Abstract
CareVid is a multi-herbal product used in southwest Kenya as an immune booster and health tonic and has been anecdotally described as improving the condition of HIV-positive patients. The product is made up of roots, barks and whole plant of 14 African medicinal plants: Acacia nilotica (L.) Willd. ex Delile (currently, Vachelia nilotica (L.) P.J.H Hurter & Mabb.), Adenia gummifera (Harv.) Harms, Anthocleista grandiflora Gilg, Asparagus africanus Lam., Bersama abyssinica Fresen., Clematis hirsuta Guill. & Perr., Croton macrostachyus Hochst. ex Delile, Clutia robusta Pax (accepted as Clutia kilimandscharica Engl.), Dovyalis abyssinica (A. Rich.) Warb, Ekebergia capensis Sparm., Periploca linearifolia Quart.-Dill. & A. Rich., Plantago palmata Hook.f., Prunus africana Hook.f. Kalkman and Rhamnus prinoides L’Her. The objective of this study was to determine the major chemical constituents of CareVid solvent extracts and screen them for in vitro and in silico activity against the HIV-1 reverse transcriptase enzyme. To achieve this, CareVid was separately extracted using CH2Cl2, MeOH, 80% EtOH in H2O, cold H2O, hot H2O and acidified H2O (pH 1.5–3.5). The extracts were analysed using HPLC–MS equipped with UV diode array detection. HIV-1 reverse transcriptase inhibition was performed in vitro and compared to in silico HIV-1 reverse transcriptase inhibition, with the latter carried out using MOE software, placing the docking on the hydrophobic pocket in the subdomain of p66, the NNRTI pocket. The MeOH and 80% EtOH extracts showed strong in vitro HIV-1 reverse transcriptase inhibition, with an EC50 of 7 μg·mL−1. The major components were identified as sucrose, citric acid, ellagic acid, catechin 3-hexoside, epicatechin 3-hexoside, procyanidin B, hesperetin O-rutinoside, pellitorine, mangiferin, isomangiferin, 4-O-coumaroulquinic acid, ellagic acid, ellagic acid O-pentoside, crotepoxide, oleuropein, magnoflorine, tremulacin and an isomer of dammarane tetrol. Ellagic acid and procyanidin B inhibited the HIV-1 reverse transcription process at 15 and 3.2 µg/mL−1, respectively. Docking studies did not agree with in vitro results because the best scoring ligand was crotepoxide (ΔG = −8.55 kcal/mol), followed by magnoflorine (ΔG = −8.39 kcal/mol). This study showed that CareVid has contrasting in vitro and in silico activity against HIV-1 reverse transcriptase. However, the strongest in vitro inhibitors were ellagic acid and procyanidin B.
Highlights
Introduction conditions of the Creative CommonsIn the developing world, a large fraction of the population is dependent on herbal remedies as their primary form of healthcare
The docking studies were performed using human immunodeficiency virus (HIV)-1 reverse transcriptase (RT) in complex with the known inhibitor Nevirapine obtained from the RCSB Protein data bank (PDB ID 1JLB)
Its use in combination with two NRTIs is recommended. Some of these components can be traced to the herbal ingredients by a cross-examination of the published literature, i.e., catechin 3-hexoside [22], ellagic acid and ellagic acid Opentoside [23] have been reported from Acacia nilotica
Summary
A large fraction of the population is dependent on herbal remedies as their primary form of healthcare. In Africa, wild harvested medicines are commonly used in the form of bark or root [1] because it is believed that these organs. Pharmaceuticals 2021, 14, 1009 have a higher accumulation of secondary metabolites. Bark and root medicines are dried, powdered and extracted into an aqueous solution with heat and consumed as a potent tea. While it is common for these therapies to be administered for acute conditions, such as gastrointestinal disturbance or fevers, there is no dearth of clients with chronic diseases, such as human immunodeficiency virus (HIV), that benefit from herbal prescriptions by attenuating symptoms, delaying their inevitable mortality, or treating comorbidities. There is plenty of scope for multi-herbal compositions to stand in as adjuvant therapies to mainstream treatments for HIV, the financial barrier to acquiring antiretroviral therapies in the remote regions of Kenya [2] means that such therapies become primary, which has persuaded herbalists to innovate multi-herbal compositions to give people with a lower socioeconomic status who are living with HIV a better quality of life
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