小檗碱的分析方法及药理作用研究进展

小檗碱是多种清热解毒类中药的有效成分,目前多用HPLC、紫外等方法进行测定。现代研究表明,小檗碱除了具有传统的抗菌、抗炎等药理作用外,还具有抗肿瘤、治疗心血管疾病、辅助治疗糖尿病等方面的作用,是一种具有广阔应用前景的化合物。本文主要对小檗碱的相关分析方法及药理研究进展进行了综述。     

小檗碱的临床新用途及其作用机制研究进展

小檗碱又称黄连素,是传统中药黄连的有效成分,是一种可治疗由各种原因引起的腹泻的传统良药。近年研究发现,小檗碱还有许多新的临床用途,如对糖尿病、高脂血症等代谢性疾病治疗有确切的疗效;还具有抗炎、抗肿瘤和免疫调节等作用,可用于肿瘤和炎症性肠病的辅助治疗。本文就小檗碱的临床新用途及其可能的作用机制作一系统综述。     

小檗碱药理作用及其临床应用研究进展

小檗碱是从传统中药黄连和黄柏中提取出的一种异喹啉类生物碱,在我国拥有悠久的药用历史。小檗碱具有多种药理作用,包括抗病原微生物、抗炎、抗肿瘤、心脏保护、降血糖、调节脂质代谢以及免疫抑制等。多年以来,小檗碱用于肠道感染性疾病的治疗取得显著疗效。近年来,随着研究的不断进展,其临床应用潜力不断被开发,对心血管系统疾病、代谢综合征及其并发症、肿瘤、腹腔黏连和沙眼衣原体感染等均具有较好的效果。本文针对小檗碱多方面的药理作用、分子机制及临床应用现状进行梳理总结,为小檗碱的临床应用和推广提供参考。     

盐酸小檗碱的心血管药理活性研究进展

小檗碱是一种异喹啉生物碱,存在于黄连、黄檗等植物中,临床常用其盐酸盐.盐酸小檗碱具有强心、抗心律失常、内皮保护、心肌保护、降压、抗动脉粥样硬化、糖尿病性心血管疾病治疗等心血管药理活性作用,是一种富有潜力的心血管疾病治疗药物.本文通过对PubMed数据库进行检索,对盐酸小檗碱的心血管药活性研究进行了综述.     

小檗碱用于结直肠癌治疗的研究现状

越来越多的研究证明,天然药物对肿瘤具有一定的治疗作用。小檗碱是从毛茛科黄连根状茎中提取的一种异喹啉生物碱,由于其清热解毒及抗菌等药理学作用而广泛用于临床。近年研究提示,小檗碱对包括结直肠癌在内的多种实体瘤具有抗肿瘤活性,AMPK信号轴、细胞周期、细胞凋亡及某些细胞因子是其作用靶标。小檗碱还能够有效逆转伊立替康的化学治疗耐受。深入探讨小檗碱在结直肠癌治疗中的作用及可能分子机制,对指导小檗碱联合化疗的结直肠癌临床应用具有积极意义。     

小檗碱的药动学研究进展

黄连是传统的中药药材,具有悠久的应用历史,含有多种生物碱,其中主要为小檗碱(berberine).黄连素是小檗碱的盐酸盐,临床上通常制成片剂,对消化道感染具有显著疗效.近年来,随着对小檗碱研究的深入,发现小檗碱具有更广泛的药理作用.笔者就生物样品中小檗碱含量测定的常用方法、动物及人体体内的药动学及代谢的特点、影响其体内过程行为的主要因素作一综述.     

异喹啉生物碱对心血管药理作用的研究与临床

<正> 异喹啉生物碱为中药黄连等植物中的主要有效成份,常用制品有小檗碱(即黄连素)和小檗胺。该类药物可用于抗菌、抗病毒、抗原虫、利胆、止血、升白细胞、治疗矽肺等。近年来发现对心血管系统具有多种作用,通过药理学实验研究,基本明确了小檗碱和小檗胺对心血管的某些作用机制,并成功地应用于临床。1 降血压作用小檗胺的降压作用国外已有报道.国内经实验证明,小檗胺与小檗碱能使多种动物(狗、猫、兔)的血压下降,其降压强     

