Screening of Anti-inflammatory and Analgesic Parts of Ardisia gigantifolia stapf.and Its Toxicological Safety Study

[Objectives] To screen out the anti-inflammatory and analgesic parts of Ardisia gigantifolia stapf.and to explore the toxicological safety of each part.[Methods]The carrageenan-induced toe swelling experiment of mice,acetic acid-induced peritoneal capillary permeability experiment,pain writhing test,and mouse maximum tolerated dose experiment were carried out.Taking mouse toe swelling,capillary permeability,pain writhing reaction times,and animal death number as indicators,anti-inflammatory and analgesic effects were screened and toxicological safety was evaluated for petroleum ether,ethyl acetate,n-butanol and water parts of A.gigantifolia.[Results] The petroleum ether part of A.gigantifolia can significantly reduce the degree of carrageenan-induced toe swelling of(P < 0.05),significantly inhibit the glacial acetic acid induced capillary permeability of mice(P < 0.05) and the times of pain writhing of mice(P < 0.01),no death was observed in each group after 150-fold of clinical equivalent dose administration,and no abnormality was observed in body weight and tissues of mice.[Conclusions]The petroleum ether part of A.gigantifolia is active part of anti-inflammatory and analgesic effect,and each part is low in toxicological safety.

Anti-inflammatory Mechanism of Yao Medicine Laggerae Alatae Herba

[Objectives]To study the anti-inflammatory effect of Laggerae Alatae Herba extract and its mechanism.[Methods]Inflammation models of xylene-induced ear edema in mice,acetic acid-induced increased permeability of abdominal capillaries in mice,and carrageenan-induced paw edema in mice were established;xylene-induced ear swelling model in bilateral adrenalectomized mice was established.The levels of MDA,NO and SOD in inflammatory tissues of paw were measured.[Results]Compared with the model group,the high and medium dose groups of Laggerae Alatae Herba extract had significant inhibitory effect on xylene-induced ear edema in mice,except for the low dose group(P>0.05);Laggerae Alatae Herba extract inhibited the increase of celiac capillary permeability induced by acetic acid and paw edema induced by carrageenan in mice.Compared with the model group,in the mice model with bilateral adrenal glands removed,the high and medium dose groups of Laggerae Alatae Herba extract could significantly inhibit the xylene induced ear swelling of the mice.The high and medium dose groups of Laggerae Alatae Herba extract could significantly decrease the levels of MDA and NO,and significantly increase the level of SOD in the paw tissue.[Conclusions]The Laggerae Alatae Herba extracts have anti-inflammatory activity,and the anti-inflammatory effect of the extracts does not depend on the hypothalamic-pituitary-adrenal axis(HPAA)system.In addition,the anti-inflammatory mechanism of Laggerae Alatae Herba extract is related to the decrease of MDA and NO and the increase of SOD.

Marine natural products with anti-inflammation effects

The ocean possesses a complex setting with high pressure,high salinity,oligotrophy,low temperature and weak illumination conditions.To survive and evolve in such harsh surroundings,marine organisms metabolize a series of chemicals known as secondary metabolites which indicate structural and functional diversity to adapt interspecific survival competition.During recent decades,the anti-inflammatory property of marine natural products has come under scrutiny as inflammation involves in the vast majority of diseases.Correspondingly,a myriad of marine bioactive molecules including terpenes,polypeptides,polysaccharides,sterols and many others may bring a new insight into inflammation therapies with multifarious sources and minimal side effects.And a better understanding of their mechanisms of anti-inflammation may lead to better treatments for numerous diseases.Herein,the research progress of marine-derived anti-inflammation compounds and the relevant mechanisms were reviewed,to provide a basis for the research and development of anti-inflammatory marine drugs.

