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Sing Yee Yeung, Matthew J Piggott
Both the traditional Chinese medicinal fungus, Antrodia camphorata, and its secondary metabolite, 4,7-dimethoxy-5-methylbenzo[d][1,3]dioxole, have been reported to possess promising anticancer activity. In this work the natural product and analogues bearing more polar substituents were synthesised and assessed for antiproliferative activity in the NCI-60 screen. Although each compound inhibited the growth of some cell lines at 10μM, none had sufficient activity to warrant further investigation.
September 16, 2017: Fitoterapia
Qing-Hua Huang, Chun Lei, Pei-Pei Wang, Jing-Ya Li, Jia Li, Ai-Jun Hou
Two new Diels-Alder adducts, albasins A and B (1 and 2), one new isoprenylated 2-arylbenzofuran, albasin C (3), one new isoprenylated flavone, albasin D (4), together with sixteen known phenolic compounds, were isolated from the root bark of Morus alba. Their structures were elucidated by extensive spectroscopic analysis, including NMR, MS, and ECD data. All the new compounds and most of the known ones showed significant inhibitory effects on PTP1B in vitro with IC50 values ranging from 0.57 to 7.49μM.
September 12, 2017: Fitoterapia
Xinglong Chen, Aixue Zuo, Zhentao Deng, Xiaoyan Huang, Xuemei Zhang, Changan Geng, Tianze Li, Jijun Chen
Seven new phenolic glycosides including two heterocyclic phenolic derivatives orcinosides I-J (1-2) and five chlorophenolic glycosides curculigines J-N (3-7), together with nineteen known compounds were isolated from the rhizome of Curculigo orchioides. Based on extensive spectroscopic analyses (UV, IR, HRESIMS, 1D and 2D NMR), the structures of the new compounds were identified. Orcinoside I (1) and J (2) displayed xanthine oxidase inhibitory activities with IC50 values 0.25 and 0.62mM respectively.
September 12, 2017: Fitoterapia
Si-Yuan Shao, Zi-Ming Feng, Ya-Nan Yang, Jian-Shuang Jiang, Pei-Cheng Zhang
In our study to investigate components with hepatoprotective activities, eight new phenylethanoid glycoside derivatives (1-8) were isolated from the 75% EtOH-H2O extract of the fruits of Forsythia suspensa along with six known compounds (9-14). These new structures were elucidated through HRESIMS and extensive NMR spectroscopic techniques. The absolute configurations of their sugars were determined by GC analysis. The pharmacological assay showed that compounds 2, 3, and 9-11 displayed remarkable hepatoprotective activities against N-acetyl-p-aminophenol (APAP)-induced HepG2 cell damage at the concentration of 10μM (Bicyclol as positive contrast)...
September 11, 2017: Fitoterapia
Marianna Nalli, Giorgio Ortar, Aniello Schiano Moriello, Vincenzo Di Marzo, Luciano De Petrocellis
A series of 33 curcumin analogues was synthesized and tested on TRPA1, TRPM8, and TRPV1 channels. Twenty of them acted as good modulators of TRPA1 channels. None was able to significantly activate TRPM8 channels, while curcumin itself and six curcuminoids belonging to the 1,3-dicarbonyl and acyclic series behaved as 'true' antagonists with IC50 values<5μM. Only few curcuminoids were able to modulate TRPV1 channels with EC50 and IC50 values ranging from 3.4 and 6.0μM.
September 10, 2017: Fitoterapia
Hui Chen, Yu-Jie Li, Yan-Jun Sun, Jian-Hong Gong, Kun Du, Yan-Li Zhang, Cheng-Fu Su, Qian-Qian Han, Xiao-Ke Zheng, Wei-Sheng Feng
Seven new lignanamides, lyciumamides D-J (1-4 and 9-11), together with nine known analogues (5-8 and 12-16), were isolated from the root bark of Lycium chinense. The structures of the isolated compounds were elucidated on the basis of NMR spectroscopic and HRESIMS data. All isolated compounds were evaluated for antihyperlipidemic activities in HepG2 cells. The primary structure-activity relationships were discussed.
September 8, 2017: Fitoterapia
Pritesh Prasad, Ailian Zhang, Angela A Salim, Robert J Capon
Chemical investigation of two Irciniidae sponges collected by hand (SCUBA) from Australian near shore waters, afforded six new examples of a rare class of sesterterpene lactam; ircinialactams B (1), G (2), H (5), and I (6), and 8-hydroxyircinialactams C (3) and G (4); together with the new biosynthetically related lactone, ircinialactone A (7). Also isolated were seven biosynthetically related known Irciniidae metabolites; ircinialactams A (8) and C (9), (7E,12E,20Z,18S)-variabilin (10), (7Z,12Z,20Z,18S)-variabilin (11), (7E,12Z,20Z,18S)-variabilin (12), (7Z,12E,20Z,18S)-variabilin (13) and irciniafuran A (14)...
