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Chemistry & Biodiversity

Mina Arbabi, Hassanali Naghdi Badi, Mohammadreza Labbafi, Ali Mehrafarin, Ebrahim Saboki
In order to determine the morphophysiological and phytochemical properties of various Ducrosia anethifolia Boiss populations, the plant samples were collected from 20 locations in native regions. Current study indicated significant differences in morphophysiological and phytochemical characteristics of D. anethifolia Boiss populations collected from 20 locations in Sistan and Baluchestan province, Iran. The highest value of plant height, number of lateral stems, node per plant, umbellate per umbel, seeds per umbellate and roots fresh and dry weight were related to the location with relatively high rainfall (130-161 mm) and low altitude (up to 1165 m) compared with other...
September 21, 2018: Chemistry & Biodiversity
Ya Li, Guangda Li, Haitao Yu, Xingzhi Jiao, Kun Gao
Fungal pathogens are a severe yield-limiting factor for the pasture crop Alfalfa (Medicago sativa L.). Eleven phenolic compounds, including a new isoflavan were isolated from the Uromyces striatus Schroet infected alfalfa. The effect of infection with Uromyces striatus Schroet on the phytochemical profile of Alfalfa was investigated using ultra-performance liquid chromatography (UPLC), and the antifungal properties of isolated compounds against a range of pathogens were tested. It was found that the contents of most of the isolated compounds in U...
September 21, 2018: Chemistry & Biodiversity
M Mahmun Hossain, Shamsul Ahmed, Damon Hinz, Marcus Jellen
We report the development of a concise method of synthesizing possible cyclooxygenase (COX) inhibitor BRL-37959, which is believed could be a potent nonsteroidal anti-inflammatory drug (NSAID). The four-step synthesis greatly increases the efficiency of compound production from commercially available salicylaldehydes. The synthesis involves an optimized, bismuth(III) tirfluoromethanesulfonate catalyzed, benzoylation of the benzofuran ring.
September 21, 2018: Chemistry & Biodiversity
Lamberto Tomassini, Marisa Piovano, Antonio Ventrone, Vincenzo Pani, Claudio Frezza, Marcello Nicoletti
The study of the main components of the alcoholic extract obtained from Chloraea chrysantha Poepp. has shown the presence of two new dihydrostilbene derivatives, together with the known gavilein, characterised by a similar structure (3). The new structures have been assigned as 2-(3-methyl-2-butenyl)-3-[2-(3-hydroxy,5-methoxyphenyl)ethyl]-benzene (1), and 2-(3-methyl-2-butenyl)-3-[2-(3,5-dimethoxyphenyl)ethyl]-benzene (2). The presence of compounds 1-3 is perfectly in accordance with the current botanical classification of the genus...
September 21, 2018: Chemistry & Biodiversity
Hong Jie Jin, Xin Zhang, Hong Cao, Yu Jing Niu, Chun Li, Hong Liu
Chemical composition, security and bio-activity of pigments from Penicillium purpurogenum Li-3 strain screened by our group were firstly studied in this papper. DPPH and filter disc diffusion method were used to determine the red pigments biological activities. The pigment was characterized by UV-Vis, FT-IR, NMR and UPLC-Q-TOF-MS. HPLC-MS was used to detect mycotoxins (citrinin) in fermentation broth. Acute toxicity were detected in embryos of the zebrafish. As a consequence, crude red pigment from ethyl acetate fraction were presented better DPPH scavenge capacity and antibacterial activity...
September 19, 2018: Chemistry & Biodiversity
Yineng Xia, Lijuan Zhu, Xinrui Yuan, Yubin Wang
Excess lipid accumulation can initiate the development and progression of atherosclerotic lesions, thus eventually leading to cardiovascular disease. Lipid-lowering medication therapy is one of the cornerstones of cardiovascular disease therapy. On the basis of the cholesterol absorption inhibitor ezetimibe, we successfully synthesized seven 2-azetidinone derivatives and eighteen 1H-pyrrole-2,5-dione derivatives. Most of the new compounds significantly inhibited cholesterol uptake in vitro. In addition, one of the most active inhibitors, compound 14q, showed no cytotoxicity in L02 and HEK293T cell lines...
September 19, 2018: Chemistry & Biodiversity
Ahmad J Obaidullah, Mostafa H Ahmed, Todd Kitten, Glen E Kellogg
The pneumococcal surface antigen A (PsaA) metal transporter protein provides manganese to bacterial cells. X-ray crystal structures of PsaA, in both closed (Mn bound) and open (metal free) conformations, were explored with virtual screening to identify potential inhibitors of manganese transport. We pursued three strategies for inhibition: 1) targeting a cavity close to the bound Mn to keep the metal in-place; 2) targeting the metal-free Mn site to prevent metal uptake; and 3) targeting a potentially druggable allosteric site involving loops that translate between the conformations...
