密蒙花中木犀草素及其糖苷的药理研究进展

木犀草素是密蒙花中主要活性成分黄酮类化合物之一,近年来多项药理研究表明木犀草素及其糖苷具有多种药理活性。本文总结了木犀草素及其糖苷的药理活性研究进展,研究表明木犀草素及其糖苷有抗肿瘤、抗炎、抗病毒、抗菌、抗氧化等多种药理活性,在抗肿瘤、抗炎和抗氧化活性方面有较大的开发前景,为密蒙花的研究开发提供理论指导。     

凤尾菇化学成分和药理活性研究进展

对凤尾菇的化学成分及药理活性的研究进展进行了综述。研究表明凤尾菇含有多糖类、氨基酸、蛋白质、三萜类、甾体类、脂肪酸类等多种化学成分,并具有免疫调节、抗肿瘤、抗氧化、抗衰老、抗菌抗炎、抗凝血等广泛的药理活性。目前对凤尾菇的化学成分研究较弱,主要集中在凤尾菇多糖药理活性方面,并取得了一定的进展。     

橙皮苷-铜(Ⅱ)配合物的配位模式和橙皮苷的抗氧化机理

结合全略微分重叠计算,摩尔比法,电导率法,等摩尔连续变化法和红外分析,研究了橙皮苷-Cu(II)配合物的配位模式和橙皮苷的抗氧化机理。结果表明,橙皮苷酚羟基含量少,不能有效清除羟基自由基,但是可通过羰基和邻羟基与Cu(II)形成2:1配合物;配合物的相对稳定常数lgK为8.05,配位过程中有H 释放。因此,在Cu(Ⅱ)催化氢过氧化物分解成自由基的反应体系中,加入橙皮苷络合掉Cu(Ⅱ),抑制氢过氧化物分解,是橙皮苷抗氧化活性的一个主要依据,而不是已形成羟基自由基的清除效应。     

糖苷水解酶——生物转化制备活性糖苷与苷元的有效工具

糖苷广泛存在于自然界,具有多种药理活性,是人类发现与生产药物的重要来源。糖苷中糖链部分的组成与其药理活性密切相关,改变糖苷分子中的糖链结构能改变糖苷的药理活性,为开发药物提供更多的化合物资源。糖苷水解酶修饰糖链具有效率高、成本低、污染小等优点,被广泛应用于活性糖苷与苷元的制备。本文系统地总结了糖苷水解酶转化制备活性糖苷与苷元的研究进展,为研究糖苷酶生物转化制备活性化合物提供数据资源,为相关的研究和生产提供有用的文献资料。     

异甾体生物碱类化合物及药理活性研究进展

异甾体生物碱类结构多变,药理活性多样,主要分布于百合科贝母属和藜芦属植物中。近十五年内共报道了80个新发现的异甾体生物碱类成分,药理活性涉及抗炎、镇痛、降压、平喘、抗血栓、胆碱酯酶抑制、抗病毒和抗肿瘤等作用。本文综述了2006至2020年间该类化合物的植物来源、化学结构及药理活性,并对该类化合物的未来研究探索进行了讨论与展望。     

鱼藤属植物的化学成分及药理作用研究进展

为更好的开发利用鱼藤属植物的药理活性,本文对其化学成分研究进行了综述.经调研文献,鱼藤属植物的化学成分主要包括黄酮、异黄酮、鱼藤酮等;药理活性主要表现在抗氧化、抗菌、杀虫等方面.     

远志属植物中(口山)酮类成分及其药理研究进展

全面总结了远志属植物中的各种口山酮类化学成分及其药理活性和最新进展。远志属植物在自然界分布广泛 ,口山酮类成分丰富且具有多方面的药理活性 ,开发前景广阔     

芹菜化学成分及药理活性研究进展

介绍了芹菜的化学成分及药理活性研究概况。芹菜主要含有挥发油、脂肪酸和黄酮类等化学成分,具有抗菌杀虫、抗氧化、抗肿瘤及抗心血管疾病等药理活性。作为药食两用且广泛种植的植物,对其进行进一步的研究和开发具有重要的意义。     

白首乌化学成分与药理活性研究进展

白首乌类植物含有C21甾体酯甙类、磷脂类、苯乙酮甙类等化学成分,具有抗氧化、调节免疫功能、抗肿瘤、抗缺氧、降血脂等多种药理活性.主要综述了近年来白首乌类植物化学成分及药理活性研究进展概况.     

