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Daniela Hulcová, Kateřina Breiterová, Tomáš Siatka, Kamila Klímová, Lara Davani, Marcela Šafratová, Anna Hošťálková, Angela De Simone, Vincenza Andrisano, Lucie Cahlíková
Glycogen synthase kinase-3β (GSK-3β) is a multifunctional serine/threonine protein kinase that was originally identified as an enzyme involved in the control of glycogen metabolism. It plays a key role in diverse physiological processes including metabolism, the cell cycle, and gene expression by regulating a wide variety of well-known substances like glycogen synthase, tau-protein, and β-catenin. Recent studies have identified GSK-3β as a potential therapeutic target in Alzheimer´s disease, bipolar disorder, stroke, more than 15 types of cancer, and diabetes...
March 21, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Weijuan Du, Lisha Jin, Liping Li, Wei Wang, Su Zeng, Huidi Jiang, Hui Zhou
The tuber of Corydalis yanhusuo is a famous traditional Chinese medicine and found to have potent pharmacological effects, such as antinociceptive, antitumor, antibacterial, anti-inflammatory, and anti-depressive activities. Although there are several methods to be developed for the analysis and detection of the bioactive ingredients' alkaloids, so far, only few prominent alkaloids could be quantified, and in vitro and in vivo changes of comprehensive alkaloids after oral administration are still little known...
March 21, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Mohamed A Farag, Amira R Khattab, Anja Ehrlich, Matthias Kropf, Andreas G Heiss, Ludger A Wessjohann
Lens culinaris and several Lupinus species are two legumes regarded as potential protein resources aside from their richness in phytochemicals. Characterization of their metabolite composition is warranted as a sustainable functional food. This study presents a discriminatory-holistic approach for metabolites profiling in accessions of four lentil cultivars and four lupinus species via gas chromatography-mass spectrometry. A total of 107 metabolites were identified encompassing organic and amino acids, sugars and sterols along with anti-nutrients viz...
March 21, 2018: Journal of Agricultural and Food Chemistry
Dieudonné Tshitenge Tshitenge, Doris Feineis, Virima Mudogo, Marcel Kaiser, Reto Brun, Ean-Jeong Seo, Thomas Efferth, Gerhard Bringmann
Four new dimeric naphthylisoquinoline alkaloids, michellamine A5 (2) and mbandakamines C-E (4-6), were isolated from the Congolese plant Ancistrocladus ealaensis, along with the known dimer mbandakamine A (3). They represent constitutionally unsymmetric dimers, each consisting of two 5,8'-coupled naphthylisoquinoline monomers. While the molecular halves of michellamine A5 (2) are linked via C-6' of both of the naphthalene moieties, i.e., via the least-hindered positions, so that the central biaryl axis is configurationally unstable and not an additional element of chirality, the mbandakamines 3-6 possess three consecutive stereogenic axes...
March 21, 2018: Journal of Natural Products
Ghulam Hussain, Azhar Rasul, Haseeb Anwar, Nimra Aziz, Aroona Razzaq, Wei Wei, Muhammad Ali, Jiang Li, Xiaomeng Li
Neurodegenerative diseases are conventionally demarcated as disorders with selective loss of neurons. Conventional as well as newer molecules have been tested but they offer just symptomatic advantages along with abundant side effects. The discovery of more compelling molecules that can halt the pathology of these diseases will be considered as a miracle of present time. Several synthetic compounds are available but they may cause several other health issues. Therefore, natural molecules from the plants and other sources are being discovered to replace available medicines...
2018: International Journal of Biological Sciences
Jin Liu, Yu Chen, Jing-Ya Li, Cheng Luo, Jia Li, Kai-Xian Chen, Xu-Wen Li, Yue-Wei Guo
Phidianidines A and B are two novel marine indole alkaloids bearing an uncommon 1,2,4-oxadiazole ring and exhibiting various biological activities. Our previous research showed that the synthesized phidianidine analogs had the potential to inhibit the activity of protein tyrosine phosphatase 1B (PTP1B), a validated target for Type II diabetes, which indicates that these analogs are worth further structural modification. Therefore, in this paper, a series of phidianidine derivatives were designed and rapidly synthesized with a function-oriented synthesis (FOS) strategy...
March 20, 2018: Marine Drugs
Subhajit Bhunia, Saikat Chaudhuri, Subhadip De, K Naresh Babu, Alakesh Bisai
The synthesis of the tetracyclic skeleton of ergot alkaloids has been developed via a key organocatalytic enantioselective aldol reaction using paraformaldehyde as the C1-unit in the presence of thiourea catalyst followed by a key Pd-catalyzed directed coupling accelerated by the DavePhos ligand. Utilizing the aforementioned strategy, we have synthesized a key tetracyclic intermediate in up to 95% ee with high yield.
