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Herbal Drug Discovery Against Inflammation: From Traditional Wisdom to Modern Therapeutics
Published in Amit Baran Sharangi, K. V. Peter, Medicinal Plants, 2023
Shalini Dixit, Karuna Shanker, Madhumita Srivastava, Priyanka Maurya, Nupur Srivastava, Jyotshna, Dnyaneshwar U. Bawankule
Chrysanthemum indicum is widely used to treat immune-related and infectious disorders in East Asia for a long time. Flower oil contains 1,8-cineole, germacrene D, camphor, α-cardinal, camphene, pinocarvone, ß-caryophyllene, 3-cyclohexane-1-on, and γ-curcumene. Octulosonic acid derivative, chrysannol A, isolated from Chrysanthemum indicum flowers has also shown in-vitro anti-inflammatory effects. Results are important in terms of the development of C. indicum as an anti-inflammatory functional food (Hwang and Kim, 2013; Luyen et al., 2015). The most valued and ancient among medicinal plants G. biloba of family Ginkgoaceae rediscover its existence as important pharmacological compounds and their therapeutic effects. The worldwide sales of ginkgo leaf products are difficult to estimate but believed to be worth around half a billion USD or more (Isah, 2015). The main constituent of oil coriander linalool from Coriandrum sativum (Umbelliferae) exhibits anti-inflammatory action. The bioactive constituent α and ß pinene of Bupleurum fructicosum L. (Umbelliferae) essential oil have shown significant anti-inflammatory activity in carrageenan-induced rat paw edema model (Perez, 2001). Lupeol, a novel dietary triterpene (also known as Fagarsterol) present in white cabbage, green pepper, strawberry, olive, mangoes, and grapes is reported to possess beneficial effects as anti-inflammatory and anti-cancer (Mohammad, 2009).
Anti-Proliferative Properties of Various South African Buddleja Species
Published in Namrita Lall, Medicinal Plants for Cosmetics, Health and Diseases, 2022
The flavonoid isolated from this species, apigenin-7-O-glucoside, exhibits anti-proliferative activity against colon cancer cell lines and can cause apoptosis by inducing pro-apoptotic proteins such as Bax and p53 (Smiljkovic et al., 2017). The terpenes lupeol and zerumbone have both been reported to have anti-proliferative activity (Abdul et al., 2008; Saleem, 2009). Zerumbone exhibited good anti-proliferative activity on laryngeal carcinoma cells (Hep-2) with an IC50 value of 15 µM and arrests the cell cycle of these cells in vitro (Jegannathan et al., 2016). The terpene aucubin exhibits anti-analgesic, anti-inflammation and anti-tumor activity by decreasing the expression of various proteins such as MMP-3, MMP-9 and MMP-13, as well as COX-2 and iNOS, which are all associated with inflammation. Finally, ferulic acid methyl ester and β-amyrin also both have anti-inflammatory activity (Nogueira et al., 2019).
Anti-Inflammatory Properties of Bioactive Compounds from Medicinal Plants
Published in Hafiz Ansar Rasul Suleria, Megh R. Goyal, Health Benefits of Secondary Phytocompounds from Plant and Marine Sources, 2021
Muhammad Imran, Abdur Rauf, Anees Ahmed Khalil, Saud Bawazeer, Seema Patel, Zafar Ali Shah
IBD (Inflammatory bowel disease) i.e., Crohn’s disease and ulcerative colitis are chronic inflammatory diseases of lower GIT (gastrointestinal tract). Lupeol significantly decreased the formation of pro-inflammatory cytokines (IL-1β, TNFα, IL-6, and IL-12), and caused remarkable elevation in formation of p38 MAPK [39]. In vivo, in silico, ex vivo and in vitro studies revealed that Lupeol significantly prevented hemorrhage, oxidative stress, cleavage of collagen and CX3CR1 receptors, edema, myotoxicity, dermonectosis, and myonecrosis in inflammatory cell induced due to Echiscarinatus (saw-scaled viper) bite venom [34]. Intraperitoneal injection of Lupeol (@ 10, 25, or 50 mg/kg) had significant effect on the severity of pancreatitis, which was proven by decreased neutrophil infiltration and pancreatic edema. Additionally, lupeol suppressed the elevated content of digestive enzymes (IL-6) and cerulean-induced acinar cell death [54].
