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Vinca rosea (Madagascar Periwinkle) and Adhatoda vesica (Malabar Nut)
Published in Azamal Husen, Herbs, Shrubs, and Trees of Potential Medicinal Benefits, 2022
Rajib Hossain, Md Shahazul Islam, Dipta Dey, Muhammad Torequl Islam
Ursolic acid is isolated from V. rosea, Prosopis glandulosa (Leguminosae), Phoradendron juniperinum (Loranthaceae), Syzygium claviflorum (Myrtaceae), and Hyptis capitata (Lamiaceae). The anti-HIV effect of ursolic acid was determined at an EC50 value of 4.4 µM and was found to exhibit a level of activity similar to that shown by oleanolic acid (Babalola et al., 2013). Thus, some ursolic acid derivatives (3-O-acyl ursolic acid derivatives) exert anti-HIV activity. (Kashiwada et al., 2000).
Ursolic Acid: A Pentacyclic Triterpene from Plants in Nanomedicine
Published in Mahfoozur Rahman, Sarwar Beg, Mazin A. Zamzami, Hani Choudhry, Aftab Ahmad, Khalid S. Alharbi, Biomarkers as Targeted Herbal Drug Discovery, 2022
Monalisha Sen Gupta, Md. Adil Shaharyar, Mahfoozur Rahman, Kumar Anand, Imran Kazmi, Muhammad Afzal, Sanmoy Karmakar
Ursolic acid (UA) has demonstrated having broad-spectrum anti-tumor activities, but its limitations restrict its clinical application and efficiency. As an in vitro model of using MCF-7 cells for anti-cancer mechanistic studies, it is found that the internalization of UA by cancer cells through a folate receptor-mediated endocytic pathway may become easy when it incorporated in a suitable matrix. A lysosomal product of UA shows a great activity by destructing the permeability of the lysosomal membrane, and then got released from lysosomes and localized into mitochondria but not nuclei. The extended retention of UA from the suitable matrix in mitochondria induced excess generation of ROS and demolition of mitochondrial membrane potential which ultimately results in the unrepairable apoptosis in carcinogenic cells. In vivo experiments demonstrated that UA in the suitable matrix could significantly reduce the burden of breast cancer particularly in the MCF-7 xenograft mouse model. These outcomes suggested that incorporated UA in a suitable matrix, can be a future prospect as an anti-cancer drug candidate against breast cancer and an upcoming perspective can provide a platform to create a novel anti-drug delivery system against cancer.
Plants from Brazil Used Against Snake Bites
Published in Mahendra Rai, Shandesh Bhattarai, Chistiane M. Feitosa, Wild Plants, 2020
Jocimar de Souza, Bruna Stramandinoli Deamatis, Fernanda Mayumi Ishii, Ingrid Francine Araújo de Oliveira, Gustavo Rodrigues Toledo Piza, Jorge Amaral Filho, Edson Hideaki Yoshida, José Carlos Cogo, Angela Faustino Jozala, Denise Grotto, Rauldenis Almeida Fonseca Santos, Yoko Oshima-Franco
The pharmacological effects of oleanolic and ursolic acids comprise a vast list of properties. Wózniak et al. (2015) and Ayeleso et al. (2017) described the properties for ursolic and oleanolic acids, respectively, as being antibacterial, antimicrobial, anticancer/antitumour, antidiabetic, antihypertensive, anti-inflammatory, antioxidant, antiparasitic, and hepatoprotective, for both triterpenes. Besides, the properties attributed to ursolic acid also include protective effects on heart, brain, skeletal muscles, bones, and other organs (skin, kidney, and lung), although some studies point out negative effects of administration of this compound (Wózniak et al. 2015). Plants and derivatives have been assayed against snake venoms and other venomous animals, since complementary alternatives to antivenom therapy are desirable mainly by lack of this product in many communities (Knudsen and Laustsen 2018).