March 20, 2018: Organic & Biomolecular Chemistry
Tianxiang Lei, Huan Wang, Songling Li, Jianwei Shen, Shilong Chen, Xiaojian Cai, Dangwei Zhou
To achieve a high yield of tropane alkaloids (TA) and exploit the alpine plant sustainably, an optimized protocol for induction and establishment of hairy roots culture of Prezwalskia tangutica Maxim was developed through selection of appropriate Agrobacterium strain and the explant type. The hypocotyl is more readily facile to induce the HR than the cotyledon is when infected with the three different agrobacterium strains. MUS440 has an efficiency (of up to 20%), whereas the ATCC10060 (A4) can induce HR on both types of explants with the highest frequency (33...
March 2018: 3 Biotech
Klara Habartova, Radim Havelek, Martina Seifrtova, Karel Kralovec, Lucie Cahlikova, Jakub Chlebek, Eva Cermakova, Nadezda Mazankova, Jana Marikova, Jiri Kunes, Lucie Novakova, Martina Rezacova
Scoulerine is an isoquinoline alkaloid, which indicated promising suppression of cancer cells growth. However, the mode of action (MOA) remained unclear. Cytotoxic and antiproliferative properties were determined in this study. Scoulerine reduces the mitochondrial dehydrogenases activity of the evaluated leukemic cells with IC50 values ranging from 2.7 to 6.5 µM. The xCELLigence system revealed that scoulerine exerted potent antiproliferative activity in lung, ovarian and breast carcinoma cell lines. Jurkat and MOLT-4 leukemic cells treated with scoulerine were decreased in proliferation and viability...
March 19, 2018: Scientific Reports
R Arunadevi, R Susila, S Murugammal, S Divya
BACKGROUND: Increasing popularity of Mathan Tailam (mattan tailam, pachai ennai) for the treatment of diabetic foot ulcer necessitated standardization and quality control of this medicated oil both in large scale production and quality check in marketed drug. OBJECTIVE: Present study aims to develop standard operating procedure for the preparation of Mathan Tailam as per Siddha Formulary of India and its standardization using suitable analytical techniques. MATERIALS AND METHODS: Mathan Tailam was prepared as per Siddha Formulary of India...
March 16, 2018: Journal of Ayurveda and Integrative Medicine
Mahendra Shukla, Femi M Francis, Jawahar Lal
Conessine, a steroidal alkaloid obtained from the bark and seeds of the plant species of Apocynaceae family, elicits a histamine antagonistic action, selectively for the H3 histaminergic receptors. This alkaloid is used mainly for the treatment of dysentery and helminthic disorders. For the quantification of conessine in serum, a liquid chromatography-tandem mass spectrometry method was developed. Chromatographic separation was achieved on a Zorbax SB-CN column (100 × 4.6 mm, 3.5 µm), and a mobile phase consisting of 90% methanol in aqueous ammonium acetate buffer (pH 3...
January 1, 2018: European Journal of Mass Spectrometry
Larisa K Shubina, Tatyana N Makarieva, Alla G Guzii, Vladimir A Denisenko, Roman S Popov, Pavel S Dmitrenok, Valentin A Stonik
The absolute configuration of the cytotoxic guanidine alkaloid monanchocidin A with 11 stereogenic centers from the marine sponge Monanchora pulchra was determined as 5 R, 8 S, 10 S, 13 R, 14 S, 15 R, 19 R, 23 R, 37 S, 42 S, 43 R after extensive reductive degradation and conversion of the resulting alcohols to MTPA derivatives.
March 19, 2018: Journal of Natural Products
Li-Li Qiu, Can Li, Shan-Shan Fan, Xu Han, Yong Yang, Rong Rong
To compare the quality difference between Mahuang Xixin Fuzi decoction(MXF) prepared by traditional decocting method and that prepared by two commonly used decocting methods, and explore the scientific nature of the traditional decocting method. By taking effect-toxic components in MXF as the research object, this article investigated these three different decocting methods from the quantitative determination of effect-toxic components in MXF. By using multivariate statistical analysis methods, three characteristic constituents were identified as kakoul, mesaconitine (MA) and hypaconitine (HA) respectively...
January 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Yu-Lan Liang, Xin Yang, Ling-Ling Pan, Ya-Fen Wu, Fei Li, Na Wan, Xiang Zhou, Bo Liu, Bin Li
Molecular imprinting technology is widely used in the separation and analysis of compounds such as flavonoids, alkaloids and polyphenols, due to its high selectivity and specific recognition and so on. However, no much of attention has been paid to the terpenoids. This paper is aimed to not only review the effects of common synthetic elements such as functional monomers, cross-linking agents and porogens on the polymer properties, but also highlight the application of terpene molecular imprinting in solid phase extraction, sensor, membrane separation and chromatographic separation by means of statistical analysis of literature...
