Betulin, a Newly Characterized Compound in Acacia Auriculiformis Bark, is a Multi-target Protein Kinase Inhibitor

Ahmadu, AA; Delehouzé, Claire; Haruna, Anas; Mustapha, Lukman; Lawal, Bilqis A.; Udobre, Aniefiok; Baratte, Blandine; Triscornia, Camilla; Autret, Axelle; Thomas, Robert; Bulinski, J. Chloë; Rousselot, Morgane; Eugenio, Mélanie Simoes; Dimanche‐Boitrel, Marie‐Thérèse; Petzer, Jacobus P.; Legoabe, Lesetja J.; Bach, Stéphane

doi:10.20944/preprints202106.0115.v1

Cited by 6 publications

(1 citation statement)

References 37 publications

(49 reference statements)

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“…eir structures have been established using their spectrometric and spectroscopic data in comparison with those reported in the literature. us, the nine compounds have been classified into four triterpenoids including lupeol (1) [22,23], betulin (2) [24], betulinic acid (3) [25,26], β-amyryl acetate (4) [27]; one anthraquinone named physcion (5) [28], two flavonoids identified as quercetin (6) and rutin (7) [29], as well as two common steroids β-sitosterol (8) and its glucoside β-sitosterol-3-O-β-D-glucopyranoside (9) [30]. To the best of our knowledge, all the isolated compounds are reported herein for the first time from this plant species.…”

Section: Phytochemical Studymentioning

confidence: 99%

Chemical Constituents from Uapaca guineensis (Phyllanthaceae), and the Computational Validation of Their Antileishmanial and Anti-inflammatory Potencies

Happi

Yimtchui

Ahmed

et al. 2022

Journal of Chemistry

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From the chemical investigations of the root bark of Uapaca guineensis, nine distinct compounds (1–9) have been isolated and characterized as lupeol, betulin, betulinic acid, β-amyryl acetate, physcion, quercetin, rutin, β-sitosterol, and β-sitosterol-3-O-β-D-glucopyranoside, respectively. The structures of all the isolated compounds have been established using their NMR data as well as the comparison of those data with the ones reported in the literature. Interestingly, to the best of our knowledge, except for the lupane-type triterpenoids (1–3) and compounds 4 and 9, all the other compounds are reported for the first time from this genus. Since the plant is widely used for the treatment of skin diseases, leishmaniasis and inflammatory diseases, the antileishmanial and anti-inflammatory potencies of all the isolated compounds have been computationally validated through their ability to inhibit the receptors 1QCC and 2XOX (for the antileishmanial studies) and 6Y3C and 1CX2 (for the anti-inflammatory studies). Furthermore, the ADMET studies of compounds have been done to evaluate their drug-likeness. Results demonstrate that all the isolated compounds showed a better affinity for both receptors’ binding sites than the standard drugs miltefosine and aspirin. Moreover, the compounds would not cause addiction when used as lead molecules whereas, aspirin is predicted to violate the BBB over a long term of usage as a drug. This study gives additional information on the chemistry of U. guineensis and its classification as a potential source of good leads for the development of potent antileishmanial and anti-inflammatory drugs.

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Section: Phytochemical Studymentioning

confidence: 99%

Chemical Constituents from Uapaca guineensis (Phyllanthaceae), and the Computational Validation of Their Antileishmanial and Anti-inflammatory Potencies

Happi

Yimtchui

Ahmed

et al. 2022

Journal of Chemistry

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Medicinal Importance and Phytoconstituents of Underutilized Legumes from the Caesalpinioideae DC Subfamily

et al. 2023

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Underutilized legumes are common crops in developing countries with superior dietary potentials that could be useful sources of protein as well as some phytoconstituents. They are more tolerant of abiotic environmental conditions like drought than the major legumes. This makes them more adapted to harsh soil and climatic conditions, which helps to minimize the pressure brought on by climate change. However, despite their potential, underutilized legumes have been greatly overlooked compared to the major legumes due to supply constraints. Underutilized legumes in the subfamily Caesalpinioideae are better suited for use as animal feeds with little or no value as food for humans, and the extracts and infusions of the different parts of plant species in this subfamily are traditionally used for the treatment of different diseases. In addition, underutilized legumes in this subfamily contain phytoconstituents that are of pharmacological relevance, some of which have been isolated, characterized and evaluated for use in the treatment of a variety of disorders. Therefore, this review describes the medicinal activities of some selected underutilized legumes from five genera in the subfamily Caesalpinioideae as well as their phytoconstituents, which could be exploited as lead compounds for drug discovery.

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Pharmacological Potential of Betulin as a Multitarget Compound

Adepoju

Duru

et al. 2023

Biomolecules

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Betulin is a natural triterpene, usually from birch bark, known for its potential wound-healing properties. Despite having a wide range of pharmacological targets, no studies have proposed betulin as a multitarget compound. Betulin has protective effects against cardiovascular and liver diseases, cancer, diabetes, oxidative stress, and inflammation. It reduces postprandial hyperglycemia by inhibiting α-amylase and α-glucosidase activity, combats tumor cells by inducing apoptosis and inhibiting metastatic proteins, and modulates chronic inflammation by blocking the expression of proinflammatory cytokines via modulation of the NFκB and MAPKs pathways. Given its potential to influence diverse biological networks with high target specificity, it can be hypothesized that betulin may eventually become a new lead for drug development because it can modify a variety of pharmacological targets. The summarized research revealed that the diverse beneficial effects of betulin in various diseases can be attributed, at least in part, to its multitarget anti-inflammatory activity. This review focuses on the natural sources, pharmacokinetics, pharmacological activity of betulin, and the multi-target effects of betulin on signaling pathways such as MAPK, NF-κB, and Nrf2, which are important regulators of the response to oxidative stress and inflammation in the body.

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Betulin, a Newly Characterized Compound in Acacia Auriculiformis Bark, is a Multi-target Protein Kinase Inhibitor

Cited by 6 publications

References 37 publications

Chemical Constituents from Uapaca guineensis (Phyllanthaceae), and the Computational Validation of Their Antileishmanial and Anti-inflammatory Potencies

Chemical Constituents from Uapaca guineensis (Phyllanthaceae), and the Computational Validation of Their Antileishmanial and Anti-inflammatory Potencies

Medicinal Importance and Phytoconstituents of Underutilized Legumes from the Caesalpinioideae DC Subfamily

Pharmacological Potential of Betulin as a Multitarget Compound

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