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Madhuri Vaghela, Niteshkumar Sahu, Prashant Kharkar, Nancy Pandita
Gymnema sylvestre (GS) is a medicinal herb used for diabetes mellitus (DM). Herbs are gaining popularity as medicines in DM for its safety purpose. The aim of the present study was to evaluate in vivo pharmacokinetic (PK) interaction between allopathic drugs tolbutamide (TOLBU), amlodipine (AMLO), and phenacetin (PHENA) at low (L) and high (H) doses with ethanolic extract (EL) from GS. EL was extracted and subjected to TLC, total triterpenoid content (19.76 ± 0.02 W/W) and sterol content (0.1837 ± 0...
October 14, 2017: Chemico-biological Interactions
Andressa Maria Pironi, Patricia Rocha de Araújo, Mariza Aires Fernandes, Hérida Regina Nunes Salgado, Marlus Chorilli
Ursolic acid (UA) is a naturally occurring triterpenoid which is a promising candidate for the development of new therapeutic approaches and for the prevention and treatment of several diseases owing to its pharmacological importance. However, its low solubility in aqueous medium affects its therapeutic application. Several strategies have been used to overcome this obstacle. In this study, the incorporation of UA in to different drug delivery systems was found to be highly efficient. In addition, important investigations were performed about methods for qualitative and quantitative analyses of UA in various raw materials, including plants, biological fluids, and drug delivery systems, were investigated...
October 17, 2017: Critical Reviews in Analytical Chemistry
Qin-Peng Zou, Xiang-Qian Liu, Jian-Jun Huang, Chang-Soo Yook, Wan-Kyunn Whang, Hyeong-Kyu Lee, Ok-Kyoung Kwon
Acanthopanax gracilistylus (AGS) has long been used in traditional Chinese medicine for the treatment of various inflammatory diseases. 3‑O‑β‑D‑glucopyranosyl 3α, 11α‑dihydroxylup‑20(29)‑en‑28‑oic acid, acantrifoside A, acankoreoside D, acankoreoside B and acankoreoside A are major lupane‑type triterpenoid saponins derived from AGS. In the present study, these five saponins were isolated from AGS by chromatography and their anti‑inflammatory activities were investigated in lipopolysaccharide (LPS)‑treated RAW264...
October 11, 2017: Molecular Medicine Reports
Wen-Di Zhou, Xiang Wang, Xing-Zhen Sun, Jian Hu, Rong-Rong Zhang, Ze Hong
Actein is a tetracyclic triterpenoid compound, extracted from the rhizome of Cimicifuga foetida, exhibiting anticancer activities as previously reported. However, the effects of actein on human leukemia have not been explored before. In this study, the role of actein in regulating apoptosis induction in human leukemia cells was investigated. Actein administration significantly enhanced apoptosis, especially in human leukemia cell line of U937 and the primary human leukemia cells. The promotion was accompanied by caspase-9, caspase-3 and poly(ADP-ribose) polymerase (PARP) cleavage, and cytochrome c (Cyto-c) release...
October 10, 2017: International Journal of Oncology
Angela Caunii, Camelia Oprean, Mirabela Cristea, Alexandra Ivan, Corina Danciu, Calin Tatu, Virgil Paunescu, Daniela Marti, George Tzanakakis, Demetrios A Spandidos, Aristides Tsatsakis, Razvan Susan, Codruta Soica, Stefana Avram, Cristina Dehelean
Among the triterpenoids, oleanolic acid (OA) and its isomer, ursolic acid (UA) are promising therapeutic candidates, with potential benefits in the management of melanoma. In this study, we aimed to examine the in vitro and in vivo anti‑invasive and anti‑metastatic activity of OA and UA to determine their possible usefulness as chemopreventive or chemotherapeutic agents in melanoma. For the in vitro experiments, the anti‑proliferative activity of the triterpenic compounds on SK‑MEL‑2 melanoma cells was examined...
