New pregnane glycosides from Brucea javanica and their antifeedant activity

Three new pregnane glycosides, 3-O-β-D-glucopyranosyl-(1→2)-α-L-arabinopyranosyl-(20R)-pregn-5-ene-3β,20-diol (1), 3-O-α-L-arabinopyranosyl-(20R)-pregn-5-ene-3β,20-diol-20-O-β-D-glucopyranoside (2), 3-O-α-L-arabinopyranosyl-(20R)-pregn-5-ene-3β,20-diol-20-O-β-D-glucopyranosyl-(1→2)-β-D-glucopyranoside (3) were isolated along with four known compounds, 4-7, from the leaves and stems of Brucea javanica. Their structures were determined by detailed analyses of 1D- and 2D-NMR spectroscopic data. All of the compounds isolated from Brucea javanica were tested for the antifeedant activities against the larva of Pieris rapae. Compounds 1, 3, and 5 showed significant antifeedant activities after 72 h incubation.     

鸦胆子油乳联合NP 方案治疗晚期非小细胞肺癌的临床疗效观察

目的:观察鸦胆子油乳联合NP方案化疗与单纯NP方案化疗对晚期肺小细胞癌患者的疗效、生活质量等因素的影响。方法:将154例患有晚期非小细胞肺癌患者随机分为两组:治疗组,在NP方案化疗基础上使用鸦胆子油乳治疗;对照组,单纯接受NP方案化疗。对154例患者追踪3个月,观察并比较患者的疗效、体质量、生活质量、毒副反应等方面的差异。结果:在NP方案化疗基础上使用鸦胆子油乳治疗在患者疗效评价方面与单纯NP方案化疗相比不具有统计学差异(P>0.05);在提高患者体质量、改善患者临床症状和生活质量等方面均优于单纯NP方案化疗(P<0.05);在化疗所引发的白细胞、血红蛋白和血小板降低等部分毒副反应发生率方面低于单纯NP方案化疗组(P<0.05)。结论:鸦胆子油乳联合NP方案化疗治疗晚期非小细胞肺癌不仅可以起到化疗增效的作用,而且能够明显提高患者生活质量,有效的改善临床症候,降低化疗引发的毒副反应,这一联合治疗方案可以在临床治疗中广泛推广。     

鸦胆子油乳注射液辅助化疗对大肠癌根治术后患者的临床疗效观察

摘要 目的：探讨鸦胆子油乳注射液辅助化疗对大肠癌根治术后患者生活质量、肿瘤标志物以及复发转移指标的影响。方法：将我院自2018年10月至2020年3月间收治的78例经病理学确诊的大肠癌并行根治术的患者作为研究对象,按照患者自愿原则及耐受情况,将患者分为对照组和观察组,每组39例。对照组患者采用常规化疗方式,观察组在常规化疗基础上辅助鸦胆子油乳注射液治疗,14 d为一个疗程,连续治疗12个疗程。分析两组患者治疗前后生活质量（KPS）评分、肿瘤标志物（血清癌胚抗原(CEA)、糖类抗原199(CA-199)、神经元特异性烯醇化酶(NSE)）和复发转移指标（转化生长因子-β1(TGF-β1)、Smad4、血管内皮细胞生长因子(VEGF)）水平的变化。结果：观察组和对照组均能提高患者的生活质量,两组治疗后的对比分析显示,观察组结果更显著提高KPS评分（P<0.05）;治疗前两组患者肿瘤标志物和复发转移指标水平差异并无统计学意义（P>0.05）,治疗后两组肿瘤标志物CEA、CA-199、NSE水平均降低,观察组患者降低程度与对照组比较具有明显统计学差异性（P<0.05）;治疗后观察组患者TGF-β1和VEGF阳性率均降低,Smad4阳性率升高,观察组患者各指标降低或升高程度与对照组比较差异有统计学意义（P<0.05）。结论：鸦胆子油乳注射液辅助用于大肠癌根治术后化疗患者中,与常规的化疗方式比较,患者生活质量提高,降低复发转移的可能性,是临床值得采用的辅助化疗方式。     

鸦胆子药渣的化学成分研究

为了解鸦胆子(Brucea javanica)药渣的化学成分,从中分离得到了10个化合物,经波谱分析分别鉴定为对羟基苯甲酸(1)、对羟基苯甲醛(2)、3,4-二羟基苯甲酸(3)、3,4-二羟基苯甲醛(4)、松柏醛(5)、芥子醛(6)、3-吲哚甲醛(7)、3-吲哚甲酸(8)、β-谷甾醇(9)和鸦胆苦醇(10)。其中化合物4～6、8为首次从鸦胆子分离得到。     

