少棘蜈蚣多肽药用价值的研究进展

少棘蜈蚣Scolopendrasubspinipesmutilans已有千年的药用历史,现代研究表明其药用活性成分主要为多肽。随着研究的不断深入,越来越多的具有不同药用潜能的多肽从少棘蜈蚣中发掘出来,这些多肽在抗微生物、抗肿瘤、心血管疾病、自身免疫疾病、镇痛等方面展现出良好的治疗潜能,为新药的设计与开发提供了候选或前体分子。针对具有良好药用前景的少棘蜈蚣多肽的药理活性及作用机制进行阐述,以期为相关药物的研发提供参考。     

白藜芦醇的研究进展

白藜芦醇作为一种热门的植物提取化合物,其抗肿瘤活性、抗心血管疾病的作用已经备受关注,对其深入的研究,尤其是在抗心血管疾病、抗肿瘤方面将会有重要的临床意义。     

亚麻木酚素的药理作用研究进展

亚麻木酚素主要来源于亚麻籽,具有显著的生物活性。亚麻木酚素具有抗氧化作用、抗炎作用、抗肿瘤作用、抗心血管疾病、抗骨质疏松作用、抗凋亡作用、降糖作用等。综述了亚麻木酚素药理作用的研究进展,以期为亚麻木酚素的研究和开发利用提供依据。     

Antihypertension and anti-cardiovascular remodeling by phenylalanine in spont aneously hypertensive rats: effectiveness and mechanisms

Objective To investigate mechanisms of anti-hypertensi on and anti-cardiovascular remodeling by phenylalanine (phe) in spontaneously h ypertensive rats (SHRs).Methods The comparison of blood pressure (BP) increment with the ages and cardiovascular changes of SHRs was made between the 3% phe-intervented group (SHR-phe) and t he control SHRs group. Detection of the structural changes with the VID AS digital vedio-fre quency processing technique and light and electron microscopy were made. The ce ll growth and proliferation of cultured smooth muscle cells (CSMCs) of the thora cic aortas or myocardial fibroblasts were evaluated by measuring the (3)H -th ymidine counts per minute (cpm) incorporated into the new synthesized desoxyribo nucleic acid (DNA) and determining the cell number with the crystal violet stain technique. The Ca((2+)) influx was measured in counts/min of (45)CaCl(2) after incubating it with 5 different concentrations of phen ylalanine and the intracellular ［Ca((2+))］(i) by Fura-Ⅱ/Am indicator. The total messenger ribonucleic acid (mRNA) of the myocardium was extracted and Northern blot analysis was performed with the probe collagen α(2)(Ⅰ)cDNA . The tyrosine hydroxylase (TH) activity was measured by high -performance liquid chromatography (HPLC) with electrochemical detector after h aving reacted with its substrate tyrosine and other reagents. The catecholamine contents in brain homogenat were detected by HPLC method. The comparison of p harmacokinetics of phenylalanine among SHR-phe, SHRs and control Wistar Kyoto (WKY) rats was made after intravenous injection of (3)H-L-phe (1 ml/k g) by PK-GRAPH Program for kinetic calculation. The (3)H-L-pheuptake by CSMCs after incubating for difinite intervals was also detected and compa red. Results Phenylalanine could prevent the increase of BP with ages and the heart weight (h eart/body weight index). The aortic media thickness and the collagen content in the myocardium were decreased significantly in SHR-phe. Whereas the dearrange d cardiovascular structure was much improved. The mechanisms might be direct and specific inhibition of the DNA synthesis and proliferation of cardiovascular cells which may be related to the inhib ition of collagen α(2)(Ⅰ)cDNA, c-fos and c-myc expression. Other mechan isms may include decrease of intracellular ［Ca((2+))］(i) and an inhibition of central sympathetic activity due to the results of higher TH activity in the caudate nucleus and higher adrenaline conte nt in the posterior hypothalamus. Besides, partial recovery of p henylalanine metabolic aberrants existed in SHRs seems to be another possibility for its effectiveness. Conclusions Phenylalanine intervention could exert a definite anti-hypertension and anti-c ardiovascular remodeling effects on SHRs like seen in human essential hypertensi on. Its mechanisms might be related to direct inhibition of growth in the cardi ovascular cells, decrease of central sympathetic activity, the reverse of the exhibited phenylalanine metabolic aberrants in SHRs, and a decrement of intracellu lar ［Ca((2+))］］(i).     

Recent progress in the development of ursolic acid derivatives as anti-diabetes and anti-cardiovascular agents

Ursolic acid (UA) is a pentacyclic triterpenoid, which exhibits many biological activities, particularly in anti-cardiovascular and anti-diabetes. The further application of UA is greatly limited due to its low bioavailability and poor water solubility. Up to date, various UA derivatives have been designed to overcome these shortcomings. In this paper, the authors reviewed the development of UA derivatives as the anti-diabetes anti-cardiovascular reagents.