五仁醇的研究进展

五仁醇为五味子核仁的乙醇提取物,临床上主要用于降低谷丙转氨酶(SGPT),治疗急慢性肝炎。随着提取分离技术的不断进步,近年来国内外研究和使用五仁醇的越来越多,因此综述了五仁醇的活性成分及药理作用、含量测定方法、剂型研究等几方面,以便今后对其进行更深入研究。     

五仁醇固体分散体的制备及体外溶出度研究

目的将五仁醇制成固体分散体,提高五仁醇中有效成分的体外溶出度。方法采用直接将载体材料溶于五仁醇提取液,然后除去溶剂的方法制备了多种五仁醇固体分散体,以五味子甲素为指标成分,研究并比较了它们的表观溶解度和体外溶出度。结果配比为1∶3的五仁醇-聚乙烯吡咯烷酮K 30(PVP K 30)固体分散体中有效成分的表观溶解度比五仁醇胶囊内容物显著提高,达到5.06μg/mL(水);溶出介质(水)中分散(包括溶解)的小于0.22μm的药物高达43.2%。结论五仁醇-PVP K 30固体分散体能明显提高五仁醇中有效成分的表观溶解度和体外溶出度。     

五仁醇分散片的制备工艺研究及体外溶出度试验

目的:制备五仁醇分散片,并对其溶出行为进行考察.方法:对五仁醇分散片的处方和制备工艺进行研究,采用单因素实验法对处方进行优化,以五味子甲素为考察指标,HPLC法研究其体外溶出度.结果:采用优化条件:50 g五仁醇浸膏以125 g磷酸氢钙分散后物料为主药(A),MCC-CMS-Na(3:1)为辅料B,A:B 3:5制备的五仁醇分散片,在(20 ±1)℃水中于3 min内可完全崩解且分散均匀,五仁醇分散片中五味子甲素的溶出量15 min达到80%以上.结论:所制分散片处方合理,崩解快、溶出快,能明显提高五仁醇总木脂素的溶出度.     

五仁醇对慢性肝炎的远期疗效观察

1977年,我们发表了“五仁醇对慢性肝炎的临床疗效观察》一文(以下简称“前报”),报告了应用五仁醇治疗慢性肝炎的经验。从近期(疗程期间及疗程后3个月内)效果看,本药对患者的症状、体征和血清谷丙转氨酶(SGPT)都可显示一定程度的影响,综合评价有效率为74%,其中显效率40.2%,与对照组(不服用五仁醇及含五味子成分之一切药物,仅给以多种维生素及肝精等保肝药)12.2%相比为显著(P<0.05)~(1)。本文报告对“前报”有效病例于停药2.5～3年期间的随访结果,以评价五仁醇对慢性肝炎的远期临床疗效。     

双波长薄层扫描法测定五仁醇胶囊中五味子乙素的含量

双波长薄层扫描法测定五仁醇胶囊中五味子乙素的含量赵晓霞（黑龙江省药品检验所哈尔滨１５０００１）来杰（哈尔滨市药品检验所）张华（哈尔滨制药四厂）五仁醇胶囊具有降低谷丙转氨酶的功能，是治疗肝炎的常用药［１］。五味子乙素为五仁醇胶囊中五味子的主要成分之一。...     

五仁醇增强皮质激素免疫抑制作用的实验观察

本文对五仁醇与皮质激素(醋酸可的松)的免疫抑制作用进行了比较,并对两者合用的效果进行了研究。结果表明,五仁醇在每日25mg/kg 剂量下,对小鼠脾抗体分泌细胞及特异玫瑰花形成细胞的抑制作用与中等剂量的皮质激素(每日20mg/kg)的抑制效能相同;二者合用有明显的协同作用。     

五仁醇胶囊质量标准研究

目的:制订五仁醇胶囊中五味子醇甲的含量测定方法。方法:采用高效液相色谱法对制剂中五味子仁的有效成分五味子醇甲进行含量测定。结果:五味子醇甲在0.0936~0.9360μg间线性关系良好,r=0.9999;回收率为97.54%,RSD=1.92%。结论:本方法准确可靠、重现性好,可用于含有五味子仁复方制剂的质量控制。     