January 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Bo-Yang Shang, Ping Yang, Li Chen, Xiao-Juan Gao, Jing-Jiao Yong, Xia Zhang, Jian-Jun Zhao, Han-Qing Wang
It was aimed at exploring the potential pharmacological effects of alkaloids in Sophora alopecuroides by means of network pharmacology in this study. The main alkaloids in S. alopecuroides were collected for analysis of drug properties, prediction of potential targets and screening of signaling pathways. DAVID analysis tool combined with KEGG database was used to annotate and analyze the signaling pathway. The alkaloids-targets-signaling pathways network was built through Cytoscape software. Results showed that 17 alkaloids in S...
January 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Yue Wei, Cui-Ping Zhang, Shuang Guo, Ke-Huan Lu, Xing Liu, Yi Yang, Zhi-Hua Liao, Neng-Biao Wu
Hyoscyamine and scopolamine are two main alkaloids in Atropa belladonna with great medicinal value. In this paper, the contents of hyoscyamine and scopolamine, the upstream products in alkaloid synthesis, and the expression levels of key enzyme genes PMT, TRⅠ and H6H in secondary metabolism of A. belladonna seedlings were measured to clarify the mechanism of nitrogen forms regulating alkaloids synthesis.The results showed that the 50/50 (NH⁺₄/NO⁻₃) treatment was more favorable for the accumulation of alkaloids and the conversion of hyoscyamine to scopolamine...
January 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Karla Soares-Weiser, John Rathbone, Yusuke Ogawa, Kiyomi Shinohara, Hanna Bergman
BACKGROUND: Antipsychotic (neuroleptic) medication is used extensively to treat people with chronic mental illnesses. Its use, however, is associated with adverse effects, including movement disorders such as tardive dyskinesia (TD) - a problem often seen as repetitive involuntary movements around the mouth and face. This review, one in a series examining the treatment of TD, covers miscellaneous treatments not covered elsewhere. OBJECTIVES: To determine whether drugs, hormone-, dietary-, or herb-supplements not covered in other Cochrane reviews on TD treatments, surgical interventions, electroconvulsive therapy, and mind-body therapies were effective and safe for people with antipsychotic-induced TD...
March 19, 2018: Cochrane Database of Systematic Reviews
Juan C Santos, Rebecca D Tarvin, Lauren A O'Connell, David C Blackburn, Luis A Coloma
Symbionts (e.g., endoparasites and commensals) play an integral role in their host's ecology, yet in many cases their diversity is likely underestimated. Although endoparasites are traditionally characterized using morphology, sequences of conserved genes, and shotgun metagenomics, host transcriptomes constitute an underused resource to identify these organisms' diversity. By isolating non-host transcripts from host transcriptomes, individual host tissues can now simultaneously reveal their endoparasite species richness (i...
March 15, 2018: Molecular Phylogenetics and Evolution
Guillermo Benítez, Martí March-Salas, Alberto Villa-Kamel, Ulises Cháves-Jiménez, Javier Hernández, Nuria Montes-Osuna, Joaquín Moreno-Chocano, Paloma Cariñanos
ETHNOPHARMACOLOGICAL RELEVANCE: The different species of the genus Datura have been used traditionally by some pre-Columbian civilizations, as well as in medieval rituals linked to magic and witchcraft in both Mexico and Europe. It is also noteworthy the use of different alkaloids obtained from the plants for medicinal purposes in the treatment of various groups of diseases, especially of the respiratory and muscularskeletal systems. AIM OF THE STUDY: A review of the ethnobotanical uses of the genus Datura in Mexico and Spain has been conducted...
March 15, 2018: Journal of Ethnopharmacology
Chen Geng, Tengfei Zhao, Chunxian Yang, Qiaozhuo Zhang, Feng Bai, Junlan Zeng, Fangyuan Zhang, Xiaoqiang Liu, Xiaozhong Lan, Min Chen, Zhihua Liao
N-methylputrescine is the precursor of nicotine and pharmaceutical tropane alkaloids such as hyoscyamine. Putrescine N-methyltransferase (PMT) catalyzes the N-methylation of putrescine to form N-methylputrescine. While the role of PMT in nicotine biosynthesis is clear, knowledge of PMT in the biosynthesis of tropane alkaloids (TAs) and the regulation of polyamines remains limited. We characterized a PMT gene from Hyoscyamus niger, designated HnPMT that was specifically expressed in roots, especially in the secondary roots and dramatically induced by methyl jasmonate (MeJA)...
March 2, 2018: Plant Physiology and Biochemistry: PPB
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