四逆汤类方不同工艺及配伍提取物对小鼠脾细胞增殖的影响

目的:观察四逆汤类方不同工艺、不同配伍提取物对小鼠脾淋巴细胞增殖的影响。方法:采用小鼠脾淋巴细胞为实验模型,MTT比色法测定细胞内线粒体脱氢酶活性。结果:与对照组比较,四逆汤类方乙醚提取物均有刺激脾淋巴细胞增殖的作用,与FGC1(四逆汤)组比较,FGR1(人参四逆汤)组作用显著低于FGC1组,四逆汤类方的乙醚提取物样品中,四逆汤的活性最强。四逆汤类方的氯仿提取物中,除FGB2(白通汤)组外,其它各组均无刺激脾淋巴细胞增殖的作用。四逆汤类方的水提取物,FGC3(四逆汤)和FGB3(白通汤)组有刺激脾淋巴细胞增殖作用。结论:四逆汤类方乙醚、氯仿和水提取物能刺激淋巴细胞增殖活性,醚提乙取物的活性较强,四逆汤类方的乙醚提取物样品中,四逆汤的活性最强。     

四逆汤对失血性休克大鼠心功能和血压调节的肾上腺素受体机制研究

 目的观察四逆汤对失血性休克大鼠心功能的保护作用及其机制探讨。方法以血流动力学为指标，观察四逆汤对失血性休克大鼠的治疗作用,及α和β受体阻断剂对其作用的影响。结果四逆汤能改善失血性休克大鼠的左心室收缩压(LVSP)、左心室等容期压力最大变化速率(±dp/dtmax)和平均动脉压(MAP)的降低，α和β受体阻断剂可不同程度地阻断四逆汤对失血性休克大鼠的保护作用。结论四逆汤对失血性休克大鼠有强心、升压作用，其作用机制可能与调节肾上腺素α和β受体有关。     

四逆汤抗失血性休克大鼠肠黏膜损伤 及菌群移位药效研究

目的:研究四逆汤对失血性休克大鼠肠黏膜损伤及肠道菌移位的影响。方法:动物分为空白组、失血性休克组、四逆汤高、低剂量组(按生药量计4.8,2.4 g.kg-1)。通过定血量放血建立大鼠失血性休克模型,观察复苏3 h后肠黏膜损伤程度,并取肝、脾、肾和肠系膜淋巴结进行细菌培养,测定肝门静脉血浆内毒素、动脉血浆D-乳酸(D-Lac)含量。并通过血浆肿瘤坏死因子-α(TNF-α)、总一氧化氮合酶(t-NOS)的测定进行作用机制的探讨。结果:四逆汤与模型组比较,肠黏膜病理学改变得到显著改善,细菌培养计数、内毒素及D-Lac含量显著减少。血浆t-NOS显著减少,TNF-α有降低趋势,四逆汤药效作用呈剂量依赖性增强。结论:四逆汤能够抑制肠道菌移位,减轻肠黏膜损伤。作用机制可能与抑制t-NOS,TNF-α有关。     

