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ursolic acid

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https://www.readbyqxmd.com/read/28719984/cytotoxic-and-immunomodulatory-potential-activity-of-physalis-peruviana-fruit-extracts-on-cervical-cancer-hela-and-fibroblast-l929-cells
#1
Helen Mier-Giraldo, Luis Eduardo Díaz-Barrera, Lucy Gabriela Delgado-Murcia, Manuel Fernando Valero-Valdivieso, Gabriela Cáez-Ramírez
It was purposed to evaluate the biological potential of ethanol and isopropanol crude extracts of ripe Physalis peruviana fruits. Cytotoxic and immunomodulatory effects of the expression of interleukin-6, interleukin-8, and monocyte chemoattractant protein-1 (MCP-1) were evaluated on human cervical cancer (HeLa) and murine fibroblast (L929) cells. The composition was evaluated by high-performance liquid chromatography diode-array detection and high-performance liquid chromatography ultraviolet/visible detection...
January 1, 2017: Journal of Evidence-based Complementary & Alternative Medicine
https://www.readbyqxmd.com/read/28714512/inhibition-of-stat3-signaling-pathway-by-ursolic-acid-suppresses-growth-of-hepatocellular-carcinoma
#2
Tianshu Liu, Haiyan Ma, Wei Shi, Jialin Duan, Yina Wang, Cuntai Zhang, Chenglong Li, Jiayuh Lin, Sheng Li, Jiagao Lv, Li Lin
The signal transducer and activator of transcription 3 (STAT3) has been found to be constitutively active in liver cancer. There is no STAT3 inhibitors approved to be used clinically for the treatment or prevention of liver cancer. Some dietary compounds including ursolic acid (UA) have been reported to inhibit the growth of cancer cells. However, whether UA could inhibit STAT3 phosphorylation in hepatocellular carcinoma has not been reported. The inhibitory effects of UA on STAT3 phosphorylation, along with cell viability, migration, colony formation in vitro, as well as tumor growth in vivo were examined in human liver cancer cell lines...
August 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28713276/structure-activity-relationships-of-pentacyclic-triterpenoids-as-potent-and-selective-inhibitors-against-human-carboxylesterase-1
#3
Li-Wei Zou, Tong-Yi Dou, Ping Wang, Wei Lei, Zi-Miao Weng, Jie Hou, Dan-Dan Wang, Yi-Ming Fan, Wei-Dong Zhang, Guang-Bo Ge, Ling Yang
Human carboxylesterase 1 (hCE1), one of the most important serine hydrolases distributed in liver and adipocytes, plays key roles in endobiotic homeostasis and xenobiotic metabolism. This study aimed to find potent and selective inhibitors against hCE1 from phytochemicals and their derivatives. To this end, a series of natural triterpenoids were collected and their inhibitory effects against human carboxylesterases (hCEs) were assayed using D-Luciferin methyl ester (DME) and 6,8-dichloro-9,9-dimethyl-7-oxo-7,9-dihydroacridin-2-yl benzoate (DDAB) as specific optical substrate for hCE1, and hCE2, respectively...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28707589/advances-in-the-anticancer-value-of-the-ursolic-acid-through-nanodelivery
#4
Azadeh Manayi, Marjan Nikan, Navid Nobakht Haghighid, Mohammad Abdollahi
Ursolic acid, a natural pentacyclic triterpenoid is commonly found in plants and foods with promising biological and pharmacological activities. The compound has been under the attention of researchers due to its considerable anticancer effects through suppression of differentiation, angiogenesis, invasion, and metastasis of tumor cells via different pathways with low toxicity. Bioavailability of ursolic acid is poor due to poor solubility of the compound in water. Low bioavailability and short plasma half-life of ursolic acid along with non-specific distribution in the body are considered as impediments in the therapeutic development of the compound...
July 13, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28678485/an-ursolic-acid-derived-small-molecule-triggers-cancer-cell-death-through-hyperstimulation-of-macropinocytosis
#5
Lin Sun, Bin Li, Xiaohui Su, Ge Chen, Yaqin Li, Linqian Yu, Li Li, Wanguo Wei
Macropinocytosis is a transient endocytosis that internalizes extracellular fluid and particles into vacuoles. Recent studies suggest that hyperstimulation of macropinocytosis can induce a novel nonapoptotic cell death, methuosis. In this report, we describe the identification of an ursolic acid derived small molecule (compound 17), which induces cancer cell death through hyperstimulation of macropinocytosis. 17 causes the accumulation of vacuoles derived from macropinosomes based on transmission electron microscopy, time-lapse microscopy, and labeling with extracellular fluid phase tracers...
