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Biobased Products for Viral Diseases
Published in Mahendra Rai, Chistiane M. Feitosa, Eco-Friendly Biobased Products Used in Microbial Diseases, 2022
Gleice Ribeiro Orasmo, Giovanna Morghanna Barbosa do Nascimento, Maria Gabrielly de Alcântara Oliveira, Jéssica Missilany da Costa
According to Aiken and Chen (2005), betulinic acid derivatives are organic compounds of low molecular weight synthesized from a natural product of plant origin, and several of them are potent and highly selective HIV-1 inhibitors. In recent decades, it has been observed that the most favorable therapeutic management for this infection consists mainly of the use of specific inhibitors of the viral replication cycle, which, administered together, reduce the viral load to undetectable levels. Betulinic acid derivatives have potential as new therapies for HIV-1. Aiken and Chen (2005) reviewed recent studies and discussed the new mechanisms of action of this interesting class of antiviral compounds.
An Introduction to the Ethnopharmacology of Wild Plants
Published in Mahendra Rai, Shandesh Bhattarai, Chistiane M. Feitosa, Ethnopharmacology of Wild Plants, 2021
Shandesh Bhattarai, Christiane Mendes Feitosa, Mahendra Rai
The Combretastatins are a family of stilbenes that act as anti-angiogenic agents resulting in tumor necrosis (Cragg et al. 2002). Combretastatins isolated from the bark of Combretum caffrum showed to be active against colon, lung and leukemia cancers (Petit et al. 1987, Ohsumi et al. 1998). Homoharringtonine isolated from the Cephalotaxus harringtonia is at present in clinical use (Itokawa et al. 2005). Betulinic acid, primarily from Betula species (Cichewitz and Kouzi 2004), but also isolated from Zizyphus mauritiana, Z. rugosa and Z. oenoplia displayed selective cytotoxicity against human melanoma cell lines. Silvestrol from the fruits of Aglaila sylvestre, exhibited cytotoxicity against lung and breast cancer cell lines (Pisha et al. 1995). Other plant derived agents in clinical use are homoharringtonine isolated from Cephalotaxus harringtonia and elliptinium isolated from species of several genera of the Apocynaceae including Bleekeria vitensis, with reputed anti-cancer properties. Several Terminalia species have reportedly been used in the treatment of cancer.
Nutraceutical’s Role in Proliferation and Prevention of Gynecological Cancers
Published in Sheeba Varghese Gupta, Yashwant V. Pathak, Advances in Nutraceutical Applications in Cancer, 2019
Aaishwarya B. Deshmukh, Jayvadan K. Patel, Bharat Mishra
In U14 cervical carcinoma cells in mice exposed to betulinic acid as a food supplement have shown antitumor activity. Ethanolic extract of Conium maculatum (hemlock) inhibits the proliferation of cells within 48 hours by arresting the cell cycle at sub-G stage. Methanol extracts and ethyl acetate of M. pajang kernel and chloroform and crude petroleum ether extracts of the stem bark, respectively, have produced strong cytotoxic activity against the HeLa cervical carcinoma cell line [72]. Oridonin has the potential to inhibit the P13K-Akt pathway in HeLa cell line. Emodin and curcumin have the ability to downregulate P-Smad3, Smad4, and TGF-β receptor II, which, in turn, suppress the migration and invasion induced by TGF of cell lines in HeLa and SiHa cervical cancers [71]. Curcumin and emodin suppresses the CyclinD1, p15, p16, p21, p27, CDK6, and Pin1 expression by upregulating the Bax:Bcl-2 ratio, thereby suppressing the Wnt/β-catenin in HeLa cells. SiHa cells were chosen for TGF-β resistance, as they lack remarkable growth inhibition when treated with TGF-β [71].