藏红花素对失血性休克所致脏器损伤大鼠的保护作用研究

目的探讨藏红花素对失血性休克所致脏器损伤大鼠的保护作用及其机制。方法应用简单随机分组法将100只实验用SD大鼠分为假手术组、失血性休克组、失血性休克+生理盐水组、失血性休克+藏红花素组,每组25只。失血性休克各组均采用颈动脉放血法制备失血性休克模型,术后各组大鼠均应用6%羟乙基淀粉溶液复苏,失血性休克+生理盐水组、失血性休克+藏红花素组在复苏时分别静脉给予生理盐水和藏红花素(60 mg/kg)。统计各组大鼠术后24 h存活率,记录术前、术后24 h各组大鼠的心率(HR)、平均动脉压(MAP)、血液pH值、血氧分压[p(O_2)]、血二氧化碳分压[p(CO_2)],检测术后24 h各组大鼠血尿素氮(BUN)、肌酐(Cr)、谷丙转氨酶(ALT)、谷草转氨酶(AST)、丙二醛(MDA)、谷胱甘肽(GSH)水平,计算各组大鼠肺组织湿/干比重(W/D)、肺组织定量评估指数(IQA),检测各组大鼠肝脏、肾脏、肺脏组织中髓过氧化物酶(MPO)活性。结果失血性休克+藏红花素组大鼠存活率显著高于失血性休克组和失血性休克+生理盐水组(P均0.05)。术后24 h,失血性休克组、失血性休克+生理盐水组、失血性休克+藏红花素组大鼠HR、MAP、血液pH值、p(O_2)均明显低于术前(P均0.05),p(CO_2)明显高于术前(P均0.05);术后24 h,失血性休克+藏红花素组大鼠的HR、血液pH值、p(O_2)均明显高于失血性休克组和失血性休克+生理盐水组(P均0.05),p(CO_2)明显低于失血性休克组和失血性休克+生理盐水组(P均0.05)。术后24 h,失血性休克组、失血性休克+生理盐水组、失血性休克+藏红花素组大鼠血清BUN、Cr、ALT、AST、MDA水平和W/D比值、IQA及肺组织、肾组织、肝组织中MPO活性均明显高于假手术组(P均0.05),但失血性休克+藏红花素组各指标均明显低于失血性休克组和失血性休克+生理盐水组(P均0.05);失血性休克组、失血性休克+生理盐水组、失血性休克+藏红花素组大鼠血清GSH水平明显低于假手术组(P均0.05),但失血性休克+藏红花素组各指标均明显高于失血性休克组和失血性休克+生理盐水组(P均0.05)。结论藏红花素可显著提高失血性休克大鼠24 h存活率,保护失血性休克所致脏器损伤,可能与抑制失血性休克后复苏期间氧化应激反应有关。     

人参四逆汤不同部分提取物对微循环的影响

目的:观察人参四逆汤各部分提取物对微循环的影响。方法:观察正常和肾上腺素致微循环障碍小鼠耳廓微循环的变化。结果:附子乙醚提取物加干姜乙醚提取物和干姜乙醚提取物均可增大小鼠耳廓微血管管径,增加微血管交叉点数,改善小鼠微循环,但对血液流态、血液颜色无明显影响。结论:附子乙醚提取物加干姜乙醚提取物对微循环有一定的改善作用。     

人参党参甘草对家兔晚期失血性休克的影响

人参、党参、甘草同属补气药。曾有人报导,狗在大失血休克时,立即用人参注射液静脉注射可使降至很低水平的血压稳固回升,延长动物存活时间。党参有扩张血管降低麻醉动物血压的作用,但在生脉散中,党参却是主药。而生脉散对狗失血性休克有升压作用。甘草酸钠使家兔血压上升.本实验拟探讨以上三种不同补气药对家兔晚期失血性休克的升压作用。     

四逆汤的药理研究进展

四逆汤是张仲景创制的著名方剂之一。药理研究表明,四逆汤及其加味人参四逆汤对动物的失血性休克、肠道因素引起的休克、内毒素性休克、纯缺氧性休克、橄榄油引起的栓塞性休克及因冠状动脉结扎所造成的心源性休克皆有显著对抗作用。四逆汤还有显著的强心作用;能增加冠脉血流量;对缺氧所致的异常心电图有一定的改善作用。四逆汤能兴奋垂体——肾上腺皮质的功能,又具有中枢性镇痛、镇静作用。毒性不大,组方精简合理。     

