Gondim Ana C S, Roberta da Silva Suzete, Mathys Leen, Noppen Sam, Liekens Sandra, Holanda Sampaio Alexandre, Nagano Celso S, Renata Costa Rocha Cintia, Nascimento Kyria S, Cavada Benildo S, Sadler Peter J, Balzarini Jan
Department of Biochemistry and Molecular Biology , Federal University of Ceará , 60455-760 , Fortaleza , Ceará , Brazil . Email:
Department of Chemistry , University of Warwick , Coventry CV4 7AL , UK . Email:
Medchemcomm. 2019 Jan 14;10(3):390-398. doi: 10.1039/c8md00508g. eCollection 2019 Mar 1.
Brazil has one of the largest biodiversities in the world. The search for new natural products extracted from the Brazilian flora may lead to the discovery of novel drugs with potential to treat infectious and other diseases. Here, we have investigated 9 lectins extracted and purified from the Northeastern Brazilian flora, from both leguminous species: (ConBr), (ConM), (DLasiL) and (DSclerL), and algae (AML), (BSL), (HML), (MEL) and (SfL). They were exposed to a panel of 18 different viruses, including HIV and influenza viruses. Several lectins showed highly potent antiviral activity, often within the low nanomolar range. DSclerL and DLasiL exhibited EC values (effective concentration of lectin required to inhibit virus-induced cytopathicity by 50%) of 9 nM to 46 nM for HIV-1 and respiratory syncytial virus (RSV), respectively, DLasiL also inhibited feline corona virus at an EC of 5 nM, and DSclerL, ConBr and ConM showed remarkably low EC values ranging from 0.4 to 6 nM against influenza A virus strain H3N2 and influenza B virus. For HIV, evidence pointed to the blockage of entry of the virus into its target cells as the underlying mechanism of antiviral action of these lectins. Overall, the most promising lectins based on their EC values were DLasiL, DSclerL, ConBr, ConM, SfL and HML. These novel findings indicate that lectins from the Brazilian flora may provide novel antiviral compounds with therapeutic potential.
巴西拥有世界上最丰富的生物多样性之一。从巴西植物群中提取新天然产物的研究可能会发现有潜力治疗传染病和其他疾病的新型药物。在此,我们研究了从巴西东北部植物群中提取并纯化的9种凝集素,它们来自豆科植物:(ConBr)、(ConM)、(DLasiL)和(DSclerL),以及藻类(AML)、(BSL)、(HML)、(MEL)和(SfL)。它们被暴露于包括HIV和流感病毒在内的18种不同病毒中。几种凝集素表现出高效的抗病毒活性,通常在低纳摩尔范围内。DSclerL和DLasiL对HIV-1和呼吸道合胞病毒(RSV)的EC值(抑制病毒诱导的细胞病变50%所需的凝集素有效浓度)分别为9 nM至46 nM,DLasiL对猫冠状病毒的EC值为5 nM,DSclerL、ConBr和ConM对甲型H3N2流感病毒株和乙型流感病毒的EC值低至0.4至6 nM。对于HIV,有证据表明这些凝集素的抗病毒作用机制在于阻止病毒进入其靶细胞。总体而言,基于其EC值最有前景的凝集素是DLasiL、DSclerL、ConBr、ConM、SfL和HML。这些新发现表明,来自巴西植物群的凝集素可能提供具有治疗潜力的新型抗病毒化合物。