瓜蒌子专属性成分的含量测定及其指纹图谱的研究

目的:通过对10个产地的瓜蒌子HPLC指纹图谱的建立,以及栝楼仁三醇和栝楼仁二醇的含量测定,从而系统地建立瓜蒌子的质量评价体系。方法:采用高效液相色谱法,测定10个产地的瓜蒌子中栝楼仁三醇和栝楼仁二醇的含量;采用高效液相色谱法,以栝楼仁三醇为参考,建立瓜蒌子的HPLC指纹图谱。结果:在10个产地中,栝楼仁三醇的含量差异不大:其中安国的栝楼仁三醇含量最高,为1.455 mg/g,河南新乡的栝楼仁三醇含量最低,为0.947 9 mg/g;栝楼仁二醇的含量差异较大:其中定州的栝楼仁二醇含量最高,为0.096 70 mg/g,山东的栝楼仁二醇含量最低,为0.022 60 mg/g。通过建立10个产地瓜蒌子的HPLC指纹图谱,共确立了13个色谱共有峰,其中13号峰为对照品栝楼仁三醇的色谱峰。各个产地瓜蒌子HPLC指纹图谱的相似度均大于0.941。结论:栝楼仁三醇和栝楼仁二醇作为瓜蒌子的专属性成分,两者可作为瓜蒌子在质量定量控制方面的两个重要指标。建立的瓜蒌子HPLC指纹图谱,可为瓜蒌子在定性鉴别方面提供科学依据。     

降酶保肝新药——五仁醇胶囊

<正> 本品为北五味子(Schizandra chinensis. Turcz. Baill)种子的乙醇提取物。按五味子乙素(C_(23)H_(28)O_6)计算,每粒不得低于10毫克。处方:五仁醇浸膏适量(含有效成份1,000克)、碳酸钙21,000克、淀粉7,000克、制成100,000粒。制法:(1)五仁醇浸膏制备:取北五味子的种子(或制备五味子酊剂、糖浆剂后的生     

五仁醇胶囊质量标准研究

目的：制订五仁醇胶囊中五味子醇甲的含量测定方法。方法：采用高效液相色谱法对制剂中五味子仁的有效成分五味子醇甲进行含量测定。结果：五味子醇甲在0．0936～0．9360gg间线性关系良好，r=0．9999；回收率为97．54％，RSD=1．92％。结论：本方法准确可靠、重现性好可用于含有五味子仁复方制剂的质量控制。     

丹参注射液对实验动物同种移植心脏存活期的影响

丹参为常用活血化瘀药物。本实验表明,肌肉注射丹参注射液,可使大鼠同种异体移植心脏的存活期延长(P<0.05)。在家兔心脏移植模型中,将丹参注射液与强的松龙合用,其抗排斥效果较两者单独使用时有明显的增强(P<0.05)。     

氧化苦参碱延长小鼠异体移植心肌存活期及其免疫机理的研究

本实验观察到肌肉注射氧化苦参碱具有明显延长小鼠异体游离移植心肌存活期的作用,并随剂量加大其作用增强。检查药物对移植和非移植小鼠的脾脏淋巴细胞转化和免疫球蛋白分泌细胞的影响。实验发现,移植术后10天小鼠体外脾脏细胞自发增殖增强,对刀豆蛋白 A(ConA)刺激的转化反应则明显减弱。氧化苦参碱显著抑制正常小鼠的脾细胞的自发增殖及对 ConA 或脂多糖(LPS)刺激的转化反应,而对手术已使之显著降低的脾细胞对 ConA 刺激的转化反应无影响。这种选择性抑制作用可能利于避免用其他常规非特异免疫抑制剂所带来的危害。     

