Evaluation of Anti-HIV-1 Integrase and Anti-Inflammatory Activities of Compounds from <i>Betula alnoides</i> Buch-Ham

Chaniad, Prapaporn; Sudsai, Teeratad; Septama, Abdi Wira; Chukaew, Arnon; Tewtrakul, Supinya

doi:10.1155/2019/2573965

Cited by 15 publications

(11 citation statements)

References 47 publications

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“…Our finding on the anti-HIV activity of these pure compounds is in agreement with previous reports. A report by Chaniad et al [ 61 ] explained the efficacy of betulin (4) as a potent anti-HIV compound with an IC 50 value of 17.7 ± 0.6 μM. Similarly, Esposito et al [ 62 ] reported that lupeol acetate and lupeol inhibited HIV-1 RT-associated RNase H function with IC 50 values of 63 and 11.6 μM, respectively.…”

Section: Resultsmentioning

confidence: 99%

“…These results are in agreement with previously reported ant-HIV activities of the known compounds. Chaniad et al [ 61 ] described the efficacy of betulin (4) against HIV with an IC 50 value of 17.7 ± 0.6 μM, whereas Esposito et al [ 62 ] reported that lupeol acetate and lupeol inhibited HIV-1 RT-associated RNase H function with IC 50 values of 63 and 11.6 μM, respectively. The current results and the described past anti-HIV effects of compounds found in C. macrostachys , ascertains the importance of the plant, as was previously reported by Maroyi (2017) [ 18 ].…”

Section: Discussionmentioning

confidence: 99%

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In vitro anti-HIV and cytotoxic effects of pure compounds isolated from Croton macrostachyus Hochst. Ex Delile

Terefe

Okalebo

Derese

et al. 2022

BMC Complement Med Ther

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Croton macrostachyus is an important plant in traditional African medicine, widely utilized to treat a variety of diseases. In Kenya, HIV-infected patients use leaf and root decoctions of the plant as a cure for cough, back pain, bleeding, skin diseases, warts, pneumonia, and wounds. This study aimed to evaluate the anti-HIV activities and cytotoxic effects of extracts and chemical constituents isolated from C. macrostachyus. In our previous study we demonstrated that the hexane, CH2Cl2, ethyl acetate and methanol soluble fractions of a 1:1 v/v/ CH2Cl2/MeOH crude extracts of the leaves and stem bark of C. macrostachyus exhibited potent anti-HIV activities against HIV-1 with IC50 values ranging from 0.02–8.1 μg/mL and cytotoxicity effects against MT-4 cells ranging from IC50 = 0.58–174 μg/mL. Hence, hexane soluble extract of 1:1 v/v/ CH2Cl2/MeOH crude extract of the leaves of C. macrostachyus, that was more potent against HIV-1 at IC50 = 0.02 μg/mL was subjected to column chromatography leading to the isolation of 2-methoxy benzyl benzoate (1), lupenone (2), lupeol acetate (3), betulin (4), lupeol (5), sitosterol (6) and stigmasterol (7). Lupenone (2), lupeol acetate (3) and betulin (4) exhibited anti-HIV-1 inhibition at IC50 = 4.7 nM, 4.3 and 4.5 μg/mL respectively. The results obtained from this study support the potential of C. macrostachyus, as a source of anti-HIV constituents.

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Section: Resultsmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

In vitro anti-HIV and cytotoxic effects of pure compounds isolated from Croton macrostachyus Hochst. Ex Delile

Terefe

Okalebo

Derese

et al. 2022

BMC Complement Med Ther

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“…Previously, pellitorine was tested for its inhibitory effect against HIV-1 reverse transcriptase [ 24 ]. In addition, lupeol ( 7 ) and betulin ( 8 ) are known HIV-1 IN inhibitors [ 11 ]. Furthermore, Huang et al, 2007 reported that oleuropein ( 2 ) inhibits HIV-1 IN, but we only observed modest inhibitory effects in the current study, inhibiting 4.7% at 25 μg/mL [ 25 ].…”

Section: Discussionmentioning

confidence: 99%

“…However, these drugs have limited clinical benefit because long-term treatments may lead to the emergence of drug resistance and side effects [ 10 ]. Therefore, finding alternative agents that take the pressure away from these more efficient INSTIs will slow the progress of resistance development [ 11 ].…”

Section: Introductionmentioning

confidence: 99%

HIV-1 Integrase Inhibitory Effects of Major Compounds Present in CareVid™: An Anti-HIV Multi-Herbal Remedy