October 16, 2017: International Journal of Oncology
Juan J Polari, David Garcí-Aguirre, Lucía Olmo-García, Alegría Carrasco-Pancorbo, Selina C Wang
Crushing is a key step during olive oil extraction. Among commercial crushers, the hammer mill is the most widely used due to its robustness and high throughput. In the present work, the impact of hammer mill rotor speed on extraction yield and overall quality of super-high-density Arbosana olive oils were assessed in an industrial facility. Our results show that increasing the rotor speed from 2400rpm to 3600rpm led to a rise in oil yield of 1.2%, while conserving quality parameters. Sensory analysis showed more pungency with increased rotation speed, while others attributes were unaffected...
March 1, 2018: Food Chemistry
Chengyue Zhang, Chao Wang, Wenji Li, Renyi Wu, Yue Guo, David Cheng, Yuqing Yang, Ioannis P Androulakis, Ah-Ng Kong
The triterpenoid ursolic acid (UA) has been proposed as a potential cancer chemopreventive agent in many preclinical and clinical studies. In the present work, we aimed to characterize the pharmacokinetics (PK) of UA and to quantitatively assess the anti-oxidative and anti-inflammatory effects of UA, which are potentially linked to its chemopreventive efficacy. UA was administered intravenously (i.v., 20 mg/kg) or by oral gavage (100 mg/kg) to male Sprague-Dawley rats, and blood samples were collected at a series of designated time points...
October 16, 2017: Molecular Pharmaceutics
Anil U Tatiya, Ajay K Saluja, Mohan G Kalaskar, Sanjay J Surana, Prakash H Patil
Several species of Bridelia have been used in the condition of pain & arthritis in Indian folk medicine. Present study revealed the preliminary phytochemical investigation and evaluation of analgesic, anti-inflammatory and anti-arthritic activity as well as underlying mechanism of bark of Bridelia retusa Spreng. (Euphorbiaceae). The bark was subjected to extraction using pet.ether, ethyl acetate and acetone. All the extracts were significantly inhibit abdominal writhings response and licking time in late phase of formalin test...
October 2017: Journal of Traditional and Complementary Medicine
Petrina Kapewangolo, Justin J Omolo, Pascaline Fonteh, Martha Kandawa-Schulz, Debra Meyer
Latent HIV reservoirs in infected individuals prevent current treatment from eradicating infection. Treatment strategies against latency involve adjuvants for viral reactivation which exposes viral particles to antiretroviral drugs. In this study, the effect of novel triterpenoids isolated from Ocimum labiatum on HIV-1 expression was measured through HIV-1 p24 antigen capture in the U1 latency model of HIV-1 infection and in peripheral blood mononuclear cells (PBMCs) of infected patients on combination antiretroviral therapy (cART)...
October 13, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Madhuri Vaghela, Krishna Iyer, Nancy Pandita
BACKGROUND AND OBJECTIVES: Gymnema sylvestre R. Br. is a well-known Indian medicinal herb. Gymnemic acids are pentacyclic triterpenes saponins and active phytoconstituents of Gymnema sylvestre. The study aimed at evaluation of the in vitro rat liver cytochrome P450 (CYP) inhibition potential of extracts and total gymnemic acid (TA)-enriched fractions from G. sylvestre. METHODS: Standardization of G. sylvestre [ethanolic (EL), hydroethanolic (HE), total acid of ethanolic (TAE), total acid of hydroethanolic (TAHE) and total acid of aqueous (TAAQ) extract] was done with respect to deacyl gymnemic acid (DAGA), using reverse phase-high performance liquid chromatography (RP-HPLC)...
