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《NAT PROD RES》上关于植物类抗痤疮活性的研究

更新日期:2017年12月15日

1.石榴的多重抗寻常痤疮活性研究


 摘要:痤疮是一种常见的皮肤疾病,往往伴随着皮脂过度生成,角化过度,痤疮丙酸杆菌(P.acnes)和金黄色葡萄球菌,以及炎症等。石榴(Punica granatum)因其抗炎作用而闻名;然而,很少有研究讨论石榴的抗痤疮作用。在本研究中,我们发现石榴提取物(PG-E)显着降低了纯种大鼠耳中由痤疮丙酸杆菌引起的水肿。结果显示PG-E可抑制细菌生长和脂肪酶活性。通过生物导向分馏-分离系统,分离出四种可水解的单宁,punicalagin(1),punicalin(2),strictinin A(3)和granatin B(4)。化合物1和化合物2比其它化合物具有更高的抗菌活性和抗睾酮诱导的HaCaT增殖作用。化合物1,3和4可以抑制脂肪酶。在热灭活的痤疮丙酸杆菌处理的RAW264.7细胞中,化合物4降低了环氧合酶-2的表达并下调了前列腺素E2的产生。总之,PG-E含有丰富的水解单宁,具有抗菌,抗脂肪酶,抗角质形成细胞增殖,抗炎作用等多重抗痤疮能力。因此,PG-E在抗痤疮和护肤品应用方面具有很大的潜力,并且PG-E中最有效的组分punicalagin(1)可用作质量控制标记。



Multiple Activities of Punica granatum Linne against Acne Vulgaris(原文)

  

  Abstract: Acne is a common skin condition with sebum overproduction, hyperkeratosis,Propionibacterium acnes (P. acnes) and Staphylococcus aureus, and inflammation. Punica granatum(pomegranate) is well-known for its anti-inflammatory effects; however, few studies have discussed the anti-acne effects of pomegranate. In this study, we found that pomegranate extract (PG-E)significantly reduced P. acnes-induced edema in Wistar rat ears. Therefore, an evaluation platform using multiple pathogenic mechanisms of acne was established to explore the anti-acne effects of pomegranate. Results showed that PG-E inhibited bacterial growth and lipase activity. Through a bioguided-fractionation-isolation system, four hydrolysable tannins, punicalagin (1), punicalin (2),strictinin A (3), and granatin B (4), were isolated. Compounds 1 and 2 had greater anti-bacterial activities and anti-testosterone-induced HaCaT proliferative effects than the others. Compounds 1,3, and 4 displayed lipase inhibitory effects. Compound 4 decreased cyclooxygenase-2 expression and downregulated prostaglandin E2 production in heat-killed P. acnes-treated RAW 246.7 cells.In conclusion, PG-E is abundant in hydrolysable tannins that display multiple anti-acne capacities,including anti-bacterial, anti-lipase, anti-keratinocyte proliferation, and anti-inflammatory actions.Hence, PG-E has great potential in the application of anti-acne and skin-care products, and punicalagin (1), the most effective component in PG-E, can be employed as a quality control marker.





 2.面包果茎皮中植物活性物质的体外抗痤疮活性研究及两种端基异构体的混合物吡喃环甲硼杂蒽酮A的表征

 

 摘要:本研究的目的是分离来自面包果茎皮的植物活性物质,并评估其体外抗痤疮活性。面包果的乙醇茎皮提取物中含有两种主要的植物活性成分:(i)吡喃环甲硼杂蒽酮A(1)和(ii)Artonine E(2),其结构已通过NMR和MS光谱分析确定。本研究首次报道了化合物1为两种端基异构体(α和β)的混合物,比例约为70:30。并且首次从这种植物中分离出化合物1和2。通过琼脂扩散法对化合物1和化合物2的体外抗痤疮活性进行评估,通过肉汤微量稀释法测定最小抑制浓度。抗菌活性的结果(MIC =2.0μg/ mL)与抗生素克林霉素(MIC =0.03μg/ mL)相当,显示了其作为抗痤疮剂的潜力。



In vitro anti-acne activity of phytoactives from the stem bark of Artocarpus hirsutus Lam. and characterisation of pyranocycloartobiloxanthone A as a mixture of two anomers(原文)

  

  Abstract: This study is aimed to isolate the phytoactives from the stem bark of Artocarpus hirsutus and evaluate their in vitro anti-acne activity.The ethanolic stem bark extract of A. hirsutus provided two major phytoactive constituents: (i)pyranocycloartobiloxanthone A, (1) and (ii) Artonine E, (2) whose structures were determined by NMR and MS spectroscopic analysis. The present study is the frst to report compound 1 as a mixture of two anomers (α and β), approximately 70:30 ratio. Both compounds 1 and 2 were isolated for the frst time from this plant. In vitro anti-acne activity of compounds 1 and 2 were evaluated by agar well diffusion method and the minimum inhibition was determined by broth micro dilution method. The result of antimicrobial activity (MIC = 2.0 μg/mL each) is comparable to antibiotic, Clindamycin (MIC = 0.03 μg/mL) and clearly demonstrate their potential as anti-acne agents.






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