Effects of Orengedoku-to and Scutellariae radix extract on aqueous flare elevation induced by intravitreal IL-1alpha in pigmented rabbits

We investigated the effects of Orengedoku-to (huanglian-jie-du-tang in Chinese) and Scutellariae radix extract on experimental aqueous flare elevation in pigmented rabbits. To produce the elevation of aqueous flare in rabbits, interleukin-1 alpha (IL-1alpha) was injected intravitreally. Animals were pretreated with oral administration of 150 g/day of food containing 0.07%, 0.2% or 0.7% (w/w) Orengedoku-to; or 0.02%, 0.07% or 0.2% Scutellariae radix extract for 5 days. The animals were further treated with the same food for 7 days after intravitreal injection of IL-1alpha. Aqueous flare was measured with a laser flare-cell meter. Treatment with 0.2% or 0.7% Orengedoku-to and 0.07% or 0.2% Scutellariae radix extract significantly (p < 0.05) suppressed elevation of aqueous flare induced by IL-1alpha. Thus, orengedoku-to and Scutellariae radix extract have an inhibitory effect on experimental elevation of aqueous flare induced by IL-1alpha in rabbits.     

Effects of Orengedoku-to and Senkanmeimoku-to, traditional herbal medicines, on the experimental elevation of aqueous flare in pigmented rabbits

We investigated the effects of Orengedoku-to (Huanglian-Jie-Du-Tang in Chinese) and Senkanmeimoku-to (Xygan-Ming-Mu-Tang in Chinese), traditional herbal medicines, on experimantal elevation of aqueous flare in pigmented rabbits. To produce the elevation of aqueous flare in rabbits, prostaglandin E2 (PGE2) was applied to the cornea with use of a glass cylinder, or lipopolysaccharides (LPS) were injected into the ear vein. Animals were pretreated by the oral administration of 150 g/day of food containing 0.7%, 0.2% or 0.07% (w/w) Orengedoku-to, or 2%, 0.6% or 0.2% (w/w) Senkanmeimoku-to for 5 days. Aqueous flare was measured with a laser flare-cell meter. Pretreatment with 0.7% or 0.2% Orengedoku-to and 2% Senkanmeimoku-to did suppress significantly (P < 0.05) elevation of aqueous flare induced by PGE2. Pretreatment with 0.7% or 0.2% Orengedoku-to and 2% or 0.6% Senkanmeimoku-to significantly suppressed (P < 0.001) elevation of aqueous flare induced by LPS. It is possible that Orengedoku-to and Senkanmeimoku-to may migrate some forms of uveitis.     

Effects of kakkon-to and sairei-to on aqueous flare elevation after complicated cataract surgery

We evaluate prospectively the effects of traditional herbal medicines on elevation of aqueous flare after complicated cataract surgery. Twenty-seven patients with bilateral complicated cataract undergoing phacoemulsification with intraocular lens implantation were studied. The patients received no herbal medicine when the right eyes underwent cataract surgery. Fifteen patients were given kakkon-to (ge-gen-yang in Chinese) granules (7.5 g daily) and 12 patients were given sairei-to (cai-ling-tang in Chinese) granules (9.0 g daily), for 3 days before surgery, the day of surgery, and for 7 days after surgery when the left eyes underwent cataract surgery. Diclofenac eyedrops were instilled in all patients. Aqueous flare was measured before and after surgery. The differences in preoperative flare intensities between groups treated with Kakkon-to and Sairei-to were not significant. In the untreated right eyes of the kakkon-to and Sairei-to groups, the flare was 99.1 and 89.6 photon counts/msec, respectively, on day 1, and then gradually decreased. The flare intensities on days 1, 3, and 5 in the kakkon-to treated left eyes were significantly lower than in those of the untreated right eyes (Fig. 1). The flare intensities in the Sairei-to treated left eyes were the same as those in the untreated right eyes. Kakkon-to contributed to a reduction of aqueous flare elevation after surgery for complicated cataract.     