小檗碱对心血管药理作用的研究进展

小檗碱是一种具有众多生物活性的植物碱。大量研究证实小檗碱对心血管疾病的药理作用,这为小檗碱在临床治疗方面的应用开辟了新方向。本文综述了小檗碱对心血管药理作用的研究进展,在临床治疗过程中的作用仍需要长期大量的临床研究来进一步证实。     

小檗碱调脂的研究进展

盐酸小檗碱（berberine）是从黄连中提取的一种天然的异喹啉类生物碱。小檗碱具有多种药理作用,包括抗病原微生物、抗炎、抗肿瘤、心脏保护、降血糖、调节脂质代谢以及免疫抑制等。近10年来,国内外学者对小檗碱调脂机制进行了广泛的研究。从调节血浆脂质合成、促进脂质分解等方面对小檗碱改善血脂机制加以综述,为其进一步开发和研究提供参考。     

小檗碱含量测定方法的研究进展

小檗碱是多种中药的有效成分,除了具有传统的消炎抗菌等药理作用外,还有抗肿瘤、抗疟、治疗心血管疾病、糖尿病等作用,目前多用HPLC、紫外、荧光等方法进行含量测定.本文主要对小檗碱的含量测定方法的研究进展进行综述.     

Progress in pharmacological effects and clinical applications of berberine北大核心CSCD

Berberine is an isoquinoline alkaloid isolated from Rhizoma Coptidis and Cortex Phellodendri, which has a long medical history in China. Recent studies have indicated that berberine has multiple pharmacological activities including anti-inflammatory, anti-microorganisms, anti-cancer, cardiac protection, glucose lowering, regulating lipid metabolism and immune suppression. Berberine has been used for the treatment of intestinal infectious diseases for many years. With the continuous progress of the research, it is reported that berberine has many new clinical applications, including treatment of the cardiovascular disease, metabolic syndrome and its complications, cancers, abdominal adhesions and chlamydia trachomatis infection. This review is intended to introduce the role of berberine in various aspects of pharmacological effects, molecular mechanisms and clinical applications.     

Pharmacological effects of berberine and its derivatives: a patent update

Introduction: A number of plant-derived agents are used in many therapeutic areas. Berberine, an important protoberberine alkaloid, is present in a number of medicinal plants that have been widely used in traditional Chinese medicine for hundreds of years. Modern research has shown that berberine and its derivatives display several pharmacological effects through various mechanisms.

Areas covered: This review discusses recent and mostly Chinese patents that report the synthesis of berberine, berberine derivatives and berberine salts, and methods of preparation for formulations (traditional Chinese medicine) containing herbal components rich in berberine, along with their applications. The review covers several therapeutic effects of berberine, its derivatives and pharmaceutical formulations against cancer, obesity, diabetes, inflammation, atherosclerosis, Alzheimer’s disease, rheumatoid arthritis and cardiovascular diseases. In addition, the mechanisms underlying the pharmacological effects are discussed.

Expert opinion: Modification of the functional groups of berberine has a significant effect on the pharmacological activity. However, studies on altering the atoms and size of the berberine skeleton are rare. Thus, it may be beneficial to initiate a drug development program focused on inserting heterocyclic rings of different sizes into berberine. Furthermore, structural modification to improve the safety, efficacy and selectivity is necessary to promote the use of berberine-based drugs in clinical settings.     

The metabolism of berberine and its contribution to the pharmacological effects

Berberine, a bioactive alkaloid isolated from several herbal substances, possesses multiple pharmacological effects, including antimicrobial, antidiabetic, anticancer activities. Meanwhile, berberine undergoes extensive metabolism after oral administration which results in its extremely low plasma exposure. Therefore, it is believed that the metabolites of berberine also contribute a lot to its pharmacological effects. Along these lines, this review covers the metabolism studies of berberine in terms of its metabolic pathways and metabolic organs based on the identified metabolites, and it also covers the pharmacological activities of its active metabolites. In brief, the predominant metabolic pathways of berberine are demethylation, demethylenation, reduction, hydroxylation and subsequent conjugation in vivo. Active metabolites such as columbamine, berberrubine and demethyleneberberine also exhibit similar pharmacological effects by comparison with berberine, such as antioxidant, anti-inflammatory, antitumor, antimicrobial, hepatoprotective, neuroprotective, hypolipidemic and hypoglycemic effects. Overall, berberine together with its metabolites formed the material basis of berberine in vivo.     