September 6, 2017: Fitoterapia
Bandi Siva, Amujuri Devi, Arramsetti Venkanna, Borra Poornima, Genji Sukumar, Solipeta Divya Reddy, Movva Vijaya, Ramesh Ummanni, Katragadda Suresh Babu
A series of Nimbolide-triazole conjugates were synthesized through copper(I)- catalyzed azide-alkyne "click" chemistry approach and these derivatives (2-4, 2a-2l) were characterized using modern spectroscopic techniques. Antifeedant activities of these derivatives were studied on Tobacco Caterpillar, Spodoptera litura (F.) using no-choice leaf disk bioassay. Interestingly, the synthesized derivatives were more effective in reducing feedancy by insect species when compared to the parent nimbolide. Among the tested compounds, 2a, 2c, and 2d showed potent antifeedancy with ED50 values of 0...
September 6, 2017: Fitoterapia
Jinqian Yu, Xiangyun Song, Daijie Wang, Xueyong Wang, Xiao Wang
Five new chromone glycosides, officinalisides A (1), B (2), C (3), D (4) and E (5) were isolated from Scindapsus officinalis (Roxb.) Schott., along with six known chromone derivatives, 7-O-α-l-rhamnosyl-nereugenin (6), undulatoside A (7), drynachromoside A (8), drynachromoside B (9), 5,7-dihydroxy-2-methyl chromone(10), 5,7-dihydroxy-2-hydroxymethyl chromone (11). Structural elucidation of the isolated compounds was established by spectroscopic analysis, especially 2D NMR techniques and comparison with literatures...
September 4, 2017: Fitoterapia
Dorcas Osei-Safo, Godwin Akpeko Dziwornu, Antonio Salgado, Suthananda Naidu Sunassee, Mary Anti Chama
Two new bisbibenzyls, heudelotol A (1) and B (2), along with the known bibenzyls, (E)-combretastatin A-1 (3) and combretastatin B-1 (4) have been isolated from the ethyl acetate extract of the roots of Dichapetalum heudelotii. Structure elucidation of all four isolated compounds was achieved using UV, IR, 1D and 2D NMR spectroscopy and HR-Mass Spectrometry. The compounds exhibited varying antiproliferative activity against six cancer cell lines using the CellTiter-Glo® Luminiscent Cell Viability Assay. Compound 3 was found to be the most active with sub-micromolar growth inhibition concentrations against all the cell lines (GI50 0...
September 4, 2017: Fitoterapia
Barbara Tóth, Norbert Kúsz, Peter Forgo, Noémi Bózsity, István Zupkó, Gyula Pinke, Judit Hohmann, Andrea Vasas
The present study aimed at the phytochemical and pharmacological investigation of Sideritis montana L. (Lamiaceae). Two new abietane diterpenes [sideritins A (1) and B (2)] were isolated from the methanol extract of the plant. Six known compounds [pomiferin E (3), 9α,13α-epi-dioxyabiet-8(14)-en-18-ol (4), paulownin (5), 6-methoxysakuranetin (6), 3-oxo-α-ionol (7) and 4-allyl-2,6-dimethoxyphenol glucoside (8)] were also obtained from the plant. The structures were determined by means of HREIMS and NMR experiments...
August 31, 2017: Fitoterapia
Yi-Guo Dai, Jun Wu, Krishna Pillai Padmakumar, Li Shen
Five new limonoids, named sundarbanxylogranins A-E (1-5), were isolated from the seeds of an Indian mangrove, Xylocarpus granatum, collected from mangrove swamps of the Sundarbans, India. The structures of these limonoids were established by HRESIMS and NMR spectroscopic data. Sundarbanxylogranin A (1) is a rare limonoid containing a bicyclo[5.2.1]dec-3-en-8-one scaffold as the ring A/B-fused core; whereas sundarbanxylogranin B (2) is a typical mexicanolide with an 8α, 30α-epoxy ring. Sundarbanxylogranins C-E (3-5), among which the former two possess a 29-OMe group with different orientation, belong to a small group of limonoids containing a C1-O-C29 oxygen bridge...
August 31, 2017: Fitoterapia
Lin Chen, Zheng-Hui Li, Jian-Neng Yao, Yue-Ling Peng, Rong Huang, Tao Feng, Ji-Kai Liu
Hericium caput-medusae is an edible and medicinal mushroom closely relative to H. erinaceus. According to our detailed chemical investigation, two novel isoindolinone-containing meroterpene dimers, caputmedusins A (1) and B (2), as well as nine analogues, caputmedusins C-K (3-11), were isolated from the fermentation broth of H. caput-medusae. Their structures were elucidated by analyses of 1D and 2D NMR spectroscopic methods. The absolute configurations of 1-4 were speculated based on the specific optical rotation and biogenetic consideration...
August 30, 2017: Fitoterapia
Ruo-Feng Sun, Chen-Cheng Zhu, Yu Yang, Neng-Jiang Yu
Nineteen secolignans (1-19), including five new ones (1-5), were isolated from the whole plant of Peperomia dindygulensis. Their structures including stereochemistry were determined by spectroscopic methods, in particular NMR and electronic CD (ECD) analysis. All the isolates were evaluated for their inhibitory activities against IFN-γ/STAT1 as well as IL-6/STAT3 signaling pathway by the method of Luciferase assay. Six 2-methene type secolignans (1, 2, 6-9) exhibited significant inhibitory activities against JAK-STAT pathways with the IC50 values both lower than 10μM...
