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Design, modification of phyllanthone derivatives as anti-diabetic and cytotoxic agents
Design, modification of phyllanthone derivatives as anti-diabetic and cytotoxic agents
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Date
2020
Authors
Ngoc-Hong Nguyen
Van-Giau Vo
Hoang-Vinh-Truong Phan
Thanh-The Ngo
Jirapast Sichaem
Thi-Phuong Nguyen
Huu-Hung Nguyen
Duc-Dung Pham
Tien-Cong Nguyen
Van-Kieu Nguyen
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Abstract
Twelve benzylidene derivatives, one Baeyer-Villiger oxidative, six imine derivatives were successfully designed and synthesized from phyllanthone. In the search for potential new anti-diabetic agents, phyllanthone along with its benzylidene and oxidation analogues were evaluated for enzyme inhibition against α-glucosidase. In the benzylidene series, most analogues displayed stronger activity than the mother compound. 1c revealed the strongest activity, outperforming the acarbose positive control with an IC50 value of 19.59 μM. Phyllanthone and
its derivatives were then tested for cytotoxic activity against the K562 cell line. The imine analogues displayed the most powerful cytotoxic activity with 3c, 3d having IC50 values of 57.55 and 68.02 μM, respectively.
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Keywords
Phyllanthus (Phyllanthaceae),
phyllanthone derivatives,
α-glucosidase inhibition,
cytotoxic activity