September 17, 2018: Chemistry & Biodiversity
Mahvash Afshari, Mehdi Rahimmalek
In the present research, essential oil composition, bioactive compounds, anatomical and antioxidant activity of Achillea aucheri was investigated at four phenological stages. Essential oil yield ranged from 0.1% (five leaves appearance stage) to 0.7% (full flowering stage). So, oils from plants harvested at the full flowering stage provide higher essential oil contents than other stages. Analysis of the essential oils by GC/MS revealed the presence of a large number of components represented mainly by oxygenated monoterpenes (24...
September 12, 2018: Chemistry & Biodiversity
Tae Kyoung Lee, Dahae Lee, Jae Sik Yu, Mun Seok Jo, Su Cheol Baek, Myoung-Sook Shin, Yoon-Joo Ko, Ki Sung Kang, Ki Hyun Kim
LC/MS-based phytochemical analysis of an EtOH extract of the roots of rice (Oryza sativa; Gramineae), which takes a crucial role in the stable crop population in Asia, resulted in the isolation of a new lignan, oryzativol C (1), as a minor component. The chemical structure of compound 1 was unambiguously confirmed using spectroscopic evidence (including 1D and 2D NMR data), HR-ESI-MS, and CD data analysis. Considering the traditional medicinal efficacy of O. sativa and its importance as a food crop, compound 1 was evaluated for effects on breast cancer cell line (MDA-MB-231) and on glucose-stimulated insulin secretion in an INS-1 pancreatic β-cell line...
September 12, 2018: Chemistry & Biodiversity
Wei-Hua Yuan, Meng-Ting Teng, Shan-Shan Sun, Lin Ma, Bo Yuan, Qiang Ren, Peng Zhang
Active metabolites investigation of Talaromyces sp. (strain no. MH551540) associated with Xanthoparmelia angustiphylla afforded a new δ-lactone, talaromycin A (1), together with six known compounds, clearanol A (2), 6'-methyl-[1,1'-biphenyl]-3,3',4',5-tetraol (3), desmethylaltenusin (4), ergone (5), ergosterol (6), palmitic acid (7). The structures of these compounds were elucidated by a combination of spectroscopic-data interpretation and single-crystal X-ray diffraction analysis. The cytotoxicities of 1 - 7, and antioxidant activities of 3 and 4 were also evaluated...
September 10, 2018: Chemistry & Biodiversity
Hongwei Han, Hongyan Lin, Deliu He, Yao Ren, Wenxue Sun, Li Liang, Meihang Du, Dengchao Li, Yichun Chu, Minkai Yang, Xiaoming Wang, Yonghua Yang
A number of podophyllotoxin derivatives (3A-J) had been designed, synthesized and their biological activities were evaluated in this study. Moreover, the anti-proliferation activities of these compounds against four human cancer cell lines (including HepG2, HeLa, A549 and MCF-7) were also tested. The results indicated that, the most promising compound 3D had displayed potent inhibitory activity over the four human cancer cell lines, which was further demonstrated to have potent tubulin polymerization inhibitory effect without damaging the non-cancer cells...
September 8, 2018: Chemistry & Biodiversity
Cheng Wang, Youjia Li, Ting Zhang, Di Wei, Yajing Hou, Huaizhen He
In continuation of our previous efforts towards the development of coumarin derivatives with potential vasodilatory activity, 5-phenyl coumarin derivatives were designed and synthesized. Target compounds and their precursors exhibited moderately vasodilatory ability with EC50 at 2.5-49.0 μM. And docking study also revealed the well binding mode of compound 8c with the target protein. Moreover, Intermediates and final product also exhibited different fluorescent properties due to the substituent effect. These results may provide new idea for synthesis and application of 5-substituted coumarins...
September 8, 2018: Chemistry & Biodiversity
Yanting Chai, Ying Si, Jiaxin Xu, Yuchen Xiang, Hongyan Zhao, Yuan Si, Te Zhang, Ying Liu
Polyphyllin I (PPI), a bioactive constituent extracted from traditional medicinal herbs, is cytotoxic to several cancer types. However, whether PPI can be used to treat t(8;21) acute myeloid leukemia (AML) cells requires further investigation. Here, we determined the inhibitory effects of PPI on t(8;21) AML cells by Cell Counting Kit-8 (CCK-8) and the trypan blue dye exclusion assay. DAPI staining and Wright-Giemsa staining were performed to check for apoptosis. Detection of apoptotic protein and AML1-ETO signaling protein expression by Western Blot analysis...
