ABSTRACT
A series of new fluoroarene derivatives of artemisinin were prepared using Suzuki and Sonogashira cross-coupling reactions. An antifungal and antitumor activity was evaluated against opportunistic pathogen Fusarium oxysporum and Hela cancer cell line. All these derivatives have shown moderate to good activity.
Subject(s)
Artemisinins/chemistry , Artemisinins/pharmacology , Fluorobenzenes/chemistry , Fusarium/drug effects , Antifungal Agents/chemical synthesis , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Cell Proliferation/drug effects , Cell Survival/drug effects , Fluorobenzenes/pharmacology , HeLa Cells , Humans , Microbial Sensitivity Tests , Structure-Activity RelationshipABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: Through one-to-one interaction with the traditional healers, the present study has identified 15 medicinal plant species traditionally used as remedies to control diabetes. MATERIALS AND METHODS: The methanolic extracts were screened for their α-glucosidase inhibitory activity. Hypoglycemic activity was assessed following glucose, sucrose and starch tolerance test on normal and STZ induced diabetic rats. RESULTS: Ficus cunia extract had the highest α-glucosidase inhibitory potency with IC50 1.39±0.74 µg mL(-1) followed by Schima wallichi (IC50 1.43±0.20 µg mL(-1)) and Wendlandia glabrata (IC50 1.67±0.33 µg mL(-1)). In STZ induced diabetic rat model, F. cunia and W glabrata extracts reduced blood glucose concentration to near normal up to 14 days when administered 48 h after STZ. CONCLUSION: The present study supports the traditional use of some of these medicinal plants in anti-diabetic remedies. The present study contributes to evidence for use of traditional medicine.