中药蔓荆子的化学成分及药理作用研究进展

蔓荆子是我国用药历史悠久的传统中药。主要含有萜类、黄酮类、木脂素类、酚酸类、甾类、蒽醌类等化学成分;具有广泛的生物活性,包括解热镇痛、抗菌、抗炎、抗氧化、抗肿瘤、降血糖等,常用于治疗风热、感冒头痛、偏头痛等症状。本文将从化学成分和药理作用方面,对蔓荆子近年来研究进展进行综合归纳整理,为蔓荆子进一步开发应用提供参考。

Natural products as a crucial source of anti-inflammatory drugs: recent trends and advancements

Natural active molecules are key sources of modern innovative drugs. Particularly, a great amount of natural active molecules have been reported to possess promising therapeutic effects on inflammatory diseases, including asthma, rheumatoid arthritis, hepatitis, enteritis, metabolic disorders and neurodegenerative diseases. However, these natural active molecules with various molecular structures usually exert anti-inflammatory effects through diversiform pharmacological mechanisms, which is necessary to be summarized systematically. In this review, we introduced the current major anti-inflammatory natural active molecules based on their chemical structures, and discussed their pharmacological mechanisms including anti-inflammatory molecular signaling pathways and potential target proteins, which providing a referential significance on the development of novel anti-inflammatory drugs, and also revealing new therapeutic strategies for inflammatory diseases.

电针在混合痔术后镇痛治疗的Meta分析

目的:探讨电针在混合痔外剥内扎术后镇痛的临床疗效。方法:计算机检索中国知网、万方、维普、Web of science、PubMed、Scopus数据库,筛选2011年1月-2021年9月收录的关于电针治疗混合痔术后疼痛的随机对照试验文献。对符合标准的研究文献数据使用RX644.0.5进行Meta分析。结果:最终有10篇随机对照试验文献纳入研究。定性分析结果显示电针治疗能提高术后镇痛有效率且能减少术后镇痛剂的使用;Meta分析结果提示与常规治疗相比,电针组术后24 h内的最强疼痛视觉模拟评分法(Visual Analogue Scale,VAS)评分、术后4 h疼痛VAS评分、术后12 h疼痛VAS评分、术后24 h VAS评分均更优(均有P<0.01)。结论:电针在混合痔外剥内扎术后的辅助镇痛效果明显,且安全性高。

基于网络药理学和分子对接的三九胃泰颗粒抗炎镇痛作用机制研究

目的:基于网络药理学探讨三九胃泰颗粒抗炎镇痛的潜在作用机制。方法:通过TCMSP数据库和相关文献筛选出三九胃泰颗粒的活性成分,并对其活性成分作用靶点进行预测,运用Cytoscape软件构建“三九胃泰颗粒-潜在活性成分-靶点”网络。通过GeneCards数据库收集炎症、疼痛相关靶点并与药物靶点相交集。通过STRING数据库对交集靶点进行蛋白质-蛋白质相互作用(PPI)分析,京都基因与基因组百科全书(KEGG)通路富集、基因本体(GO)分析于DAVID数据库中进行。Cytoscape软件构建“三九胃泰颗粒潜在活性成分-炎症疼痛相关靶点-通路”网络。AutoDockTools和PyMOL软件用于三九胃泰颗粒抗炎镇痛核心成分和核心靶点的分子对接。结果:共获取三九胃泰颗粒的潜在活性成分73种,其中核心活性成分15个,包括槲皮素、山柰酚、β-谷甾醇等;三九胃泰颗粒发挥抗炎镇痛作用的核心靶点22个,包括PTGS2、HSP90AB1、PTGS1等,参与药物的应答、炎症应答、MAPK级联的正调节等生物过程,涉及脂质和动脉粥样硬化、TNF、PI3K-AKT、MAPK等信号通路。核心成分槲皮素、山柰酚、β-谷甾醇、汉黄芩素、黄芩素与核心靶点PTGS2、HSP90AB1、PRKACA、PTGS1、RELA的结合能均﹤-5.0 kJ/mol,能较好地结合在一起。结论:基于网络药理学分析揭示了三九胃泰颗粒多成分、多靶点、多途径抗炎镇痛的作用机制,为其临床上治疗慢性胃炎提供理论依据。

ANALGESIC ACTION OF INTERFERON

Interferon is a protein with high activity. Its effects on preventing and curing viral diseases have aroused the interest of many clinicians. and its prominent analgesic effect after local injection of interferon around the tumor has been reported. Whether the interferon would create the activity of analgesia is a problem worthy of studying. In order to know its function and reasonable use, we have investigated the analgesic action on the injection of interferon into brain.

