壮药材红根草的化学成分及生物活性研究

Chemical compositions and biological activities of Zhuang medicine Salviae prionitis

目的 研究红根草(黄埔鼠尾草Salvia prionitis全草)的化学成分,并对部分化合物进行初步的抗炎、抗肿瘤活性筛选。方法 应用正、反相硅胶,Sephadex LH-20,制备液相色谱等方法分离纯化,并结合核磁共振氢谱、碳谱和质谱等技术鉴定其结构。采用Griess法和MTT法对分离得到的部分三萜化合物进行初步的抗炎活性筛选和抗肿瘤活性研究。结果 从红根草50%乙醇提取物中分离得到15个化合物,分别鉴定为8,11,14-三烯-松香烷(1)、柳杉酚(2)、泪杉醇(3)、狗脊蕨酸(4)、白桦脂酸(5)、白桦脂醇(6)、桦木酮酸(7)、齐墩果酸(8)、3-表齐墩果酸(9)、23-羟基齐墩果酸(10)、常春藤皂苷元(11)、3α,24-二羟基-12-烯-28-齐墩果酸(12)、2α,3α,24-三羟基-12-烯-28-乌苏酸(13)、熊果酸(14)、α-香树脂醇(15)。化合物8、14对NO生成抑制率达到60%以上;化合物8、13对人膀胱癌EJ细胞的半数抑制浓度(median inhibition concentration,IC50)分别为(24.32±1.60)、(44.23±0.82)μmol/L;化合物8对人胰腺癌PANC-1细胞的IC50值为(25.13±7.07)μmol/L。结论 化合物4、7、10、14、15为首次从该植物中分离得到;其中化合物8、14抗炎活性较强;化合物8、11、13对EJ细胞有较强抑制作用;化合物8、10、11对PANC-1细胞有良好抑制作用。

Objective To study the chemical composition of Salvia prionitis, and screen its anti-inflammatory and anti-tumor activities. Methods Normal phase silica gel, reversed-phase silica gel, Sephadex LH-20, preparative liquid chromatography were used for separation and purification of the chemical composition from S. prionitis, and the structures of the isolated compounds were identified by NMR and MS. The methods of Griess and MTT were used to conduct preliminary anti-inflammatory activity screening and anti-tumor activity research on some of the isolated triterpenoids from S. prionitis. Results A total of 15 compounds were isolated from the 50% ethanol extracts of S. prionitis, their structures were determined as abieta-8,11,13-trien(1), sugiol(2), manoo1(3), woodwardic acid(4), betulinic acid(5), betulin(6), betulonic acid(7), oleanic acid(8), 3-epioleanolic acid(9),23-hydroxy-oleanolic acid(10), hederagenin(11), 3α,24-dihydroxy-12-en-28-oleanolic acid(12), 2α,3α,24-trihydroxy-12-en-28-ursic acid(13), ursolic acid(14) and α-amyrin(15). The inhibition rate of compounds 8 and 14 on NO production reached more than 60%, the IC50 of compounds 8 and 13 on human bladder cancer cells(EJ) were(24.32 ± 1.60) μmol/L and(44.23 ± 0.82) μmol/L,respectively;the IC50 value of compound 8 on human pancreatic cancer cells(PANC-1) was(25.13 ± 7.07) μmol/L. Conclusion Compounds 4, 7, 10, 14, 15 are isolated from S. prionitis for the first time. Compounds 8 and 14 have better anti-inflammatory activity.Compounds 8, 11, 13 have a strong inhibitory effect on human bladder cancer cells(EJ);Compound 8, 10, 11 have an inhibitory effect on human pancreatic cancer cells(PANC-1).