黄连素合用环孢素A对小鼠皮肤移植排斥反应的影响

目的观察黄连素合用环孢素A抗同种异体小鼠皮肤移植排斥反应的影响,探讨其作用机制。方法以BALB/c小鼠为供体,以C57BL/6小鼠为受体,采用背-背皮肤移植手术法制备模型。将受体小鼠按随机数字表法分为模型组、黄连素组、环孢素A组、联合组,每组20只;另取20只健康C57BL/6小鼠作为假手术组。造模后黄连素组小鼠腹腔注射黄连素100 mg/kg,环孢素A组小鼠腹腔注射环孢素A注射液10 mg/kg,联合组腹腔注射黄连素100 mg/kg及环孢素A注射液5 mg/kg,假手术组和模型组小鼠腹腔注射等体积0.5%羧甲基纤维素钠。1次/d,连续10 d。记录受体小鼠移植皮片的存活时间;采用ELISA法检测血浆Th1类细胞因子[IL-2、γ-干扰素(interferon-γ,IFN-γ)]和Th2类细胞因子(IL-4、IL-10)水平;采用流式细胞术检测脾脏T淋巴细胞亚群CD4+CD25+比例。结果与模型组比较,各给药组受体小鼠移植皮片的存活时间延长(P<0.01);联合组移植皮片存活时间较黄连素组或环孢素A组延长(P<0.01)。与模型组比较,联合组血浆IL-2[(11.55±3.14)pg/ml比(19.85±2.42)pg/ml]、IFN-γ[(26.41±6.20)pg/ml比(57.23±10.15)pg/ml]水平降低,IL-4[(192.45±70.12)pg/ml比(61.09±21.61)pg/ml]、IL-10[(106.79±27.83)pg/ml比(40.08±11.23)pg/ml]水平升高(P<0.05),脾脏CD4+CD25+调节性T细胞比例[(7.65±2.42)%比(3.69±0.83)%]升高(P<0.01)。结论黄连素合用环孢素A通过促使Thl向Th2细胞的偏移、诱导免疫耐受、刺激CD4+CD25+调节性T细胞的表达等途径,抑制同种异体小鼠的皮肤移植排斥反应。     

Cardiac protective effect of Astragalus on viral myocarditis mice: comparison with Perindopril

In clinical practice, Astragali Radix (Astragalus), the root of Astragalus membranaceus Bunge, has been widely applied to treat patients with viral diseases, including viral myocarditis in China. The present study was designed to evaluate the protective effects of Astragalus on the function of sarcoplasmic reticulum calcium ATPase (SERCA2) activity and endothelin system at acute and chronic periods of myocarditis mice induced by CVB(3) infection. Astragalus feeding (2.2 mg/kg/day) could significantly increase the survival rate, alleviate pathological alterations and serum cardiac troponin I (cTnI), as well as restore impaired SERCA activity at the acute stage. Low affinity and capacity of ETR were reversed with Astragalus after the first CVB(3) inoculation up to 7 days and after the second virus inoculation up to 150 days. In the meantime, the contents of cardiac ET-1 and ANP were reduced. Comparison the myocarditis mice treated with Perindopril (0.44 mg/kg/day), an ACE inhibitor, shows that Astragalus achieved a similar effect on survival rate, SERCA2 and ET system. These results indicated that the beneficial effects of Astragalus and Perindopril for treating viral myocarditis might be partly mediated by preserving the functions of SERCA 2 activity and ET system.     

Acute and Sub‐Acute Oral Toxicity Assessment of the Hydroalcoholic Extract of Withania somnifera Roots in Wistar Rats

Withania somnifera is a widely used medicinal plant for several disorders. Toxicity studies on Withania somnifera are not available. Acute and sub‐acute oral toxicities of Withania somnifera root extract in Wistar rats were evaluated in the present study. In the acute toxicity study, WSR extract was administered to five rats at 2000 mg/kg, once orally and were observed for 14 days. No toxic signs/mortality were observed. In the sub‐acute study, WSR extract was administered once daily for 28 days to rats at 500, 1000 and 2000 mg/kg, orally. No toxic signs/mortality were observed. There were no significant changes (P < 0.05) in the body weights, organ weights and haemato‐biochemical parameters in any of the dose levels. No treatment related gross/histopathological lesions were observed. The present investigation demonstrated that the no observed adverse effect level was 2000 mg/kg body weight per day of hydroalcoholic extract of W. somnifera in rats and hence may be considered as non‐toxic. Copyright © 2012 John Wiley & Sons, Ltd.     