July 19, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28675237/ursolic-acid-induces-mitochondrial-biogenesis-through-the-activation-of-ampk-and-pgc-1-in-c2c12-myotubes-a-possible-mechanism-underlying-its-beneficial-effect-on-exercise-endurance
#6
Jihang Chen, Hoi Shan Wong, Pou Kuan Leong, Hoi Yan Leung, Wing Man Chan, Kam Ming Ko
Mitochondrial biogenesis, which involves an increase in mitochondrial number and the overall capacity of oxidative phosphorylation, is a critical determinant of skeletal muscle function. Recent findings have shown that some natural products can enhance mitochondrial adaptation to aerobic exercise, which in turn improves exercise performance, presumably by delaying muscle fatigue. Ursolic acid (UA), a natural triterpene, is commonly found in various vegetables and fruits. In the current study, UA was shown to increase mitochondrial mass and ATP generation capacity, with a concomitant production of a low level of mitochondrial reactive oxygen species (ROS) in C2C12 myotubes...
July 19, 2017: Food & Function
https://www.readbyqxmd.com/read/28673026/3%C3%AE-hydroxy-urs-12-en-28-oic-acid-modulates-dietary-restriction-mediated-longevity-and-ameliorates-toxic-protein-aggregation-in-c-elegans
#7
Hema Negi, Shilpi Khare Saikia, Rakesh Pandey
Species from lower invertebrates to a spectrum of mammals show anti-aging health benefits of phytochemical(s). Here, we explored the pro-longevity effects of a natural triterpenoid, ursolic acid (3β-hydroxy-urs-12-en-28-oic acid; UA) in Caenorhabditis elegans with maximal lifespan being evident at 25µM UA. Similar to eat-2 mutants, UA uptake by worm results in reduced fat storage and attenuation of reactive oxygen species (ROS), independent of superoxide dismutase(s) activation. The genetic requirements for UA mediated longevity are quite similar to dietary restriction (DR) achieved through SKN-1/ NRF-2 exhibiting up regulation of downstream target genes gcs-1 and daf-9...
June 30, 2017: Journals of Gerontology. Series A, Biological Sciences and Medical Sciences
https://www.readbyqxmd.com/read/28672060/phytochemical-and-biological-activities-of-pseudocalymma-elegans-a-false-garlic
#8
Sana Wahid, Muhammad Ali Versiani, Sajid Jahangir, Khurshid Jawaid, Maryam Shafique, Huma Khan, Shaheen Faizi
Evaluation of phytochemical constituents and antioxidant and antimicrobial activities of hexane (PELH), dichloromethane (PELDCM), ethyl acetate (PELEA) and methanolic (PELM) extracts of young leaves of P. elegans have been carried out. Moreover, extracts have also been explored for the presence of sulphur containing compounds, 1, 2-dithiolane (33), diallyl disulphide (35), 3-Vinyl-1,2-dithiacyclohex-5-ene (37), diallyl trisulphide (38) responsible for the garlic like smell of P. elegans. All the extracts were found to be antioxidant and showed potent inhibition with IC50 values 0...
July 3, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28670276/potential-protective-effects-of-ursolic-acid-against-gamma-irradiation-induced-damage-are-mediated-through-the-modulation-of-diverse-inflammatory-mediators
#9
Hong Wang, Meng-Kwoon Sim, Weng Keong Loke, Arunachalam Chinnathambi, Sulaiman Ali Alharbi, Feng Ru Tang, Gautam Sethi
This study was aimed to evaluate the possible protective effects of ursolic acid (UA) against gamma radiation induced damage both in vitro as well as in vivo. It was observed that the exposure to gamma radiation dose- and time-dependently caused a significant decrease in the cell viability, while the treatment of UA attenuated this cytotoxicity. The production of free radicals including reactive oxygen species (ROS) and NO increased significantly post-irradiation and further induced lipid peroxidation and oxidative DNA damage in cells...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28663034/interference-of-ursolic-acid-treatment-with-glioma-growth-an-in-vitro-and-in-vivostudy
#10
Letícia Scussel Bergamin, Fabrício Figueiró, Fabrícia Dietrich, Fabiana de Mattos Manica, Eduardo C Filippi-Chiela, Franciane Brackman Mendes, Elisa Helena Farias Jandrey, Daniela Vasconcelos Lopes, Francine H Oliveira, Isis C Nascimento, Henning Ulrich, Ana Maria Oliveira Battastini
Glioblastoma multiforme is the most devastating tumor in the brain. Ursolic acid (UA) is found in a variety of plants, and exhibits several pharmacological activities. In this study, we investigated the effects of UA in vitro, clarifying the mechanisms that mediate its toxicity and the long-lasting actions of UA in C6 glioma cells. We also evaluated the antitumor activity of UA in an in vivo orthotopic glioma model. Cell numbers were assessed using the Trypan blue exclusion test, and the cell cycle was characterized by flow cytometry using propidium iodide staining...
