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Ursolic acid AND diabetes

Jeyakumaran Poongunran, Handunge Kumudu Irani Perera, Lalith Jayasinghe, Irushika Thushari Fernando, Ramaiah Sivakanesan, Hiroshi Araya, Yoshinori Fujimoto
CONTEXT: Pancreatic α-amylase and α-glucosidase inhibitors serve as important strategies in the management of blood glucose. Even though Syzygium cumini (L.) Skeels (Myrtaceae) (SC) is used extensively to treat diabetes; scientific evidence on antidiabetic effects of SC leaves is scarce. OBJECTIVE: SC leaf extract was investigated for α-amylase inhibitory effect and continued with isolation and identification of α-amylase inhibitors. MATERIALS AND METHODS: Bioassay-guided fractionation was conducted using in vitro α-amylase inhibitory assay (with 20-1000 μg/mL test material) to isolate the inhibitory compounds from ethyl acetate extract of SC leaves...
December 2017: Pharmaceutical Biology
Hui Teng, Lei Chen, Hongbo Song
Agrimonia pilosa Ledeb (AP) has already been applied in practice for the treatment of different disorders and is available to access without the provision of a medical prescription. The present study aims at investigating the effect of bioactive compounds isolated from AP on the improvement of insulin resistance, figuring out the mechanism in insulin-responsive cell lines. Five compounds were isolated from AP using column chromatography, including agrimonolide (K1), desmethylagrimonolide (K2), tormentic acid (K3), ursolic acid (K4), and quercetin (K5)...
October 12, 2016: Food & Function
Lara F Azevedo, Simone Maria da Silva, Lucas B Navarro, Lydia F Yamaguchi, Carlos Giovani O Nascimento, Roseli Soncini, Tati Ishikawa
ETHNOPHARMACOLOGICAL RELEVANCE: Plinia edulis (Vell.) Sobral (Myrtaceae) is native and endemic to the Brazilian Atlantic Rainforest. Popularly known as "cambucá", it has been used in folk medicine for the treatment of stomach disorders, diabetes, bronchitis, inflammation and as tonic. Although there are numerous records concerning its popular use as analgesic and anti-inflammatory, scientific information regarding these pharmacological activities is limited. Therefore, the aim of this study was to characterize the anti-inflammatory and antinociceptive activity of P...
November 4, 2016: Journal of Ethnopharmacology
Azis Saifudin, Subehan Ab Lallo, Yasuhiro Tezuka
BACKGROUND: Melaleuca leucadendron (Myrtaceae) is a kind of fruit used as Indonesian medicinal component and recorded in Jamu (tonic made of medical herbs) prescription records for the diabetes treatment. Its methanol extract exhibited a strong inhibitory activity with the half maximal inhibitory concentration (IC50) value of 2.05 μg/mL, while it is the same value with positive control RK-682. OBJECTIVE: To isolate the chemical constituents of M. leucadendron and to evaluate their activity against protein tyrosine phosphatase 1B (PTP1B)...
March 2016: Pharmacognosy Research
Bing Tian Zhao, Duc Dat Le, Phi Hung Nguyen, Md Yousof Ali, Jae-Sue Choi, Byung Sun Min, Heung Mook Shin, Hae Ik Rhee, Mi Hee Woo
Two new flavonoids, bismilachinone (11) and smilachinin (14), were isolated from the leaves of Smilax china L. together with 14 known compounds. Their structures were elucidated using spectroscopic methods. The PTP1B, α-glucosidase, and DPP-IV inhibitory activities of compounds 1-16 were evaluated at the molecular level. Among them, compounds 4, 7, and 10 showed moderate DPP-IV inhibitory activities with IC50 values of 20.81, 33.12, and 32.93 μM, respectively. Compounds 3, 4, 6, 11, 12, and 16 showed strong PTP1B inhibitory activities, with respective IC50 values of 7...
