Supramolecular combinations of humic polyanions as potent microbicides with polymodal anti-HIV-activities

Abstract

This article focuses on linking structures of fractionated humic polyanions (PAs), which were molecularly defined using ultrahigh resolution Fourier transform mass spectrometry (FTMS), to their antiviral activities with respect to laboratory HIV-1 strains. Anti-HIV-1 activity was proven using a full HIV-1 replication system validated for antiviral testing. We demonstrated that all humic PAs tested in our study were capable of inhibiting HIV fusion. The most hydrophobic fractions of humic and hymatomelanic PAs also strongly inhibited HIV-1 reverse transcriptase. The structure-activity analysis revealed the direct relationship of antiviral activities with contribution of CHO molecules in humic PA composition and lipophilicity index, and the inverse relationship with their carboxylic and total acidity. This was explained by the supramolecular character of humic PAs, the properties of which are ruled rather by the contribution of most potent scaffolds than by the total charge density. It is concluded that all humic PAs tested in this study can be considered as promising precursors for developing cost-effective combinatorial microbicides with polymodal anti-HIV activity and low cytotoxicity capable of preventing HIV-1 transmission.

Novel water-soluble lignin derivative BP-Cx-1: identification of components and screening of potential targets in silico and in vitro

“…By the structural type we assume them to be terpenoids and lignans. For example, the role of lignans in biological activity was reported in our previous work [ 58 ]. It should be noted that the database query returned BP-Cx-1 components with the highest relative intensity in mass-spectrum.…”

Application of topical peloid-derived humic acid suppresses allergic contact dermatitis in mice model

“…The source for HA used in this study was the silt sulphide mud, which is used for medicinal purposes. [1,2] Aqueous HA cream (5%) produced by blending appropriate quantities of HA and additional water into emulsifying ointment BP. For induction of ACD-like skin disorders, DNCB was applied onto the BALB/c mouse dorsal skin.…”

Microbicides for topical immunoprevention of HIV infection

“…Достаточно перспективными, по мнению авторов, природными дендримероподобными микробицидами могут стать гуминовые кислоты [29,30]. Гуминовые кислоты являются сверхразветвленными полиýлектролитами, которые широко распространены в окружающей среде и представляют органические компоненты почвы, торфа, угля, пелоидов и водных систем.…”