肉桂的温中止痛药理研究

观察到肉桂水提物和醚提物对4个实验胃溃疡模型有显著保护作用,对2种药物引起的小鼠腹泻有显著对抗作用,对麻醉大鼠有明显利胆作用,并有明显镇痛作用。这是肉桂温中止痛的药理学基础。

附子的温中止痛药理研究

本文观察附子水煎剂能显著对抗小鼠水浸应激型和大鼠盐酸损伤性溃疡。附子煎剂能显著对抗蓖麻油和番泻叶引起的小鼠药物性腹泻。在热板法和乙酸扭歪试验中它有明显镇痛效应。认为这是附子温中止痛的药理学基础。

臭牡丹提取物抗炎镇痛抗过敏作用的实验研究

目的:探讨臭牡丹提取物的抗炎、镇痛、抗过敏作用。方法:以醋酸致小鼠腹腔毛细血管通透法、二甲苯致小鼠耳肿胀法观察其抗炎作用;以小鼠醋酸扭体法观察其镇痛作用;以2,4-二硝基氟苯(DNFB)致敏法观察其抗过敏作用。结果:臭牡丹提取物显著抑制小鼠腹腔毛细血管炎性渗出,抑制二甲苯所致小鼠耳廓肿胀。减少醋酸致小鼠扭体次数;并降低DNFB诱导的小鼠过敏反应。结论:臭牡丹提取物具有较好的抗炎、镇痛及抗过敏作用,与其相关的中医临床疗效相符。

苦参碱的镇痛作用部位及机制研究

目的 研究苦参碱的镇痛作用部位及机制。方法 采用小鼠醋酸扭体法、热板法 ,观察用药后扭体反应数、舔后足潜伏期及脑组织 NO含量的变化。结果 苦参碱侧脑室注射 (icv) 0 .2 5 ,0 .5 mg/ kg,ip或 iv 3.75 ,7.5 ,15 ,30mg/ kg均可显著减少小鼠扭体反应数 ,并呈量效关系 ;ip与 iv同等剂量的苦参碱 ,对小鼠扭体反应的抑制程度多以iv为强 ,给药后各时段的 ip抗扭体半数有效量 (ED5 0 )均大于 iv抗扭体 ED5 0 ;ip苦参碱 7.5 ,30 mg/ kg可显著降低醋酸致痛小鼠脑组织 NO含量 ;进一步研究发现苦参碱延长小鼠舔后足潜伏期的作用可被氯化钙所拮抗 ,而被维拉帕米所增强。结论 苦参碱的镇痛作用部位在中枢 ,其镇痛作用可能与影响 Ca2 + 内流和减少

冰片抗炎镇痛作用的实验研究

目的研究冰片的镇痛、抗炎作用。方法采用热板刺激、冰醋酸刺激小鼠扭体、冰醋酸致小鼠腹腔毛细血管通透性增加、角叉菜胶致大鼠足肿胀等方法研究冰片的镇痛及抗炎作用。结果冰片能明显抑制大鼠足跖肿胀度,其半数有效量(ED50)=0.3242g·kg-1;延长小鼠疼痛反应时间,ED50=0.3870g·kg-1;减少小鼠扭体次数,ED50=0.5813g·kg-1。同剂量条件下,冰片的镇痛效应比抗炎效应更为明显。结论冰片具有显著的镇痛、抗炎作用。

