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Chuwen Li, Chao Zhang, Hefeng Zhou, Yu Feng, Fan Tang, Maggie P M Hoi, Chengwei He, Dan Ma, Chao Zhao, Simon M Y Lee
In response to the microenvironment, microglia may polarize into either an M1 pro-inflammatory phenotype, exacerbating neurotoxicity, or an M2 anti-inflammatory phenotype, conferring neuroprotection. Betulinic acid (BA) is a naturally pentacyclic triterpenoid with considerable anti-inflammatory properties. Here, we aim to investigate the potential effects of BA on microglial phenotype polarization and to reveal the underlying mechanisms of action. First, we confirmed that BA promoted M2 polarization and inhibited M1 polarization in lipopolysaccharide (LPS)-stimulated BV-2 microglial cells...
2018: Frontiers in Molecular Neuroscience
Jasmine Phillips, Iesha Phillips, Blessing Enya, Hua Zhao, Takayuki Nitta
Murine leukemia virus (MuLV) is a retrovirus known causing leukemia and neurological disorders in mice, and its viral life cycle and pathogenesis have been investigated extensively over the past decades. As a natural antiviral agent, betulinic acid is a pentacyclic triterpenoid that can be found in the bark of several species of plants (particularly the white birch). One of the hurdles for betulinic acid to release its antiviral potency is its poor water solubility. In this study, we synthesized more water-soluble ionic derivatives of betulinic acid, and examined their activities against Moloney MuLV (M-MuLV)...
April 13, 2018: Biochemical and Biophysical Research Communications
Jiao-Jiao Zhu, Hui-Xiang Yang, Zheng-Hui Li, Guo-Kai Wang, Tao Feng, Ji-Kai Liu
A new lupane triterpenoid, 23-O-trans-feruloylcylicodiscic acid (1), as well as four known analogues (2‒5), was isolated from the EtOAc fraction of Menyanthes trefoliata. The structure of compound 1 was elucidated on the basis of extensive spectroscopic analysis, including 2D NMR data. The structures of the known compounds were established by comparison of their spectroscopic data with that in the literature. Compounds 1, 2, and 4 exhibited certain anti-NO production activities.
April 16, 2018: Journal of Asian Natural Products Research
Xiao-Kui Huo, Jing Liu, Zhen-Long Yu, Yi-Fei Wang, Chao Wang, Xiang-Ge Tian, Jing Ning, Lei Feng, Cheng-Peng Sun, Bao-Jing Zhang, Xiao-Chi Ma
BACKGROUND: Cholestasis is a clinical syndrome of liver damage that is caused by accumulation of bile acids in the liver and systemic circulation. Farnesoid X receptor (FXR) can regulate synthesis, metabolism, and excretion of bile acids. The rhizomes of Alisma orientale is a well-known traditional Chinese medicine to treat edema, obesity, gonorrhea, leukorrhea, diarrhea, hyperlipidemia, and diabetes in China. HYPOTHESIS/PURPOSE: We hypothesized Alisma orientale extract (AOE) to exert hepatoprotective effect against α-naphthylisothiocyanate (ANIT) induced cholestasis in rat...
March 15, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Hua Chen, Tian Yang, Min-Chang Wang, Dan-Qian Chen, Yang Yang, Ying-Yong Zhao
BACKGROUND: Tubulo-interstitial fibrosis (TIF) is the common pathway in the chronic kidney disease (CKD). Epithelial-to-mesenchymal transition (EMT) is a major contributor to the TIF by the increased myofibroblasts. Renin-angiotensin system (RAS) is critical mediator on EMT in progressive CKD. Angiotensin II (ANG) mediates EMT and causes TIF by stimulating transforming growth factor-β1 (TGF-β1). RAS activation could further activate TGF-β1. Inhibition of the RAS is one of the most powerful therapies for progressive CKD...
March 15, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Ju-Hyung Park, Jin-Kyung Kim
BACKGROUND: Pristimerin is a quinonemethide triterpenoid with anti-cancer, anti-angiogenic, anti-inflammatory and anti-protozoal activity. However, the therapeutic role of pristimerin in colitis-associated colorectal carcinogenesis is unknown. PURPOSE: We sought to examine the therapeutic effects of pristimerin on colitis-associated colon cancer induced in mice using azoxymethane (AOM)/dextran sulfate sodium (DSS). The goal was to identify the potential mechanism of action underlying the pharmacological activity of pristimerin...
March 15, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Dante J Marciani
Numerous triterpenoid saponins are adjuvants that modify the activities of T cells and antigen-presenting cells, like dendritic cells (DCs). Saponins can induce either proinflammatory Th1/Th2 or sole anti-inflammatory Th2 immunities. Structure-activity relationships (SARs) have shown that imine-forming carbonyl groups are needed for T cell activation leading to induction of Th1/Th2 immunities. While saponins having different triterpenoid aglycons and oligosaccharide chains can activate DCs to induce Th1/Th2 immunoresponses, fucopyranosyl residues from their oligosaccharides by binding to the DC-SIGN receptor can bias DCs toward a sole Th2 immunity...
