水龙骨镇痛抗炎有效部位的筛选

目的:观察水龙骨提取物各极性部位的镇痛抗炎效果.方法:镇痛实验采用小鼠扭体法和小鼠热板法,抗炎实验采用二甲苯致鼠耳肿胀法和角叉菜胶致大鼠足趾肿胀法.结果:水龙骨提取物的A部分对二甲苯所致的小鼠耳廓肿胀以及角叉菜胶所致的大鼠足肿胀的抑制作用最强,能明显地抑制小鼠的化学性或物理性疼痛.结论:水龙骨大孔树脂25%乙醇洗脱部分应为抗炎镇痛的有效部位.     

正交试验优化冬凌草中冬凌草甲素的提取工艺

目的:进行冬凌草甲素的提取工艺筛选和含量测定,为其临床应用及生产提供实验依据。方法:以正交试验筛选冬凌草甲素的提取工艺,采用HPLC法测定冬凌草甲素的含量。结果:优选冬凌草甲素的提取工艺为75%乙醇回流提取2次(1 h,1 h),以药材质量2%的活性炭脱色10 min。结论:该提取工艺得到的冬凌草甲素含量较高且提取时间较短,经HPLC法检测冬凌草甲素,重现性好,回收率高。     

三种红毛七提取物的抗炎镇痛作用实验研究

目的初步探讨红毛七的乙醇、氯仿和正丁醇提取物的抗炎、镇痛作用,以了解红毛七产生镇痛抗炎作用的有效成分。方法取红毛七的乙醇、氯仿和正丁醇提取物,应用大鼠足跖肿胀法、小鼠耳廓肿胀法及小鼠去除双侧肾上腺素耳廓肿胀法、小鼠扭体法和热板法研究其抗炎镇痛作用。结果红毛七的乙醇和氯仿提取物对蛋清所致大鼠足趾肿胀有明显抑制作用;红毛七的乙醇、正丁醇提取物对二甲苯引起的耳廓肿胀有明显抑制作用;但对去除双侧肾上腺素的小鼠耳廓肿胀无明显作用;红毛七的乙醇、氯仿和正丁醇提取物能减少醋酸所致的小鼠扭体次数,延长小鼠热痛阈值。乙醇提取物的作用强于其他有机提取物。结论红毛七乙醇提取物有明显的抗炎、镇痛作用。     

仙鹤草提取物镇痛抗炎试验的实验研究

目的:初步探讨中药仙鹤草提取物的镇痛抗炎作用.方法:取仙鹤草的水提取物和乙醇提取物,应用醋酸致小鼠扭体法、小鼠热板法、二甲苯致小鼠耳廓肿胀法和大鼠角叉菜胶足跖肿胀法研究其镇痛抗炎作用.结果:仙鹤草乙醇提取物和水提起物可减少醋酸致小鼠扭体次数,延长小鼠舔足时间,减轻二甲苯致小鼠耳廓肿胀程度,减小角叉菜胶致足跖肿胀程度;乙醇提取物作用强于水提取物.结论:中药仙鹤草乙醇提取物具有明显的镇痛抗炎作用.     

正交试验优化冬凌草冷浸提取工艺

目的探讨冷浸法提取冬凌草的最佳工艺条件。方法采用高效液相色谱法(HPLC)测定冬凌草甲素的含量,考察不同浓度乙醇对冬凌草甲素提取率的影响。在此基础上,选取乙醇用量、冷浸时间、提取次数和药材规格4个因素进行正交设计优化。结果乙醇用量、冷浸时间、提取次数和药材规格对冬凌草甲素的提取效果均有显著影响,最佳提取工艺:冬凌草粉碎成细粉,加入15倍量体积分数95%乙醇,冷浸提取2次,每次4 d。结论此工艺条件简单易行,适用于冷浸法提取冬凌草。     

苦玄参叶抗炎药理作用研究

目的研究苦玄参叶抗炎药理作用。方法采用小白鼠二甲苯耳廓肿胀法、抑制小白鼠腹腔毛细血管通透性实验法和小白鼠鸡蛋清足跖肿胀法。结果苦玄参叶60%乙醇提取物对冰醋酸引起小白鼠腹部毛细血管通透性增加、二甲苯所致的小白鼠耳肿胀、小白鼠蛋清足跖肿胀均具有抑制作用。结论苦玄参叶有明显的抗炎作用。     

