Anti-cataract effects of Dajizhi(Euphorbium) eye drops on selenite-induced cataracts in rats

OBJECTIVE:To evaluate the effects of Dajizhi(Euphorbium)on selenite-induced cataracts.METHODS:Wistar rat pups were divided into 9 groups.Rats in group 1 were subcutaneously injected with saline,and rats in the other groups were injected with sodium-selenite.Every right eye was treated with 5μL eye drops 3 times per day,and the left eye received no treatment.The eyes of rats in group 3 were treated with pirenoxine;rats in groups 4,5,6,7,8 and 9 were respectively treated with Dajizhi(Euphorbium)(25 mg/m L),Dajizhi(Euphorbium)(5 mg/m L),Dajizhi(Euphorbium)methanol extract(25 mg/m L),Dajizhi(Euphorbium)methanol extract(5 mg/m L),euphol(25 mg/m L),euphol(5 mg/m L).Cataracts were observed by a slit lamp before and after treatment.Electroretinograms were acquired at set intervals.The morphological changes of the rat eyes were observed in vitro,and the levels of glutathione peroxidase(GSH-Px)and superoxide dismutase(SOD)in the lenses and aqueous humour were estimated at set intervals.RESULTS:Slit lamp examination showed decreased degrees of cataracts after administration of the different treatments.Morphological comparison showed that Dajizhi(Euphorbium)can reduce the turbidity of the lenses,meaning that Dajizhi(Euphorbium)has the anti-cataract effects.Low-concentration of Dajizhi(Euphorbium),its methanol extract and euphol treatment prevented the b-wave amplitudes of the electroretinograms from falling.Euphorbium treatment significantly restored GSH-Px and SOD levels in the lenses and aqueous humour,especially after 10 and 25 d of administration.Euphorbium may help lenses fight oxidative stress caused by selenite.CONCLUSION:The administration of Dajizhi(Euphorbium)can inhibit selenite-induced cataracts.

大戟脂中二萜类成分及细胞毒活性研究

〔目的〕研究大戟脂中二萜类抗肿瘤活性成分。〔方法〕通过硅胶柱色谱、ODS柱色谱和RP-HPLC等方法,从大戟脂的甲醇提取物中共分离得到5个二萜类化合物,利用各种波谱学手段及理化性质确定化合物的结构。对分离得到的二萜类化合物的生合成途径进行了简单推测,并采用MTT法对分离得到的单体化合物进行细胞毒活性测试。〔结果〕分离得到的5个二萜类化合物包括3个Ingol烷型二萜、2个巴豆烷型二萜,分别鉴定为:ingol7,8,12-triacetate-3-(4-me-thoxy-phenyl)acetate(1)、ingol7,8,12-triacetate-3-phenylacetate(2)、ingol3,8,12-triacetate(3)、12-deoxyphorbol-13-isobu-tyrate-20-acetate(4)、12-deoxyphorbol-13-angelate-20-acetate(5)。〔结论〕化合物1~3是首次从该植物中分离得到,并对C6细胞株有较强的细胞毒活性。

大戟脂药材中四环三萜类成分大戟二烯醇、大戟醇的含量测定及提取工艺优化

目的:建立同时测定大戟脂药材中大戟二烯醇和大戟醇含量的方法,并优化其提取工艺。方法:采用高效液相色谱法。色谱柱为Agilent ZORBAX Eclipse Plus C8,流动相为乙腈-水(90∶10,V/V),流速为1.0 mL/min,检测波长为210 nm,柱温为30℃,进样量为10μL。以大戟二烯醇、大戟醇含量、出膏率为评价指标进行综合评分,以乙醇体积分数、提取时间、溶剂用量为考察因素,采用L9(34)正交试验优化其提取工艺并进行验证。结果:大戟二烯醇、大戟醇检测质量浓度的线性范围分别为0.0304~1.216mg/mL(r=0.9996)、0.01~0.4 mg/mL(r=0.9999);精密度、稳定性(24 h)、重复性试验的RSD均小于2%,平均加样回收率分别为100.46%(RSD=1.03%,n=6)、99.36%(RSD=0.91%,n=6)。最优提取工艺为40 mL的95%乙醇回流提取1 h。经3次试验验证结果显示,大戟二烯醇的平均含量为94.43 mg/g(RSD=0.92%,n=3),大戟醇的平均含量为25.42 mg/g(RSD=0.98%,n=3),平均出膏率为51.42%,(RSD=1.95%,n=3),平均综合评分为98.87(RSD=0.92%,n=3)。结论:所建含量测定方法简便、准确,重复性好,可用于大戟脂的质量控制;优化所得提取工艺稳定、可行。

大戟脂有效部位及大戟二烯醇抗炎镇痛作用研究

目的考察大戟脂有效部位和大戟二烯醇的抗炎镇痛作用。方法取昆明种小鼠80只,随机分为8组,分别为大戟脂有效部位大、中、小(60,30,15 mg·kg^(-1))剂量组,大戟二烯醇大、中、小(30,15,7.5 mg·kg^(-1))剂量组,0.5%CMC-Na组和吲哚美辛组(10 mg·kg^(-1)),每组10只。通过二甲苯致小鼠耳肿胀法、毛细血管通透性实验和棉球肉芽肿实验,综合观察大戟脂有效部位和大戟二烯醇的抗炎作用;采用热板法、醋酸扭体法和福尔马林法,评价其镇痛作用。结果大戟脂有效部位和大戟二烯醇在三种炎症模型上均显示了一定的抗炎作用,同时表现出良好的镇痛作用,其中以大戟二烯醇高剂量组效果最佳。结论大戟脂有效部位和大戟二烯醇具有显著的抗炎镇痛作用,其中大戟二烯醇发挥主要作用。

狼毒大戟的研究现状及其藏医临床应用分析

基于对中藏药材狼毒大戟的药用价值及其安全性的考究,笔者通过查阅藏医药古籍及相关文献,从狼毒大戟的药理活性、毒性实验以及藏医中狼毒大戟的炮制方法、组方特点和临床价值等方面进行分析。发现狼毒大戟不仅有着可观的药用价值,而且在低剂量或治疗剂量下对正常组织及细胞没有毒性或毒性作用较小,尤其是经过炮制加工后更是起到了减毒存效甚至增效的双重作用。因此,在未来研究中若能考证以狼毒大戟为主的藏药方剂及其药理作用,将为狼毒大戟的进一步开发利用提供有力的参考依据,更能为狼毒大戟的临床治疗提供更多的选择。

维吾尔药大戟脂中2个新的三萜

目的研究大戟脂(多脂大戟Euphorbia resinifera的树脂状分泌物)的化学成分。方法采用反相C18、硅胶、凝胶柱色谱、制备型HPLC等方法进行分离纯化,通过红外、紫外、高分辨质谱、一维和二维的核磁数据和结合参考文献鉴定化合物的结构。结果从大戟脂甲醇提取物中分离得到了2个化合物,分别鉴定为大戟烷-8-烯-3,25-二醇-24-氯-7-酮(1)和22,23,24,25,26,27-六降大戟烷-8-烯-20-醇-3,7-二酮(2)。结论化合物1为新的三萜,化合物2为新的降三萜,分别命名为大戟脂A和大戟脂B。