Effects of cerebral ischemia-reperfusion on pharmacokinetic fate of paeoniflorin after intravenous administration of Paeoniae Radix extract in rats

The objective of the present study was to investigate the effects of cerebral ischemia-reperfusion on pharmacokinetics of paeoniflorin after intravenous administration of Paeoniae Radix extract (PRE) in rats. The cerebral ischemia-reperfusion rats were induced by occluding the bilateral carotid arteries of normal rats for 2 h, followed by reperfusion. The resultant animals were immediately administrated by PRE (at a dose of 60 mg/kg of paeoniflorin) via the femoral vein, whilst the same dose was injected to the normal rats. Plasma samples were collected at different time to construct pharmacokinetic profiles by plotting drug concentration versus time. Quantification of paeoniflorin in rat plasma was achieved by using a simple and rapid high-performance liquid chromatographic method. In normal rats, the major parameters of distribution half-life (t1/2alpha), elimination half-life (t1/2beta), area under the plasma concentration-time (AUC), mean retention time (MRT), and clearance (CL), estimated by an open two-compartmental model, were 0.69, 18.77 min, 5338.71 (microg min)/ml, 18.13 min and 0.0162 mg/(kg min), respectively. However, in ischemia-reperfusion rats, the corresponding parameters were 2.04, 24.51 min, 9626.00 (microg min)/ml, 29.75 min and 0.0071 mg/(kg min), respectively. The results showed that ischemia- reperfusion significantly increased AUC values, decreased CL values, and prolonged the terminal half-life of paeoniflorin. These findings suggest that the injuries of ischemia-reperfusion could play an important role in pharmacokinetic process of paeoniflorin.     

Effects of oral administration of aqueous extract of Fadogia agrestis (Schweinf. Ex Hiern) stem on some testicular function indices of male rats

AIM OF THE STUDY: The effects of administration of aqueous extract of Fadogia agrestis (Schweinf. Ex Hiern) stem on some testicular function indices of male rats (Rattus norvegicus) and their recovery potentials for 10 days were investigated. MATERIALS AND METHODS: Rats were grouped into four: A, B, C and D where A (the control) received orally 1 ml of distilled water (the vehicle), B, C and D (the test groups) received orally on daily basis graded doses of 18, 50 and 100mg/kg body weight of the plant extract, respectively, for 28 days. RESULTS: Compared with the control, extract administration for 28 days at all the doses resulted in significant increase (P<0.05) in percentage testes-body weight ratio, testicular cholesterol, sialic acid, glycogen, acid phosphatase and gamma-glutamyl transferase activities while there was significant decrease (P<0.05) in the activities of testicular alkaline phosphatase, acid phosphatase, glutamate dehydrogenase and concentrations of protein. Recoveries were made by the animals on some of the testicular function indices mainly at 18 mg/kg body weight. CONCLUSIONS: The alterations brought about by the aqueous extract of Fadogia agrestis stem are indications of adverse effects on the male rat testicular function and this may adversely affect the functional capacities of the testes. The recovery made at the dose of 18 mg/kg body weight as used in folklore medicine suggests that it does not exhibit permanent toxicity at this dose.     

氯诺昔康注射液椎管内给药对家兔脊髓的影响

目的探讨氯诺昔康椎管内给药对家兔的镇痛效果及不良反应。方法选择健康成年大白兔24只,随机分成A组、B组和C组各8只,A组和B组均行硬膜外置管。A组从硬膜外腔缓慢给生理盐水2 mL,B组给氯诺昔康0.75 mg/kg(共2 mL),C组静脉给氯诺昔康0.75 mg/kg(共2 mL)。给药5 min和术后12 min分别观察家兔对热敏度的耐受情况并记录耐受时间t1和t2。实验完毕后处死兔子取出脊髓标本并观察受损情况。结果与A组比较,B组和C组耐受时间延长(P均<0.05);C组与B组耐受时间比较亦有显著性差异(P<0.05);C组t2较t1延长,有显著性差异(P<0.05);A、C 2组兔脊髓切片内未见损害性改变,B组绝大部分切片均可见神经元细胞变性等损害性改变。结论氯诺昔康对痛觉过敏状态有良好的镇痛效应,但椎管内给药后对脊髓有一定的损害作用,故不适合硬膜外腔给药。     