芍药甘草汤总苷抗炎镇痛作用的配伍研究

目的阐明芍药甘草汤总苷抗炎镇痛作用及其配伍机制。方法观察芍药甘草汤总苷、甘草总苷和白芍总苷对二甲苯致小鼠耳肿胀、棉球致大鼠肉芽肿、鸡蛋清致大鼠足跖肿胀、小鼠醋酸扭体法和小鼠热板法致痛的影响。结果芍药甘草汤总苷在150～600mg·kg-1·d-1剂量下显著抑制二甲苯所致小鼠炎性耳肿胀,在75～300mg·kg-1·d-1剂量下显著抑制棉球引起的大鼠肉芽肿和鸡蛋清诱发的大鼠足跖肿胀。在150～600mg·kg-1·d-1剂量下显著减少醋酸所致小鼠的扭体次数,显著延长小鼠热板法的痛阈值。甘草总苷的抗炎作用优于白芍总苷,但镇痛效应弱于白芍总苷,甘草总苷和白芍总苷抗炎镇痛作用明显弱于芍药甘草汤总苷。结论芍药甘草汤总苷具有明显抗炎和镇痛作用,其组成成分甘草总苷和白芍总苷具有一定的协同效应。

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。

金丝桃甙镇痛作用的机制

用小鼠光热辐射甩尾模型证明,低钙和高钙分别能增强和拮抗Hyp的镇痛作用。在痛介质诱发传入神经放电的模型上,同样证明低钙或高钙能显著加强或拮抗Hyp对组胺和氯化钾诱发神经放电的抑制作用。促进Ca^(2+)内流的A_(23187)几乎完全拮抗Hyp的末梢镇痛作用,并且在蛙坐骨神经标本上,Hyp可抑制KCl诱发的Ca^(2+)内流。提示Hyp的镇痛作用与减少感觉神经末梢Ca^(2+)内流有密切关系。

前列泰片对前列腺增生及其抗炎镇痛作用的实验研究

前列泰片ｉｇ对丙酸睾丸素所致小鼠前列腺增生有预防和治疗作用。对５—ＨＴ和角叉菜胶引起大鼠足肿胀、二甲苯致小鼠耳壳炎症及小鼠棉球肉芽肿的形成等均有明显的抑制作用。体外对５种菌株有不同程度的抑菌作用。小鼠热板法和醋酸扭体法证明尚有明显的镇痛作用。最大浓度的混悬液给小鼠ｉｇ未见明显中毒症状。长期毒性实验也表明本品毒性低、安全范围大。

罗汉果咽喉片的药理研究

罗汉果咽喉片对小鼠棉球肉芽肿的形成,二甲苯致小鼠耳壳水肿及角叉菜胶引起的足肿胀具有明显的抑制作用;醋酸扭体法实验表明它有明显的镇痛作用,体外实验对5种菌株具有明显的抑菌作用。

芭蕉根不同提取物的抗炎镇痛作用研究

目的探讨芭蕉根不同极性溶剂提取物的抗炎、镇痛活性。方法采用二甲苯致小鼠耳肿胀实验、角叉菜胶致小鼠足肿胀和小鼠棉球肉芽肿等实验进行抗炎实验,采用醋酸扭体法进行镇痛实验,对芭蕉根的石油醚提取物、正丁醇提取物,80%乙醇提取物和水提取物进行抗炎和镇痛实验研究。结果芭蕉根石油醚和正丁醇提取物可以明显的减轻二甲苯所致的小鼠耳廓肿胀和棉球肉芽肿的重量,对角叉菜胶所致的小鼠足肿胀也有明显的抑制作用;芭蕉根乙醇提取物和水提取物对醋酸所致小鼠扭体反应有较好的抑制作用。结论在相同剂量下,芭蕉根石油醚提取物和正丁醇提取物显示出较好的抗炎活性,而80%乙醇和水提取物相对具有较好的镇痛活性。

红毛五加镇痛解热作用及毒性的实验观察

实验结果证明，红毛五加醇提物有明显镇痛作用，并能降低家兔正常及蛋白陈致发热体温，但对霍乱菌苗引起的发热体温无影响。红毛五加醇提物的小鼠ｉｐＬＤ＿（５０）为７３．３４±７．２９ｇ／ｋｇ，长期大量ｐｏ红毛五加醇提物对大鼠血象、肝肾功能无影响。