Vasorelaxant and antihypertensive effect of Cocos nucifera Linn. endocarp on isolated rat thoracic aorta and DOCA salt-induced hypertensive rats

Ethnopharmacological relevance

The fruits of Cocos nucifera Linn. (Arecaceae) have long been used in traditional medicine for the treatment of cardio-metabolic disorders.

Aim of the study

To evaluate the ethanolic extract of Cocos nucifera Linn. endocarp (CNE) for its vasorelaxant activity on isolated rat aortic rings and antihypertensive effects in deoxycorticosterone acetate (DOCA) salt-induced hypertensive rats.

Materials and methods

Cocos nucifera Linn. endocarp was extracted with ethanol and characterized by HPLC. CNE was examined for its in vitro vascular relaxant effects in isolated norepinephrine, phenylephrine or potassium chloride pre-contracted aortic rings (both intact endothelium and denuded). In vivo anti-hypertensive studies were conducted in DOCA salt-induced uninephrectomized male Wistar rats.

Results

Removal of endothelium or pretreatment of aortic rings (intact endothelium) with l-NNA (10 μM) or ODQ (10 μM) followed by addition of contractile agonists prior to CNE significantly blocked the CNE-induced relaxation. Indomethacin (10 μM) and atropine (1 μM) partially blocked the relaxation, whereas glibenclamide (10 μM) did not alter it. CNE significantly reduced the mean systolic blood pressure in DOCA salt-induced hypertensive rats (from 185.3 ± 4.7 mmHg to 145.6 ± 6.1 mmHg). The activities observed were supported by the polyphenols, viz. chlorogenic acid, vanillic acid and ferulic acid identified in the extract.

Conclusions

These findings reveal that the vasorelaxant and antihypertensive effects of CNE, through nitric oxide production in a concentration and endothelium-dependent manner, is due to direct activation of nitric oxide/guanylate cyclase pathway, stimulation of muscarinic receptors and/or via cyclooxygenase pathway.     

RP-HPLC法测定不同产地荜澄茄中芦丁的含量

目的建立测定不同产地荜澄茄中芦丁含量的RP-HPLC法。方法采用Kromasil C18色谱柱(250 mm×4.6 mm,5μm),以甲醇-体积分数为0.05%的磷酸(体积比为38∶62)为流动相,流速为1 mL.min-1,检测波长为254 nm。结果芦丁的质量浓度在1.664~62.400 mg.L-1(r=0.999 4)内与色谱峰面积呈良好线性关系,平均回收率为101.2%(RSD=2.3%)。结论该方法可作为该药材质量控制的一项指标。     

Rutin inhibits human leukemia tumor growth in a murine xenograft model in vivo

Numerous studies have shown that rutin has anticancer effects. We have previously reported that rutin induced cell cycle arrest and apoptosis in murine leukemia WEHI‐3 cells in vitro and in vivo. However, there are no data showing that rutin inhibits human leukemia HL‐60 cells in vivo in a murine xenograft animal model. Human leukemia HL‐60 cells were implanted into mice and treated with vehicle (1% DMSO), rutin (120 mg/kg of body weight) or vinblastine (120 μg/kg of body weight). Compounds and agents were injected once every four days intraperitoneally (i.p.) for 36 days. Treatment with 120 mg/kg of rutin or with 120 μg/kg of vinblastine resulted in a reduction of tumor weight and volume when compared with the control groups. Tumor size in xenograft mice treated with 120 mg/kg of rutin was significantly smaller than that in the untreated‐control group. These novel findings indicate that rutin inhibits tumor growth in a xenograft animal model. Rutin may be useful in treating leukemia but certainly much more research is needed. © 2011 Wiley Periodicals, Inc. Environ Toxicol, 2012.     

天然产物5,7-二甲氧基木犀草素的合成

5,7-二甲氧基木犀草素是中药枳椇中一种黄酮类主要化合物之一。本文以芦丁为原料,经水解还原得到木犀草素,再经羟基保护、醚化及脱保护基等反应合成了5,7-二甲氧基木犀草素,总收率为7.9%。其结构经1HNMR和13C NMR表征。     

Research on analgesic effect and prospect of clinical application of rutin北大核心CSCD

Rutin is extracted from Ruta graveolens L. with many pharmacological activities such as anti-inflammation, anti-oxidation , protecting cardiovascular system and analgesia. As a natural product, rutin has the advantages of low side effects and difficult tolerance, but its instability and low bioavailability still limit its clinical application. This paper summarizes the analgesic mechnism of rutin, and looks forward to the clinical applica¬tion of rutin based on its derivative and dosage forms. It is expected to provide ideas for further analgesic research and drug development and application of rutin in the future. © 2023 Publication Centre of Anhui Medical University. All rights reserved.     

