Protective effect of Clerodendron glandulosum extract against experimentally induced metabolic syndrome in rats

Context: Metabolic syndrome (MetS) has become one of the major health burdens worldwide. To date, no single pharmacological agent has been developed to correct metabolic abnormalities associated with MetS. Use of indigenous medicinal plants as alternative medicines against MetS could be beneficial due to multiple therapeutic usage, easy availability, and relatively few side effects.

Objective: To investigate the protective effect of Clerodendron glandulosum Coleb. (Verbenaceae) aqueous leaf extract (CgE) against experimentally induced MetS in rats.

Methods: Changes in body weight, food and fluid intake, plasma glucose, insulin, fasting insulin resistance index (FIRI), plasma total lipid profile, free fatty acids (FFA), oral glucose tolerance test (OGTT), blood pressure and vascular reactivity have been investigated in various experimental groups.

Results: Fructose+CgE groups recorded significant decrement (P <0.05) in plasma glucose, insulin, FIRI, total cholesterol, triglycerides, LDL, VLDL and FFA, whereas plasma HDL level was significantly increased (P <0.05) along with an efficient clearance of glucose during OGTT and lowered area under curve values. FRU+CgE groups also showed significantly decreased (P <0.05) mean arterial blood pressure along with decreased vasoconstriction and increased vasorelaxation in response to administration of various pharmacological agents. These results were comparable with metformin treated rats.

Discussion: C. glandulosum leaf extract ameliorates experimentally induced MetS by improving dyslipidemia and insulin resistance.

Conclusion: This study provides the first pharmacological evidence for the protective role of C. glandulosum leaves against experimentally induced MetS. Thus, therapeutic use of C. glandulosum in controlling MetS is indicated.     

毛菊苣种子化学成分研究

对毛菊苣种子进行化学成分研究,从中分离鉴定了9个化合物：β-香树脂醇（1）、α-香树脂醇（2）、β-谷甾醇（3）、旋覆花素（4）、山莴苣苦素（s）、莴苣苦素（6）、秦皮乙素（7）、绿原酸（8）和胡萝卜苷（9）。其中化合物1和4为首次从该属植物中分离,所有化合物均为首次从毛菊苣种子中分离。     

毛菊苣根化学成分研究

从毛菊苣的根分离鉴定了9个化合物,分别为β-谷甾醇（1）、旋覆花素（2）、山莴苣苦素（3）、咖啡因（4）、香草醛（5）、3,4,5-三甲氧基-桂皮酸甲酯（6）、5,8,3′,4′-四羟基-7-甲氧基黄酮（7）、5,8,4′-三羟基-7,3′-二甲氧基黄酮（8）和黄芩苷（9）。其中化合物2、6、7、8、9为首次从该属植物中分离。     

苦菊乙酸乙酯提取物的体外抗氧化活性研究

目的:研究苦菊乙酸乙酯提取物(CEE)的体外抗氧化活性。方法:苦菊经95%乙醇加热回流、石油醚脱脂和乙酸乙酯萃取,挥干乙酸乙酯后得到CEE。通过二苯代苦味酰自由基(DPPH.)清除能力、还原能力和2,2′-偶氮-双(-2-脒基丙烷)氯化二氢(AAPH)诱导的红细胞溶血模型,检测CEE的抗氧化活性。结果:在DPPH.清除能力试验中,CEE和阳性对照药的清除率为50%时所需待测液的浓度(EC50)分别为(59.76±6.11)mg·L-1和(3.89±0.23)mg·L-1,两者相差1.54个数量级。CEE和阳性对照药(抗坏血酸)皆能使还原能力测试体系的吸光度增加,并呈浓度-效应关系(P<0.01),但CEE的还原能力不如抗坏血酸(P<0.01)。在AAPH诱导的红细胞溶血模型中,CEE能有效降低兔血红细胞的溶血率(P<0.01),且高剂量(20 mg·L-1)CEE可使溶血率恢复到空白对照的水平。结论:CEE能有效清除自由基,具有一定的还原能力,并对AAPH诱导的兔红细胞溶血具有很好的保护作用。提示CEE具有一定的抗氧化活性,可对其抗氧化活性及其有效成分作进一步的研究。     

The effects of cichorium intybus extract on the maturation and activity of dendritic cells

Background

Cichorium intybus is a medicinal plant commonly used in traditional medicine for its benefits in immune-madiated disorders. There are several evidences showing that C. intybus can modulate immune responses. In the present study we have investigated the effects of the ethanolic root extract of this plant on the immune system by targeting dendritic cells (DCs). For this purpose, phenotypic and functional maturity of murine DCs after treatment with the extract was analyzed by flow cytometry and mixed lymphocyte reaction (MLR) assay.

