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1.
Carbohydr Res ; 453-454: 10-18, 2017 Dec 01.
Article in English | MEDLINE | ID: mdl-29107814

ABSTRACT

Mycothiol cysteine ligase (MshC) is a key enzyme in the mycothiol (MSH) biosynthesis and a promising target for developing new anti-mycobacterial compounds. Herein, we report on the synthesis of substrate analogues, as potential inhibitors, for the MshC enzyme. The target molecules were synthesized employing a Schmidt glycosylation strategy using an enantiomerically pure inositol acceptor and 2-deoxy trichloroacetimidate glycosyl donors with glycosylation yields greater than 70% and overall yields >5%. The inositol acceptor was obtained via chiral resolution of (±)-myo-inositol.


Subject(s)
Bacterial Proteins/metabolism , Enzyme Inhibitors/chemical synthesis , Mycobacterium tuberculosis/enzymology , Cysteine/chemistry , Cysteine/metabolism , Enzyme Inhibitors/chemistry , Glycopeptides/chemistry , Glycopeptides/metabolism , Glycosylation , Inositol/chemistry , Inositol/metabolism , Stereoisomerism
2.
Ayu ; 32(4): 576-84, 2011 Oct.
Article in English | MEDLINE | ID: mdl-22661858

ABSTRACT

The whole plant of Stellaria media (family: Caryophyllaceae) has been tested for its antiobesity activity by using progesterone-induced obesity model in female albino mice. The effect of S. media on food consumption pattern, change in body weight, thermogenesis, lipid metabolism, and histology of fat pad. were examined. Methanolic and alcoholic extracts of the S. media were used in the study. Methanolic extract of S. media (MESM) have prevented the increase in body weight, adipose tissue weight and size, and upturned obesity and associated complications. MESM has also shown promising effects compared with alcoholic extract of S. media may be because of its multiple mechanisms. These findings suggest that antiobesity activity produced by MESM is because of its anorexic property mediated by saponin and flavonoid and partly of by its ß-sitosterol content. ß-Sitosterol in the plant extract was confirmed by thin-layer chromatography study. ß-sitosterol is plant sterol having structural similarity with dietary fat which do the physical competition in the gastrointestinal tract and reduces fat absorption. Before carrying in vivo activity detail pharmacognostic and phytochemical analysis of the extracts was carried out. The plant has shown the presence of saponin, flavonoids, steroids and triterpenoids, glycosides, and anthocynidine. By this study, it can be concluded that, MESM is beneficial in suppression of obesity induced by progesterone.

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