October 10, 2017: European Journal of Drug Metabolism and Pharmacokinetics
Yoshihiro Watanabe, Yukihiro Asami, Satomi Narusawa, Shohei Hashimoto, Masato Iwatsuki, Kenichi Nonaka, Yasuo Shinohara, Takahiro Shiotsuki, Naoya Ichimaru, Hideto Miyoshi, Satoshi Ōmura, Kazuro Shiomi
A new lanostane-type triterpenoid, ascosteroside D, was isolated from a fungus, Aspergillus sp. FKI-6682. It inhibited insect ADP/ATP carrier protein (AAC)-expressing Saccharomyces cerevisiae in glycerol-containing medium, but did not inhibit Δaac S. cerevisiae in glucose-containing medium. It is hypothesized that ascosteroside D inhibits ATP production in mitochondria.The Journal of Antibiotics advance online publication, 11 October 2017; doi:10.1038/ja.2017.118.
October 11, 2017: Journal of Antibiotics
Chao Wang, Xiao-Kui Huo, Zhi-Lin Luan, Fei Cao, Xiang-Ge Tian, Xin-Yu Zhao, Cheng-Peng Sun, Lei Feng, Jing Ning, Bao-Jing Zhang, Xiao-Chi Ma
Alismanin A (1), a novel aromatic triterpenoid with a C34 skeleton, was isolated from Alisma orientale together with a rearranged nor-triterpenoid (2) and a 13,17-seco triterpenoid (3). Their structures were determined by a combination of HRESIMS, 2D NMR spectra, electronic circular dichroism (ECD), theoretical calculations, and X-ray diffraction analysis. Compounds 1 and 2 displayed significant activation effects on pregnane X receptor (PXR) at 10 nM. A plausible biosynthetic pathway for 1-3 is also discussed...
October 10, 2017: Organic Letters
P Rameshreddy, V V Sathibabu Uddandrao, Parim Brahmanaidu, S Vadivukkarasi, Ramavat Ravindarnaik, Pothani Suresh, K Swapna, A Kalaivani, Parimi Parvathi, P Tamilmani, Ganapathy Saravanan
The present study evaluated the effects of asiatic acid (AA), a pentacyclic triterpenoid from Centella asiatica on lipid metabolism parameters in a rat model of obesity induced using a high fat diet (HFD) for 42 days. AA (20 mg/kg body weight [BW]) was administered orally once daily for 42 days, and an orlistat-treated group of rats (10 mg/kg BW) was included for comparison. Changes in BW, blood glucose levels, insulin resistance and leptin, adiponectin, amylase, and lipase levels in the blood; lipid profiles of plasma; liver antioxidants levels; and acetyl CoA carboxylase(ACC), uncoupling protein-2 (UCP2), and carnitine palmitoyltransferase-1 (CPT1) mRNA expression were observed in the experimental rats...
October 9, 2017: Molecular and Cellular Biochemistry
Feng-Xiang Zhang, Min Li, Zhi-Hong Yao, Chang Li, Li-Rui Qiao, Xiu-Yu Shen, Kate Yu, Yi Dai, Xin-Sheng Yao
A target and non-target strategy based on in-house chemical components library was developed for rapid and comprehensive analysis of complicated components from traditional Chinese medicine (TCM) preparation Shuang-Huang-Lian oral liquid (SHL). The sample was analyzed by ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC/Qtof MS) using generic acquisition parameters. Automated detection and data filtering were performed on the UNIFI(TM) software and the detected peaks were evaluated against an in-house library...
October 9, 2017: Biomedical Chromatography: BMC
Jan Pokorný, Lucie Borková, Milan Urban
Triterpenoids are natural compounds with a large variety of biological activities such as anticancer, antiviral, antibacterial, antifungal, antiparazitic, antiinflammatory and others. Despite their low toxicity and simple availability from the natural resources, their clinical use is still severely limited by their higher IC50 and worse pharmacological properties than in the currently used therapeutics. This fact encouraged a number of researchers to develop new terpenic derivatives more suitable for the potential clinical use...
