TY - DATA T1 - Semisynthesis of Mallotus B from Rottlerin: Evaluation of Cytotoxicity and Apoptosis-Inducing Activity PY - 2013/09/27 AU - Shreyans K. Jain AU - Anup S. Pathania AU - Samdarshi Meena AU - Rajni Sharma AU - Ashok Sharma AU - Baljinder Singh AU - Bishan D. Gupta AU - Shashi Bhushan AU - Sandip B. Bharate AU - Ram A. Vishwakarma UR - https://acs.figshare.com/articles/journal_contribution/Semisynthesis_of_Mallotus_B_from_Rottlerin_Evaluation_of_Cytotoxicity_and_Apoptosis_Inducing_Activity/2372668 DO - 10.1021/np400433g.s001 L4 - https://ndownloader.figshare.com/files/4012168 KW - Mallotus philippensis KW - cell morphology KW - G 1 phase KW - cell cycle arrest KW - HL KW - PC KW - IC 50 values KW - Mallotus B KW - cell division KW - semisynthetic preparation KW - prenylated dimeric phloroglucinol compound KW - cancer cell lines KW - mallotus B KW - Microscopic studies KW - HEPG KW - 16 μ M N2 - Mallotus B (2d) is a prenylated dimeric phloroglucinol compound isolated from Mallotus philippensis. There have been no reports on the synthesis or biological activity of this compound. In the present paper, a semisynthetic preparation of mallotus B is reported via base-mediated intramolecular rearrangement of rottlerin (1), which is one of the major constituents of M. philippensis. The homodimer “rottlerone” was also formed as one of the products of this base-mediated intramolecular reaction. Rottlerin (1), along with rottlerone (2c) and mallotus B (2d), was evaluated for cytotoxicity against a panel of cancer cell lines including HEPG2, Colo205, MIAPaCa-2, PC-3, and HL-60 cells. Mallotus B (2d) displayed cytotoxicity for MIAPaCa-2 and HL-60 cells with IC50 values of 9 and 16 μM, respectively. Microscopic studies in HL-60 cells indicated that mallotus B (2d) induces cell cycle arrest at the G1 phase and causes defective cell division. It also induces apoptosis, as evidenced by distinct changes in cell morphology. ER -