4种黄酮类化合物对CCl4致小鼠肝纤维化的防治作用

目的探讨芹菜素、根皮苷、原花青素和新橙皮苷二氢查尔酮等黄酮类化合物在CCl4诱导的小鼠肝纤维化模型中的抗肝纤维化作用。方法将♂昆明种小鼠105只随机均分为正常对照组、CCl4模型组、秋水仙碱组、芹菜素组、根皮苷组、原花青素组、新橙皮苷二氢查尔酮组。给药5周后采血并处死小鼠,测定并比较各组小鼠血清中丙氨酸氨基转移酶(ALT)、天门冬氨酸氨基转移酶(AST)的活性,总蛋白(TP)、白蛋白(ALB)及肝组织中的羟辅氨酸(HYP)的含量,计算小鼠的肝指数,观察肝脏的病理变化。结果 4种黄酮类化合物均可使模型小鼠血清中ALT、AST的含量、肝组织中羟脯氨酸的含量降低;病检也证明各组小鼠的肝细胞变性、坏死和肝纤维化均有不同程度的减轻。结论芹菜素、根皮苷、原花青素及新橙皮苷二氢查尔酮有抗CCl4致小鼠肝纤维化的作用。     

聚酰胺柱层析-紫外可见分光光度法测定桑叶中总黄酮的含量

目的:采用柱层析-紫外可见分光光度法测定6批桑叶中总黄酮的含量。方法:以芦丁为对照品,510nm处测定桑叶中总黄酮的吸收度。结果:线性范围为0.0090～0.0452mg/ml,r=0.9999,平均回收率为98.5%,RSD为1.3%。结论:该方法测定桑叶中总黄酮,方法简便,灵敏度和准确度高。     

Quercetin regulates oxidized LDL induced inflammatory changes in human PBMCs by modulating the TLR-NF-κB signaling pathway

Toll-like receptors (TLRs) have been shown to play a pivotal role in both innate and adaptive immune responses. TLR family is the essential recognition and signaling component of mammalian host defense. Both genetic and biochemical data support a common signaling pathway that finally leads to the activation of NF-κB and induction of the cytokines and co-stimulatory molecules required for the activation of the adaptive immune response. The present study was designed to examine the involvement of TLR2 and TLR4 in the oxidized LDL induced inflammation in human PBMCs and the effect of flavonoid quercetin on TLR-NF-κB signaling mechanism. LDL was isolated from human plasma and oxidation of LDL was done by incubating with 10 μM CuSO₄ overnight at 37 °C. The isolated human PBMCs in culture were used as the model system. 50 μg/ml ox-LDL treatment significantly up regulated TLR2 and TLR4 expression in isol human PBMCs after 24 h of culture and this was down regulated by quercetin at 25 μM concentration. ox-LDL caused a significant activation of NF-κB as evidenced by the detection of enhanced p65 subunit in nuclear extracts. Supplementation of quercetin significantly modulates the NF-κB p65 nuclear translocation. The cytokine IL-6 production was significantly increased in ox-LDL treated group and was decreased by quercetin treatment. Quercetin mediated reduction of TLR2 and TLR4 expression and the inhibition of nuclear translocation of NF-κB p65 in turn decreased the inflammatory enzymes like 5-LOX and COX and also decreased the mRNA expression of inducible enzymes like COX-2 and iNOS. Quercetin inhibited the ox-LDL induced TLR2 and TLR4 expression at mRNA level and modulated the TLR-NF-κB signaling pathway thereby inhibited the cytokine production and down regulated the activity of inflammatory enzymes thus have protective effect against the ox-LDL induced inflammation in PBMCs.     

Insights into the intestinal bacterial metabolism of flavonoids and the bioactivities of their microbe-derived ring cleavage metabolites

Abstract

Flavonoids are a group of phytochemicals widely distributed in plants, fruits, and vegetables that possess numerous bioactivities. After oral administration, flavonoids can be metabolized by the intestinal bacteria into a wide range of low-molecular-weight phenolic acids. In this review, the intestinal bacterial metabolic pathways of different flavonoids (flavones, isoflavones, flavonols, flavanones, and chalcones) and the bioactivities of their microbe-derived ring cleavage metabolites are summarized. Flavonoids undergo different intestinal bacterial metabolic reactions, depending on the characteristics of their structure. Free hydroxyl groups, especially 5 and 4’ free hydroxyl groups play significant roles in fission metabolism. Microbe-derived ring cleavage metabolites such as 3,4-dihydroxyphenylacetic acid (3,4-DHPAA) and 3,4-dihydroxytoluene (3,4-DHT) possess various bioactivities including antioxidant, anti-inflammatory, antidiabetic, neuroprotective, and anti-colon cancer effects. Also, the intestinal bacteria associated with the bacterial metabolism of flavonoids are covered in this review.     