鸦胆子油乳抗肿瘤机制及其临床应用研究进展

鸦胆子油乳是临床上广泛应用的抗肿瘤中药,毒副作用小,疗效确切,临床应用安全。我们针对鸦胆子油乳的抗肿瘤机制,在分子基础、改变细胞周期分布、诱导细胞凋亡、破坏细胞结构、逆转多药耐药和临床应用等几方面进行了简要综述,为鸦胆子油乳的进一步应用研究提供参考。     

中药补骨脂及鸦胆子对大鼠卡氏肺孢子虫肺炎的防治研究

目的探讨中药补骨脂及鸦胆子对大鼠卡氏肺孢子虫肺炎的防治效果。方法用地塞米松皮下注射建立大鼠卡氏肺孢子虫肺炎动物模型,用补骨脂、鸦胆子及两者合剂治疗实验鼠,观察其肺脑组织病理、肺脑组织和血清中MDA(丙二醛)、XOD(黄嘌呤氧化酶)、GSH(谷胱甘肽)等指标变化。结果补骨脂、鸦胆子及合剂治疗实验大鼠体重明显回升,与模型对照差异有显著性(P<005);各治疗组的包囊减少率均高于60%,合剂治疗组不优于各单独治疗组,鸦胆子及合剂治疗组清除氧自由基能力较强。结论鸦胆子及补骨脂对大鼠卡氏肺孢子虫肺炎具有一定疗效。     

鸦胆子化学成分及肿瘤细胞毒活性研究(英文)

从鸦胆子(Brucea javanica)种子的甲醇提取物中分离和鉴别得到11个化合物,经波谱数据分析分别鉴定为鸦胆子内酯A(1),鸦胆子素D(2),鸦胆子苷A(3),C(4),F(5),G(6),L(7),3β-羟基-孕甾-5-烯-20-酮(8),3β-羟基-5α-孕甾-20-酮(9),3-O-β-D-吡喃葡萄糖基-(1→2)-α-L-吡喃阿拉伯糖基-(20R)-孕甾-5-烯-3β,20-二醇(10)和6,22-二烯-3β-羟基5,8-过氧麦角甾(11)。其中化合物8、9和11为首次从该植物中分离得到。鸦胆子内酯A(1)和鸦胆子素D(2)对人类癌细胞株BGC-823,Huh-7,KE-97和Jurkat具有很好的细胞毒作用。     

Quassinoid glucosides from seeds of Brucea amarissima

Quassinoid glucosides, javanicosides I, J, K and L, were isolated from the seeds of Brucea amarissima (Lour.) Desv. ex B. A. Gomes (Simaroubaceae), along with two known quassinoids, i.e. bruceins D and E, and seven known quassinoid glucosides, yadanziosides B, C, E, I and K, bruceoside B and yadanzigan. Their structures were elucidated by analysis of the spectral data and chemical evidence.     

Brucin,an antibacterial peptide derived from fruit protein of Fructus Bruceae,Brucea javanica (L.) Merr

A novel antibacterial peptide specific to Streptococcus pyogenes was produced from dried fruit protein of Brucea javanica (L.) Merr. A mixture of active peptides from the fruit protein was produced in vitro by pepsin hydrolysis. The hydrolysate was purified by reverse‐phase HPLC, and antimicrobial peptides active against Gram‐negative and Gram‐positive bacteria were analysed using SDS‐PAGE and nanoLC‐MS/MS. Here, four possible peptides were obtained and chemically synthesized for comparative study of the growth inhibition of Strep. pyogenes. One chemically synthesized peptide with a molecular mass of 1168·31 Da, His‐Thr‐Leu‐Cys‐Met‐Asp‐Gly‐Gly‐Ala‐Thr‐Tyr, showed the most potent antibacterial activity against Strep. pyogenes. This 11‐amino acid peptide was named Brucin. Its bacterial inhibitory activity was 16‐fold and 12·5‐fold higher than penicillin G and chloramphenicol, respectively, with a MIC value of 20 μmol l^?1. The results suggest that Brucin, a potent antibiotic peptide, may be developed as an alternative drug for the treatment of the disease caused by Strep. pyogenes.

Significance and Impact of the Study

An antibacterial peptide, named Brucin with specificity for Streptococcus pyogenes, was produced in vitro from dried fruit protein of Brucea javanica (L.) Merr. by pepsin‐catalysed hydrolysis. Its inhibitory activity towards the Gram‐positive bacteria was higher than penicillin G and chloramphenicol. The result suggested that Brucin may be applied for the treatment of the disease caused by Strep. pyogenes^*.