Lim Hee-Sun, Chun Seung-Min, Soung Min-Gyu, Kim Jenny, Kim Seong-Jin
Department of Dermatology, Chonnam National University Medical School, Gwangju, South Korea.
Department of Applied Biology and Chemistry, College of Agriculture and Life Science, Chungnam National University, Daejeon, South Korea.
Int J Dermatol. 2015 Jul;54(7):853-62. doi: 10.1111/ijd.12756. Epub 2015 Jan 20.
Antimicrobial peptides are considered as a potential alternative to antibiotic treatment in acne vulgaris because the development of a resistant strain of Propionibacterium acnes is problematic. Granulysin can be regarded as an ideal substance with which to treat acne because it has antimicrobial and anti-inflammatory effects.
This study was performed to explore the effectiveness of granulysin-derived peptides (GDPs) in killing P. acnes in vitro under a standard microbiologic assay and to evaluate their potential use in a topical agent for the treatment of acne vulgaris.
Twenty different peptides based on the known sequence of a GDP were synthesized and tested in vitro for antimicrobial activity. Thirty patients with facial acne vulgaris were instructed to apply a topical formulation containing synthetic GDP to acne lesions twice per day for 12 weeks.
A newly synthesized peptide in which aspartic acid was substituted with arginine, and methionine was substituted with cysteine, showed the highest antimicrobial activity against P. acnes. Moreover, it was effective against both Gram-positive and Gram-negative bacteria in vitro. After treatment with the topical formulation containing 50 ppm of synthetic peptide for 12 weeks, a significant reduction in the number of pustules was observed, regardless of the increase in the number of comedones. In addition, a significant reduction in the clinical grade of acne based on the Korean Acne Grading System (KAGS) was evident.
Synthesized GDP shows strong antimicrobial activity against P. acnes in vitro. The clinical improvement observed suggests a topical formulation containing the GDP has therapeutic potential for the improvement of inflammatory-type acne vulgaris by its antimicrobial activity.
抗菌肽被认为是寻常痤疮抗生素治疗的一种潜在替代方法，因为痤疮丙酸杆菌耐药菌株的出现是个问题。颗粒溶素可被视为治疗痤疮的理想物质，因为它具有抗菌和抗炎作用。
本研究旨在通过标准微生物学检测方法，探讨颗粒溶素衍生肽（GDPs）在体外杀灭痤疮丙酸杆菌的有效性，并评估其在治疗寻常痤疮外用制剂中的潜在用途。
基于一种GDP的已知序列合成了20种不同的肽，并在体外测试其抗菌活性。30例面部寻常痤疮患者被指导每天两次将含有合成GDP的外用制剂涂抹于痤疮皮损处，持续12周。
一种新合成的肽，其中天冬氨酸被精氨酸取代，甲硫氨酸被半胱氨酸取代，对痤疮丙酸杆菌显示出最高的抗菌活性。此外，它在体外对革兰氏阳性菌和革兰氏阴性菌均有效。用含有50 ppm合成肽的外用制剂治疗12周后，无论粉刺数量增加与否，脓疱数量均显著减少。此外，基于韩国痤疮分级系统（KAGS）的痤疮临床分级也显著降低。
合成的GDP在体外对痤疮丙酸杆菌显示出强大的抗菌活性。观察到的临床改善表明，含有GDP的外用制剂通过其抗菌活性对改善炎症型寻常痤疮具有治疗潜力。