Rotich

Mas‐Claret

Sadgrove

et al. 2022

Life

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In our continued study on the anti-HIV activity of compounds present in CareVidTM, we report the HIV-1 integrase ((HIV-1 IN) inhibitory effects of pellitorine (1), oleuropein (2), magnoflorine (3), crotepoxide (4), ent-kaurane-16β,17-diol (5), crotocorylifuran (6), lupeol (7), betulin (8), and ellagic acid (9) in an in vitro enzyme assay, and in an in silico study. Ellagic acid, pellitorine, lupeol, and betulin showed an in vitro percentage inhibition against HIV-1 IN of 21.1%, 19.0%, 18.5%, and 16.8%, respectively, at a standard concentration of 25 μg/mL. However, from a pharmacokinetic perspective, ellagic acid has poor bioavailability, due to rapid elimination in metabolism in the gut microbiome. It was postulated that known gut catabolites of ellagic acid, urolithin A (10) and urolithin B (11) could be more promising candidates in exploring the anti-HIV activity of ellagic acid-rich medicinal species consumed orally. On the contrary, urolithin A and urolithin B demonstrated lower activity with comparison to ellagic acid. The binding affinity of compounds 1–9, urolithin A, and urolithin B against the catalytic domain of HIV-1 IN was also explored by in silico methods. Docking studies showed oleuropein as the best candidate, with a predicted energy of binding of ΔG −5.81 kcal/mol, while ellagic acid showed moderate predicted inhibition (ΔG −4.38 kcal/mol) caused by the interaction between the carbonyl and the key Mg2+ ion in the active site.

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“…These polypeptides are then processed by several virus-encoded proteases viz., chymotrypsin like-3CL pro , main protease-M pro -NSp5 and papain like NSP3 proteases into 16 nonstructural proteins (nsps) that constitute the viral replicase-transcriptase system consisting of helicases, RNA-dependent RNA polymerase, and other nonstructural proteins that are packed in membrane vesicles and involved in viral multiplication and assembly [97]. The natural ursolic acid (3β-3hydroxyl-urs-12-ene-28-oic acid, a pentacyclic triterpenoid) and its derivatives present in Hyptis suaveolens and other plants of family Lamiaceae act as potent antiviral agent against rotaviruses, HIV, influenza, and hepatitis B and C viruses [10,53,88,98,99].…”

Section: Hyptis Suaveolens As a Source Of Potential Therapeutic Agentmentioning

confidence: 99%

A review on the phytochemical and pharmacological properties of Hyptis suaveolens (L.) Poit

2021

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Background Plants are the repository of variable number of valuable secondary metabolites that bears pharmacognostic and pharmacological implications having potentiality to emerge as super drugs in future. In-vivo production of these metabolites is influenced by the biotic and abiotic stresses resulting in continuous accumulation of diverse phytochemicals and their derivatives that can be useful in designing and developing potential drugs for future. The aim of the present study is to review the existence of medicinally important secondary metabolites and possible pharmacological and pharmacognostic importance of under-explored weed plant species Hyptis suaveolens (L.) Poit., to explore the potentiality of the plant for developing and designing the drugs for future. Main body of the abstract Hyptis suaveolens belonging to family Lamiaceae is the rich source of medicinally important phytochemicals like essential oils, tannins, saponins, phenols, flavonoids, terpenoids, alkaloids, and sterols. One or many of these compounds have antioxidative, anti-inflammatory, antispasmodic, anti-septic, anti-cancer, anti-ulcer, antimicrobial, antibacterial, antiviral, antifungal, anti-diabetic, anti-fertility, diaphoretics, anticutaneous, anticatarrhal, antirheumatic, anti-ulcer, gastroprotective, immunomodulatory, analgesic, and antiviral activity. Short conclusion Hyptis suaveolens contains unique terpenoid metabolites like suaveolic acid, suaveolol, methyl suaveolate, beta-sitosterol, ursolic acid, and phenolic compound like rosamarinic acid, methyl rosamarinate that have potentiality to substitute the traditional drugs as therapeutic agent against the resistant and newly emerged bacterial and viral pathogens. Pentacyclic triterpenoid, ursolic acid have been reported to have effective antiviral response against the SARS-CoV2 responsible for the present COVID-19 pandemic and HIV virus for which no effective vaccines are available till date. Ursolic acid has the ability to modulate the activity of main protease (Mpro) that is essential for processing of SARS-CoV2 replicase-transcriptase machinery needed for viral replication and particle assembly.

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Evaluation of Anti-HIV-1 Integrase and Anti-Inflammatory Activities of Compounds from Betula alnoides Buch-Ham

Cited by 15 publications

References 47 publications

In vitro anti-HIV and cytotoxic effects of pure compounds isolated from Croton macrostachyus Hochst. Ex Delile

In vitro anti-HIV and cytotoxic effects of pure compounds isolated from Croton macrostachyus Hochst. Ex Delile

HIV-1 Integrase Inhibitory Effects of Major Compounds Present in CareVid™: An Anti-HIV Multi-Herbal Remedy

A review on the phytochemical and pharmacological properties of Hyptis suaveolens (L.) Poit

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