Pharmacokinetic comparisons of schizandrin after oral administration of schizandrin monomer, Fructus Schisandrae aqueous extract and Sheng-Mai-San to rats

Sheng-Mai-San (SMS) is a famous traditional Chinese medicine (TCM) recipe, containing Radix Ginseng (Panax ginseng C.A. Mey., Araliaceae), Radix Ophiopogonis (Ophiopogon japonicus (Thunb.) Ker-Gawl., Liliaceae) and Fructus Schisandrae (Schisandra chinensis (Turcz.) Baill., Magnoliaceae), and has been used more than one thousand years. In this research, pharmacokinetics of one component of this TCM recipe was studied. Schizandrin is the main absorbed effective ingredient of Fructus Schisandrae and its pharmacokinetics were studied following oral administration of pure schizandrin, Fructus Schisandrae aqueous extract, and SMS decoction in rats with approximately the same dose of 5mg/kg. At different time points (0, 0.083, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 and 12h) after administration, the concentrations of schizandrin in rat plasma were determined by LC-MS, and main pharmacokinetic parameters were estimated. It was found that both AUC0-tn and T1/2 of schizandrin in Fructus Schisandrae aqueous extract and in SMS decoction were increased significantly (p<0.05) comparing with that in monomer. The content assay also revealed that the concentrations of lignans would increase when SMS decocting, comparing with Fructus Schisandrae. These results indicate that some ingredients in SMS may increase the dissolution of schizandrin when decocting in vitro, and delay its elimination and enhance its bioavailability in rat.     

The pharmacokinetics and oral bioavailability studies of columbianetin in rats after oral and intravenous administration

Ethnopharmacological relevance

The roots of Angelica pubescens Maxim. f. biserrata Shan et Yuan (RAP) has been used as Traditional Chinese medicine to treat rheumatic disease in China since ancient times, but its action mechanisms was not well understood. Columbianetin is one of the main active constituents isolated from RAP, which has been shown to have various biological activities, but the absorption characteristics and oral bioavailability dose proportionality of columbianetin in vivo were not studied.

Materials and methods

Male Sprague Dawley rats (210–230 g) received either an intravenous (i.v. 5, 10 and 20 mg kg⁻¹) or oral (5, 10 and 20 mg kg⁻¹) dose of columbianetin. The levels of columbianetin in plasma were measured by a simple and sensitive reversed-phase high-performance liquid chromatography (HPLC) method. The simple liquid–liquid extraction with ethyl acetate was used for sample preparation. Osthole was selected as internal standard (IS).

Results

The chromatographic separation was accomplished on a C₁₈ column at a flow rate of 1 mL min⁻¹, where water–methanol was used as mobile phase. The calibration curve of the method was linear in the concentration range of 0.05–2000 μg mL⁻¹. The intra and inter-day accuracy for columbianetin in rat plasma samples were within 8% and the variation was less than 8.3%. This method was suitable for the determination and pharmacokinetic study of columbianetin in rat plasma after both intravenous and oral administration. The results indicated that maximum plasma concentrations(C_max) for the columbianetin (17–42 μg mL⁻¹) were achieved at 0.3–0.5 h post-oral dosing and the apparent volume of distribution (V/F) ranged from 0.38 to 0.44 L. Absolute bioavailability of columbianetin was assessed to be 81.13±45.85, 81.09±33.63 and 54.30±23.19%, respectively. Terminal elimination half-life (T_1/2) of the columbianetin after oral dosing was 60–90 min and were 2.5–3.3 fold longer than those observed for the i.v. dosing.

Conclusions

The pharmacokinetic properties of columbianetin in rat after oral administration were characterized as rapid oral absorption, quick clearance and good absolute bioavailability. The bioavailability of columbianetin ranged from 54 to 81% for 5, 10 and 20 mg kg⁻¹ oral doses. The bioavailability of columbianetin is independent of the doses studied. Columbianetin showed dose proportionality over the dose range 5–20 mg kg⁻¹. The results clearly demonstrated that columbianetin was one of the material bases of RAP. Furthermore, an HPLC method was demonstrated in this study for the research of traditional Chinese medicine.     

