ABSTRACT
Robustic acid is reported to be a bioactive compound, isolated from the medicinal plant Dalbergia benthamii Prain. Ten alkyl and benzyl derivatives (2a-2j) of robustic acid were designed and synthesized based on molecular docking approaches. The biological activities of most of the synthesized compounds (such as 2g, 2h, and 2i) were closely consistent with the docking results. In particular, 4-O-phenylpropyl substituted compound 2g displayed potent topoisomerase I inhibitory activity as well as cytotoxicity against SMMC-7721, HepG2, and HeLa cell lines. Further biological testing suggests that compound 2g acted mainly by an arrest of the tumor cells in G1 phase of the cell cycle and suppressed cell proliferation by inducing apoptosis. The findings of this study are encouraging with respect to potential utilization of these compounds as new topoisomerase I inhibitors.
Subject(s)
Antineoplastic Agents/pharmacology , DNA Topoisomerases, Type I/metabolism , Drug Design , Isoflavones/pharmacology , Molecular Docking Simulation , Topoisomerase I Inhibitors/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Apoptosis/drug effects , Cell Cycle/drug effects , Cell Line, Tumor , Cell Proliferation/drug effects , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Humans , Isoflavones/chemical synthesis , Isoflavones/chemistry , Molecular Structure , Structure-Activity Relationship , Topoisomerase I Inhibitors/chemical synthesis , Topoisomerase I Inhibitors/chemistryABSTRACT
OBJECTIVE: In order to prove a basis for rational exploitation and utilization of the herb, the charaeteristic feature for Acanthus iliciflius was studied. METHOD: The botanical and pharmacognostic features of the collected original plant were stadied. RESULT: A. ilicifolius showed obvious pharmacognostic characters. The aerate cells of the root were upgrowth. and four vascular bundles were found in leaf venation. CONCLUSION: The distinct characteristic features revealed in this studies can serve as evidence for the identification of A. ilicifolius.
Subject(s)
Acanthaceae/anatomy & histology , Pharmacognosy , Plants, Medicinal/anatomy & histology , Acanthaceae/chemistry , Chromatography, Thin Layer , Plant Leaves/anatomy & histology , Plant Leaves/chemistry , Plant Roots/anatomy & histology , Plant Roots/chemistry , Plant Stems/anatomy & histology , Plant Stems/chemistry , Plants, Medicinal/chemistryABSTRACT
OBJECTIVE: To study the characteristic features of Desmodium gyrans in order to provide a basis for rational exploitation and utilization of the herb. METHOD: Samples of the title plant were collected, the microscopic features of cross sections and powders were studied. TLC profiles and UV absorption of the plant extract were examined. RESULT: Calcium oxalate crystals were found in cells of transverse sections. Nonglandular hairs were observed on leaf surfaces. Characteristic peaks in the UV spectrum were identified. CONCLUSION: The distinct characteristic features revealed in this studies can serve as evidence for the identification of D. gyrans.