半边莲不同提取物镇痛抗炎作用

目的研究半边莲不同溶剂提取物的镇痛抗炎作用。方法制备半边莲水提取物和75%乙醇提取物,采用醋酸扭体实验和热板实验测定半边莲提取物镇痛作用,二甲苯致小鼠耳廓肿胀实验和10%蛋清致小鼠足跖肿胀实验测定半边莲提取物抗炎作用。结果半边莲水提取物可明显抑制醋酸所致小鼠扭体反应（P＜0.01）;给予半边莲水提取物和醇提取物1,2 h,小鼠热板痛阈值明显提高（P＜0.05或P＜0.01）;半边莲提取物能抑制二甲苯所致小鼠耳廓肿胀（P＜0.05或P＜0.01）;半边莲提取物在致炎后0.5,1,2,4 h能显著抑制10%蛋清所致小鼠足跖肿胀（P＜0.05或P＜0.01）。结论半边莲提取物有明显的镇痛和抗炎作用。     

东北贯众抗炎镇痛作用有效部位研究

目的:确定东北贯众抗炎镇痛作用的有效部位,为进一步研究东北贯众抗炎镇痛作用的活性成分奠定基础.方法:热板法测定痛阈值,观察其镇痛作用;二甲苯诱发小鼠耳廓肿胀及甲醛致足跖肿胀观察其抗炎作用,研究东北贯众抗炎镇痛的有效部位.结果:东北贯众对小鼠热板致痛、二甲苯所致的小鼠耳肿胀及甲醛致小鼠足跖肿胀均有一定的抑制作用,且30%...     

金玄痔科熏洗散与其有效部位新制剂的抗炎镇痛作用比较

目的:比较金玄痔科熏洗散有效部位新制剂与原制剂的抗炎镇痛作用,以期为该传统中药制剂点的工艺改革提供实验依据。方法:采用二甲苯所致小鼠耳廓肿胀,蛋清所致大鼠足跖肿胀等急性炎症模型,比较观察金玄痔科熏洗散有效部位新制剂与原制剂的抗炎作用;采用热板至痛实验观察其镇痛作用。结果:金玄痔科熏洗散有效部位新制剂能明显抑制二甲苯所致小鼠耳郭肿胀和蛋清所致大鼠足跖肿胀;明显提高热板所致小鼠的痛阈。结论:金玄痔科熏洗散有效部位新制剂的抗炎镇痛作用优于原制剂,且具有有效物质基础明确、质量控制标准完善、临床使用剂量减少等优势。     

一口钟提取物治疗大鼠佐剂性关节炎研究

目的 探讨一口钟不同溶剂提取物对大鼠佐剂性关节炎的治疗作用。方法 采用不同有机溶剂对一口钟进行提取,得到各溶剂的提取物。将70只雄性Wistar大鼠随机分为正常组、模型组、石油醚组、三氯甲烷组、乙酸乙酯组、95%乙醇组和5%乙醇组各10只;正常组大鼠左后足跖皮内注射0.9%氯化钠注射液,每只0.1 mL;其他各组大鼠左后足跖皮内注射弗氏完全佐剂,每只0.1 mL。实验第10天,正常组和模型组给予0.9%氯化钠注射液灌胃,其他各组分别灌胃给予一口钟不同溶剂提取物,均0.5 mL•（200 g） 1,连续16 d。检测各组大鼠足跖肿胀、脾脏指数、胸腺指数及血清一氧化氮含量。结果 除一口钟石油醚提取物组外,与模型组比较,其他各提取物均能显著抑制大鼠左后足跖肿胀;一口钟不同溶剂提取物组大鼠胸腺指数、脾脏指数均显著增高,血清一氧化氮浓度显著降低。结论 一口钟提取物对大鼠佐剂性关节炎有显著治疗作用,推测一口钟治疗佐剂性关节炎有效部位为脂溶性成分。     

广西莪术抗血栓作用有效部位的筛选

目的：观察广西莪术经大孔树脂不同洗脱部位的抗血栓作用。方法：采用断尾法测定小鼠出血时间;玻片法测定小鼠凝血时间;胶原蛋白-肾上腺素诱发小鼠体内血栓形成模型;大鼠体内静脉血栓形成模型,观察抗血栓作用。结果：广西莪术50%乙醇洗脱部位、70%乙醇洗脱部位能明显延长小鼠出血时间和凝血时间;明显抑制胶原蛋白-肾上腺素诱发的小鼠体内血栓形成;明显减轻大鼠体内静脉血栓湿质量。结论：广西莪术50%乙醇洗脱部位、70%乙醇洗脱部位具有明显的抗血栓作用。     

Oridonin induced A375-S2 cell apoptosis via bax-regulated caspase pathway activation, dependent on the cytochrome c/caspase-9 apoptosome

