Monday, July 25, 2011

Ephedra is Back! 'Mahabala', Featuring PEA, Ephedrine, Choline, Betaine & More, Is Nature's Hypolipidemic, Anti-Diabetic and Cardioprotective Fat Burning Stack

Image 1: Sida rhomboidea
leafs contain ephedrine and
other fat loss related alkaloids
(Tan Hoard Exports)
If you are a supplement producer, I suppose you will soon drop me an email to get the phone number of Ranjitsinh V. Devkar from the Division of Phytothrapeutics and Metabolic Endocrinology at the Department of Zoology of the M. S. University of Baroda in Gujarat, India. And, I must admit, if I had not always believed that "Nature knows best!", I would probably have been similarly surprised as some of you will have been, when they read the title of this blogpost - the 'ingredient profile' of Sida rhomboidea (also Sida rhombifolia), or  "Mahabala", a weed that is found in marshy places all across India and that has been used in Ayurvedic medicine for centuries to treat fever, heart disease, ever, heart diseases, burning sensations, urinary disorders, piles and all kinds of inflammation, looks like it had been printed on a non-FDA-approved (and thus potentially effective ;-) fat burner.
Figure 1: Alkaloid content of Sida rhomboidea extract (data adapted from Prakash. 1981)
If you have been following the exponential growth of the supplement market and the allegedly creative ideas the supp-designers had as far as fat burners were/are concerned, you will notice that, vasicinol and vasicinone aside, all the alkaloids, as well as choline and betaine Prakash et al. found in an extract from 5kg of Sida rhomboidea sound vaguely familiar.

Figure 2: Chemical structure
of the alkaloid vasicinone
(extracted from seeds of
Peganum Nigellastrum
by Zhang. 2009)
Vasicinol, vasicinone? What is that? Despite the fact that there is not much reliable data on the pharmacology of vasicinol and vasicinone, the two less well-known alkaloids in Sida rhomboidea, the available scientific data and information on their traditional use in Ayurveda suggests that these compounds, which are also present in other Ayurevedic herbs, exhibit hyopglycemic, as well as weak anti-acetylcholinesterase (Zhang. 2009) and bronchodilatory (Amin. 1959) effects. All three of these, which entail lower blood sugar levels, increased levels of acetylcholine and beta-adrenergic activity (which is the most likely explanation for bronchodilatory effect of the alkaloids), could synergistically help facilitate weightloss.
In view of this potent 'ingredient profile', it is no wonder that the addition of 1% of this natural fat loss wonder to the hypercaloric high fat diet (+58% more energy than low fat chow) of male C57BL/6J mice (6–8 weeks of age) staved off >25% of the 20-week weight gain (cf. figure 3) the unsupplemented HFD group experienced with respect to a low fat fed control group in the most recent of a whole series of rodent studies, Devkar et al. have conducted over the course the last years (Thounaojam. 2011).
Figure 3: Weight [in g] of mice during 20 weeks on control, high fat (HFD) and high fat diet with 1% Sida rhomboeidea extract (data adapted from Thounaojam. 2011)
From a health perspective, it may yet be even more important that the Mahabala supplement also prevented the "HFD induced increment in [...] plasma lipids and leptin, visceral adiposity and adipocyte hypertrophy" the scientists had observed in the unsupplemented group. The authors attribute these effects to the down-regulation of PPARĪ³2 and leptin gene expression that went hand in hand with an attenuation of food intake in the C57BL/6J mice.

Image 2: Mice on low fat (A), high fat (B)
and high fat diet + 1% Sida rhomboeidea
extract after 20 weeks (Thounaojam. 2011)
The decline in food intake, the scientists had already observed in previous studies , makes it quite difficult to give a definite number on the absolute amount of Sida rhomboeidea extract the mice consumed on a daily basis. It ranges from 25mg at the beginning of the study to ~13mg at the end and would translate into a human equivalent dose of 2mg/kg and 1mg/kg of Sida rhomboeidea extract per day. If the simple mathematical calculation that is solely based on the ratio of body surface to weight would suffice to reliably translate data from a rodent model to humans, an 80kg human being would thus have to consume somewhere between 80mg and 160mg of Mahabala per day to see similar effects.

Now, you may argue that, after all, this "wonder extract" turns out to be just another appetite suppressant. Yet, while Mahabala did affect the appetite of the laboratory animals, its profound in-vitro effects on pre-adipocytes differentiation and leptin release, as well as the previously mentioned changes in PPARĪ³2 and leptin gene expression, the scientists observed in the rodent model, suggest that the primary mechanisms for Mahabala's preventive effects against weight and fat gain (-56% less abdominal fat, -46% less epidididymal fat) is unrelated to the reduction in food intake.
Figure 4: Effect of Sida rhomboeidea extract (SR) and Rosiglitazone (ROS) on insulin tolerance in C57BL/6J mice after 16 weeks on low fat (LFD) or high fat diet (HFD) containing 1% (SR1) or 3% (SR2) SR or  0.05% ROS (data adated from Thounaojam. 2010)
Add to that its profound (as potent as the anti-diabetes drug Rosiglitazone) effects on insulin sensitivity (cf. figure 4) the researchers had observed in a previous study (Thounaojam. 2010) and remind yourself of the fact that not ephedrine, but its foolish and unnecessary abuse / overconsumption were responsible for the unfortunate deaths of a handful of people, the majority of whom had preexisting health problems (yes, being severely overweight is a health problem), and you will probably agree with Ranjitsinh V. Devkar and his colleagues who conclude that their findings "validate the potential application of SRLE as a therapeutic agent against obesity". And, if you asked me, I bet that it won't take long until you see the first Mahabala supplements hit the highly competitive fat loss market - despite the fact that an ephedrine-containing Ayurvedic herb probably ain't FDA compliant ;-)