/g/h, and TMF reached with a Cmax of 1.41+/-0.58ug/g at a Tmax of 1.76+/-0.19 hours giving an AUC of 1.88+/-0.35ug/g/h.
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