海洋中药牡蛎的化学成分、药理活性及开发应用

本文对近十年来牡蛎的化学成分、药理活性及开发应用情况进行了综述,牡蛎的化学成分主要包括蛋白质、糖类等物质,具有提高机体免疫力、抗肿瘤等药理活性,具有作为保健品及海洋中药新药的开发及应用价值。     

Hesperidin-CAMKIV interaction and its impact on cell proliferation and apoptosis in the human hepatic carcinoma and neuroblastoma cells

Calcium/calmodulin-dependent protein kinase IV (CAMKIV) is a key regulatory molecule of cell signaling, and thereby controls its growth and proliferation, including expression of certain genes. The overexpression of CAMKIV is directly associated with the development of different types of cancers. Hesperidin is abundantly found in citrus fruits and exhibits wide range of pharmacological activities including anti-inflammatory, antibacterial and anticancerous effects. We have investigated binding mechanism of hesperidin with the CAMKIV using molecular docking methods followed by fluorescence quenching and isothermal titration calorimetric assays. An appreciable binding affinity of hesperidin was observed with CAMKIV during fluorescence quenching and isothermal titration calorimetric studies. Efficacy of hesperidin to inhibit the growth of human hepatic carcinoma (HepG2) and neuroblastoma (SH-SY5Y) cancer cell lines were investigated. Hesperidin has significantly reduced the proliferation of HepG2 and SH-SY5Y cells and induces apoptosis by activating the caspase-3-dependent intrinsic pathway through the upregulation of proapoptotic Bax protein. Hesperidin treatment reduces the mitochondrial membrane potential of HepG2 and SH-SY5Y cells. All these observations clearly anticipated hesperidin a potent inhibitor of CAMKIV which may be further exploited a newer therapeutic approach for the management of different cancer types.     

Hesperidin and its aglycone hesperetin in breast cancer therapy: A review of recent developments and future prospects

Breast cancer (BC) has high incidence and mortality rates, making it a major global health issue. BC treatment has been challenging due to the presence of drug resistance and the limited availability of therapeutic options for triple-negative and metastatic BC, thereby urging the exploration of more effective anti-cancer agents. Hesperidin and its aglycone hesperetin, two flavonoids from citrus species, have been extensively evaluated for their anti-cancer potentials. In this review, available literatures on the chemotherapeutic and chemosensitising activities of hesperidin and hesperetin in preclinical BC models are reported. The safety and bioavailability of hesperidin and hesperetin as well as the strategies to enhance their bioavailability are also discussed. Overall, hesperidin and hesperetin can inhibit cell proliferation, migration and BC stem cells as well as induce apoptosis and cell cycle arrest in vitro. They can also inhibit tumour growth, metastasis and neoplastic changes in tissue architecture in vivo. Moreover, the co-administration of hesperidin or hesperetin with doxorubicin, letrozole or tamoxifen can enhance the efficacies of these clinically available agents. These chemotherapeutic and chemosensitising activities of hesperidin and hesperetin have been linked to several mechanisms, including the modulation of signalling pathways, glucose uptake, enzymes, miRNA expression, oxidative status, cell cycle regulatory proteins, tumour suppressor p53, plasma and liver lipid profiles as well as DNA repair mechanisms. However, poor water solubility, extensive phase II metabolism and apical efflux have posed limitations to the bioavailability of hesperidin and hesperetin. Various strategies for bioavailability enhancement have been studied, including the utilisation of nano-based drug delivery systems and the co-administration of hesperetin with other flavonoids. In particular, nanoformulated hesperidin and hesperetin possess greater chemotherapeutic and chemosensitising activities than free compounds. Despite promising preclinical results, further safety and efficacy evaluation of hesperidin and hesperetin as well as their nanoformulations in clinical trials is required to ascertain their potentials to be developed as clinically useful agents for BC treatment.     

