Institute of Highland Forest Science, Chinese Academy of Forestry, Kunming, China.
College of Forestry, Nanjing Forestry University, Nanjing, Jiangsu, China.
Microbiol Spectr. 2023 Jun 15;11(3):e0308922. doi: 10.1128/spectrum.03089-22. Epub 2023 May 4.
Drug resistance against bacteria and fungi has become common in recent years, and it is urgent to discover novel antimicrobial peptides to manage this problem. Many antimicrobial peptides from insects have been reported to have antifungal activity and are candidate molecules in the treatment of human diseases. In the present study, we characterized an antifungal peptide named blapstin that was isolated from the Chinese medicinal beetle Blaps rhynchopetera used in folk medicine. The complete coding sequence was cloned from the cDNA library prepared from the midgut of . It is a 41-amino-acid diapause-specific peptide (DSP)-like peptide stabilized by three disulfide bridges and shows antifungal activity against Candida albicans and Trichophyton rubrum with MICs of 7 μM and 5.3 μM, respectively. The C. albicans and T. rubrum treated with blapstin showed irregular and shrunken cell membranes. In addition, blapstin inhibited the activity of C. albicans biofilm and showed little hemolytic or toxic activity on human cells and it is highly expressed in the fat body, followed by the hemolymph, midgut, muscle, and defensive glands. These results indicate that blapstin may help insects fight against fungi and showed a potential application in the development of antifungal reagents. Candida albicans is one of the conditional pathogenic fungi causing severe nosocomial infections. Trichophyton rubrum and other skin fungi are the main pathogens of superficial cutaneous fungal diseases, especially in children and the elderly. At present, antibiotics such as amphotericin B, ketoconazole, and fluconazole are the main drugs for the clinical treatment of C. albicans and T. rubrum infections. However, these drugs have certain acute toxicity. Long-term use can increase kidney damage and other side effects. Therefore, obtaining broad-spectrum antifungal drugs with high efficiency and low toxicity for the treatment of C. albicans and T. rubrum infections is a top priority. Blapstin is an antifungal peptide which shows activity against C. albicans and T. rubrum. The discovery of blapstin provides a novel clue for our understanding of the innate immunity of and provides a template for designing antifungal drugs.
近年来，细菌和真菌的耐药性已经变得很普遍，因此迫切需要发现新的抗菌肽来解决这个问题。许多来自昆虫的抗菌肽已被报道具有抗真菌活性，是治疗人类疾病的候选分子。在本研究中，我们从民间药用的中国药用甲虫 Blaps rhynchopetera 中分离到一种具有抗真菌活性的抗菌肽 blapstin，将其命名为 blapstin。它是一种 41 个氨基酸的休眠特异性肽（DSP）样肽，由三个二硫键稳定，对白色念珠菌和红色毛癣菌具有抗真菌活性，MIC 分别为 7 μM 和 5.3 μM。用 blapstin 处理的白色念珠菌和红色毛癣菌表现出不规则和皱缩的细胞膜。此外，blapstin 抑制白色念珠菌生物膜的活性，对人细胞几乎没有溶血或毒性活性，并且在脂肪体中高度表达，其次是血淋巴、中肠、肌肉和防御腺。这些结果表明，blapstin 可能有助于昆虫对抗真菌，并显示出在开发抗真菌试剂方面的潜在应用。白色念珠菌是引起严重医院感染的条件致病性真菌之一。红色毛癣菌和其他皮肤真菌是浅部皮肤真菌病的主要病原体，尤其是在儿童和老年人中。目前，两性霉素 B、酮康唑和氟康唑等抗生素是治疗白色念珠菌和 T. rubrum 感染的主要药物。然而，这些药物具有一定的急性毒性。长期使用会增加肾脏损伤等副作用。因此，获得高效低毒的广谱抗真菌药物治疗白色念珠菌和 T. rubrum 感染是当务之急。Blapstin 是一种抗真菌肽，对白色念珠菌和红色毛癣菌均有活性。发现 blapstin 为我们理解 的先天免疫提供了新线索，并为设计抗真菌药物提供了模板。