四逆汤对内毒素性休克大鼠脑组织肿瘤坏死因子-α及超氧化物歧化酶的影响

目的:以内毒素休克脑损伤的研究为切入点,对内毒素休克大鼠脑组织肿瘤坏死因子-α(TNF-α)及超氧化物歧化酶(SOD)含量的规律性变化进行分析,探求不可逆休克时微循环障碍的中枢变化过程,为急症救治技术提供新的途径。方法:选用体质量180-200g的6-8周龄SD大鼠72只,随机分为假手术组、模型组与四逆汤组,每组24只。建立内毒素休克大鼠模型,采用ELISA法测定脑组织TNF-α含量,分光光度法进行SOD定量测定,检测并分析各组大鼠脑组织1、2、3、6h不同时间段的TNF-α及SOD含量。结果:①内毒素休克后模型组大鼠脑组织中TNF-α含量于6h达峰值,模型组与假手术组比较各时间段均明显升高(P<0.01),四逆汤组与模型组3、6h时间段比较明显下降(P<0.05或P<0.01)。②内毒素休克后模型组大鼠脑组织中SOD含量于6h达峰值,模型组与假手术组比较各时间段均明显下降(P<0.01),四逆汤组与模型组1、2、3h时间段均明显升高,6h明显下降(P<0.05或P<0.01)。结论:四逆汤对内毒素休克大鼠脑损伤具有明显的保护效应,其机制可能是通过抑制促炎性细胞因子TNF-α和促进自由基清除剂SOD的合成,从...     

四逆汤及组方药提取物对内毒素血症大鼠血浆中血管活性物质和细胞因子含量的影响

目的观察四逆汤及其组方药提取物对内毒素血症大鼠血浆中6-酮-前列腺素 F_(1α)(6-keto-PGF_(1α)),血管紧张素Ⅱ(AgⅡ)、肿瘤坏死因子(TNF)、内皮素(ET)、血栓素 A_2(TXA_2)、前列环素(PGI_2)含量的影响。方法经四逆汤及其组方药提取物作用后,取内毒素休克模型大鼠的血浆,采用放射免疫法测定上述指标。结果与模型组比较,四逆汤提取物可以提高内毒素血症大鼠血浆中6-keto-PGF_(1α)含量及6-keto-PGF_(1α)/TXB_2比值,降低 ET、TNF 和 AgⅡ含量;甘草提取物可以提高内毒素血症大鼠血浆中6-keto-PGF_(1α)含量,降低 TNF 和 AgⅡ含量,但对 ET 含量没有显著影响;附子提取物可以提高内毒素血症大鼠血浆中6-keto-PGF_(1α)。含量,降低 ET、TNF 和 AgⅡ的含量;干姜提取物可以降低 AgⅡ的含量,但对 ET、TNF 和6-keto-PGF_(1α)含量没有显著影响;甘草加附子提取物可以显著提高内毒素血症大鼠血浆中6-keto-PGF_(1α)含量,降低 AgⅡ的含量,但对ET 和 TNF 含量影响不显著;干姜加附子提取...     

探讨四逆汤抗急性失血性休克的氧自由基、一氧化氮机制

目的：从整体初步探讨四逆汤(附子，干姜，炙甘草)抗失血性休克的氧自由基、一氧化氮机制。方法：复制急性失血性休克大鼠模型，分为假手术对照组；休克模型组；休克 生理盐水复苏组；休克 四逆汤复苏组。监测各组血压变化。测定休克前、休克lh、复苏后lh、复苏后3h血浆中的SOD(超氧化物歧化酶)活性、MDA(丙二醛)的含量，各组观察结束后血浆乳酸、NO(一氧化氮)含量。结果：四逆汤组与生理盐水相比较，复苏3h后，血中SOD活性明显升高(P＜0．01)，MDA明显降低(P＜0．01)，乳酸含量也显著下降(P＜0．01)、血中NO含量则明显升高(P＜0．01)，平均动脉血压也明显高于生理盐水组。结论：四逆汤通过清除氧自由基，减少体内乳酸的堆积，升高NO，改善机体微循环，维持机体复苏后的血压，理论了减轻了由于休克后缺血缺氧、体内乳酸的堆积、微循环功能障碍造成的不可逆性的休克。     

New evidences of antimalarial activity of Bidens pilosa roots extract correlated with polyacetylene and flavonoids

