虎杖蒽醌化合物抗CVB3病毒的实验研究

目的：为了解虎杖蒽醌化合物晶Ⅰ,晶Ⅳ抗ＣＶＢ３病毒的药效从而明确虎杖的抗病毒性能并开发利用。方法;以病毒唑为阳性对照,利用空斑减数实验进行研究。结果：在ＨＥＰ－２细胞系统中,晶Ⅰ对ＣＶＢ３直接杀灭,增殖抑制,感染阻断ＥＤ５０分别为１．５４μｇ／ｍＬ,８．３４μｇ／ｍＬ,３．０６μｇ／ｍＬ,晶Ⅳ的相 系数分别为１．７９μｇ／ｍＬ,７．０５μｇ／ｍＬ,３．１７μｇ／ｍＬ,而病毒唑的相应系数分别为６．２     

Hepatoprotective and antioxidant potential of Asphodeline lutea (L.) Rchb. roots extract in experimental models in vitro/in vivo

The aim of this study was to investigate the effect of Asphodeline lutea (L.) Rchb. dry root extract (ALE) administered alone and against carbon tetrachloride (CCl₄)-induced liver injury in vitro/in vivo. The dried roots of A. lutea were extracted with 70% ethanol and was characterized with HPLC-UV. Hepatoprotective potential was investigated by in vivo/in vitro assays in Wistar rats as well as antioxidant properties. At concentrations ranging from 10 to 200 μg/mL of ALE significant cytotoxic effects on isolated hepatocytes were found. ALE showed some toxicity in Wistar rats discerned by increased ALT (Alanine transaminase), ALP (Alkaline phosphatase) activities and MDA (malondialdehyde) quantity, decreased GSH (reduced glutathione) levels without affecting the activity of the antioxidant enzymes (GPx (Gluthatione peroxidase), GR (Glutathione reductase) and GST (Glutathione-S-transferase activity)). The antioxidant and hepatoprotective potential of ALE was also observed in vitro/in vivo against CCl₄-induced liver injury, where ALE normalizes all the examined parameters perturbated by CCl₄ administration. In addition, ALE preserved the decreased cytochrome P450 level and EMND (Ethylmorphine-N-Demethylase) activity without affecting AH (Aniline 4-Hydroxylase) activity. ALE is rich in anthraquinones, naphthalenes and caffeic acid. The pro-oxidant effects of ALE could be due to naphthalene and anthraquinone bioactivation pathways involving toxic metabolites.     

何首乌吸收动力学研究进展

何首乌作为传统常用中药,被广泛应用于临床,在疾病治疗中发挥重要作用。临床上,何首乌饮片及制剂主要以口服为主,所含化学成分被吸收进入机体并与机体相互作用是其发挥药效的前提,因此,研究何首乌的吸收机制具有重要意义。本文通过查阅文献,对何首乌主要成分的吸收动力学研究进行综述,以期为评价何首乌的生物利用度、改善剂型、提高药效提供参考。     

大黄配方颗粒蒽醌成分的HPLC指纹图谱研究

目的：建立大黄配方颗粒中蒽醌成分为特征的HPLC指纹图谱.方法：以大黄酸为参照物,利用高效液相色谱梯度洗脱,测定了11批大黄配方颗粒样品;色谱柱为Waters SunFire C18（250 mm×4.6 mm,5μm）;流动相：甲醇（A）-0.1％磷酸溶液（B）,检测波长：254 nm,柱温：30℃,流速：1.0 ml·min-1.结果：通过HPLC指纹图谱分析,标示出大黄配方颗粒8个共有的蒽醌成分色谱峰,11批样品指纹图谱的相似度均大于0.93,并确认4个已知峰为芦荟大黄素、大黄酸、大黄素和大黄酚.结论：建立的大黄配方颗粒蒽醌成分的HPLC指纹图谱稳定可靠,操作简便,可为大黄配方颗粒质量控制提供科学依据.     

“Melanosis” in the small and large intestine

Deposition of pigment in the intestinal mucosa is commonly observed by the endoscopist, especially within the colon, and particularly during investigations for constipation. Pigment may also be detected in the small intestine. Although labeled as melanosis, electron microscopy and X-ray analytical methods have provided evidence that this pigment is not melanin at all, but lipofuscin. Often, herbal remedies or anthracene containing laxatives are often historically implicated, and experimental studies in both humans and animal models have also confirmed the intimate relationship with these pharmacological or pseudo-pharmacological remedies. The appearance of melanosis coli during colonoscopy is largely due to pigment granule deposition in macrophages located in the colonic mucosa. The pigment intensity is not uniform, being more intense in the cecum and proximal colon compared to the distal colon. Possibly, this reflects higher luminal concentrations of an offending agent in the proximal compared to distal colon, differential absorption along the length of the colon, or finally, differences in macrophage distribution within the colon. Mucosal lymphoid aggregates normally display a distinct absence of pigment producing a ＂starry sky＂ appearance, especially in the rectosigmoid region. Interestingly, some focal, usually sessile, colonic mucosal neoplastic lesions, rather than submucosal lesions, may be better appreciated as pigment deposition may be absent or limited. If detected, removal and further histopathologic analysis of the polyp may be facilitated.     