黄酮类稀土金属配合物的研究进展

黄酮类化合物是一类重要的中药有效成分,现代研究表明稀土金属在生物医药领域也有很大的应用前景。稀土配合物的合成主要是集中在将具有特定生物活性的配体与稀土离子配合,以期达到更好的生物活性。现对近年来黄酮类稀土金属配合物的合成方法和生物活性进行综述,为今后的黄酮类稀土金属配合物的深入研究提供理论支持。     

大理食用葛根中葛根素和葛根总黄酮含量分析与评价

目的：分析食用葛根中葛根素和葛根总黄酮含量,为进一步加快大理食用葛根开发打下基础。方法：采用紫外分光光度计比色法,对来自大理古城镇2个乡8个样品食用葛根鲜品进行葛根素和葛根总黄酮的含量测定。结果：采集样品中葛根素和葛根总黄酮含量分别为6．6246mg／g、25．374mg／g,高于其它产地水平。结论：大理食用葛根中总黄酮量多质优,有较好的开发前景。     

山楂叶总黄酮分散片的制备

目的研究山楂叶总黄酮分散片的制备工艺。方法以崩解时间为指标,采用正交设计法对山楂叶总黄酮分散片的处方进行筛选,并对最佳处方进行溶出度测定。结果分散片在30s内完全崩解,分散均匀度测定能通过2号筛网,体外溶出度优于市售片。结论本实验山楂叶总黄酮分散片制备处方和工艺可行。     

An oxepinoflavone from <Emphasis Type="Italic">Artocarpus elasticus</Emphasis> with cytotoxic activity against P-388 cells

A new oxepinoflavone, artoindonesianin E1 (1), was isolated from the wood of Artocarpus elasticus, along with four known prenylated flavones: artocarpin (2), cycloartocarpin (3), cudraflavones A (4) and C (5). The structure of the new compound was identified by spectroscopic methods. Upon cytotoxic evaluation against murine leukemia P-388 cells, the new compound showed IC₅₀ 5.0 μg/mL.     

棉花花总黄酮片中黄酮类化合物的测定

目的建立棉花花总黄酮片中总黄酮、金丝桃苷、异槲皮素的测定方法。方法利用紫外分光光度计,以芦丁为对照品测定总黄酮,HPLC同时测定黄酮类化合物金丝桃苷和异槲皮素。结果 3批棉花花总黄酮片中总黄酮分别为71.6、73.5、75.2 mg/片,金丝桃苷分别为4.28、4.35、4.23 mg/片,异槲皮素分别为18.55、18.73、18.31 mg/片。结论该方法专属性强,灵敏度高、重现性好,可用于棉花花总黄酮片中黄酮类化合物的测定。     

Antiepileptic potential of flavonoids fraction from the leaves of Anisomeles malabarica

Ethnopharmacological relevance

The plant Chodara (Anisomeles malabarica R.Br. Family: Lamiaceae) has numerous therapeutic utilities in folk medicine.

Aim of the study

To isolate and evaluate the anti-epileptic potential of fractions from the ethyl acetate extract (EAE) of Anisomeles malabarica leaves.

Materials and methods

The EA extract (2.12% w/w) of the leaves of Anisomeles malabarica was prepared and fractionated into total flavonoids fraction (AMFF) and tannins fraction (AMTF), which subsequently evaluated for the antiepileptic activity against PTZ- and MES model in wistar rats. Diazepam and phenytoin (2 mg/kg and 25 mg/kg, i.p., respectively), were used as a reference drugs. Further, the presence of flavonoid was confirmed by chemical test, TLC and HPTLC were done for the identification of the number of flavonoids with reference to standard.

Results

Single dose pretreatment with AMFF (25 and 50 mg/kg, i.p.) has found to be effective against both MES and PTZ-convulsions, but associated with a marked decrease in locomotor activity and motor activity performance (i.e., neurotoxic effects), similar to that of diazepam treatment. Interestingly, chronic treatment with AMFF at lower doses (6.25 and 12.5 mg/kg, i.p., 1 week) has also produced significant antiepileptic activity, but without causing neurotoxic effects.

Conclusion

Thus, it may be concluded that the flavonoids fraction of the EA extract of Anisomeles malabarica leaves has antiepileptic potential against both MES and PTZ convulsion models. Acute treatment (25 and 50 mg/kg, i.p.) is associated with neurotoxic activity. Whereas, chronic treatment (6.25 and 12.5 mg/kg, i.p., 1 week) also shown significant antiepileptic effect without causing neurotoxic side effects. However, further research is in progress to determine the component(s) of the flavonoids fraction of Anisomeles malabarica involved and their mechanism of action in bringing about the desirable anti-epileptic effect.