September 7, 2018: Chemistry & Biodiversity
Nora S Engels, Birgit Waltenberger, Barbara Michalak, Loi Huynh, Hung Tran, Anna K Kiss, Hermann Stuppner
In an initial screening, the dichloromethane extract from the leaves of Melodorum fruticosum showed distinct inhibitory effects on the release of interleukin-8 (IL-8) in human neutrophils. Therefore, the aim of the present study was the phytochemical and pharmacological investigation of this extract, to better understand which compounds might be responsible for the anti-inflammatory effect. Phytochemical analysis led to the isolation of 12 known compounds and two new natural products, 5-hydroxy-4',7-dimethoxy-6(2˝-hydroxybenzyl)flavanone and 2',4'-dihydroxy-4,6'-dimethoxy-3'(2˝-hydroxybenzyl)chalcone...
September 7, 2018: Chemistry & Biodiversity
Jajula Kashanna, Rathod Arvind Kumar, Ravada Kishore, Doddukuri Nandhan Kumar, Alleni Suman Kumar
Novel 2,3-dihydrofuran derivatives were accomplished by a Tandem Knoevenagel Michael cyclization in good yield by reacting α-tosyloxy ketone, 5,5-Dimethyl-1,3-cyclohexandione and various aldehydes in the presence of phthalazine in acetonitrile. These compounds were subjected to in vitro antibacterial screening against eight micro-organisms by using diffusion method and also in vitro cytotoxicity screening against four human cancerous cell lines by applying MTT assay. Some of the compounds showed impressive activities...
September 6, 2018: Chemistry & Biodiversity
Nemesio Villa-Ruano, Elvia Becerra-Martínez, Ramiro Cruz-Durán, José Alejo Zarate-Reyes, Gerardo Landeta-Cortés, Omar Romero-Arenas
The present research describes the chemical composition and biological activities of the leaf essential oil from B. glabrifolia obtained in four consecutive years (2015-2018). The essential oil contained α-terpineol (17.9-29.7%), α-terpinene (12.6-17.4%), limonene (14.9-26.8%) and β-pinene (2.1-16.7%) as the most abundant volatiles. The essential oil and these volatiles showed a significant adulticide activity (p<0.01; LC50 <100 μg mL-1 ) on the maize weevil (Sitophilus zeamais), with a 100% mortality rate within a period of 5 hours...
September 6, 2018: Chemistry & Biodiversity
Xiao-Hang Wang, Ke-Xin Zhu, Jing-Ya Li, Chun Lei, Ai-Jun Hou
Two new triterpenoids, vistriterpenoids A (1) and B (2), and four known ones, were acquired from Dodonaea viscosa. Compounds 1 and 2 represent the first 24-nor-oleanane triterpenoids from the genus Dodonaea. Their structures were identified based on extensive spectroscopic methods. Compounds 1, 2, 5, and 6 exerted inhibitory activities against PTP1B in vitro. This article is protected by copyright. All rights reserved.
September 6, 2018: Chemistry & Biodiversity
Yao Ma, Yuan Wang, Xuan Li, Li-Xiu Hou, An-Zhi Wei
In this study, Zanthoxylum bungeanum extracts were prepared using seven solvents: de-ionized water, methanol, ethanol, acetic acid, ethyl acetate, chloroform, and benzene. The volatile compositions in the extracts were qualitatively analyzed using headspace solid-phase microextraction coupled with gas chromatography mass spectrometry detection, and the alkylamide composition was determined using high-performance liquid chromatography. The extract compositions differed with respect to the solvents. A total of 49 volatile components belonging to four groups - terpenoids, alcohols, esters, and ketones -were identified in the extracts...
September 3, 2018: Chemistry & Biodiversity
Hua Shao, Yunxia Hu, Caixia Han, Caixia Wei, Shixing Zhou, Chenpeng Zhang, Chi Zhang
To evaluate the potential value of Seriphidium terrae-albae (Krasch) Poljak essential oil as bioherbicide, its chemical composition as well as phytotoxic activity were investigated. Seventeen compounds were identified via GC-MS, representing 98.1% of the total oil, and the most abundant constituents were α-thujone (43.18%), β-thujone (16.92%), eucalyptol (17.55%) and camphor (13.88%). Phytotoxic assay revealed that the essential oil as well as its major constituents exhibited inhibitory activity on root and shoot growth of receiver plants in a dose-dependent manner...
August 31, 2018: Chemistry & Biodiversity
Ilya I Voronov, Vyacheslav M Martynenko, Alexander V Chernyak, Jan Balzarini, Dominique Schols, Pavel A Troshin
We have synthesized a series of water-soluble polycarboxylic derivatives of [60]fullerene with a gradually changed polarity by combining 3 to 5 polar (ionic) malonate addends with 2 to 0 hydrophobic dichlorobenzene units and explored their antiviral activity. It has been shown that decreasing the number of the ionogenic carboxylic groups in the molecules enhanced their antiviral activity against HIV-1 and suppressed their action against HIV-2. The obtained results implied that the charged states and hydrophobicity of the water-soluble polycarboxylic fullerene derivatives affect significantly their biological properties...
August 31, 2018: Chemistry & Biodiversity
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