Bidens pilosa is among the several plants used in Brazil to treat malaria. It was demonstrated that crude extracts from roots prepared with 80% ethanol by percolation are active in vitro against Plasmodium falciparum and the activity is correlated with the presence of polyacetylene and flavonoids. This extract was submitted to column chromatography with ether and ether methanol (1:1) and two fractions, enriched in polyacetylene and flavonoids, respectively, were obtained. The extract and the fractions were assessed by HPLC/DAD analysis and antimalarial tests in vivo. Ethanol extract showed by HPLC the presence of several peaks for polyacetylene and flavonoids, compounds corresponding to quercetin-3,3'-dimethoxy-7-0-rhamnoglucopyranose and the acetylene 1-phenyl-1,3-diyn-5-en-7-ol-acetate, previously identified in this extract. The peaks for flavonoids were absent in ether fraction and those ones for polyacetylene in ether:methanol. In in vivo tests, ethanol extract caused 36% of reduction of parasitaemia at fifth day, and 29% at seventh day. Ether:methanol fraction caused 38% of reduction at fifth day but was inactive at day 7. The survival of the animals treated with 80% ethanol extract was higher than in the fractions. The results showed that the in vivo activity of ethanol extract depends on the presence of polyacetylene and flavonoids.     

Studies on diuretic and hypouricemic effects of Orthosiphon stamineus methanol extracts in rats

AIM OF THE STUDY: Orthosiphon stamineus (Labiatae) is a traditional folk medicine widely used in Southeast Asia for the treatment of several kidney disorders, gout and as a diuretic. This study was conducted to examine the diuretic and hypouricemic effects of Orthosiphon stamineus leaf extracts. MATERIALS AND METHODS: The diuretic effect of different methanol extracts was examined by treating different groups of Sprague-Dawley rats with single (2g/kg) oral doses of methanol and methanol:water (1:1) extracts. Hydrochlorothiazide (10mg/kg) was used as positive control in acute study. Methanol and methanol water (1:1) extracts at 0.5 g/kg were administered for a period of 7 consecutive days. Cumulative urine volume and electrolytes (Na+ and K+) concentrations at different time intervals were measured. On the other hand, hypouricemic activity of methanol:water extract (1:1) was experimented using different oral single doses (0.25, 0.5, 1 and 2g/kg). Allopurinol was used as positive control. Uric acid concentration in serum was analyzed by using RP-HPLC at 280 nm. RESULTS: Sodium and potassium excretion increased significantly (p<0.05 and <0.01) in the first 8h of treatment with a single dose (2g/kg) of the extracts in a pattern comparable to that of the known diuretic hydrochlorothiazide. Meanwhile, repeated administration of 0.5 g/kg methanol:water (1:1) extract showed a significant increase in urine volume (from day 3 to day 7) (p<0.01) and electrolytes excretion (Na+ and K+) from day 2 to day 7 (p<0.05 and <0.01). On the other hand, 0.5, 1 and 2g/kg of methanol:water (1:1) extract and the standard allopurinol reduced the serum urate level in hyperuricemic rats at hour 6. CONCLUSION: These results provided an evidence of the high tendency of methanol:water (1:1) extract of Orthosiphon stamineus towards diuretic and hypouricemic effects in rats.     

Synergistic effect of methanol extract of Abies webbiana leaves on sleeping time induced by standard sedatives in mice and anti-inflammatory activity of extracts in rats

During the determination of LD50 values of extracts of Abies webbiana, it was observed that the methanol extract (MEAW) produces sedation of animals. This led to investigation of the effect of MEAW on sleeping time in mice. When various doses of the methanol extract (100, 150, and 200 mg/kg body weight) were administered alone, no hypnotic activity was observed. However, these exhibited significant synergistic effects (P < 0.001) at those dose levels in mice when administered prior to the administration of standard sedatives (pentobarbitone sodium: 50 mg/kg and diazepam: 6 mg/kg, respectively). In addition anti-inflammatory effects of methanol, chloroform, and petroleum ether extracts of Abies webbiana leaves in rats were performed to assess scientific validity of the medicinal claim of Indian folk medicine. The effects of leaf extracts (methanol, chloroform, and petroleum ether) against inflammation were studied by carrageenan-induced paw edema model in rats. The methanol extract (400 mg/kg p.o.) of leaves of Abies webbiana showed the best significant anti-inflammatory activity as compared to that of diclofenac sodium (150 mg/kg p.o.). The LD50 values of methanol, chloroform, and petroleum ether extracts were found to be 986, 1387, and > 3200 mg/kg, respectively. Thus, the therapeutic index of methanol extract may be favorable to open a new vista on combination therapy of hypnotics and may also against inflammation.     