Results

C. intybus did not change the expression of CD40, CD86 and MHC-II molecules as important co-stimulatory markers on DCs compared to the control, indicating that it could not promote DCs phenotypic maturation. Treatment of DCs with lower concentrations of the extract resulted in an increased production of IL-12 by these cells with no change in IL-10 release. The capacity of treated DCs to stimulate allogenic T cells proliferation and cytokines secretion was examined in the co-cuture of these cells with T cells in MLR. C. intybus at higher concentrations inhibited proliferation of allogenic T cells and in lower concentrations changed the level of cytokines such that IL-4 decreased and IFN-γ increased.

Conclusions

These results indicated that C. intybus extract at higher concentrations can inhibit T cell stimulating activity of DCs, whereas at lower concentrations can modulate cytokine secretion toward a Th1 pattern. These data may in part explain the traditional use of this plant in treatment of immune-mediated disorders.     

毛菊苣的化学成分

目的：对毛菊苣地上部分的化学成分进行研究。方法：运用多种柱层析方法进行分离纯化, 通过 1H, 13C NMR等波谱技术进行结构鉴定。结果：从毛菊苣地上部分的乙酸乙酯和正丁醇部位分离得到了11个化合物, 分别鉴定为莴苣苦素（1）,山莴苣苦素（2）,七叶内酯（3）,菊苣苷（4）,槲皮素-3-O-β-D-葡萄糖醛酸苷（5）,山柰酚-3-O-β-D-葡萄糖醛酸苷（6）,异槲皮苷（7）,异鼠李素（8）,槲皮素（9）,肌苷（10）,对羟基苯甲酸 （11）。结论：化合物4-11为首次从毛菊苣中分得,5-6,8-11为首次从菊苣属中分得。     

HPLC法测定菊苣中黄酮类成分的含量

目的：建立HPLC法测定菊苣中黄酮类成分含量的方法。方法：色谱柱：Scienhome C18（4.6mm×200mm,5μm）,检测波长350nm;柱温30℃;流速1mL/min。结果：木犀草素-7-O-β-D-葡萄糖苷在0.0024～0.0192μg内线性良好,y=2000000x-443.39r,=0.9999,回收率为102.7%,RSD为0.82%;木犀草素在0.01464-0.11712μg内线性良好,y=2000000x-2058.1r,=0.9999,回收率为103.4%,RSD为0.52%。结论：采用该方法进行含量测定准确可靠,重现性好。     

苦菊提取物对HepG2细胞的抗氧化作用及其机制研究

目的：考察苦菊提取物（CEE）对H₂O₂致HepG2细胞氧化应激损伤的保护作用,并探讨苦菊提取物在HepG2细胞中抗氧化作用机制。方法：通过MTT法和DCFH-DA荧光染色,检测H₂O₂处理HepG2细胞的活性和胞内ROS水平;在抗氧化反应元件（ARE）报告基因转染稳定的HepG2细胞内检测ARE-Luciferase活性;并通过荧光定量RT-PCR测定HepG2细胞内含有ARE序列相关基因的mRNA表达水平。结果：H₂O₂处理HepG2细胞后,细胞存活率下降,胞内ROS水平上升,而加入不同浓度的CEE则可明显改善上述结果。不同浓度的CEE处理转染ARE报告基因的HepG2细胞,可使细胞内的ARE活性呈浓度依赖性增强。此外,CEE可使HepG2细胞中含ARE序列的调控基因GCLC,GCLM和HMOX-1的mRNA表达水平上调,并呈浓度依赖性。结论：CEE通过降低ROS水平,抑制H₂O₂诱导的HepG2细胞损伤,而CEE对HepG2细胞的抗氧化保护作用机制可能与其激活HepG2细胞内Nrf2-ARE通路相关的抗氧化防御系统密切相关。     

Hydroxycinnamic acid derivatives occurring in Cichorium endivia vegetables

The hydroxycinnamic acid derivatives found in Chicorium endivia var. crispum and var. latifolium polyphenolic extracts were detected and characterized by high-performance liquid chromatography (HPLC) combined with photodiode array detector (DAD) and electrospray ionization-tandem mass spectrometry (ESI-MS/MS). The method provides data (molecular weight and diagnostic fragment ions) on the molecular structure of compounds. The combined approach enabled identification of four hydroxycinnamic derivatives in each chicory extract; three derivatives (5-O-caffeoylquinic acid, 3,4-di-O-caffeoylquinic acid, and 5-O-feruloylquinic acid) were found in both chicories, while 3,5-di-O-caffeoylquinic acid was typical of var. crispum and cis-caftaric acid of var. latifolium.