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Ursolic acid AND diabetes

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https://www.readbyqxmd.com/read/28637397/ursolic-acid-derivatives-for-pharmaceutical-use-a-patent-review-2012-2016
#1
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/28474555/isolated-compounds-from-natural-products-with-potential-antidiabetic-activity-a-systematic-review
#2
Antonio C M Munhoz, Tânia S Fröde
BACKGROUND: Worldwide, Type 2 diabetes has become a growing health problem. While many research articles in the field of ethnopharmacology have focused on the antidiabetic properties of medicinal plant species, insufficient evidence remains regarding their therapeutic use. Studies using both in vitro and in vivo models are necessary to evaluate various medicinal plants species, used in folk medicine, by using scientific criteria. METHODS: This review focuses on isolated compounds from medicinal plant species that have reported antidiabetic activity in diabetes models...
May 5, 2017: Current Diabetes Reviews
https://www.readbyqxmd.com/read/28465178/oral-delivery-of-ursolic-acid-loaded-nanostructured-lipid-carrier-coated-with-chitosan-oligosaccharides-development-characterization-in-vitro-and-in-vivo-assessment-for-the-therapy-of-leishmaniasis
#3
Suman Das, Santanu Ghosh, Asit Kumar De, Tanmoy Bera
Visceral leishmaniasis (VL) is a life-threatening disease caused by Leishmania donovani due to uncontrolled parasitisation of liver, spleen, and bone marrow. Ursolic acid (UA), a promising anti-inflammatory, anti-bacterial and anti-diabetic drug used successfully for treatment of ailments. Development of new delivery system is extremely urgent for UA with better efficacy and fewer side effects. The aim of present research work was to formulate and evaluate the potential anti-leishmanial activity of UA loaded N-octyl-chitosan surface decorated nanostructured lipid carrier system (UA-NLC) for delivery to the macrophages for VL...
September 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28454670/structure-related-protein-tyrosine-phosphatase-1b-inhibition-by-naringenin-derivatives
#4
Hyun Ah Jung, Pradeep Paudel, Su Hui Seong, Byung-Sun Min, Jae Sue Choi
Naturally occurring flavonoids co-exist as glycoside conjugates, which dominate aglycones in their content. To unveil the structure-activity relationship of a naturally occurring flavonoid, we investigated the effects of the glycosylation of naringenin on the inhibition of enzyme systems related to diabetes (protein tyrosine phosphatase 1B (PTP1B) and α-glycosidase) and on glucose uptake in the insulin-resistant state. Among the tested naringenin derivatives, prunin, a single-glucose-containing flavanone glycoside, potently inhibited PTP1B with an IC50 value of 17...
April 18, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28423086/evaluation-of-cytogenotoxicity-antioxidant-and-hypoglycemiant-activities-of-isolate-compounds-from-mansoa-hirsuta-d-c-bignoniaceae
#5
Joquebede R Pereira, Raphael F Queiroz, Erlânia A DE Siqueira, Ana Christina Brasileiro-Vidal, Antônio E G Sant'ana, Daniel M Silva, Paulo R A DE Mello Affonso
Mansoa hirsuta (Bignoniaceae) is a native plant from caatinga in Brazilian semiarid. This plant has been locally used as antimicrobial and hypoglycemiant agents, but their action mechanisms and toxicity remain largely unknown. Therefore, we evaluated the composition and antioxidant, cytoprotective and hypoglycemiant effects of raw extract, fractions and compounds from leaves of M. hirsuta. The cytogenotoxic effects of ursolic and oleanolic acids, the main phytotherapic components of this plant, were assessed...
