Abstract
Aster glehni F. Schmidt (AG), is a natural product known to have anti-obesity effects, but the mechanism underlying these effects is not well documented. We hypothesized that AG may have inhibitory effects on enzymes related to lipid accumulation. Herein, AG fractions were tested against HMG-CoA reductase (HMGR) and fatty acid synthase (FAS), two important enzymes involved in cholesterol and fatty acid synthesis, respectively. We found that dicaffeoylquinic acid (DCQA) methyl esters present in AG are largely responsible for the inhibition of HMGR and FAS. Since free DCQA is a major form present in AG, we demonstrated that a simple methylation of the AG extract could increase the overall inhibitory effects against those enzymes. Through this simple process, we were able to increase the inhibitory effect by 150%. We believe that our processed AG effectively modulates the HMGR and FAS activities, providing promising therapeutic potential for cholesterol- and lipid-lowering effects.
Highlights
IntroductionDietary supplements and herbal medicines derived from natural products purified or isolated from edible plants have always been popular due to their effectiveness and lower toxicity [1,2]
For the first time, we targeted two of the important enzymes, HMG-CoA reductase (HMGR) and fatty acid synthase (FAS), involved in cholesterol and lipid biosynthesis that may be important in regulating lipid metabolism as therapeutic targets of Aster glehni F. Schmidt (AG)
We identified 3,5-dicaffeoylquinic acid methyl ester (3) as the most active compound that is isolated from AG for inhibiting HMGR
Summary
Dietary supplements and herbal medicines derived from natural products purified or isolated from edible plants have always been popular due to their effectiveness and lower toxicity [1,2]. 50%–80% of the Asian and African population reportedly takes herbal medicines according to the World Health Organization (WHO) [3]. Due to their demonstrated safety and effectiveness, drugs derived from natural products comprise approximately a quarter of the total drug market [4]. Efforts to develop new drugs based on plant extracts or their derivatives are ongoing [5]. Schmidt (AG), a natural product mostly found on Ulleung Island, Korea.
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