June 26, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28662529/bioactivity-guided-investigation-of-the-anti-inflammatory-activity-of-hippophae-rhamnoides-fruits
#11
Dóra Rédei, Norbert Kúsz, Nikoletta Jedlinszki, Gábor Blazsó, István Zupkó, Judit Hohmann
According to modern ethnobotanical records, the fruit of Hippophae rhamnoides is effective in the treatment of different allergic symptoms. In order to obtain pharmacological evidence for this observation, the fruit was investigated for anti-inflammatory activity using in vivo animal models. Aqueous and 70% MeOH extracts were tested in 48/80-induced rat paw edema assay after oral administration, and it was found that the 70% MeOH extract (500 mg/kg) reduced significantly edema volume (0.660 ± 0.082 mL vs...
June 29, 2017: Planta Medica
https://www.readbyqxmd.com/read/28660943/a-smart-ph-responsive-nano-carrier-as-a-drug-delivery-system-for-the-targeted-delivery-of-ursolic-acid-suppresses-cancer-growth-and-metastasis-by-modulating-p53-mmp-9-pten-cd44-mediated-multiple-signaling-pathways
#12
Kai Jiang, Ting Chi, Tao Li, Guirong Zheng, Lulu Fan, Yajun Liu, Xiufen Chen, Sijia Chen, Lee Jia, Jingwei Shao
Ursolic acid (UA) has been recently used as a promising anti-tumor and cancer metastatic chemo-preventive agent due to its low toxicity and liver-protecting property. However, the low bioavailability and nonspecific tumor targeting restrict its further clinical application. To address the problem, a silica-based mesoporous nanosphere (MSN) controlled-release drug delivery system (denoted UA@M-CS-FA) was designed and successfully synthesized, and was functionalized with folic acid (FA) and pH-sensitive chitosan (CS) for the targeted delivery of UA to folate receptor (FR) positive tumor cells...
July 13, 2017: Nanoscale
https://www.readbyqxmd.com/read/28657349/a-new-triterpene-ester-and-other-chemical-constituents-from-the-aerial-parts-of-anodendron-paniculatum-and-their-cytotoxic-activity
#13
Ho Viet Duc, Hoang Thi Nhu Hang, Vo Quoc Hung, Nguyen Minh Hien, Ain Raal, Nguyen Thi Hoai
The aim of the research was to study the active constituents of Anodendron paniculatum Roxb. (Apocynaceae). A new triterpene ester, named anopaniester (1), and cycloartenol (2), ursolic acid (3), esculenic acid (4), bis-(2-ethylhexyl) phthalate (5), desmosterol (6), stigmasterol (7), vaniline (8), and (E)-phytol (9), were isolated from the aerial parts of A. paniculatum. Compounds 3 and 6 showed the significant inhibitory effect (IC50 values ranging from 30.89 ± 3.60 to 44.37 ± 5.40 μg/ml) against tested human cancer cell lines LU-1 and MKN-7...
June 28, 2017: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/28642128/immunomodulation-of-parkinson-s-disease-using-mucuna-pruriens-mp
#14
REVIEW
Sachchida Nand Rai, Hareram Birla, Walia Zahra, Saumitra Sen Singh, Surya Pratap Singh
Immune control is associated with nigrostriatal neuroprotection for Parkinson's disease (PD); though its direct cause and effect relationships have not yet been realized and modulating the immune system for therapeutic gain has been openly discussed. While the pathobiology of PD remains in study, neuroinflammation is thought to speed nigrostriatal degeneration. The neuroinflammatory cascade associated with PD begins with aggregation of misfolded or post-translationally modified α-synuclein (α-syn). Such aggregation results in neuronal cell death and the presence of chronically activated glia (microglia and astroglia), leading to the production of proinflammatory cytokines like tumor necrosis factor alpha (TNF-α), interleukin-1 beta (IL-1β), IL-6, and enzymes such as nicotinamide adenine dinucleotide phosphate (NADPH) oxidase and cyclooxygenase-2 (COX-2)...
June 19, 2017: Journal of Chemical Neuroanatomy
https://www.readbyqxmd.com/read/28640753/mechanism-of-antihypertensive-effect-of-mucuna-pruriens-l-seed-extract-and-its-isolated-compounds
#15
Mohammad Yaseen Khan, Vimal Kumar
Background In the search of safe and effective lead molecules from natural sources, Mucuna pruriens (MP) L. (Fabaceae) seeds were utilized for exploring the antihypertensive potential. Traditionally, it is used as diuretic and hypotensive. Methods Bioassay-guided fractions were utilized for the isolation of active compounds by column chromatography. IC50 value, enzyme kinetics and inhibition mechanism were determined. In vivo time and dose-dependent hypotensive study followed by changes in mean arterial pressure (MAP) induced by angiotensin I (3 nmol/kg), angiotensin II (3 nmol/kg), and bradykinin (10 nmol/kg) in anesthetized rats was done...