Two diterpenoids, oridonin (1) and ponicidin (2), were isolated from the 95% ethanol extract of Rabdosia rubescens and were evaluated for antiproliferative activity on cancer cells and human peripheral blood mononuclear cells (PBMC) in vitro. Oridonin has much more potent cytotoxic effects on four tumor cells (human melanoma A375-S2, human cervical cancer HeLa, human breast adenocarcinoma MCF-7, murine fibrosarcoma L929) than does ponicidin. The growth-inhibitory activity of oridonin for A375-S2 cells was more potent than that for the other cell lines, with an IC₅₀ of 15.1±1.2 μmol L^-1. Treatment with oridonin (34.3 μmol L_-1) for 12 h significantly inhibited A375-S2 cell growth, and showed weaker cytotoxicity against PBMC. By contrast, ponicidin markedly inhibited the growth of PBMC under the same conditions. When caspases-3 and -8 were activated at early stages after treatment of A375-S2 cells with oridonin (34.3 μmol L_-1), apoptotic bodies were formed, nuclear damage was observed by Hoechst 33258 staining and DNA fragmentation was exhibited. In addition, oridonin increased the expression of the apoptosis inducer, Bax, promoted the release of cytochrome c without affecting Bcl-2 expression, and activated down-stream caspase-9 in the mitochondrial pathway. These observations indicated that an appropriate dose of oridonin gave an initial premitochondrial phase that involved the Bcl-2 family of the pro-apoptotic protein Bax that required the participation of caspase-9 and caspase-3. However, on treatment with oridonin (137.4 μmol L_-1) for 12 h, the majority of A375-S2 cells underwent necrosis as measured by an LDH activity-based assay. Our results suggest that oridonin induces A375-S2 cell death on the balance of apoptosis and necrosis.     

黄芩抗乙酰胆碱酯酶活性部位的RRLC-DAD-ESI-MS/MS分析

目的：筛选黄芩体外抑制乙酰胆碱酯酶（AChE）的活性部位，并对其化学成分进行分析。方法：黄芩提取物经反相C₁₈填料进行固相萃取（SPE）制备不同浓度甲醇醇梯度洗脱部位，以体外抑制AChE能力评价其抗阿尔茨海默症（AD）作用，采用高分离快速液相色谱-质谱联用技术（RRLC-MS/MS）对黄芩抑制AChE活性部位化学成分进行分析。结果：黄芩提取物的50%甲醇洗脱部位的AChE抑制活性明显强于其他洗脱部位并存在明显的量效关系，为其体外抑制的活性部位，经液质联用分析共鉴定出15种化合物。结论：黄芩具有体外抑制AChE活性，其主要有效部位为50%甲醇洗脱部位，其主要有效成分为黄芩苷为代表的黄酮类成分。     

雪荔组方总黄酮有效部位胶囊的制备和体外溶出评价

目的：研究雪荔组方有效部位的制剂工艺,并对体外溶出情况进行考察。方法：以辅料的种类、内容物的吸湿性、流动性和乙醇的浓度为考察指标,研究雪荔组方有效部位胶囊的制剂工艺;采用HPLC法以高车前苷、高车前素为指标,对其体外溶出度进行考察。结果：制得胶囊外观整洁,无粘结、变形、渗漏或囊壳破裂现象。药物在60 min 内体外溶出达90.0% 左右。胶囊中高车前苷的溶出趋向于Weibull分布模型、高车前素的溶出趋向于Higuchi方程。结论：本法研制的雪荔组方有效部位胶囊,工艺合理可行,且溶出符合要求。     

大孔吸附树脂联用硅胶柱层析法分离纯化冬凌草甲素

目的:建立大孔吸附树脂联用硅胶柱层析法分离纯化冬凌草甲素的工艺流程。方法:将冬凌草粉碎,用95%乙醇提取,浓缩成浸膏;以冬凌草甲素含量为指标,采用大孔吸附树脂联用硅胶柱层析法分离纯化冬凌草甲素,并用红外光谱、熔点测定和高效液相色谱(HPLC)法对重结晶产品的纯度和结构进行分析和表征。结果:优化的工艺为采用苯乙烯型大孔吸附树脂(HZ-841)先对浸膏进行粗分离,再选取乙酸乙酯-石油醚(6:4,V/V)为洗脱溶剂,石油醚-丙酮(2:3,V/V)为重结晶溶剂进行硅胶柱分离纯化,在此条件下,得到的冬凌草甲素含量为96.11%,提取率达到0.86‰。结论:所选工艺简单、可行,使用溶剂安全、无毒,提取效率高,可用于分离纯化冬凌草甲素。     