Antiandrogen enzalutamide induced genetic, cellular, and hepatic damages: amelioration by triterpene Lupeol
Published in Drug and Chemical Toxicology, 2023
Mohammad A. Khan, Deepti Singh, Homa Fatma, Kafil Akhtar, Farruk Arjmand, Santosh Maurya, Hifzur R. Siddique
Lupeol is a triterpene found in a variety of fruits and vegetables, including white cabbage, pepper, olive, fig, mango, etc. (Siddique et al.2011). Various reports have been published describing the anti-inflammatory, antiarthritic, and anti-cancer properties of Lupeol both in vitro and in vivo (Siddique et al.2011). In a study, Siddique et al. (2011) demonstrated that Lupeol significantly inhibits the R1881 (androgen-analog)-induced transcriptional activity of AR and expression of PSA. Moreover, Lupeol also sensitizes the CRPC cells to ADT and anti-hormonal therapy (Siddique et al.2011). Further, Lupeol has also been reported to significantly sensitize the cancer cells to Bicalutamide and inhibit cell proliferation (Siddique et al.2011). Our study explores the combination of Lupeol and Enzalutamide in treating prostate cancer via increasing sensitivity to Enzalutamide and minimizing the Enzalutamide-induced adverse effects. In this context, the present study aimed to provide the data supporting the ameliorating effects of Lupeol on the Enzalutamide-induced adverse effects at genetic, cellular, biochemical, and tissue level.
Macrophage polarization: an effective approach to targeted therapy of inflammatory bowel disease
Published in Expert Opinion on Therapeutic Targets, 2021
Yaoyao Du, Lan Rong, Yuanhua Cong, Lan Shen, Ning Zhang, Bing Wang
Lupeol (pentacyclic triterpene lup-20(29)-en-3β-ol) is a natural triterpene compound that is widely found in various vegetables (e.g. cabbage, cucumber), fruits (e.g. figs, mangoes), and medicinal plants (e.g. American ginseng, shea butter plants) [179]. It has a variety of pharmacological activities both in vivo and in vivo. It can induce apoptosis, exert anti-inflammatory and anti-mutagenic effects, and inhibit tumor growth [180]. In the study of IBD, lupeol can reduce intestinal inflammation by inhibiting the NF-κB signaling pathway and can convert the macrophage phenotype from M1 to M2 [181]. Thus, it is beneficial in the treatment of IBD. Zhu et al. found that lupeol regulates macrophage polarization due to its downregulation of IRF5 expression, which is related to a significant decrease in phosphorylation of p38 MAPK [182]. Lupeol treatment resulted in a significant reduction of pro-inflammatory cytokines (including IL-12, IL6, IL-1β, and TNF-α) secreted by M1 macrophages, whereas the production of IL-10 and CD206 (a typical marker of M2 macrophage) is remarkably increased [182]. Furthermore, lupeol treatment prevents the destruction of the epithelial barrier [182].
New and emerging drugs for the treatment of acne vulgaris in adolescents
Published in Expert Opinion on Pharmacotherapy, 2019
Isabel Cristina Valente Duarte De Sousa
Lupeol, a pentacyclic triterpene extracted from the Solanum melongena L. plant, decreases lipogenesis in sebocytes in vitro by suppressing the IGF-1R/phosphatidylinositide 3 kinase (PI3K)/SREBP signaling pathway. Furthermore, lupeol has anti-proliferative effects and has the ability to lower intracellular lipid content by 58% by reducing fatty acid content in sebocytes in vitro. Lupeol also exerts anti-inflammatory properties by decreasing cytokine gene expression in both cultured sebocytes and keratinocytes. Moreover, in HaCat keratinocytes, lupeol suppresses protein and mRNA expression of IL-1α, a strong inducer of comedogenesis. Lupeol also shows direct antimicrobial activity against P. acnes [94], thus making it an interesting novel way to treat acne vulgaris. Histopathological and immunohistochemical analysis of human acne lesions treated with 2% lupeol twice daily for 4 weeks, showed a significant decrease in IGF-1R, SREBP-1, IL-8, IL-1α, TLR-2, and keratin 16 expression, as well as a reduction in inflammatory, infiltrates around comedones and sebaceous glands, thus confirming its ability to decrease lipogenesis, inflammation and IL-1α-induced comedone formation [94]. Two small clinical studies have assessed the safety and efficacy of topical lupeol 2% in the treatment of mild to moderate acne vulgaris in patients 15 years old and older, however, official results are not available yet [95,96].