April 11, 2018: Trends in Pharmacological Sciences
Feng Xu, Xulong Huang, Hongmei Wu, Xiangpei Wang
There are a large number of new structure compounds with good pharmacological activity in the natural plants, can be applied to the treatment of human diseases. Finding active ingredients from the plants is one of the important ways to develop new drugs. Triterpenes are widespread in plants, and lupenone belongs to lupane type triterpenoids. Lupenone is very common natural ingredient distributed in multi-family plants including Asteraceae, Balanophoraceae, Cactaceae, Iridaceae, Musaceae, Urticaceae, Leguminosae, Bombacaceae, etc...
April 10, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Yang Liu, Jia Liu, Ke-Xin Wu, Xiao-Rui Guo, Zhong-Hua Tang
Astragalus is one of the most popular Chinese herbal. Control of Astragalus quantity is most important, since that various varieties and ages largely affect bioactive metabolites and different pharmacological effects. Astragalus mongholicus and Astragalus membranaceus are both major sources of Astragalus according to the provisions in the Chinese Pharmacopoeia. Thus, a sensitive and rapid UPLC-MS/MS method for the simultaneous determination of l-Phenylalanine, Isoliquiritigenin, Liquiritigenin, Daidzein, Formononetin, Ononin, Calycosin, Calycosin-7-glucoside, Cycloastragenol, Astragaloside I, Astragaloside II, Astragaloside III and Astragaloside IV was established in this study...
April 4, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
E Gómez, S Carrocera, D Martin, P Herrero, N Canela, M Muñoz
Male and female early bovine embryos show dimorphic transcription that impacts metabolism. Individual release of metabolites was examined in a 24h single culture medium from Day-6 male and female morulae that developed to Day-7 expanded blastocysts. Embryos were produced in vitro, fertilized with a single bull and cultured in SOFaaci+6  g/L BSA. The embryonic sex was identified (amelogenin gene amplification). Embryos (N = 10 males and N = 10 females) and N = 6 blank samples (i.e. SOFaaci+6  g/L BSA incubated with no embryos) were collected from 3 replicates...
April 5, 2018: Theriogenology
Keita Tamura, Koki Yoshida, Yasuko Hiraoka, Daiki Sakaguchi, Ayaka Chikugo, Keiichi Mochida, Mareshige Kojoma, Nobutaka Mitsuda, Kazuki Saito, Toshiya Muranaka, Hikaru Seki
Glycyrrhiza uralensis (licorice) is a widely used medicinal plant belonging to the Fabaceae. Its main active component, glycyrrhizin, is an oleanane-type triterpenoid saponin widely used as a medicine and as a natural sweetener. Licorice also produces other triterpenoids, including soyasaponins. Recent studies have revealed various oxidosqualene cyclases and cytochrome P450 monooxygenases (P450s) required for the biosynthesis of triterpenoids in licorice. Of these enzymes, β-amyrin synthase (bAS) and β-amyrin C-24 hydroxylase (CYP93E3) are involved in the biosynthesis of soyasapogenol B (an aglycone of soyasaponins) from 2,3-oxidosqualene...
April 1, 2018: Plant & Cell Physiology
Xiaotian Zhang, Feng Ji, Yueqi Li, Tian He, Ya Han, Daidong Wang, Zongtao Lin, Shizhong Chen
In this study, an on-line supercritical fluid extraction (SFE) and supercritical fluid chromatography (SFC) method was developed for the rapid determination of oleanoic acid and ursolic acid in Chaenomelis Fructus. After optimization of the conditions, the two triterpenoid acids was obtained by SFE using 20% methanol as a modifier at 35°C in 8 min. They were resolved on a Shim-pack UC-X Diol column (4.6 × 150 mm, 3 μm) in 14 min (0 - 10 min, 5 - 10%; 10 - 14 min, 10% methanol in CO2 ) with a backpressure of 15 MPa at 40°C...
2018: Analytical Sciences: the International Journal of the Japan Society for Analytical Chemistry
Sha Zhang, Liang Cao, Zong-Ren Wang, Zhe Li, Jing Ma
Toosendanin (TSN) is a triterpenoid purified from the medicinal herb Melia toosendan Sieb. et Zucc and has been used as an insecticide for decades. Recent studies have attracted increasing interest of TSN due to its novel anti-cancer effect in diverse cancer models. The broad spectrum anti-cancer activity suggests that TSN inhibits multiple pathways/targets that are critical for cancer cell survival and proliferation. Our recent study indicated that TSN has anti-cancer effect in glioblastoma through induction of estrogen receptor β (ERβ) and p53...