大孔吸附树脂纯化新疆大叶补血草根茎中总黄酮工艺考察

目的:利用大孔吸附树脂纯化新疆大叶补血草根茎中的总黄酮。方法:通过比较10种大孔吸附树脂对新疆大叶补血草根茎提取物中黄酮类化合物的吸附和解吸性能,综合考察不同类型的吸附树脂对总黄酮的吸附和解吸效果。结果:HPD100型大孔吸附树脂对新疆大叶补血草根茎提取物中的总黄酮具有较强的吸附性能和较好的解吸能力。当总黄酮上样质量浓度为0.25 mg·ml^-1,上样量为树脂体积的1.8倍(1.8 BV),吸附平衡后,先用2~3 BV纯化水洗去水溶性较大的成分,再用2.1 BV的70%乙醇洗脱,分段收集,可获得总黄酮含量为(43.26±2.33)%(n=5)的有效部位。结论:HPD100型大孔吸附树脂可以作为纯化新疆大叶补血草根茎提取物中的总黄酮的材料。     

多指标正交试验优选丹参黄连的提取工艺

目的: 优选丹参黄连提取工艺。方法: 采用正交设计,以丹酚酸B、丹参酮Ⅱ_A和表小檗碱、黄连碱、巴马汀、小檗碱4种生物碱总量的质量分数和干膏得率为评价指标,用高效液相色谱法测定其含量,对提取工艺中乙醇体积分数、乙醇用量、提取次数、提取时间4个因素进行考察,采用综合加权评分法处理数据。结果: 优选工艺:加70%乙醇10倍量,回流提取3次,每次0.5 h。结论: 优选所得的工艺合理可行,可作为丹参黄连的提取工艺。     

Alkaloid and flavonoid rich fractions of fenugreek seeds (Trigonella foenum-graecum L.) with antinociceptive and anti-inflammatory effects

The seeds of fenugreek (Trigonella foenum-graecum L.) have medicinal uses as hypoglycemic, antinociceptive and anti-inflammatory agents. We aimed to evaluate the antinociceptive and anti-inflammatory effects of the major fractions of fenugreek seeds. The methanolic extract of the plant seeds was partitioned using a liquid–liquid extraction procedure to give six major fractions. Following phytochemical screening of isolated fractions, the total extract and each fraction were evaluated for their antinociception and anti-inflammatory effects using formalin and carrageenan-induced paw edema tests respectively. The methanolic extract exhibited both antinociceptive and anti-inflammatory effects at a dose of 100 mg/kg. Among the tested fractions, alkaline chloroform fraction (AKC), which was alkaloid positive in screening tests, showed the most anti-nociceptive effect in a dose-dependent manner. AKC fraction was as effective as morphine (5 mg/kg) in this regard. Both aqueous and acidified chloroform fractions (ACC) could significantly inhibit paw edema at a different dose. The latter fraction dose-dependently inhibited carrageenan-induced paw edema. The results of phytochemical screening tests confirmed the presence of flavonoids in both ACC and aqueous fractions. It can be concluded that the alkaloid and flavonoid content of fenugreek seeds can be responsible for antinociception and anti-inflammatory effects of the plant respectively.     

Oridonin induces human epidermoid carcinoma A431 cell apoptosis through tyrosine kinase and mitochondrial pathway

Oridonin, a diterpenoid isolated from the plant Rabdosia rubescens, induces human epidermoid carcinoma A431 cell death through apoptosis and tyrosine kinase pathway. To examine the pathway of oridonin-induced A431 cell death, morphologic observation, lactate dehydrogenase activity-based assay, DNA agarose gel electrophoresis and Western blot analysis were carried out. When A431 cells, which overexpress epidermal growth factor receptor (EGFR), were treated with oridonin, caspase-3 was activated followed by the degradation of caspase-3 substrates, inhibitor of caspase-activated DNase (ICAD) and poly(ADP-ribose) polymerase (PARP) in a time-dependent manner. Oridonin promoted the release of cytochrome c and the down-regulation of mitochondrial transmembrane potential (ΔΨm). Oridonin up-regulated the expression ratio of mitochondrial proteins, Bax/Bcl-2. In addition, the total tyrosine kinase activity of A431 cellular proteins and the expression of EGFR were markedly reduced after oridonin treatment. Taken together, oridonin induced apoptosis in A431 cells via mitochondrial pathway, activation of caspase-3 and inhibition of tyrosine kinase activities.