Nghiên cứu phân lập, nhận dạng cleistantoxin từ quả cây chà chôi (Cleistanthus tonkinensis Jabl., Euphorbiaceae) làm nguyên liệu thiết lập chất chuẩn

Abstract

On continuance of the previous programmed screening to reveal that ethyl acetate extracts from the fruits of the 2 Cleistanthus species (C. indochinensls Merr. ex Croiz and C. tonkinensis Jab!., Euphorbiaceae) possessing a strong cytotoxicity against KB cells (88.4 and 95.2 % inhibition at 1 µg/mL), cleistantoxin and some aryltetralin lignans were isolated from these species. The obtained cleistantoxin was identified physically by appearance, melting range (199 - 202 °C), specific rotation ([α]D²⁰= -133,400), and spectrometrically by 1D-NMR, 2D-NMR, HR-MS, CD, IR, UV, etc. As the major active component of the plant, Cleistantoxin proved to have a significant cytotoxicity against the following cancer cell lines: MCF-7 (IC₅₀ = 0.036 µM), MCF-7R (ICX= 0.014 µM) and HT29 (IC₅₀= 0.035 µM). In addition, cleistantoxin showed structural similarity to etoposide which is currently used for lung cancer treatment. To establish a primary chemical reference substance (PCRS). 4.023 g cleistantoxin was purified (>99.0% by HPLC/DAD analysis), meeting the quality and purity requirments of the International Pharmacopoeia (IP) and World Health Organization (WHO) guide.