January 2017: Anais da Academia Brasileira de Ciências
https://www.readbyqxmd.com/read/28372473/selection-of-chemical-markers-for-the-quality-control-of-medicinal-plants-of-the-genus-cecropia
#6
Andrés Rivera-Mondragón, Orlando O Ortíz, Sebastiaan Bijttebier, Arnold Vlietinck, Sandra Apers, Luc Pieters, Catherina Caballero-George
CONTEXT: Several Cecropia (Cecropiaceae) species are traditionally used in Latin America for the treatment of a variety of diseases including diabetes, arterial hypertension, asthma, bronchitis, anxiety, and inflammation. At present, a number of commercial products based on these plants have been introduced into the market with very little information on methods for guaranteeing their quality and safety. OBJECTIVE: This work proposes potential chemical markers for the quality control of the raw materials of Cecropia obtusifolia Bertol...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28358057/synthesis-and-biological-evaluation-of-novel-ursolic-acid-analogues-as-potential-%C3%AE-glucosidase-inhibitors
#7
Pan-Pan Wu, Bing-Jie Zhang, Xi-Ping Cui, Yang Yang, Zheng-Yun Jiang, Zhi-Hong Zhou, Ying-Ying Zhong, Yu-Ying Mai, Zhong Ouyang, Hui-Sheng Chen, Jie Zheng, Su-Qing Zhao, Kun Zhang
Ursolic acid (UA) is a major pentacyclic triterpenoid in plants, vegetables and fruits, which has been reported to have a potential anti-diabetic activity. Despite various semi-synthetic ursolic acid derivatives already described, new derivatives still need to be designed and synthesized to further improve the anti-diabetic activity. In the present study, two series of novel UA derivatives, were synthesized and their structures were confirmed. The enzyme inhibition activities of semi-synthesized analogues against α-glucosidase were screened in vitro...
March 30, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28318895/competitive-protein-tyrosine-phosphatase-1b-ptp1b-inhibitors-prenylated-caged-xanthones-from-garcinia-hanburyi-and-their-inhibitory-mechanism
#8
Xue Fei Tan, Zia Uddin, Chanin Park, Yeong Hun Song, Minky Son, Keun Woo Lee, Ki Hun Park
Protein tyrosine phosphatase 1B (PTP1B) plays important role in diabetes, obesity and cancer. The methanol extract of the gum resin of Garcinia hanburyi (G. hanburyi) showed potent PTP1B inhibition at 10µg/ml. The active compounds were identified as prenylated caged xanthones (1-9) which inhibited PTP1B in dose-dependent manner. Carboxybutenyl group within caged motif (A ring) was found to play a critical role in enzyme inhibition such as 1-6 (IC50s=0.47-4.69µM), whereas compounds having hydroxymethylbutenyl 7 (IC50=70...
March 6, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27927056/bioassay-guided-fractionation-and-identification-of-%C3%AE-amylase-inhibitors-from-syzygium-cumini-leaves
#9
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
https://www.readbyqxmd.com/read/27704066/the-potential-beneficial-effects-of-phenolic-compounds-isolated-from-a-pilosa-ledeb-on-insulin-resistant-hepatic-hepg2-cells
#10
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
https://www.readbyqxmd.com/read/27377340/evidence-of-anti-inflammatory-and-antinociceptive-activities-of-plinia-edulis-leaf-infusion
#11
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
https://www.readbyqxmd.com/read/27114690/the-potent-inhibitors-of-protein-tyrosine-phosphatase-1b-from-the-fruits-of-melaleuca-leucadendron
#12
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
https://www.readbyqxmd.com/read/27060210/ptp1b-%C3%AE-glucosidase-and-dpp-iv-inhibitory-effects-for-chromene-derivatives-from-the-leaves-of-smilax-china-l
#13
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
https://www.readbyqxmd.com/read/27051429/chemical-constituents-of-swertia-longifolia-boiss-with-%C3%AE-amylase-inhibitory-activity
#14
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
https://www.readbyqxmd.com/read/27012451/oleanolic-ursolic-and-betulinic-acids-as-food-supplements-or-pharmaceutical-agents-for-type-2-diabetes-promise-or-illusion
#15
REVIEW
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
https://www.readbyqxmd.com/read/26711605/-inhibitory-effects-of-ursolic-acid-on-diabetic-retinopathy-in-mice
#16
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]
https://www.readbyqxmd.com/read/26619955/the-hypoglycemic-and-synergistic-effect-of-loganin-morroniside-and-ursolic-acid-isolated-from-the-fruits-of-cornus-officinalis
#17
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
https://www.readbyqxmd.com/read/26406581/synthesis-and-evaluation-of-novel-triterpene-analogues-of-ursolic-acid-as-potential-antidiabetic-agent
#18
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
https://www.readbyqxmd.com/read/26331671/apple-pomace-extract-improves-endurance-in-exercise-performance-by-increasing-strength-and-weight-of-skeletal-muscle
#19
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
https://www.readbyqxmd.com/read/26260291/inhibitory-effects-and-actions-of-pentacyclic-triterpenes-upon-glycation
#20
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
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