目的 研究喙尾琵琶甲Blaps rhynchoptera的化學成分及其細胞毒活性。方法 采用硅膠、Sephadex LH-20凝膠、MCI柱色譜，以及制備高效液相色譜等技術進行化合物的分離純化，通過理化性質及波譜學方法鑒定結構，運用MTT法評價化合物的細胞毒活性。結果 從喙尾琵琶甲蟲體的95%乙醇提取物中分離得到了21個化合物，分別鑒定為 (3R)-6-羥基-3-甲基-3, 8-二乙基-2-吲哚酮（1）、blapindole I（2）、blapindole K（3）、尿嘧啶（4）、胸腺嘧啶（5）、胸腺嘧啶脫氧核苷（6）、對羥基苯甲酸（7）、對羥基苯乙酸（8）、對苯二酚（9）、2-甲基對苯二酚（10）、2-乙基對苯二酚（11）、原兒茶酸（12）、羥基酪醇（13）、香草醇（14）、原兒茶醛（15）、N-乙酰基多巴胺（16）、對羥基苯丙酸甲酯（17）、苯乙酸（18）、1-H-吲哚-3-羧酸（19）、12-羥基硬脂酸（20）和烏金苷（21）?；衔?b>1、10和11對人白血病K562細胞的半數抑制濃度（median inhibition concentration，IC₅₀）值分別為7.95、3.23和4.13 μmol/L；化合物10對人結腸癌HCT116細胞的IC₅₀值為19.11 μmol/L。結論 化合物1為新的吲哚酮類化合物，命名為琵琶甲酮A?；衔?b>4、5、8、14、17、18、20、21為首次從琵琶甲屬中分離得到。9個化合物對K562細胞表現出抑制活性，其中化合物1、10和11顯著強于順鉑（IC₅₀＝40.90 μmol/L）?；衔?b>10對HCT116細胞具有抑制作用，與順鉑作用相當（IC₅₀＝19.80 μmol/L）。

Objective To study the chemical constituents from Blaps rhynchoptera and their cytotoxicity. Methods By various isolation methods, such as silica gel, Sephadex LH-20 and MCI column chromatographies, together with semi-preparative HPLC, components in the ethanol extract of B. rhynchoptera were isolated, then their structures were identified by physical and chemical properties and spectroscopic methods. The cytotoxicity of the compounds on three cancer cells was tested. Results A total of 21 compounds were obtained and identified as (3R)-6-hydroxy-3-methyl-3, 8-diethyloxindole (1), blapindole I (2), blapindole K (3), uricil (4), 5-methyuricil (5), thymidine (6), 4-hydroxybenzoic acid (7), 4-hydroxyphenylacetic acid (8), hydroquinone (9), 2-methyl-1, 4-benzenediol (10), 2-ethyl-1, 4-benzenediol (11), protocatechuic acid (12), hydroxytyrosol (13), vanillic alcohol (14), protocatechnic aldehyde (15), N-acetyldopamine (16), methyl 3-(4-hydroxyphenyl) propionate (17), phenylacetic acid (18), 1-H-indole-3-carboxylic acid (19), 12-hydroxystearic acid (20), and robustaside B (21). Compounds 1, 10 and 11 showed significant cytotoxicity on K562 cells with the IC₅₀ values of 7.95, 3.23 and 4.13 μmol/L, respectively. Compound 10 showed strong cytotoxicity on HCT-116 cells with an IC₅₀ of 19.11 μmol/L. Conclusion Compound 1 was a new oxindole derivative and was named blapoxindole A. Compounds 4, 5, 8, 14, 17, 18, 20 and 21 were isolated from the Blap genus for the first time. Nine compounds exhibited cytotoxicity against K562 cells and compounds 1, 10 and 11 presented better efficiency than cisplatin (IC₅₀= 40.90 μmol/L). The compound 10 showed strong cytotoxicity on HCT-116 cells, with the IC₅₀ value roughly equal to that of cisplatin (IC₅₀= 19.80 μmol/L).

R284.1

云南省科技廳-昆明醫(yī)科大學應用基礎研究聯(lián)合專項[2018FE001(-040)];云南省中青年學術和技術帶頭人后備人才項目（202205AC160073）;云南省本科教育教學改革研究項目（JG2023001）