April 9, 2018: Journal of Asian Natural Products Research
Younes Najafian, Shokouh Sadat Hamedi, Masoumeh Kaboli Farshchi, Zohre Feyzabadi
Plantago major has been used widely since ancient times, to manage a wide range of diseases including constipation, coughs and wounds. The aim of this study is to review the traditional application, botanical characterization, pharmacological activities, phytochemistry effects and toxicity of Plantago major. In this review study, medicinal properties of Plantago major are collected from credible pharmacopeias, textbooks of traditional Persian medicine (TPM) belonging to the 10-18th century AD, such as "The Canon of Medicine", "Makhzan-Al- Advia" and so on...
February 2018: Electronic Physician
Zhijian Li, Qingxi Min, Haoji Huang, Ruixuan Liu, Yongyan Zhu, Quanhong Zhu
A series of seco-A-pentacyclic triterpenoids-3,4-lactone were synthesized and the anti-HBV activities were evaluated in vitro. Several compounds inhibited the secretion of HBV antigen and the replication of HBV DNA in micromolar level. Compounds D7 and D10, seco-A-oleanane-3,4-lactone, suppressed the HBeAg secretion with IC50 values of 0.14 μM and 0.86 μM respectively, and the inhibitory activities were also confirmed by detecting the fluorescence intensity of FITC-labeled monoclonal mouse HBeAg antibody via flow cytometry...
March 29, 2018: Bioorganic & Medicinal Chemistry Letters
Ahmed A Shaaban, Dalia H El-Kashef, Mohamed F Hamed, Dina S El-Agamy
Pristimerin (Pris) is a triterpenoid derivative obtained from Celastraceae and Hippocrateaceae families. This compound has been extensively tested for its potent anti-cancer activity against different types of tumors. However, its effects against acute lung injury (ALI) remain to be investigated. This study explored the efficacy of Pris to protect against lipopolysaccharide (LPS)-induced ALI and its possible pathways. Results have shown that Pris possesses potent protective activity against LPS-induced acute lung damage...
April 2, 2018: International Immunopharmacology
Florian Bartels, Young J Hong, Daijiro Ueda, Manuela Weber, Tsutomu Sato, Dean J Tantillo, Mathias Christmann
The first chemical synthesis of pentacyclic onocerane triterpenoids has been achieved. A putative biomimetic tricyclization cascade is employed to forge a fused decalin-/oxepane ring system. The synthetic route proceeds to (+)-cupacinoxepin in seven steps and to (+)-onoceranoxide in eight steps in the longest linear sequence, when starting from geranyl chloride and (+)-sclareolide. The bioinspired epoxypolyene cyclization is supported by computational and enzymatic studies.
December 1, 2017: Chemical Science
Zhen-Zhen Yuan, You-Rui Suo, Xue-Yan Hao, Shu-Lin Wang, Gang Li, Hong-Lun Wang
Six triterpenic acids were separated and purified from the ethyl acetate extractive fraction of ethanol extracts of Potentilla parvifolia Fisch. using a variety of chromatographic methods. The neuroprotective effects of these triterpenoids were investigated in the present study, in which the okadaic acid induced neurotoxicity in human neuroblastoma SH-SY5Y cells were used as an Alzheimer's disease cell model in vitro. The cell model was established with all trans-retinoic acid (5 μmol/L, 4 days) and okadaic acid (40 nmol/L, 6 hours) treatments to induce tau phosphorylation and synaptic atrophy...
April 3, 2018: Biological & Pharmaceutical Bulletin
Rui Yang, Wendong Li, Bochuan Yuan, Guangxi Ren, Liqiang Wang, Ting Cheng, Ying Liu
Licorice is one of the most frequently used Chinese herbs, mainly containing triterpenoids and flavonoids. Three original plants, Glycyrrhiza glabra L., Glycyrrhiza uralensis Fisch., and Glycyrrhiza inflata Bat., are defined as licorice in Chinese pharmacopeia. In this study, 40 G. uralensis samples (Group A), 60 G. glabra samples (Group B, C and D) and 40 G. inflata samples (Group E and F), were used as plant materials, the genetic diversity of samples were determined by gene sequencing technology and the chemotypic diversity were detected by HPLC...
March 2018: Pakistan Journal of Pharmaceutical Sciences
Chun-Hong Li, Hua-Li Zuo, Cen Chen, Yuan-Jia Hu, Zheng-Ming Qian, Wen-Jia Li, Zhi-Ning Xia, Feng-Qing Yang
Ganoderma lucidum (Chizhi in Chinese) is one of the most valuable and widely used medicinal fungi in traditional Chinese medicines (TCMs). Most of previous studies were focused on the triterpenoids and polysaccharides of G. lucidum, whereas less attention had been paid on the protein, which is another bioactive compound in it. In the present study, protein maps of fourteen G. lucidum samples were comprehensively analyzed by sodium dodecyl sulfate - polyacrylamide gel electrophoresis (SDS-PAGE) and two-dimensional electrophoresis (2-DE)...
March 2018: Pakistan Journal of Pharmaceutical Sciences
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