June 25, 2016: Chemico-biological Interactions
Soodabeh Saeidnia, Leila Ara, Homa Hajimehdipoor, Roger W Read, Sattar Arshadi, Marjan Nikan
α-Amylase inhibitors play a critical role in the control of diabetes and many of medicinal plants have been found to act as α-amylase inhibitors. Swertia genus, belonging to the family Gentianaceae, comprises different species most of which have been used in traditional medicine of several cultures as antidiabetic, anti-pyretic, analgesic, liver and gastrointestinal tonic. Swertia longifolia Boiss. is the only species of Swertia growing in Iran. In the present investigation, phytochemical study of S. longifolia was performed and α-amylase inhibitory effects of the plant fractions and purified compounds were determined...
January 2016: Research in Pharmaceutical Sciences
Filomena S G Silva, Paulo J Oliveira, Maria F Duarte
Oleanolic (OA), ursolic (UA), and betulinic (BA) acids are three triterpenic acids (TAs) with potential effects for treatment of type 2 diabetes (T2DM). Mechanistic studies showed that these TAs act as hypoglycemic and antiobesity agents mainly through (i) reducing the absorption of glucose; (ii) decreasing endogenous glucose production; (iii) increasing insulin sensitivity; (iv) improving lipid homeostasis; and (v) promoting body weight regulation. Besides these promising beneficial effects, it is believed that OA, UA, and BA protect against diabetes-related comorbidities due to their antiatherogenic, anti-inflammatory, and antioxidant properties...
April 20, 2016: Journal of Agricultural and Food Chemistry
Yan Sun, Xiaonan Sun, Fang Wang, Shanshan Liu
OBJECTIVE: To explore the protective effect and its mechanisms of intravitreal injection of ursolic acid (UA) on retinal injury in diabetic retinopathy (DR) mice. METHODS: DR model was set up by using alloxan. 60 C57BL/6 male mice (clean animal, aged 12 weeks) were randomly and evenly divided into 6 groups: blank control group, DR model group, positive control group (triamcinolone acetonide), UA intervention groups (low, moderate and high dose). Mice were killed one week after drug intervention and the eyeballs were removed to prepare paraffin section...
August 25, 2015: Zhonghua Yi Xue za Zhi [Chinese medical journal]
Kai He, Shanghua Song, Zongyao Zou, Min Feng, Dezhen Wang, Yanzhi Wang, Xuegang Li, Xiaoli Ye
Hypoglycemic activity-guided separation of ethanol extracts from the fruits of Cornus officinalis Sieb. et Zucc (CO) led to the isolation of loganin, morroniside, and ursolic acid. The antidiabetic capacity of CO extracts and related compounds was further investigated in diabetes mellitus mice. The results suggested that both CO extracts and pure compounds could ameliorate diabetes-associated damages and complications. Oral administration of loganin and morroniside decreased fasting blood glucose levels in diabetes mellitus mice...
February 2016: Phytotherapy Research: PTR
Panpan Wu, Jie Zheng, Tianming Huang, Dianmeng Li, Qingqing Hu, Anming Cheng, Zhengyun Jiang, Luoying Jiao, Suqing Zhao, Kun Zhang
Ursolic acid (UA) is a naturally bioactive compound that possesses potential anti-diabetic activity. The relatively safe and effective molecule intrigued us to further explore and to improve its anti-diabetic activity. In the present study, a series of novel UA analogues was synthesized and their structures were characterized. Their bioactivities against the α-glucosidase from baker's yeast were determined in vitro. The results suggested that most of the analogues exhibited significant inhibitory activity, especially analogues 8b and 9b with the IC50 values of 1...
