Abstract：
:Tocotrienols are farnesylated benzopyran natural products that exhibit hypocholesterolemic activity in vitro and in vivo. The mechanism of their hypolipidemic action involves posttranscriptional suppression of HMG-CoA reductase by a process distinct from other known inhibitors of cholesterol biosynthesis. An efficient synthetic route to tocotrienols and their isolation from palm oil distillate using an improved procedure is presented. gamma-Tocotrienol exhibits a 30-fold greater activity toward cholesterol biosynthesis inhibition compared to alpha-tocotrienol in HepG2 cells in vitro. The synthetic (racemic) and natural (chiral) tocotrienols exhibit nearly identical cholesterol biosynthesis inhibition and HMG-CoA reductase suppression properties as demonstrated in vitro and in vivo.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Pearce BC,Parker RA,Deason ME,Qureshi AA,Wright JJdoi
10.1021/jm00098a002keywords:
subject
Has Abstractpub_date
1992-10-02 00:00:00pages
3595-606issue
20eissn
0022-2623issn
1520-4804journal_volume
35pub_type
杂志文章abstract：:Prevalence of drug-resistant bacteria has emerged to be one of the greatest threats in the 21st century. Herein, we report the development of a series of small molecular antibacterial agents that are based on the acylated reduced amide scaffold. These molecules display good potency against a panel of multidrug-resista...
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pub_type： 杂志文章
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pub_type： 杂志文章
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journal_title：Journal of medicinal chemistry
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