刺五加注射液中3个主要活性成分与相应单体在大鼠体内的药动学比较

研究刺五加注射液中3个活性成分,紫丁香苷、刺五加苷E及异嗪皮啶在大鼠体内的药动学行为,并与相应单体分别经静脉注射给药后大鼠体内药动学行为比较。将24只雄性大鼠随机分为4组,分别经静脉注射给予紫丁香苷、刺五加苷E、异嗪皮啶及相当剂量的刺五加注射液。采用液相色谱-串联四级杆质谱（liquid chromatography tandem mass spectrometry,LC-MS/MS）法测定不同时间点血浆中紫丁香苷、刺五加苷E及异嗪皮啶的浓度并采用DAS 2.0 数据处理软件及SPSS 17.0 统计软件分别进行药动学参数计算及比较。静脉给药后,3种单体成分与刺五加注射液主要药动学参数如血药浓度-时间曲线下面积（AUC）、血浆清除率（CL）、消除半衰期（t_1/2）等存在显著性差异（P<0.05）。刺五加注射液中紫丁香苷AUC较单体给药组明显增大,CL较单体给药组明显减小;刺五加苷E的AUC较单体给药组明显减小,CL较单体给药组明显增大;注射液中异嗪皮啶较单体给药组t_1/2延长。可见与单体给药相比,刺五加注射液中紫丁香苷、刺五加苷E及异嗪皮啶大鼠体内的代谢动力学过程存在差异。刺五加注射液中的其他共存成分可能对单个有效成分的主要药动学参数产生影响。     

栀子与柴芩承气汤中栀子苷在大鼠体内的药动学比较

目的:研究中药配伍对栀子苷在大鼠体内药动学的影响。方法:血浆样本采用70℃水浴法沉淀蛋白后进行HPLC分析,色谱条件:固定相为Dikma,Diamonsil,C18(5μm,150×4.6mm);流动相为甲醇-0.2%乙酸(28:72,v/v),流速:1ml/min;检测波长:240nm;以芍药苷为内标进行定量。结果:线性范围0.025~2.5μg/ml(r=0.9998),最低检测浓度0.025μg/ml,回收率分别为97.60%,98%,99.2%;日内和日间精密度RSD均小于10%。大鼠灌胃栀子和柴芩承气汤后的药动学行为均符合一室模型,栀子苷在柴芩承气汤和单味栀子给药情况下药动学参数T1/2,Cmax和AUC0-24有明显差别(P<0.05)。结论:栀子和柴芩承气汤复方在同一给药途径下,栀子苷在柴芩承气汤中比单味栀子的消除半衰期长,达峰时间长,消除速率慢,生物利用度比单味栀子给药高。     

Effects of aqueous extract of Sophora flavescens on the expression of cell cycle regulatory proteins in human oral mucosal fibroblasts

Sophorae Radix, the dried roots of Sophora flavescens AITON (Leguminosae), has been used in Oriental traditional medicine for treatment of skin and mucosal ulcers, sores, gastrointestinal hemorrhage, diarrhea, inflammation and arrhythmia. In the present study, we examine the effect of the aqueous extract of Sophorae Radix (AESR) on cell proliferation and cell cycle regulation in human oral mucosal fibroblasts (HOMFs). To study the molecular mechanisms of cell cycle regulation by AESR, we also measured the intracellular levels of cell cycle regulatory proteins such as cyclin D, cyclin-dependent kinases (CDK)-4, CDK-6, cyclin E, CDK-2, p53, p21WAF1/CIP1 and p16INK4A. Cell proliferation was increased in the presence of 10 approximately 500 microg/ml of AESR. Maximal growth stimulation was observed in those cells exposed to 100 microg/ml of AESR. Exposure of HOMFs to 100 microg/ml of AESR resulted in an increase of cell cycle progression. The levels of cyclin E and CDK-2 were increased in HOMFs after 100 microg/ml of AESR treatment, but the levels of cyclin D, CDK-4, and CDK-6 were unchanged. After exposure to 100 microg/ml of AESR, the protein levels of p16INK4A and p53 were decreased as compared to that of the control group, but the level of p21WAF1/CIP1 was similar in the cells treated with 100 microg/ml of AESR and untreated cells. The results suggest that AESR may increase cell proliferation and cell cycle progression in HOMFs, which is linked to increased cellular levels of cyclin E and CDK-2 and decreased cellular levels of p53 and p16INK4A. Further studies are necessary to clarify the active constituents of AESR responsible for such biomolecular activities.     

