Novel protostane-type triterpenoids with inhibitory human carboxylesterase 2 activities
نویسندگان
چکیده
منابع مشابه
In vitro evaluation of inhibitory effects of antidiabetic and antihyperlipidemic drugs on human carboxylesterase activities.
Human carboxylesterase (CES) 1A is responsible for the biotransformation of angiotensin-converting enzyme (ACE) inhibitors such as imidapril and temocapril. Because antidiabetic or antihyperlipidemic drugs are often coadministered with ACE inhibitors in clinical pharmacotherapy, the inhibitory effect of these drugs on CES1A1 enzyme activity was investigated. In addition, the inhibitory effect o...
متن کاملStructure-Activity Relationships of Pentacyclic Triterpenoids as Potent and Selective Inhibitors against Human Carboxylesterase 1
Human carboxylesterase 1 (hCE1), one of the most important serine hydrolases distributed in liver and adipocytes, plays key roles in endobiotic homeostasis and xenobiotic metabolism. This study aimed to find potent and selective inhibitors against hCE1 from phytochemicals and their derivatives. To this end, a series of natural triterpenoids were collected and their inhibitory effects against hu...
متن کاملIn Vitro Evaluation of the Inhibitory Potential of Pharmaceutical Excipients on Human Carboxylesterase 1A and 2
Two major forms of human carboxylesterase (CES), CES1A and CES2, dominate the pharmacokinetics of most prodrugs such as imidapril and irinotecan (CPT-11). Excipients, largely used as insert vehicles in formulation, have been recently reported to affect drug enzyme activity. The influence of excipients on the activity of CES remains undefined. In this study, the inhibitory effects of 25 excipien...
متن کاملHighly regioselective glucosylation of alcoholic hydroxyls of protostane triterpenoids mediated by fungal biotransformation
Article history: Received 22 August 2016 Received in revised form 7 October 2016 Accepted 23 October 2016 Available online 24 October 2016 An efficient glucosylation of alcoholic hydroxyls in the structures of protostane triterpenoids catalyzed by fungus has been developed. Four protostanes 1–4 as the substrates have been transformed by Syncephalastrum racemosumAS 3.264 and generated correspond...
متن کاملAntioxidant and Inhibitory Activities of Enzymes Linked to Type II Diabetes Mellitus: The novel role of Chrysobalanus orbicularis leaf extract
Background: Chrysobalanus orbicularis is commonly used as food, the seeds as a spice for the popular pepper soup, and the leaves are traditionally utilized for managing type II diabetes mellitus (T2DM) in the Niger Delta area of Nigeria. Due to the limited scientific evidence on C. orbicularis, this study investigated its antioxidant and inhibitory properties against major enzymes linked to T2D...
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ژورنال
عنوان ژورنال: RSC Advances
سال: 2017
ISSN: 2046-2069
DOI: 10.1039/c7ra04841f