The effects of rutin flavonoid supplement on glycemic status,lipid profile,atherogenic index of plasma,brain-derived neurotrophic factor (BDNF), some serum inflammatory,and oxidative stress factors in patients with type 2 diabetes mellitus: A double-blind,placebo-controlled trial

This study aimed to investigate the effects of rutin flavonoid in type 2 diabetes mellitus (T2DM) patients. In this trial (double-blind, placebo-controlled), 50 T2DM patients (supplement, n = 25 and placebo, n = 25) were randomized and supplemented with 500 mg rutin or placebo per day for 3-months. At the beginning and at the end of the study, metabolic parameters including fasting blood glucose (FBG), insulin, glycosylated hemoglobin (HbA1c), homeostasis model assessment of insulin resistance (HOMO-IR), quantitative insulin sensitivity check index (QUICKI), homeostasis model assessment of β-cell function (HOMA-β), triglyceride (TG), total cholesterol (CHOL), high-density and low-density lipoprotein cholesterol (HDL-c and LDL-c), and atherogenic index of plasma (AIP), inflammatory and oxidative stress markers such as interleukin 6 (IL-6), total antioxidant capacity (TAC), and malondialdehyde (MDA) and brain-derived neurotrophic factor (BDNF) were assessed. The results showed a significant decrease in FBG, insulin, HbA1c, HOMO-IR, LDL-c, TG, VLDL, CHOL, LDL-c.HDL-c ratio, AIP, IL-6, and MDA and a significant increase in HDL-c, QUICKI index, BDNF, and TAC compared with the initial value (p for all <.05). In the adjusted model, the mean changes of FBG, insulin, HbA1c, HOMO-IR, LDL-c, CHOL, LDL.HDL ratio, AIP, MDA, and IL-6 were significantly lower and mean changes of QUICKI index, HDL-c, and TAC were significantly higher in the rutin group compared with the placebo group (adjusted p for all <.05). It seems that rutin may have beneficial effects on improving metabolic parameters, BDNF, and inflammatory and oxidative stress factors in T2DM patients.     

Box-Behnken设计-响应面法优化蒲公英根产地初加工工艺

目的 通过多种评价指标，利用综合加权评分法以及Box-Behnken设计-响应面法（Box-Behnken design-response surface method，BBD-RSM）全面优化蒲公英Taraxacum mongolicum产地加工关键技术。方法 蒲公英根的产地加工主要与切制前不同含水量、不同干燥方式及烘干温度、不同切制厚度3个因素密切相关。比较了蒲公英根在10种不同干燥方法、5种不同切制厚度下各类化学成分的变化。结果 优选了蒲公英根产地初加工工艺最优参数为含水量70%，烘干温度50℃，切制厚度（13±2）mm。结论 优化出的蒲公英根产地最佳工艺切实可行，工艺简便，可操作性强，进一步丰富蒲公英根质量评价标准，为蒲公英根产地初加工提供参考依据。     

Quantitative Metabolomics: Analysis on Active Components in Extracts from Kaki Folium

Objective In order to analyze the active components in the extracts from Kaki Folium (KF), quantitative metabolomics approach was adopted to investigate the number of active components existing among the different extracts and their variation. Methods LC-MS method was established for the quantitative determination of the active components taking the mixture with reference substance as tested sample. Results In terms of the number of active components and amount presented in the different tested samples of KF extracted by many types of solvents, variation was observed. But rutin, astragalin, and kaempferol were presented in all samples. Difference was found between the samples extracted from the products on market and from the raw materials of KF processed by polar solvents with different recipes, however, the three active components were found in all samples examined. Conclusion These results might be valuable as all information could be used for the optimization of raw materials extraction procedure to enhance the productivity.     

HPLC-MS/MS法测定桑菊感冒片中5种成分的含量

目的：建立高效液相色谱-串联质谱法同时测定桑菊感冒片中芦丁、绿原酸、连翘苷、桔梗皂苷D和苦杏仁苷的含量。方法：采用Waters Atlantis C18色谱柱(2.1×150mm,5μm),以乙腈(A)-0.1%甲酸(B)为流动相,梯度洗脱(0～3min,20%A；3～15min,20%A→60%A；15～23min,60%A；23～24min,60%A→20%A；24～30min,20%A),流速0.2mL.min_-1,柱温35℃,采用电喷雾离子源(ESI),以多反应监测(MRM)方式进行正离子扫描。结果：芦丁、绿原酸、连翘苷和桔梗苷D分别在浓度0.01～2 μg.mL_-1的线性范围内线性关系良好(r＞0.999),苦杏仁苷在浓度0.25～50μg.mL_-1的线性范围内线性关系良好(r＞0.999),平均回收率(n=6)分别为98.86%、99.80%、100.61%、99.35%、99.60%,RSD%分别为0.84%、0.90%、1.19%、1.28%、0.86%。结论：所建立的方法准确、可靠、重复性好,灵敏度高,为桑菊感冒片的全面质量控制提供科学依据。