疏肝健脾方醇水双提物对CCl_4诱导的肝纤维化大鼠的保护作用

目的探讨疏肝健脾方(柴胡、黄芪、白芍、白术等)醇水双提物对四氯化碳诱导肝纤维化大鼠的保护作用。方法除正常组外,其余各组采用皮下注射50%四氯化碳,每周2次,持续12周,复制肝纤维化大鼠模型。造模后第7周,分别灌胃给予疏肝健脾方醇水双提物(1.5、3.0、6.0 g/kg)剂量组和阳性药秋水仙碱组,每天1次,连续6周。实验结束后,Masson染色观察肝脏组织胶原沉积;放射免疫法检测血清中透明质酸(hyaluronic acid,HA)、层黏蛋白(laminin,LN)、Ⅲ型前胶原肽(procollagen-Ⅲ-peptide,PⅢNP)、Ⅳ型胶原(collagen typeⅣ,Ⅳ-C)的水平;免疫组化染色检测α-平滑肌肌动蛋白(α-smooth muscle actin,α-SMA)、Ⅰ型胶原(collagen typeⅠ,COL-Ⅰ)的表达。结果与模型组比较,疏肝健脾方醇水双提物不仅可减轻胶原纤维的沉积,改善肝纤维化损伤程度,还可显著降低血清中透明质酸、层粘蛋白、Ⅲ型前胶原肽、Ⅳ型胶原的水平,抑制肝组织中α-平滑肌肌动蛋白、Ⅰ型胶原蛋白的表达。结论疏肝健脾方醇水双提物对化学性肝纤维化大鼠具有很好的抗肝纤维化作用,其可能机制与抑制肝星状细胞活化、减少细胞外基质的合成有关。     

盐酸川芎嗪滴眼液在兔眼房水中的药动学研究

目的 探讨兔眼局部应用盐酸川芎嗪滴眼液后在房水中的药代动力学特征.方法 将新西兰白兔27只,随机分为9组,分别于兔眼滴入盐酸川芎嗪滴眼液50 μL,并于不同时间点抽取房水.采用高效液相色谱法测定盐酸川芎嗪浓度,DAS2.1.1软件拟合药代动力学参数.结果 兔眼滴用盐酸川芎嗪后,盐酸川芎嗪在房水中的浓度变化呈二室模型,盐酸川芎嗪在房水中的药代动力学参数分别为达峰浓度(Cmax),( 16.202±2.564) μg/mL;达峰时间(Tmax),0.083 h;吸收相半衰期(t1/2α),(0.509±0.179)h;消除相半衰期(t1/2β),(0.857±0.278)h;曲线下面积(AUC),(14.584±2.950)μg·h/mL.结论 盐酸川芎嗪滴眼后能快速渗透到房水中,且浓度较高,但消除也较快.     