2015: PloS One
Ji-Woong Jeong, Jae-Jung Shim, Il-Dong Choi, Sung-Hwan Kim, Jehyeon Ra, Hyung Keun Ku, Dong Eun Lee, Tae-Youl Kim, Woonhee Jeung, Jung-Hee Lee, Ki Won Lee, Chul-Sung Huh, Jae-Hun Sim, Young-Tae Ahn
Ursolic acid is a lipophilic pentacyclic triterpenoid found in many fruits and herbs and is used in several herbal folk medicines for diabetes. In this study, we evaluated the effects of apple pomace extract (APE; ursolic acid content, 183 mg/g) on skeletal muscle atrophy. To examine APE therapeutic potential in muscle atrophy, we investigated APE effects on the expression of biomarkers associated with muscle atrophy and hypertrophy. We found that APE inhibited atrophy, while inducing hypertrophy in C2C12 myotubes by decreasing the expression of atrophy-related genes and increasing the expression of hypertrophy-associated genes...
December 2015: Journal of Medicinal Food
Mei-Chin Yin
Pentacyclic triterpenic compounds including asiatic, betulinic, maslinic, oleanolic and ursolic acid occur naturally in many herbs and plant foods. It is well known that these triterpenoids possess anti-oxidative and anti-inflammatory activities. Furthermore, recent in vitro and in vivo researches indicated that these compounds could inhibit the production of advanced glycation end-products (AGEs). The impact of these triterpenes upon the activity and protein expression of enzymes involved in polyol pathway including aldose reductase and sorbitol dehydrogenase has been examined, and positive results are reported...
September 2015: BioMedicine
Estela Giménez, M Emília Juan, Sara Calvo-Melià, José Barbosa, Victoria Sanz-Nebot, Joana M Planas
Pentacyclic triterpenes are gaining interest due to their beneficial health effects, as anti-inflammatory, anti-diabetic and anti-tumoral, among others. In this study, an analytical LC-MS method was developed for the simultaneous determination of maslinic, oleanolic and ursolic acids along with erythrodiol and uvaol, which are the main triterpenic compounds present in the fruits and leaves of Olea europaea L. A Zorbax Eclipse PAH column at 30°C with mobile phase of water (17%) and methanol (83%) at 0.8mL/min conformed the optimal chromatographic conditions that allowed the separation of the compounds of interest, two pairs of which are isomers differing only in the position of one methyl group (oleanolic-ursolic and erythrodiol-uvaol)...
September 4, 2015: Journal of Chromatography. A
Juan Zhang, Jun Lv, Xiaonan Wang, Defeng Li, Zhaoxia Wang, Genxi Li
Inhibitors of protein tyrosine phosphatase 1B (PTP1B) are promising agents for the treatment of type 2 diabetes and obesity, so a colorimetric method has been developed in this work for PTP1B assay and screening of its inhibitors. The method is based on the chelation effect of zirconium (Zr(4+)) ions on the phosphate group, which may induce aggregation of 4-aminophenylphosphate-functionalized gold nanoparticles (APP/AuNPs) and the corresponding color change of the testing solution. Owing to the dephosphorylation of PTP1B, the aggregation of AuNPs will be influenced by PTP1B since there is no coordination reactivity between Zr(4+) ions and 4-aminophenol, the hydrolyzed product of APP catalyzed by the enzyme...
August 21, 2015: Analyst
Muhammad Raza Shah, Ishtiaq, Syed Muhammad Hizbullah, Solomon Habtemariam, Armando Zarrelli, Akhtar Muhammad, Simona Collina, Inamulllah Khan
Artemisia roxburghiana is used in traditional medicine for treating various diseases including diabetes. The present study was designed to evaluate the antidiabetic potential of active constituents by using protein tyrosine phosphatase 1B (PTP1B) as a validated target for management of diabetes. Various compounds were isolated as active principles from the crude methanolic extract of aerial parts of A. roxburghiana. All compounds were screened for PTP1B inhibitory activity. Molecular docking simulations were performed to investigate the mechanism behind PTP1B inhibition of the isolated compound and positive control, ursolic acid...
