AsterBioChem Research Team, School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Avenida do Café s/n, Ribeirão Preto 14040-020, SP, Brazil.
Gilson Purification, 22 rue Bourseul, ZI du Poteau, 56890 Saint Avé, France.
Int J Mol Sci. 2023 Feb 7;24(4):3333. doi: 10.3390/ijms24043333.
Chikungunya virus (CHIKV) is an arthropod-borne virus that belongs to the genus (family Togaviridae). CHIKV causes chikungunya fever, which is mostly characterized by fever, arthralgia and, sometimes, a maculopapular rash. The bioactive constituents of hops (, Cannabaceae), mainly acylphloroglucinols, known as well as - and -acids, exerted distinct activity against CHIKV, without showing cytotoxicity. For fast and efficient isolation and identification of such bioactive constituents, a silica-free countercurrent separation method was applied. The antiviral activity was determined by plaque reduction test and was visually confirmed by a cell-based immunofluorescence assay. All hops compounds demonstrated a promising post-treatment viral inhibition, except the fraction of acylphloroglucinols, in mixture. -acids fraction of 125 µg/mL expressed the strongest virucidal activity (EC = 15.21 µg/mL), in a drug-addition experiment on Vero cells. Hypothesis for mechanism of action were proposed for acylphloroglucinols based on their lipophilicity and chemical structure. Therefore, inhibition of some steps of the protein kinase C (PKC) transduction cascades was also discussed.
基孔肯雅病毒(CHIKV)是一种虫媒病毒,属于 (黄病毒科)属。CHIKV 引起基孔肯雅热,主要表现为发热、关节痛,有时伴有斑丘疹。啤酒花(大麻科)的生物活性成分,主要是酰基间苯三酚,俗称 - 和 - 酸,对 CHIKV 表现出明显的活性,而没有显示出细胞毒性。为了快速有效地分离和鉴定这些生物活性成分,应用了无硅胶逆流分离法。抗病毒活性通过蚀斑减少试验测定,并通过基于细胞的免疫荧光法进行了直观确认。除混合物中的酰基间苯三酚部分外,所有啤酒花化合物在后处理病毒抑制方面表现出很大的潜力。在 Vero 细胞中的药物添加实验中,125 µg/mL 的 - 酸部分表现出最强的病毒杀灭活性(EC = 15.21 µg/mL)。基于酰基间苯三酚的亲脂性和化学结构,提出了其作用机制的假设。因此,还讨论了对蛋白激酶 C(PKC)转导级联的某些步骤的抑制。