小檗碱对多柔比星的增效减毒作用及其机制研究进展

多柔比星是临床治疗中有效的抗肿瘤药,但其严重的心脏、肝脏毒性使其临床应用受到了极大限制。小檗碱是从黄连属植物分得的生物碱,具有多种生物活性和药理作用,对痢疾、真菌感染、糖尿病、肿瘤等都有治疗作用。研究发现小檗碱不仅可以通过诱导肿瘤细胞的凋亡来增强多柔比星的抗肿瘤活性;还可以通过改变多柔比星引起心肌病的相关指标来降低多柔比星引起的心肌细胞的损伤;另外,小檗碱对多柔比星引起的肝脏损伤也有一定的保护作用。综述了小檗碱对多柔比星的增效减毒作用及其机制的研究进展,这种发现提供了一种新颖的治疗方法,对多柔比星临床治疗的发展具有重要的意义。     

小檗碱改善胰岛素抵抗的新进展

小檗碱又名黄连素．是从黄连等植物中提取的异喹啉类生物碱,具有广泛的药理作用。近年来,随着对小檗碱及其衍生物的深入研究发现。小檗碱具有改善胰岛素抵抗作用。现综合国内外对小檗碱的研究,对小檗碱改善胰岛素抵抗及作用机制进行综述。     

小檗碱通过改善代谢水平抗肝细胞癌的研究进展

肝细胞癌的发病分子机制十分复杂,具有预后差、死亡率高的特点,并且对其有效的系统的治疗方案非常有限。近年来,随着国家对传统民族医药发展的重视,涌现出许多具有较好临床疗效的中药化合物。其中,天然产物小檗碱包含多种药理活性并且无明显毒副作用。最近的研究表明小檗碱可以通过多个方面发挥预防和降低肝细胞癌的作用,包括改善糖脂代谢,作用于线粒体有氧呼吸链,调节肠道微生态,作用于micro RNAs,以及诱导p53上调和抑制分化抑制因子-1(Id-1)表达等。综述小檗碱通过改善代谢水平抗肝细胞癌的研究进展,为临床应用提供依据。     

Neuropharmacological and pharmacokinetic properties of berberine: a review of recent research

Objectives This review summarizes recent research on the neuropharmacological and pharmacokinetic properties of berberine, an isoquinoline alkaloid extracted from Coptidis rhizoma. Key findings Berberine has multiple neuropharmacological properties, such as neuroprection, anti‐neuronal apoptosis, improvement of cerebral microcirculation and anti‐Alzheimer's disease, and so on. The pharmacokinetic characteristics of berberine are that it is not easily absorbed and it is not stable in the gastrointestinal tract of animals or humans. Summary Further studies need to be carried out to develop berberine as a drug for nervous system diseases, such as brain ischaemia and Alzheimer's disease, that has favorable pharmacokinetic properties.     

复方黄连凝胶剂体内抗菌活性研究

将药理学研究的基础方法与组织学技术相结合,以细菌和真菌感染皮肤的日本大白兔模型为研究对象,研究了复方黄连凝胶剂对细菌和真菌皮肤感染的治疗效果。并通过皮肤组织学实验,以皮肤细胞修复状况和炎性细胞浸润为主要指标,从组织学角度进一步阐述复方黄连凝胶剂促进皮肤愈合的疗效。结果显示,治疗组愈合率均高于对照组。研究表明复方黄连凝胶剂抗菌作用强,是一种较好的外用抗菌药。     

小檗属植物抗糖尿病及糖尿病并发症的研究进展

小檗属植物资源丰富,药用历史悠久,可用于治疗多种疾病,其中刺檗、具芒小檗、毛叶黄耆和豪猪刺等植物的研究较为深入。小檗属植物的主要成分为生物碱类和黄酮类,研究最多的是小檗碱,其具有降血糖血脂、抗炎、抑菌等药理作用,可用于治疗糖尿病及其并发症。然而,对小檗碱的研究并不能代替对小檗属植物的研究。对小檗属植物提取物抗糖尿病及其并发症的药理作用和作用机制进行综述,为促进该属植物及其有效成分的临床应用提供理论基础。