Assessment of the renal protection and hepatotoxicity of rhubarb extract in rats

Aim of the study

Rhubarb is well used to treat chronic renal failure (CRF) in China and Japan, but recent studies reported that the anthraquinone derivatives contained in rhubarb had nephrotoxicity. In this investigation an attempt was made to assess the value and toxic potential of rhubarb to treat CRF.

Materials and methods

Histopathologic and biochemical tests combined with toxicokinetic analysis were performed to investigate the nephrotoxic potential and protective effect of rhubarb extract.

Results

In normal rat groups, no death was observed and no renal lesion was found after repetitive administration of rhubarb for 3 weeks. The survival rate, pathologic conditions and biochemical indexes of CRF rats treated with rhubarb at two dosages were all improved and significant amelioration was found in the low dosage group compared to the untreated CRF group. Rhein was the mainly absorbable anthraquinone derivative into systemic circulation after oral administration and the area under curve of rhein in CRF groups was lower than that in normal groups at same dosage.

Conclusions

After 3 weeks of administration of rhubarb extract, there was evidence of protective effect to CRF rats, while incidences of hepatotoxicity with minimal to mild hyaline droplets were also observed in normal rats.     

Observations on the immunocytes and macrophages in megacolon

An immunoperoxidase staining method was used to study specific immunoglobulin-containing cells in the intestinal mucosa of children who presented with features suggestive of Hirschsprung's disease. No evidence was found to substantiate the hypothesis of an immunologic component in the etiology of Hirschsprung's disease. The megacolon in this condition had an increased proportion of IgG-containing cells and a reduced proportion of IgA-containing cells when compared with normal and unobstructed colon; this may be a reflection of an abnormal mucosal immune defense leading to susceptibility to the enterocolitis found in Hirschsprung's disease. Numerous lipofuscin-bearing macrophages were seen in the colonic mucosa of children with anal stenosis who were given anthraquinone laxatives for varying periods. The possibility that this represents an early stage of melanosis coli, as well as the likelihood of anthraquinones contributing to the pathogenesis of acquired megacolon, are considered. S. S. Wijesinha was on study leave from the Department of Health, Republic of Sri Lanka, and was supported by a Scholarship awarded by the Association of Commonwealth Universities.     

比色法测定巴天酸模水提物中蒽醌类成分的含量

目的 测定巴天酸模水提取物中蒽醌类成分的含量.方法 运用比色法,以1,8-二羟基蒽醌为对照品,用0.8％乙酸镁甲醇溶液显色;在510 nm波长处测定巴天酸模水提取物中蒽醌类成分含量.结果 巴天酸模水提取物中蒽醌类成分含量达到31.07 mg/g,以结合型蒽醌为主.结论 比色法简便、精确、重现性好,可以作为巴天酸模水提取物中蒽醌类成分的含量测定方法.     

非水液相微萃取-高效液相色谱法测定大黄中5种游离葸醌类化合物

目的利用非水液相微萃取-高效液相色谱法（HPLC）同时测定大黄中游离蒽醌类化合物的含量。方法利用自制的液相微萃取装置,以聚偏氟乙烯中空纤维为溶剂载体,正己醇为萃取溶剂,供相为甲醇,接受相为1mmol／L NaOH,搅拌速度为1500r／min,萃取时间为50min。萃取结束,接受相在434nm处进行HPLC分析。结果在优化的液相微萃取条件下,芦荟大黄素、大黄酸、大黄素、大黄酚和大黄素甲醚的线性范围、回收率、精密度和检测限分别为：0.015～13.2、0.075～11.2、0.085～12.8、0.096～14.4、0.117～17.6μg／ml;103.8％～106.1％;2.5％～5.2％和2.9.20.0ng／ml。结论本法选择性高,有机溶剂消耗少,能快速、准确地测定大黄药材中游离蒽醌类化合物。     

The diarrhoeogenic and antidiarrhoeal bidirectional effects of rhubarb and its potential mechanism

Aim of the study

The present study investigated the pharmacological effects of different extracts of rhubarb on intestinal function of mice, further to explore possible reasons for the adverse effects of long-term use of rhubarb as a purgative.

Materials and methods

The total extract of rhubarb (TR) was extracted with 60% ethanol and the total anthraquinones extract (TA), total tannins extract (TT) and remaining components extract (RC) of rhubarb were separated from TR using macroporous resin. The pharmacological effects of each extract on the intestinal function of mice were evaluated by defecation test and the antidiarrhoeal activity of rhubarb tannins as well as its mechanism was studied by different animal models and histopathological examination.

Results

Both TR and TA produced purgative activities, but the purgative activity of TA was stronger than that of TR. Successive administration of TT produced an antidiarrhoeal activity in a time- and dose-dependent manner. Besides, successive administration of RC showed no significant effect on the intestinal function of mice. The antidiarrhoeal activity of rhubarb tannins was confirmed directly for the first time and its mechanism was probable that rhubarb tannins generated protein-precipitating reaction to the gastrointestinal mucosa due to its protein-precipitating action.

Conclusions

The results confirmed that rhubarb had the diarrhoeogenic and antidiarrhoeal bidirectional effects due to the coexistence of anthraquinones and tannins. The bidirectional effects might be the reason or one of the reasons for the adverse effects of long-term use of rhubarb as a purgative.