红芪对血液流变性的影响

目的：研究红芪对血液流变性的影响。方法：采用正常、寒凝血瘀(肾上腺素 冰水应激)、气虚血瘀(灌服番泻叶)模型大鼠,观察红芪醇提物和水提物对血液粘度、血沉、红细胞压积、电泳时间等血液流变学指标影响,并考察其对ADP诱导家兔体外血小板聚集的影响。结果：红芪醇提物可明显降低正常大鼠高切(80s^-1)和低切(20s^-1)下全血比粘度,红芪水提物可明显减轻正常大鼠体外血栓的干重,显降低肾上腺素加冰水浴所致血瘀模型大鼠体外血栓湿重及干重,对血栓长度、全血比粘度及血沉等指标有一定抑制趋势;二均可明显降低番泻叶所致气虚血瘀模型大鼠红细胞压积。缩短其红细胞电泳速率;体外125、250、500μm／m1可剂量依赖性地抑制ADP引起的家兔血小板聚集。结论：红芪具有一定活血化瘀作用。     

注射用炎琥宁对脂多糖发热模型家兔解热机制的研究

目的 研究注射用炎琥宁对脂多糖发热模型家兔血清中细胞因子（TNF-α、IL-1β、IL-6、cAMP、PGE2）和下丘脑中升温介质（cAMP、PGE2）的影响。方法 建立家兔脂多糖（10 EU/kg）发热模型,监测不同时间点注射用炎琥宁对脂多糖发热模型家兔体温影响,绘制平均升温曲线;模型升温峰值时收集指标,ELISA法检测血清中细胞因子、下丘脑中升温介质变化。结果 注射用炎琥宁能显著降低脂多糖发热模型家兔的体温,且量效关系较显著;注射用炎琥宁能显著抑制发热模型家兔血清中IL-6、cAMP、PGE2增加和下丘脑中cAMP、PGE2的释放。结论 注射用炎琥宁对脂多糖发热模型家兔有较好的解热作用,其解热效果可能与其抑制外周IL-6、cAMP、PGE2增加和下丘脑cAMP、PGE2释放有关。     

槲皮素对乳腺癌细胞MCF-7增殖及凋亡的影响

槲皮素具有广泛的生理及药理活性 [1] ,因其扩张冠脉、调血脂、降低血管通透性被作为心血管药物而在临床广泛应用。已有文献报道槲皮素在体外对肿瘤的化学预防和治疗作用及其机制[2 ,3 ] 。此前 ,已对槲皮素抑制 DMBA (二甲基苯并蒽 )诱导的 SD大鼠乳腺癌的发生及增殖进行了研究并探讨机制 [4,5]。本实验采用 ER(雌激素受体 )阳性的乳腺癌细胞株 MCF- 7,初步观察槲皮素在体外对该细胞增殖、凋亡及细胞周期的影响 ,为进一步探讨其作用机制及其应用于临床治疗乳腺癌提供部分依据。1　材料与方法1 .1　药物与细胞系 :Quercetin (槲皮素 ,…     

基于蛋白质组学分析栀子水提液肝损伤时-毒关系及其机制

研究栀子水提液致大鼠肝毒性的时-毒关系及其作用机制。大鼠随机分为C组(0 d),D5组(5 d),D12组(12 d),D19组(19 d),D26组(给药19 d停药7 d)。各组灌胃给予对应时长栀子水提物,给药剂量为10 g·kg^-1,C组给予等量生理盐水。各组末次给药后麻醉大鼠,摘取肝脏,苏木精-伊红(hematoxylin-eosin,HE)染色法观察肝脏形态变化。提取肝脏蛋白,Nano-ESI液相-质谱联用系统检测蛋白,Protein Discovery软件鉴定蛋白,SIEVE软件对蛋白进行相对定量定性分析,基于STRING构建蛋白互作(protein-protein interaction,PPI)网络,使用Cytoscape软件对差异蛋白进行聚类分析。Kyoto encyclopedia of genes and genomes(KEGG)数据库对聚类蛋白进行富集信号通路分析。将筛选的差异蛋白表达与肝脏病理等级评分结果进行Pearson相关性分析。结果发现D5组、D12组、D19组大鼠肝损伤程度均显著高于C组,D5组肝损伤程度略高于D12组、D19组,D26组与C组无显著差异。蛋白质组学筛选重点差异蛋白147个,主要形成6大聚类,涉及主要通路5条,包括药物代谢通路、视黄醇代谢通路、蛋白酶体、氨基酸的生物合成通路以及糖酵解/糖异生通路。Pearson相关分析发现不同给药时间差异蛋白表达与肝脏病理程度的变化具有一定的时序关系。上述结果表明由栀子引起的肝损伤程度并不随着给药时间增加而增加,停止给药后可恢复正常。以上通路可能与栀子水提液致肝损伤作用机制相关。     