Hesperidin,a Flavone Glycoside,as Mediator of Neuronal Survival

Flavonoids comprise the most common group of plant polyphenols and provide much of the flavor and color to fruits and vegetables. More than 5,000 different flavonoids have been described. The biological activities of flavonoids cover a very broad spectrum, from anticancer and antibacterial activities to inhibition of bone reabsorption and neuroprotection effect. Although emerging evidence suggests that flavonoids have an important role on brain development, little is known about their mechanisms of action. In the present work, we performed a screening of flavonoid actions by analyzing the effects of these substances (hesperidin and rutin) on neural progenitors and neuronal morphogenesis in vitro. We demonstrated that treatment of neural progenitors with the flavonoid hesperidin enhanced neuronal population as revealed by an 80% increase in the number of β-tubulin III cells. This effect was mainly due to modulation of neuronal progenitor survival. Pools of astrocyte and oligodendrocyte progenitors were not affected by hesperidin whereas rutin had no effect on neuronal population. We also demonstrated that the flavonoid hesperidin modulates neuronal cell death by activating MAPK and PI3K pathways. This opens the possibility of using flavonoids for potential new therapeutic strategies for neurodegenerative diseases.     

HPLC separation of hesperidin and the C-2 epimer in commercial hesperidin samples and herbal medicines

Hesperidin (2S-form), the flavanone 7-O-glycoside, is the main constituent of some Citrus species. The peels of two Citrus species are used as a crude drug, Aurantii nobilis pericarpium, in the Japanese Pharmacopoeia and as components in Kampo formulae. Thus, HPLC analysis of hesperidin as a marker compound is needed for quality control of medicines. Hesperidin was separated from the corresponding C-2 epimer by normal-phase HPLC using a chiral column. Moreover, narirutin and neohesperidin were also separated from the corresponding C-2 epimer. The analyses of commercial hesperidin samples revealed that they contained the C-2 epimer and that the relative ratio of hesperidin to the epimer ranged from 92:8 to 59:41. The HPLC application to Citrus extracts suggested that naturally occurring hesperidin in Citrus has the 2S configuration; however, the dry extracts of rikkunshito and chotosan, which are Kampo formulations containing Aurantii nobilis pericarpium, were found to contain a considerable amount of the (2R)-epimer. These data suggest that the decoction process of the formulae partly converts hesperidin to the epimer. Because diastereomers differ from each other in physicochemical and biological activities, HPLC to separate hesperidin from the C-2 epimer should be introduced into the letter of approval for herbal medicines.     

Apoptotic effect of hesperidin through caspase3 activation in human colon cancer cells, SNU-C4.

Hesperidin, a known flavonoid constituent of citrus, reduces the proliferation of many cancer cells. The apoptotic effects of hesperidin on human colon cancer cells, SNU-C4, were determined at concentrations of 1-100 microM. At 100 microM, hesperidin reduced cell viability to 65.00+/-0.05% of control values in a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cell death induced by hesperidin showed apoptotic features in 4,6-diamidino-2-phenylindole (DAPI) staining and in terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) assays. Examination of the expression of apoptosis-regulating genes indicated that hesperidin treatment decreased the expression of B-cell CLL/lymphoma 2 (BCL2) mRNA, and increased the expression of BCL2-associated X protein (BAX). The expression and activity of the major apoptotic factor caspase3 (CASP3) was increased significantly with hesperidin treatment. Hesperidin down-regulated the protein expression of pro-CASP3, and up-regulated the level of active CASP3. Thus, these results suggest that hesperidin could induce apoptosis in human colon cancer cells through CASP3 activation.     

虫草菌素药理学研究进展

虫草菌素是一种脱氧核苷类似物,对多种疾病都有潜在的治疗作用。综述了国内外虫草菌素药理学的研究概况,主要概括了虫草菌素在调节免疫、抗肿瘤、抗真菌、抗病毒、抗白血病、降血糖、降血脂等方面的研究进展。提出了虫草菌素在临床应用时存在的问题,并对如何开展虫草菌素药理学研究及其应用进行了展望。     

Possible nitric oxide mechanism in the protective effect of hesperidin against ischemic reperfusion cerebral injury in rats