August 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Su-Guo Yu, Cheng-Jie Zhang, Xiu-E Xu, Ji-Hua Sun, Li Zhang, Peng-Fei Yu
OBJECTIVE: This study was performed to investigate bone deteriorations of diabetic mice in response to the treatment of ursolic acid derivative (UAD). METHODS: The biomarkers in serum and urine were measured, tibias were taken for the measurement on gene and protein expression and histomorphology analysis, and femurs were taken for the measurement on bone Ca and three-dimensional architecture of trabecular bone. RESULTS: UAD showed a greater increase in bone Ca, BMD and significantly increased FGF-23 and OCN, reduced PTH and CTX in diabetic mice...
2015: International Journal of Clinical and Experimental Pathology
Jae Sue Choi, Md Yousof Ali, Hyun Ah Jung, Sang Ho Oh, Ran Joo Choi, Eon Ji Kim
ETHNOPHARMACOLOGIC RELEVANCE: Rhizoma Coptidis (the rhizome of Coptis chinensis Franch) has commonly been used for treatment of diabetes mellitus in traditional Chinese medicine due to its blood sugar-lowering properties and therapeutic benefits which highly related to the alkaloids therein. However, a limited number of studies focused on the Coptis alkaloids other than berberine. MATERIALS AND METHODS: In the present study, we investigated the anti-diabetic potential of Coptis alkaloids, including berberine (1), epiberberine (2), magnoflorine (3), and coptisine (4), by evaluating the ability of these compounds to inhibit protein tyrosine phosphatase 1B (PTP1B), and ONOO(-)-mediated protein tyrosine nitration...
August 2, 2015: Journal of Ethnopharmacology
Jian-Shuang Li, Wen-Jun Wang, Yu Sun, Yu-Hao Zhang, Ling Zheng
Ursolic acid (UA) is a natural pentacyclic triterpenoid compound, which is enriched with many herbs and plants, such as apple, cranberry and olive. UA performs multiple biological activities including anti-oxidation, anti-inflammation, anti-cancer and hepatoprotection. However, the exact mechanism underlying the hepatoprotective activity of UA remains unclear. In this study, the effects of UA on the development of nonalcoholic fatty liver disease (NAFLD) were investigated. In vivo, UA treatment (0.14%, w/w) significantly decreased the liver weight, serum levels of ALT/AST and hepatic steatosis in db/db mice (a type 2 diabetic mouse model)...
May 2015: Food & Function
Xinxing Lu, Qiuling Fan, Li Xu, Lin Li, Yuan Yue, Yanyan Xu, Yan Su, Dongcheng Zhang, Lining Wang
OBJECTIVE: To investigate the effect of ursolic acid on autophagy mediated through the miRNA-21-targeted phosphoinositide 3 kinase (PI3K)/protein kinase B (Akt)/mammalian target of rapamycin (mTOR) pathway in rat mesangial cells cultured under high glucose (HG) conditions. METHODS: Rat glomerular mesangial cells were cultured under normal glucose, HG, HG with the PI3K inhibitor LY294002 or HG with ursolic acid conditions. Cell proliferation and hypertrophy were assayed using an MTT assay and the ratio of total protein to cell number, respectively...
2015: PloS One
S S Chowdhury, M N Islam, H A Jung, J S Choi
In an attempt to develop alternative medicine for the treatment of diabetes and related complications, the antidiabetic potential of the fruits of Crataegus pinnatifida was evaluated. The antidiabetic potential of the methanol (MeOH) extract as well as different solvent soluble fractions of the fruits of C. pinnatifida was evaluated via α-glucosidase, protein tyrosine phosphatase 1B (PTP1B), rat lens aldose reductase (RLAR), and advanced glycation end products (AGEs) formation inhibitory assays. The MeOH extract showed potent inhibitory activity against α-glucosidase, PTP1B, and AGEs formation with IC50 values of 122...
January 2014: Research in Pharmaceutical Sciences
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