五指毛桃水提物对免疫抑制小鼠细胞免疫的影响

目的:研究五指毛桃水提物对免疫抑制小鼠细胞免疫的影响。方法:取小鼠50只,随机分为生理盐水对照组、环磷酰胺模型组、五指毛桃水提物组(6.6 g/kg、4.4 g/kg、2.2 g/kg),通过腹腔注射环磷酰胺制备免疫功能低下小鼠模型,连续灌胃给药14d后,测定各组小鼠的脾脏指数、巨噬细胞吞噬功能、T淋巴细胞的增殖能力和杀伤活性、T细胞亚群比例及血清IL-1、INF-γ的含量。结果:五指毛桃水提物组(6.6 g/kg、4.4 g/kg)可明显提高环磷酰胺免疫抑制小鼠的脾脏指数,明显增强巨噬细胞吞噬功能、T淋巴细胞的增殖能力和杀伤活性,增加T细胞亚群数量及IL-1、INF-γ的含量。结论:五指毛桃水提物能够提高免疫抑制小鼠的免疫功能,其机制与调节机体细胞免疫作用相关。     

木香中主要活性成分的药代动力学研究

目的建立高效液相色谱测定大鼠血样中木香烃内酯及去氢木香内酯药物浓度的分析方法。方法以穿心莲内酯为内标物,血样采用甲醇沉淀蛋白,色谱条件采用反相色谱柱Agilent C18,流动相体系0.1%甲酸水(A)-甲醇(B)(35∶65),检测波长设置为225 nm,对大鼠口服给予木香提取物后木香烃内酯、去氢木香内酯血药浓度进行测定。结果血浆样品中2种倍半萜内酯类成分在0.05～10.00μg/mL浓度范围内线性关系良好,且精密度、稳定性及提取回收率实验结果表明该类成分血药浓度的测定方法稳定可靠。结论高效液相色谱法测定木香提取物口服给药后倍半萜内酯类成分木香烃内酯及去氢木香内酯的药代动力学过程简便、可靠,为揭示中药木香中主要成分的体内代谢过程提供了依据。     

The hypoglycaemic and antihyperglycaemic effect of citrullus colocynthis fruit aqueous extract in normal and alloxan diabetic rabbits

Effects of the aqueous, glycosidic, alkaloidal and saponin extracts of the rind of Citrullus colocynthis on the plasma glucose levels were investigated in normal rabbits, while the effects of saponin extract on the fasting plasma glucose levels were studied in alloxan induced diabetic rabbits. In normal rabbits, oral administration of aqueous extract (300 mg/kg) produced significant reduction in plasma glucose after 1 h and highly significant after 2,3 and 6 h. Phytochemical screening revealed that the rind of C. colocynthis and its aqueous extract contains tertiary and quaternary alkaloids, glycoside and saponin components. The hypoglycaemic effects of these components given orally at a dose (50 mg/kg) were studied in normoglycaemic rabbits. Result showed that the alkaloidal extract did not significantly lower the blood glucose levels from 132 mg/100 ml at 0 h to 120 mg/100 ml after 6 h, while the glycosidic extract significantly lowered the fasting glucose levels after 2 and 3 h and highly significant after 6 h. The effect was more pronounced with saponin extract, the saponin significantly lowered the fasting glucose levels after 1 and 2 h and highly significant (P<0.001) after 3 and 6 h. Graded doses (10, 15 and 20 mg/kg) of saponin extract, when given orally to alloxan diabetic rabbits, produced a significant reduction of plasma glucose concentration. These results suggest that the aqueous extract of the rind of C. colocynthis possesses a hypoglycaemic effect and its hypoglycaemic action could be attributed for more extent to the presence of saponin in addition to the presence of glycosidic components.