Enhancing effect of calaguala on the prevention of rejection on skin transplants in mice

Calaguala, an extract from the fern Polypodium decumanum, has been used to treat psoriasis and other immunologically related disorders. In order to elucidate whether an immunosuppressive mechanism could explain the clinical effect, Calaguala was studied in a skin model of allograft rejection in mice. Calaguala significantly prolonged the allograft survival compared with untreated transplanted mice. The results indicate that Calaguala exerts an immunosuppressive effect which could explain at least partly, the positive clinical results on psoriasis.     

Sabinyl Acetate,the Main Component of Juniperus sabina L'Hérit. Essential Oil,is Responsible for Antiimplantation Effect

The essential oil of Juniperus sabina , containing 50% sabinyl acetate, was administered s.c. to mice at doses of 15, 45 and 135 mg/kg either on days 0–4 of pregnancy (implantation period) or on days 8–11 (organogenesis) to investigate its mechanism of action. The mice were killed on days 9 and 17 respectively. Subsequently to the previous assays, sabinyl acetate was injected s.c. at a dose of 70 mg/kg, corresponding to the higher dose of essential oil, on days 0–4, the mice being killed on day 9. The number of prominent corpora lutea and implantation sites were recorded for mice killed on day 9. The uterine content of those killed on day 17 were examined and the fetuses removed and examined for malformations. Treatment with the oil on days 0–4 prevented pregnancy in half the mice treated with the two higher doses. The same pattern was observed with sabinyl acetate (70 mg/kg). In contrast, treatment with the oil on days 8–11 did not impair fertility, nor did it increase the incidence of malformations compared with the results obtained for the control group. This result indicates that the abortifacient effect of Juniperus sabina essential oil is related to an implantation inhibiting effect, induced by sabinyl acetate, the mechanism of which is being investigated.     

杞棋饮醇提取物对小鼠酒精性肝损伤的治疗作用

目的观察杞椇饮醇提取物对小鼠酒精性肝损伤的治疗作用。方法采用56度白酒12 m l/kg灌胃,1次/d,连续30d,制备酒精性肝损伤模型。将模型小鼠随机分为杞椇饮醇提取物75,150,300 mg/kg组,益肝灵70 mg/kg组和模型组,连续给药20 d。末次给药后24 h,去眼球取血,进行肝功能检测。结果杞椇饮醇提取物150,300 mg/kg组小鼠血清中谷氨酸氨基转移酶(ALT)、天门冬氨酸氨基转移酶(AST)和丙二醛(MDA)水平明显降低,与模型组比较(P<0.05或P<0.01),谷胱甘肽过氧化物酶(GSH-Px)、超氧化物歧化酶(SOD)水平明显增高,与模型组比较(P<0.05~0.01)。结论杞椇饮醇提取物对慢性酒精性肝功能损伤有明显的治疗作用。     

Thymoquinone attenuates ifosfamide-induced Fanconi syndrome in rats and enhances its antitumor activity in mice

The effect of thymoquinone (TQ), the main constituent of the Nigella sativa L. oil, on ifosfamide (IFO)-induced Fanconi syndrome (FS) and its antitumor activity were investigated in rats and mice, respectively. In rats, a daily injection of IFO (50 mg/kg per day, i.p.) for 5 days induced a FS characterized by wasting off glucose, electrolytes and organic acids, along with elevated serum creatinine and urea, as well as decreased creatinine clearance rate. Administration of TQ with the drinking water of rats, (5 mg/kg per day) for 5 days before and during IFO treatment, ameliorated the severity of IFO-induced renal damage. TQ significantly improved IFO-induced phosphaturia, glucosuria, elevated serum creatinine and urea, and significantly normalized creatinine clearance rate. Moreover, TQ significantly prevented IFO-induced renal glutathione (GSH) depletion and lipid peroxide accumulation. In mice bearing Ehrlich ascites carcinoma (EAC) xenograft, TQ (10 mg/kg per day) administered in drinking water significantly enhanced the antitumor effect of IFO (50 mg/kg per day, i.p. on days 1-4 and 15-18). Furthermore, mice treated with IFO in combination with TQ showed less body weight loss and mortality rate compared to IFO single therapy. These observations demonstrate that TQ may improve the therapeutic efficacy of IFO by decreasing IFO-induced nephrotoxicity and improving its antitumor activity.