June 21, 2017: Journal of Complementary & Integrative Medicine
https://www.readbyqxmd.com/read/28640347/psychotria-viridis-chemical-constituents-from-leaves-and-biological-properties
#16
Débora B S Soares, Lucienir P Duarte, André D Cavalcanti, Fernando C Silva, Ariadne D Braga, Miriam T P Lopes, Jacqueline A Takahashi, Sidney A Vieira-Filho
The phytochemical study of hexane, chloroform and methanol extracts from leaves of Psychotria viridis resulted in the identification of: the pentacyclic triterpenes, ursolic and oleanolic acid; the steroids, 24-methylene-cycloartanol, stigmasterol and β-sitosterol; the glycosylated steroids 3-O-β-D-glucosyl-β-sitosterol and 3-O-β-D-glucosyl-stigmasterol; a polyunsaturated triterpene, squalene; the esters of glycerol, 1-palmitoylglycerol and triacylglycerol; a mixture of long chain hydrocarbons; the aldehyde nonacosanal; the long chain fat acids hentriacontanoic, hexadecanoic and heptadenoic acid; the ester methyl heptadecanoate; the 4-methyl-epi-quinate and two indole alkaloids, N,N-dimethyltryptamine (DMT) and N-methyltryptamine...
April 2017: Anais da Academia Brasileira de Ciências
https://www.readbyqxmd.com/read/28637397/ursolic-acid-derivatives-for-pharmaceutical-use-a-patent-review-2012-2016
#17
Hidayat Hussain, Ivan R Green, Iftikhar Ali, Ikhlas A Khan, Zulfiqar Ali, Abdullah M Al-Sadi, Ishtiaq Ahmed
Ursolic acid (UA), belongs to a group of pentacyclic triterpenoids and is known to possess some very interesting biological properties. Protocols have been developed in order to synthesize bioactive UA analogs which have resulted in numerous ursolic acid analogs being synthesized during the period 2012-2016. Ursolic acid and its analogues can be employed to treat various cancers, inflammatory diseases, diabetes, Parkinson's disease, Alzheimer's disease, hepatitis B, hepatitis C and AIDS to mention but a few...
June 21, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28606081/isolation-of-anti-mycobacterial-compounds-from-curtisia-dentata-burm-f-c-a-sm-curtisiaceae
#18
Victor O Fadipe, Nkoana I Mongalo, Andy R Opoku, Preachers M Dikhoba, Tshepiso J Makhafola
BACKGROUND: Tuberculosis is counted amongst the most infectious and lethal illnesses worldwide and remains one of the major threats to human health. The aim of the current study was to isolate and characterize anti-mycobacterial compounds present in Curtisia dentata (Burm.f.) C.A.Sm , a medicinal plant reportedly used in the treatment of tuberculosis, stomach ailments and sexually transmitted infections. METHODS: The bioassay guided principle was followed to isolate the anti-mycobacterial compounds...
June 12, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28598231/effect-of-ursolic-acid-on-metabolic-syndrome-insulin-sensitivity-and-inflammation
#19
Alejandra M Ramírez-Rodríguez, Manuel González-Ortiz, Esperanza Martínez-Abundis, Natalhie Acuña Ortega
To evaluate the effect of ursolic acid on metabolic syndrome, insulin sensitivity, and inflammation. A randomized, double-blind, placebo-controlled clinical trial was carried out in 24 patients (30-60 years) with a diagnosis of metabolic syndrome without treatment. They were randomly assigned to two groups of 12 patients, each to receive orally 150 mg of ursolic acid or homologated placebo once a day for 12 weeks. Before and after the intervention, the components of metabolic syndrome, insulin sensitivity (Matsuda index), and inflammation profile (interleukin-6 and C-reactive protein) were evaluated...
June 9, 2017: Journal of Medicinal Food
https://www.readbyqxmd.com/read/28597426/anti-hepatitis-antioxidant-activities-and-bioactive-compounds-of-dracocephalum-heterophyllum-extracts
#20
Qiang-Qiang Shi, Jun Dang, Huai-Xiu Wen, Xiang Yuan, Yan-Duo Tao, Qi-Lan Wang
BACKGROUND: Dracocephalum heterophyllum was a traditional Tibetan medicine possesses various pharmacological effects involved in anti-inflammatory, antibacterial activities. However, its anti-hepatitis, antioxidant activity and bioactive compounds have not been reported, the objective of this research work was to investigate the pharmacological activity and bioactive compounds of D. heterophyllum extracts. RESULTS: In the present study, the anti-hepatics and antioxidant activities of four D...
December 2016: Botanical Studies (Taipei, Taiwan)
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