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.
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.