Betulinic acid improves insulin sensitivity, hyperglycemia, inflammation and oxidative stress in metabolic syndrome rats via PI3K/Akt pathways
Published in Archives of Physiology and Biochemistry, 2020
R. A. Ajala-Lawal, N. O. Aliyu, T. O. Ajiboye
Elevated levels of TC, TAG, LDLc and VLDLc with concomitant reduction in HDLc reported in high-fructose diet-fed rats were consistent with previous studies (Shi et al. 2013; Prakash et al. 2014; Ajiboye et al. 2016a,b, 2017). Reversal of HFD-mediated alterations in lipid profile suggests antidyslipidaemic activity. Previous studies have demonstrated protective influence of betulinic acid on lipid alterations (Silva et al. 2016). This could have resulted from increased adiponectin, reported to inhibit sterol regulatory element-binding protein-1c (SREBP-1c) and fatty acid synthesis through AMP-activated protein kinase (AMPK) activation (Da Silva Morais et al. 2009). Interestingly, betulinic acid and its derivative (betulin) have been reported to inhibit SREBP-1c (Tang et al. 2011, Quan et al. 2013). These events could translate to reduced predisposition to and improved coronary artery and cardiovascular diseases.
Lactoferrin-tethered betulinic acid nanoparticles promote rapid delivery and cell death in triple negative breast and laryngeal cancer cells
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2020
Asim Halder, Megha Jethwa, Pritha Mukherjee, Subarna Ghosh, Suvadra Das, A. B. M. Helal Uddin, Arup Mukherjee, Urmi Chatterji, Partha Roy
Drug selection is very crucial for successes in cancer chemotherapy. Betulinic acid [BA, 3β, hydroxy-lup-20(29)-en-28-oic acid] is a pentacyclic triterpenoid found abundantly in the bark of Betula alba (white birch). The bioactive is also available in different types of plants including Eucalyptus camaldulensis, Syncarpa glomulifera, Tetracentron sinense and others [7]. BA is currently enlisted under the rapid access to intervention development program by the NIH, USA, against cancer conditions [8]. BA inhibits topoisomerase, induces apoptosis by caspase 3 activation and incites mitochondrial membrane damage [9–11]. It also stimulates reactive oxygen species (ROSs) and impairs antioxidant systems in cancer cells [12]. Betulinic acid is thus very well poised as a chemotherapeutic candidate. Betulinic acid saturation solubility in water is particularly low at 2 µg/mL [13] and is the major impediment in translational chemotherapy with BA. In general, BA is one valuable anticancer moiety if it can be aptly targeted into specific cancer cells. Compared to other plant-derived chemotherapeutic agents like taxol, camptothecine or vincristine, BA shows high degree of cancer cell selectivity minimizing the chances of toxicity to normal cells [14].
Modulating effect of a new ester, 28-O-phosphatidylbetulin (DAPB), obtained from hen egg yolk lecithin and betulin on lymphocyte subsets and humoral immune response in mice
Published in Immunopharmacology and Immunotoxicology, 2019
Magdalena Lis, Barbara Barycza, Angelika Sysak, Aleksandra Pawlak, Agnieszka Suszko-Pawłowska, Marianna Szczypka, Czesław Wawrzeńczyk, Bożena Obmińska-Mrukowicz
Betulin is a lupane-type triterpene alcohol, abundant (up to 30%) especially in the bark of Betula species. Betulin protects plant cells mainly due to its antibacterial and antifungal activity [1,2]. Anti-inflammatory and anti-allergic properties of this substance were also confirmed [3,4]. Unfortunately, betulin exhibits nonselective cytotoxic effects towards normal and cancer cell lines [5]. However, a nontoxic product of betulin oxidation, betulinic acid, is a selective apoptotic factor in various animal and human cancers [6]. Betulinic acid is a promising anticancer, antiviral, antiparasitic, and anti-inflammatory drug, at final steps clinical trials [7,8]. Cytotoxic activity of betulin and betulinic acid has been studied extensively against normal and tumor cell lines, whereas the immunomodulatory activity of other betulin derivatives enjoyed less attention.