Inhibitory Effect of Lithospermic Acid on the HIV-1 Nucleocapsid Protein

Mori, Mattia; Ciaco, Stefano; Karioti, Anastasia

doi:10.3390/molecules25225434

Cited by 7 publications

(2 citation statements)

References 44 publications

(76 reference statements)

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“…In contrast, 4′7-dihydroxyflavan (4,6)-3, 4´, 5,7- tetrahydroxyflavan and cassiabrevone share only a moderate similarity with piceatannol, which suggests that these molecules might inhibit HIV-1 replication through a mechanism that is different from that observed for piceatannol itself and norartocarpetin. The SAR study also emphasized the key role of polyphenols in providing anti-HIV activity, in agreement with recent reports [ 32 , 36 , 37 ]. One may note that piceatannol has a catechol moiety, widespread in natural products, which is considered as a protein-reactive species [ 38 , 39 ].…”

Section: Discussionsupporting

confidence: 90%

Active Components from Cassia abbreviata Prevent HIV-1 Entry by Distinct Mechanisms of Action

Zheng

Yang

Schols

et al. 2021

IJMS

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Cassia abbreviata is widely used in Sub-Saharan Africa for treating many diseases, including HIV-1 infection. We have recently described the chemical structures of 28 compounds isolated from an alcoholic crude extract of barks and roots ofC. abbreviata, and showed that six bioactive compounds inhibit HIV-1 infection. In the present study, we demonstrate that the six compounds block HIV-1 entry into cells: oleanolic acid, palmitic acid, taxifolin, piceatannol, guibourtinidol-(4α®8)-epiafzelechin, and a novel compound named as cassiabrevone. We report, for the first time, that guibourtinidol-(4α®8)-epiafzelechin and cassiabrevone inhibit HIV-1 entry (IC50 of 42.47 µM and 30.96 µM, respectively), as well as that piceatannol interacts with cellular membranes. Piceatannol inhibits HIV-1 infection in a dual-chamber assay mimicking the female genital tract, as well as HSV infection, emphasizing its potential as a microbicide. Structure-activity relationships (SAR) showed that pharmacophoric groups of piceatannol are strictly required to inhibit HIV-1 entry. By a ligand-based in silico study, we speculated that piceatannol and norartocarpetin may have a very similar mechanism of action and efficacy because of the highly comparable pharmacophoric and 3D space, while guibourtinidol-(4α®8)-epiafzelechin and cassiabrevone may display a different mechanism. We finally show that cassiabrevone plays a major role of the crude extract of CA by blocking the binding activity of HIV-1 gp120 and CD4.

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Section: Discussionsupporting

confidence: 90%

Active Components from Cassia abbreviata Prevent HIV-1 Entry by Distinct Mechanisms of Action

Zheng

Yang

Schols

et al. 2021

IJMS

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“…Lithospermic acid and lithospermic acid B are two selective HIV-1 integrase inhibitors present in Dan shen which strongly suppressed the acute HIV-1 infection of H9 cells (72). Lithospermic acid is also a noncovalent competitive inhibitor of nucleic acid binding to HIV nucleocapsid making it a potential representative of a new class of HIV inhibitor (73). Gan cao was identified to be one of the 10.3389/fcvm.2022.922497 most frequent clinically used herbs in PWH with hyperlipidemia (31.58%) in a population-based study conducted in Taiwan (11).…”

Section: Discussionmentioning

confidence: 99%

Effects and safety of Chinese herbal medicine on inflammatory biomarkers in cardiovascular diseases: A systematic review and meta-analysis of randomized controlled trials

Zhou²,

Trevillyan³

et al. 2022

Front. Cardiovasc. Med.

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Inflammation drives cardiovascular disease (CVD) in individuals with underlying chronic inflammatory diseases, including People with HIV (PWH), independently of dyslipidemia. Adjunctive treatments that lower inflammation may be useful to lower CVD risk in such populations. There is very little data on the efficacy of Chinese herbal medicine (CHM) in reducing inflammation in PWH to address its potential in reducing this CVD risk factor, therefore we evaluated its impact on inflammatory biomarkers relevant to CVD risk in the general population. Six English and Chinese databases were searched for studies investigating CHM’s effects on inflammatory biomarkers relevant to CVD from respective inceptions to February 2022. A systematic review and meta-analysis of randomized controlled trials (RCTs) were conducted and the most-frequently prescribed herbs were identified. Thirty-eight RCTs involving 4,047 participants were included. Greater than or equal to 50% of included studies had a low risk of bias in five domains (random sequence generation, detection, attrition, reporting and other bias) and 97% had a high risk of performance bias. CHM provided significant additive effects on attenuating relevant inflammatory indices including hs-CRP (SMD −2.05, 95% CI −2.55 to −1.54), IL-6 (SMD −1.14, 95% CI −1.63 to −0.66) and TNF-α levels (SMD −0.88, 95% CI −1.35 to −0.41), but no significant effects on hs-CRP were found between CHM and placebo when co-treating with Western drugs (MD 0.04, 95% CI −1.66 to 1.74). No severe adverse events were reported in CHM groups. The two most prevalent herbs present in formulae demonstrating reduction of at least one inflammatory biomarker were Dan shen (Salviae Miltiorrhizae Radix et Rhizoma) and Huang qi (Astragali Radix). CHM, in combination with standard anti-inflammatory medications, may depress inflammation and reduce the risk of inflammatory conditions such as CVD. Rigorously-conducted trials and adequate reporting are needed to provide more robust evidence supporting the use of CHM to reduce CVD risk in people with underlying chronic inflammation such as PWH.

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