October 9, 2017: Current Medicinal Chemistry
Barbara Eignerova, Michal Tichy, Jana Krasulova, Miroslav Kvasnica, Lucie Rarova, Romana Christova, Milan Urban, Barbara Bednarczyk-Cwynar, Marian Hajduch, Jan Sarek
To improve the properties of cytotoxic triterpenoid acids 1-5, a large set of hydrophilic esters was synthesized. We choose betulinic acid (1), dihydrobetulinic acid (2), 21-oxoacid 3 along with highly active des-E lupane acids 4 and 5 as a model set of compounds for esterification of which the properties needed to be improved. As ester moieties were used - methoxyethanol and 2-(2-methoxyethoxy)ethanol and glycolic unit (type a-d), pyrrolidinoethanol, piperidinoethanol and morpholinoethanol (type f-h), and monosaccharide groups (type i-l)...
September 21, 2017: European Journal of Medicinal Chemistry
Gervais Mouthé Happi, Ferdinand Mouafo Talontsi, Hartmut Laatsch, Sebastian Zühlke, Bonaventure Tchaleu Ngadjui, Michael Spiteller, Simeon Fogue Kouam
Chemical investigation of the roots of Entandrophragma congoënse (Meliaceae) led to the isolation of two new 3,4-seco-tirucallane triterpenes, namely seco-tiaminic acids B and C (1 and 2) together with nine known compounds: 3,4-secotirucalla-21-formyl-23-oxo-4(28),7,24-trien-3-oic acid (3), methyl angolensate (4), molucensin N (5), molucensin O (6), piscidinol A (7), 7α,20(S)-dihydroxy-4,24(28)-ergostadien-3-one (8), 24-methylene-cholest-5-en-3β,7α-diol (9), entilin A (10), and entilin B (11). Their structures were determined using extensive spectroscopic methods including 1D and 2D NMR, HRMS, and CD analyses; new results were compared to existing data in the literature...
October 5, 2017: Fitoterapia
Yeon Hee Lee, Bokyeong Kim, Soyoung Kim, Min-Sun Kim, Hyunji Kim, Seung-Ryul Hwang, Kyun Kim, Jin Hwan Lee
The objective of this research was to access the determination of metabolite profiles and antioxidant properties in the leaves of green perilla (Perilla frutescens), where these are considered functional and nutraceutical substances in Korea. A total of 25 compositions were confirmed as six phenolic acids, two triterpenoids, eight flavonoids, seven fatty acids, and two glucosides using an ultra high performance liquid chromatography coupled with electrospray ionization quadrupole time-of-flight mass spectrometry (UPLC-ESI-Q-TOF-MS/MS) technique from the methanol extract of this species...
October 2017: Journal of Food and Drug Analysis
Shu-Ling Wang, Zhen-Kun Zhao, Jian-Feng Sun, Yun-Ting Sun, Xiao-Qing Pang, Zhao-Wu Zeng, Tian Xie
The chemical compositions of Anemone raddeana Rhizome, a kind of traditional Chinese medicine, were reviewed, along with its bioactivity and pharmacological properties and method improvements of extracting and detecting triterpenoid saponins. A. raddeana Rhizome is used to treat neuralgia and rheumatism, and is rich in triterpenoid saponins, most of which are pentacyclic, with oleanane as the nucleus. So far, 37 triterpenoid saponins have been determined from the herb. Its reported bioactivity and pharmacological properties have been described as anticancerous, antimicrobial, anti-inflammatory, analgesic, antipyretic, anticonvulsive, antihistaminic, and sedative...
October 6, 2017: Chinese Journal of Integrative Medicine
Zhongyan Tang, Junmei Shen, Feng Zhang, Jingyu Liang, Zhengxiang Xia
Three novel neo-clerodane diterpenoids Sheareria A-C (1-3) together with three known triterpenoid saponins were isolated from the whole herb of Sheareria nana S. Moore. Their structures were established by spectroscopic and chemical method. This is the first natural sulfated neo-clerodane diterpenoids. This is the first report of all these compounds from this plant. These neo-clerodane diterpenoids and triterpenoid saponins from S. nana S. Moore may be considered as chemotaxonomic markers for the genus. The compounds isolated were evaluated for their cytotoxic effects against three cancer cell lines, the test substances demonstrated selectivity toward the cancer cells...
October 3, 2017: Fitoterapia
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