Stroke is the third leading cause of death and disability around the globe. The aim of the present investigation was to evaluate the protective effect of hesperidin and its nitric oxide mechanism against cerebral ischemia reperfusion injury. Bilateral common carotid artery occlusion for 30 min followed by 24 h reperfusion was given to induce ischemia in rats. Animals were pretreated with hesperidin (50 and 100 mg/kg, po) for 7 days. Various behavioural tests, oxidative stress parameters, endogenous antioxidant system, antioxidant enzyme activity and mitochondrial enzyme complex (I, II, III and IV) dysfunctions in cortex and striatum were assessed subsequently. Hesperidin (50 and 100 mg/kg) significantly improved neurobehavioral alterations (neurological score, locomotor activity, resistance to lateral push and hanging wire latency), attenuated oxidative damage, restored antioxidant and mitochondrial complex enzyme activities in cortex and in striatum regions of the brain as compared to their respective controls. L-arginine (100 mg/kg) or L-NAME (10 mg/kg) pretreatment with lower dose of hesperidin (50 mg/kg) significantly reversed or potentiated its protective effect, respectively which was significant as compared to hesperidin (50 mg/kg). The results highlight the involvement of nitric oxide mechanism in the protective effect of hesperidin against ischemia reperfusion injury induced alterations.     

Effect of citrus flavonoids on lipid metabolism and glucose-regulating enzyme mRNA levels in type-2 diabetic mice

Flavonoids have been identified as the antidiabetic components in a number of traditional ethnic remedies. However, the mechanisms whereby these compounds exert their hypoglycemic and hypolipidemic action in type-2 diabetes have rarely been investigated. Therefore, this study investigated the effect of the flavonoids hesperidin and naringin on glucose and lipid regulation in C57BL/KsJ-db/db mice. Hesperidin and naringin both significantly increased the glucokinase mRNA level, while naringin also lowered the mRNA expression of phosphoenolpyruvate carboxykinase and glucose-6-phosphatase in the liver. In addition, the hepatic glucose transporter 2 protein expression was significantly reduced, while the expression of adipocyte glucose transporter 4 and hepatic and adipocyte peroxisome proliferator-activated receptor gamma were elevated in the hesperidin and naringin groups when compared with the control group. Furthermore, hesperidin and naringin effectively lowered the plasma free fatty acid and plasma and hepatic triglyceride levels, and simultaneously reduced the hepatic fatty acid oxidation and carnitine palmitoyl transferase activity. These changes were seemingly attributable to a suppression of the hepatic fatty acid synthase, glucose-6-phosphate dehydrogenase, and phosphatidate phosphohydrolase activities and an increase in the fecal triglycerides. The two flavonoids also led to a decrease in the plasma and hepatic cholesterol levels that may have been partly due to the decreased hepatic 3-hydroxy-3-methylglutaryl-coenzyme (HMG-CoA) reductase and acyl CoA: cholesterol acyltransferase (ACAT) activities and increased fecal cholesterol. Consequently, the current results suggest that hesperidin and naringin are beneficial for improving hyperlipidemia and hyperglycemia in type-2 diabetic animals by partly regulating the fatty acid and cholesterol metabolism and affecting the gene expression of glucose-regulating enzymes.     

Biotransformation of ginsenoside Rb1, crocin, amygdalin, geniposide, puerarin, ginsenoside Re, hesperidin, poncirin, glycyrrhizin, and baicalin by human fecal microflora and its relation to cytotoxicity against tumor cells

To understand the role of intestinal microflora in the biological effect of functional herbs, which have been used in Korea, Japan, and China as traditional medicines, and suggest new bioactive compounds transformed from herbal constituents, the metabolic activities of the functional herb components (ginsenoside Rb1, crocin, amygdalin, geniposide, puerarin, ginsenoside Re, poncirin, hesperidin, glycyrrhizin, and baicalin) toward their bioactive compounds (compound K, crocetin, benzaldehyde, genipin, daidzein, ginsenoside Rh1, ponciretin, hesperetin, 18b-glycyrrhetic acid, and baicalein) were measured in fecal specimens. The metabolic activities of these components were 882.7 +/- 814.5, 3,938.1+/- 2,700.8, 2,375.5 +/- 913.7, 1,179.4 +/- 795.7, 24.6 +/- 10.5, 11.4 +/- 10.8, 578.8+/- 206.1, 1,150.0+/- 266.1, 47.3 +/- 58.6, and 12,253.0 +/- 6,527.6 mmol/h/g, respectively. No differences were found in the metabolic activities of the tested components between males and females, although these metabolic activities between individuals are extensively different. The metabolites of functional herb components showed more potent cytotoxicity against tumor cells than nonmetabolites. These findings suggest that intestinal microflora may activate the pharmacological effect of herbal food and medicines and must be the biocatalytic converter for the transformation of herbal components to bioactive compounds.