Anti-HIV-1 and cytotoxicity of a new dimeric thiazepine alkaloid isolated from Ixora undulata Roxb. leaves

作者：Mohammed Magdy M D; Mohamed Khaled M

来源：Medicinal Chemistry Research, 2017, 26(9): 2119-2126.

DOI：10.1007/s00044-017-1921-y

• Ixora undulata Roxb.
• Rubiaceae
• Dimeric thiazepine alkaloids
• Anti-HIV-1
• Cytotoxicity
• Structure-activity relationship

The crude alkaloidal extract of Ixora undulata Roxb. leaves recorded a cytotoxicity of IC50 = 125 mu g/mL against EL4 and revealed a reduction with CC50 = 47 mu g/mL in the viability of MT-4 cells, beside a 50% protection with EC50 > 47 mu g/mL against HIV-1IIIB. Bioassay guided fractionation of the crude alkaloidal extract of I. undulata leaves led to the isolation of a new dimeric thiazepine alkaloid, together with the monomer and its glycoside. The isolated alkaloids were structurally elucidated based on extensive nuclear magnetic resonance spectroscopy, infrared, and HRESI/MS. The isolated alkaloids were evaluated for their anti-HIV-1 and cytotoxic activities, while the obtained results revealed promising activity with structure-based relationship, which is discussed briefly.

• 出版日期2017-9