August 30, 2017: Fitoterapia
Gregorio Peron, Stefania Sut, Anna Pellizzaro, Paola Brun, Dario Voinovich, Ignazio Castagliuolo, Stefano Dall'Acqua
Cranberry procyanidins and quercetin derivatives are considered possible active compounds against urinary tract infections (UTIs). In this paper a small group (n=6) of healthy subjects consumed a product containing 360mg of cranberry extract (42.6% w/w of PAC-A and 14.6% w/w of PAC-B) and 200mg of quercetin. Urine samples were collected after 2,4,6,8, and 24h. The changes in antiadhesive properties against urophatogenic E. coli of the urinary output were determined in vitro and modification to urinary metabolome were studied by LC-MS...
August 26, 2017: Fitoterapia
Cong Zhang, Shou-Jin Liu, Liu Yang, Ming-Yan Yuan, Jin-Yu Li, Bo Hou, Hong-Mei Li, Xing-Zhi Yang, Chang-Chun Ding, Jiang-Miao Hu
A new bibenzyl derivative, dendrocandin V (1) and a new sesquiterpene amino ether, wardianumine A (2), together with eleven known compounds, including phenanthrenes (denbinobin (3), 9,10-dihydro-denbinobin (4), mostatin (5), loddigesiinols A (6)), bibenzyls (moscatilin (7), 5-hydroxy-3,4'-dimethoxybibenzyl (8), 3,4-dihydroxy-5,4'-dimethoxy bibenzyl (9), dendrocandin A (10), gigantol (11), dendrocandin U (12)) and an alkaloids (dihydroshihunine, 13) were isolated from the EtOH extraction of stems of Dendrobium wardianum Warner...
August 24, 2017: Fitoterapia
Ren-Yu Song, Xiao-Bing Wang, Guo-Ping Yin, Rui-Huan Liu, Ling-Yi Kong, Ming-Hua Yang
Five new isocoumarin derivatives, pestalactone A-C (1-3) and pestapyrone D-E (4-5), together with two known compounds (6-7) were isolated from the solid cultures of the endophytic fungus Pestalotiopsis sp. obtained from Photinia frasery. Their structures were mainly determined by extensive spectroscopic analysis, Mo2(OCOCH3)4-induced electronic circular dichroism (ECD), and ECD calculation. Compounds 1 and 2 were rare isocoumarin derivatives and derived from distinctive polyketide pathways. Compound 3 exhibited potent antifungal activity against Candida glabrata (ATCC 90030) with an MIC50 value of 3...
August 23, 2017: Fitoterapia
Deepak M Kasote, Minal V Pawar, Riya S Bhatia, Vinod S Nandre, Shridevi S Gundu, Suresh D Jagtap, Mohan V Kulkarni
The present study aimed to investigate chemical profile, antioxidant and antimicrobial activities of Indian Melifera propolis (IMP) samples collected from 13 different states. Chemical characterisation of ethanolic extracts of IMP (EEMP) samples was carried out by using HPLC and (1)HNMR spectroscopy. The antioxidant activity of EEMP samples was measured by DPPH, ABTS, and FRAP assay. Moreover, the antimicrobial activity of each EEMP sample tested against bacteria and yeast using a 96 well plate microdilution method...
August 23, 2017: Fitoterapia
Dan Xu, Xue-Jiao Pang, Ting Zhao, Lu-Lin Xu, Xiao-Long Yang
Six new alkenylated tetrahydropyran derivatives belonged to polyketides, designated as (12R,13R)-dihydroxylanomycinol (1), (12S,13S)-dihydroxylanomycinol (2), (12R,13S)-dihydroxylanomycinol (3) and (12S,13R)-dihydroxylanomycinol (4), (12S,13R)-N-acetyl-dihydroxylanomycin (5) and (12S,13S)-N-acetyl-dihydroxylanomycin (6), together with one related known compound lanomycinol (7) were isolated from the liquid cultures of Westerdykella dispersa obtained from the marine sediments. Their structures and absolute configurations were determined on the basis of extensive analysis of NMR spectra combined with comparison of NMR data to those of known compound, and computational method via calculation of the electronic circular dichroism (ECD)...
August 23, 2017: Fitoterapia
Blessing O Umeokoli, Felix A Onyegbule, Festus B C Okoye, Hao Wang, Rainer Kalscheuer, Werner E G Müller, Rudolf Hartmann, Zhen Liu, Peter Proksch
The first chemical investigation of leaves of Breynia nivosa from Nigeria resulted in the isolation of two new amide derivatives breynivosamides A and B (1 and 2) and two new dioxopiperazine derivatives breynivosines A and B (4 and 5) together with seven known compounds (3, 6-11). The structures of the new compounds were elucidated by 1D, 2D NMR and HRESIMS data as well as by comparison with the literature. All isolated compounds were tested for the cytotoxic and antimicrobial activities. Only cristatin A (6) showed cytotoxicity against the L5178Y mouse lymphoma cell line with an IC50 value of 13...
August 19, 2017: Fitoterapia
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