抗逆转录病毒治疗显著降低了人类免疫缺陷病毒感染和死亡率。然而,目前的治疗方案受到不良副作用的限制,耐药性的出现,以及无法消除病毒库。这里,从球茎植物和Hypoxis植物中分离出15种内生真菌。15种分离物的粗提物中的链格孢菌(菌株IDPO4PR1,PO4PR2和PO2PL1)的粗提物在TZM-bl细胞系中显示出抗HIV-1活性,其抑制浓度(IC50)值为0.017至1.170μg/ml。三种粗提物还在0.3至50.2ng/ml的浓度范围内维持PBMC和CD4+T细胞上的病毒复制抑制谱。使用固相萃取进行部分纯化,并用气相色谱-质谱法进行分析,显示出不同的特征。根据峰面积鉴定生物活性化合物,保留时间,相似性指数。A.Alternata的GC-MS分析的主要化合物显示存在环三硅氧烷八甲基(22.92%);丙腈(16,67%);吡咯[1,2-a]吡嗪-1,4-二酮,六氢-3-(2-甲基丙基)(10.42%);硅烷,二乙基乙氧基(2-乙氧基乙氧基)(4.17%);香豆素,3,4-二氢-4,5,7-三甲基-4,5,7-三甲基-2-色满酮(13.7%)和1,2-环丁烷二甲腈(2.08%)具有先前报道的生物活性,例如抗微生物,抗炎和抗氧化特性。因此,这些生物活性化合物从A.alternata真菌内生菌可以被重新用作潜在的抗HIV药物。这项研究显示了内生真菌的潜力,来自S.birrea的链格孢菌,和Hypoxis物种作为抗HIV化合物的生产者。
Antiretroviral treatment has significantly reduced human immunodeficiency virus infection and mortality. However, the current treatment regimen is limited by adverse side effects, the emergence of drug resistance, and the inability to eliminate viral reservoirs. Here, fifteen endophytic fungi were isolated from Sclerocarya birrea and Hypoxis plants. Crude extracts of Alternaria alternata (strain ID PO4PR1, PO4PR2, and PO2PL1) of the fifteen isolate\'s crude extracts showed anti-HIV-1 activity in TZM-bl cell line at inhibitory concentration (IC50) values ranging from 0.017 to 1.170 μg/ml. The three crude extracts also maintained the virus replication inhibition profile on PBMCs and CD4+ T cells at concentrations ranging from 0.3 to 50.2 ng/ml. Partial purification using the solid phase extraction and analysis with Gas Chromatography-Mass spectrophotometry showed a diverse profile. The bioactive compounds were identified based on peak area, retention time, similarity index. The major compounds from GC-MS analysis of A. Alternata revealed the existence of cyclotrisiloxane octamethyl (22.92%); Propaninitrile (16,67%); Pyrrolol[1,2-a]pyrazine-1,4-dione, hexahydro-3-(2-methyl propyl) (10.42%); Silane, diethylethoxy(2-ethoxyethyloxy) (4.17%); Coumarin, 3,4-dihydro-4,5,7-trimethyl- 4,5,7-Trimethyl-2-chromanone (13.7%) and 1,2-Cyclobutanedicarbonitrile (2.08%) with previously reported biological activities such as antimicrobial, anti-inflammatory and antioxidant properties. Therefore, these bioactive compounds from A. alternata fungal endophytes could be repurposed as potential anti-HIV agents. This study showed the potential of endophytic fungi, Alternaria alternata from S. birrea, and Hypoxis species as producers of anti-HIV compounds.