Deciphering the anti-filarial potential of bioactive compounds from Ocimum sanctum: a combined experimental and computational study
Published in Pharmaceutical Biology, 2022
Ayushi Mishra, Vipin Kumar, Anchal Singh
To further investigate the stability of interactions between eight OS bioactive compounds and filarial antioxidant enzymes/proteins we performed molecular dynamics simulation. The simulation data obtained in this study clearly shows that OS bioactive compounds remained bound to the proteins throughout the run suggesting that these complexes are well stabilized. Ursolic acid, chlorogenic acid, and luteolin were most stable during the simulation run showing the lowest RMSD and RMSF values. Ursolic acid (UA) has preventive and curative properties against many diseases affecting the liver and brain, and also in cancers and metabolic syndromes etc. (Seo et al. 2018). UA has been found to be effective against B. malayi GST in a previous study (Kalani et al. 2014). Luteolin has antioxidant properties and has shown potential as anti-inflammatory agent in a gut inflammation model (Mizuno and Nishitani 2013). Chlorogenic acid is an important bioactive polyphenol and many studies confirm it as antidiabetic, anti-obesity, anti-tumor, neuro protector, hepatoprotective, antioxidant, and anti-inflammatory activity (Tajik et al. 2017). Therefore, the combined results of these ex vivo and in silico studies with OS and its bioactive compounds strongly indicate towards their anti-filarial potential which should be explored further for developing adulticidal filarial drugs.
Ursolic acid derivative UA232 evokes apoptosis of lung cancer cells induced by endoplasmic reticulum stress
Published in Pharmaceutical Biology, 2020
Wenfeng Gou, Na Luo, Huiqiang Wei, Hongying Wu, Xiaojun Yu, Yuqing Duan, Changfen Bi, Hongxin Ning, Wenbin Hou, Yiliang Li
Ursolic acid (UA) is a pentacyclic triterpene complex that can be isolated from a variety of plants and fruits, such as rosemary, lavender, thyme, and apple peel (Chang et al. 2017). The early research of UA it was mainly used in antibacterial, antiviral, and immune regulation (Kim et al. 2013; do Nascimento et al. 2014). Multiple studies further demonstrated that UA had more pharmacological effects, such as blocking the process of chronic disease (Yu et al. 2017), radiosensitization (Yang et al. 2015), neuroprotective (Habtemariam 2019), antidiabetic (Xu et al. 2018), and antitumor (Zang et al. 2014). Studies have confirmed that UA plays an antitumor role in a variety of tumours, including colorectal cancer (Kim et al. 2018), breast cancer (Yin et al. 2018), endometrial carcinoma (Achiwa et al. 2013), and lung cancer (Yang et al. 2019). UA plays an antitumor role in a variety of ways, including inhibition of proliferation, angiogenesis, invasion, metastasis, differentiation, and induction of tumour cell apoptosis (Zhang et al. 2014). However, the poor bioavailability and efficacy of UA limit its clinical application in the treatment of lung cancer (Biswas et al. 2019).
Triterpenoids and steroids isolated from Anatolian Capparis ovata and their activity on the expression of inflammatory cytokines
Published in Pharmaceutical Biology, 2020
Isil Gazioglu, Sevcan Semen, Ozden Ozgun Acar, Ufuk Kolak, Alaattin Sen, Gulacti Topcu
The effect of the purified secondary metabolites (PSM) on the expression of the selected genes participating in inflammation was determined in this study (Supplementary Table S1). The CCL5, CXCL9, CXCL10, HIF1A, IL6, NFKB1 and TNFα genes are known to be major players in the TNF signalling pathway. Their functional and physical association in this pathway were also depicted by STRING (Search Tool for the Retrieval of Interacting Genes/Proteins) analysis (Figure 2). TNF signalling plays a central role in inflammation and promotes inflammatory responses. The effect of the PSM on these genes was evaluated since caper is known to be utilized for its anti-inflammatory actions (Bektas et al. 2012). The new compound olean-12-en-28-ol, 3β-pentacosanoate (1) inhibited significantly the expression of all these inflammatory cytokines in SH-SY5Y cells, particularly CXCL9 and TNF-α. Both oleanolic acid (2) and its isomer ursolic acid (3) did inhibit the expression of TNF-α, additionally CXCL9 and CCL5. Moreover, ursolic acid inhibited nearly the same expression in all the genes tested. It has been shown that the agents blocking the TNF-α action may be used to treating problems associated with autoimmune diseases such as rheumatoid arthritis, inflammatory bowel disease and multiple sclerosis (Dinarello 2010).