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In vitro Inhibitory Effect of Lanostane Triterpenoids of Kadsura coccinea on the Human Immunodeficiency Virus Type-1 Protease

By: Nguyen, Hong-Loan.
Contributor(s): Tran, Thu-Huyen Thi | Phuong, Thuong Thien.
Publisher: Mumbai Indian Journal of Pharmaceutical Science 2018Edition: Vol. 80 (04) July-August.Description: 755-761.Subject(s): PHARMACEUTICS | HIV-I protease inhibitor | Seco-coceinic acid F | Seco-lanostane trierpenoidOnline resources: Click here In: Indian journal of pharmaceutical sciencesSummary: Human immunodeficiency virus type-1 is the causative pathogen of acquired immunodeficiency syndrome and its protease is one of the primary targets for human immunodeficiency virus/acquired immune deficiency syndrome therapy. In this study, two seco-lanostane triterpenoids, 3,4-seco-9βH-lanost-4(28),7,24-trien-3-oic acid and 24(E)-3,4-seco-9βH-lanost-4(28),7,24-trien-3,26-dioic acid isolated from the roots of Kadsura coccinea, were found to significantly inhibit human immunodeficiency virus-1 protease, with IC50 values of 1.0±0.03 µM and 0.05±0.009 µM, respectively. Neither compound was toxic to human embryonic kidney 293T cells at concentrations effective against human immunodeficiency virus-1 protease. Our findings indicate that these triterpenoids are potential candidates for development of antihuman immunodeficiency virus/acquired immune deficiency syndrome drugs.
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Human immunodeficiency virus type-1 is the causative pathogen of acquired immunodeficiency syndrome and its protease is one of the primary targets for human immunodeficiency virus/acquired immune deficiency syndrome therapy. In this study, two seco-lanostane triterpenoids, 3,4-seco-9βH-lanost-4(28),7,24-trien-3-oic acid and 24(E)-3,4-seco-9βH-lanost-4(28),7,24-trien-3,26-dioic acid isolated from the roots of Kadsura coccinea, were found to significantly inhibit human immunodeficiency virus-1 protease, with IC50 values of 1.0±0.03 µM and 0.05±0.009 µM, respectively. Neither compound was toxic to human embryonic kidney 293T cells at concentrations effective against human immunodeficiency virus-1 protease. Our findings indicate that these triterpenoids are potential candidates for development of antihuman immunodeficiency virus/acquired immune deficiency syndrome drugs.

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