均匀设计法结合药效学指标优选金铁锁提取工艺

目的：针对抗炎、镇痛和急性毒性作用，优选金铁锁药材的最佳提取工艺条件，探讨几种浸出物量与药效学指标间关系。方法：采用均匀设计法，部分指标取相对水平，以抗炎、镇痛实验结果和LD₅₀作为评价指标，对金铁锁的提取工艺条件进行优选，同时测定干膏率、水浸出物、醋酸乙酯浸出物、乙醚浸出物。结果：最佳提取工艺为：8倍量pH 6～7的水回流提取2次，每次2 h；最佳提取工艺条件验证结果满意；干膏率、水浸出物、醋酸乙酯浸出物、乙醚浸出物与药效学指标不存在明显相关关系。结论：用均匀设计法结合药效学指标优选金铁锁提取工艺条件，具有与功能主治密切结合的特点，所得最佳提取工艺条件适合工业生产，且药效学验证结果较为稳定。研究结果还表明，所测定的几种浸出物均不宜作为与功能主治有关的质量控制指标。     

HIV-1 integrase inhibitory substances from Coleus parvifolius

For the purpose of discovering anti-HIV-1 agents from natural sources, water and EtOH extracts of 50 Thai plants were screened for their inhibitory activity against HIV-1 integrase (IN), an enzyme essential for viral replication. Of these plants, an EtOH extract of Coleus parvifolius Benth. (aerial parts) showed potent activity against HIV-1 IN with an IC50 value of 9.2 microg/mL. From this extract, 11 compounds were isolated and identified as luteolin 5-O-beta-d-glucopyranoside (1), luteolin (2), luteolin 7-methyl ether (3), luteolin 5-O-beta-d-glucuronide (4), 5-O-beta-d-glucopyranosyl-luteolin 7-methyl ether (5), rosmarinic acid (6), rosmarinic acid methyl ester (7), daucosterol (8), a mixture of alpha- and beta-amyrin (9, 10) and phytol (11). Of these compounds, rosmarinic acid methyl ester (7), rosmarinic acid (6), luteolin (2) and luteolin 7-methyl ether (3) exhibited inhibitory activities against HIV-1 IN with IC50 values of 3.1, 5.0, 11.0 and 11.0 microM, respectively. Among rosmarinic acid derivatives, the HIV-1 IN inhibitory activity increased in turn for a dimer (IC50 = 5.0 microM), a trimer (IC50 = 1.4 microM), and a tetramer (IC50 = 1.0 microM).     

桃仁提取物对不同病因所致大鼠血液循环障碍的影响

目的 研究桃仁提取物对寒凝血瘀证(寒证)和瘀热互结证(热证)大鼠血液循环障碍的不同药效.方法 80只大鼠随机均分为寒证对照组、寒证模型组、桃仁提取物(8 g/kg)组、川芎(8g/kg)阳性对照组,以及热证对照组、热证模型组、桃仁提取物(8 g/kg)组、丹参(14 g/kg)阳性对照组.分别采用全身低温冷冻和注射角叉菜胶法建立寒证、热证大鼠模型,造模同时各给药组每天ig给药1次,连续给药7d.检测微循环血流速率、全血黏度:取大鼠心、肺、肝、肾、牌进行组织病理学观察,病理图像分析软件测量微小血管管径,观察血栓、组织损伤等情况.结果 与模型组相比,桃仁提取物能明显加快寒证和热证大鼠的血流速率(P＜0.05),降低全血黏度(P＜0.05),使寒证大鼠小动脉收缩、热证大鼠小动脉舒张(P＜0.05);根据器官损伤严重度评分得知桃仁提取物可减轻寒证大鼠心、肺、肝、肾器官的损伤(P＜ 0.05),但仅能减轻热证大鼠的肾损伤(P＜0.05).结论 桃仁提取物能改善寒凝血瘀证和瘀热互结证大鼠的血液循环障碍;对不同证型大鼠小动脉的舒缩状态和心、肿、肝、肾的保护作用不同.     

