The fingerprints of Rhizoma coptidis (Huanglian) collected in different growing periods were established by high-performance liquid chromatography (HPLC), and the seasonal variations of six alkaloids, namely berberine, palmatine, jateorrhizine, coptisine, epiberberine and columbamine were assessed. In order to highlight the differences of their HPLC fingerprints, three chemometrics methods including Spearman's rank correlation, hierarchical clustering analysis (HCA) and principal component analysis were applied. The anti-inflammatory activity of R. coptidis collected in different developing stages was measured by NO inhibition assay. The relationship between HPLC fingerprints and anti-inflammatory activity named spectrum-effect relationship was investigated by partial least squares regression. The anti-inflammatory activity was positively correlated with the alkaloid contents. Berberine, palmatine, coptisine, jateorrhizine and epiberberine were the main anti-inflammatory components on the basis of the quantitative determination of the six alkaloids and spectrum-effect investigation. The collecting time of R. coptidis impacted the plant's alkaloid contents and its anti-inflammatory activity.
Study on the pharmacophore model of α 1 -adrenoceptor (α 1 -AR) antagonists led to design a series of novel 7-mercaptocoumarin derivatives as α 1 -AR antagonists. All designed compounds have been synthesized and biologically evaluated. The results showed that most of them exhibited strong antagonistic activity. Especially compound 6 showed excellent activity, which was better than that of the reference compound prazosin. Structure-activity relationship studies revealed that small hydrophobic group at the terminal heterocyclic ring and ortho substituents on the phenyl ring of phenylpiperazine moiety were the essential structural factors for α 1 -AR antagonistic activity. The pharmacophore modeling studies further clarified their structural contributions to antagonistic activity and also demonstrated that 7-mercaptocoumarin moiety could be a useful scaffold for design of α 1 -AR antagonists.Key words α 1 -adrenoceptor antagonist; pharmacophore model; coumarin; phenylpiperazine Benign prostatic hyperplasia (BPH) is a highly prevalent disorder, which increases dramatically with age. Although not a life-threatening disease, BPH can significantly affect quality of life. BPH manifests clinically with lower urinary tract symptoms (LUTS) and is associated with sexual dysfunction. As many as 60% of men aged 60 years have some degree of clinical BPH. With the increases in the distribution of people over the age of 60, BPH is set to become an even greater problem in men's health. The previous studies demonstrate that α 1 -adrenoceptors (α 1 -ARs) play a significant role in the treatment of BPH, selective antagonism of α 1 -ARs can relax prostatic muscle tone and decrease the symptoms of BPH.
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