Terminalia arjuna,an ayurvedic cardiotonic,increases contractile force of rat isolated atria

The direct effects of aqueous, ethanolic, chloroform and petroleum ether extracts of Terminalia arjuna (family: Combretaceae) bark, an ayurvedic remedy for cardiovascular disorders, were studied on isolated atria of rats. The aqueous extract produced a substantial positive inotropic effect (EC₅₀ = 0.25 mg/mL) but no change in the rate. The ethanol, chloroform and petroleum ether extracts all decreased the rate of contraction. A slight increase in force was seen with ethanol and chloroform extracts. Higher concentrations of the chloroform extract had a negative inotropic effect. The ethanol extract decreased the maximum following frequency of the left atria. It is concluded that Terminalia arjuna has a significant positive inotropic property on rat atria in vitro which could contribute to its efficacy in treating cardiovascular disorders.     

Protective effects of Ginkgo biloba, Panax ginseng, and Schizandra chinensis extract on liver injury in rats

This study investigated the effects of the combined extracts of Ginkgo biloba, Panax ginseng, and Schizandra chinensis at different doses on hepatic antioxidant status and fibrosis in rats with carbon tetrachloride (CCl4)-induced liver injury. Male Sprague-Dawley rats (n = 8-12 per group) were divided into the control, CCl4, CCl4 + silymarin (0.35%), CCl4 + low-dose herbal extract (0.24% of Ginkgo biloba, Panax ginseng, and Schizandra chinensis extract at 1:1:1; LE), and CCl4 + high-dose herbal extract (1.20% of the same herbal extract; HE) groups. Silymarin or herbal extract was orally given to rats a week before chronic intraperitoneal injection with CCl4 for 6 weeks. The pathological results showed that herbal extract suppressed hepatic bile duct proliferation, and low-dose herbal extract inhibited liver fibrosis. Hepatic superoxide dismutase (SOD) activity was lower in the CCl4 group, but there was no difference in the silymarin or herbal extract treated groups compared to the control group. Hepatic catalase activity and the ratio of reduced to oxidized glutathione were significantly higher (p < 0.05) in the HE group than those in the CCl4 group. Silymarin and herbal extract reversed the impaired hepatic total antioxidant status (p < 0.05). Herbal extract partially reduced the elevated hepatic lipid peroxides. Hepatic transforming growth factor-beta1 (TGF-beta1) level decreased significantly (p < 0.05) in the LE group. Therefore, high-dose herbal extract improved hepatic antioxidant capacity through enhancing catalase activity and glutathione redox status, whereas low-dose herbal extract inhibited liver fibrosis through decreasing hepatic TGF-beta1 level in rats with CCl4-induced liver injury.     

小蓟三萜类化合物成分的研究

对小蓟乙醇提取物中显示细胞毒活性的石油醚萃取部位进行化学成分的系统研究。运用正反相硅胶、凝胶、反相高效液相等色谱方法进行分离;应用NMR和MS等波谱学方法,并结合文献对照确定化合物结构。从小蓟乙醇提取物的石油醚萃取部位分离得到12个三萜类化合物,分别鉴定为羽扇豆醇乙酸酯(1),羽扇豆醇(2),羽扇豆酮(3),β-香树酯醇(4),伪蒲公英甾醇(5),伪蒲公英甾醇乙酸酯(6),蒲公英甾醇乙酸酯(7),marsformoxide B(8),α-香树酯酮(9),β-香树酯酮(10),蒲公英甾酮(11),伪蒲公英甾酮(12)。化合物3,5,7～12为首次从蓟属植物中分离得到。