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Marine Drugs

Emily M Harris, Jonathan D Strope, Shaunna L Beedie, Phoebe A Huang, Andrew K L Goey, Kristina M Cook, Christopher J Schofield, Cindy H Chau, Melissa M Cadelis, Brent R Copp, Kirk R Gustafson, William D Figg
Elements of the hypoxia inducible factor (HIF) transcriptional system, a key regulator of the cellular hypoxic response, are up-regulated in a range of cancer cells. HIF is fundamentally involved in tumor angiogenesis, invasion, and energy metabolism. Inhibition of the transcriptional activity of HIF may be of therapeutic benefit to cancer patients. We recently described the identification of two marine pyrroloiminoquinone alkaloids with potent activity in inhibiting the interaction between the oncogenic transcription factor HIF-1α and the coactivator protein p300...
July 19, 2018: Marine Drugs
Michael Groll, Henry Nguyen, Sreekumar Vellalath, Daniel Romo
Upon acylation of the proteasome by the β-lactone inhibitor salinosporamide A (SalA), tetrahydrofuran formation occurs by intramolecular alkylation of the incipient alkoxide onto the choroethyl sidechain and irreversibly blocks the active site. Our previously described synthetic approach to SalA, utilizing a bioinspired, late-stage, aldol-β-lactonization strategy to construct the bicyclic β-lactone core, enabled synthesis of (⁻)-homosalinosporamide A (homoSalA). This homolog was targeted to determine whether an intramolecular tetrahydropyran is formed in a similar manner to SalA...
July 19, 2018: Marine Drugs
Lei Wang, WonWoo Lee, Jae Young Oh, Yong Ri Cui, BoMi Ryu, You-Jin Jeon
Our previous study evaluated the antioxidant activities of sulfated polysaccharides from Celluclast-assisted extract of Hizikia fusiforme (HFPS) in vitro in Vero cells and in vivo in zebrafish. The results showed that HFPS possesses strong antioxidant activity and suggested the potential photo-protective activities of HFPS. Hence, in the present study, we investigated the protective effects of HFPS against ultraviolet (UV) B-induced skin damage in vitro in human dermal fibroblasts (HDF cells). The results indicate that HFPS significantly reduced intracellular reactive oxygen species (ROS) level and improved the viability of UVB-irradiated HDF cells in a dose-dependent manner...
July 17, 2018: Marine Drugs
Jing-Ru Weng, Chang-Fang Chiu, Jing-Lan Hu, Chia-Hsien Feng, Chiung-Yao Huang, Li-Yuan Bai, Jyh-Horng Sheu
The peroxisome proliferator-activated receptor γ (PPARγ) is a nuclear receptor that plays a key role in regulating cellular metabolism, and is a therapeutic target for cancer therapy. To search for potential PPARγ activators, a compound library comprising 11 marine compounds was examined. Among them, a sterol, 3β,11-dihydroxy-9,11-secogorgost-5-en-9-one (compound 1 ), showed the highest PPARγ activity with an IC50 value of 8.3 μM for inhibiting human breast adenocarcinoma cell (MCF-7) growth. Western blotting experiments showed that compound 1 induces caspase activation and PARP cleavage...
July 17, 2018: Marine Drugs
Ana M L Seca, Diana C G A Pinto
Hypertension and obesity are two significant factors that contribute to the onset and exacerbation of a cascade of mechanisms including activation of the sympathetic and renin-angiotensin systems, oxidative stress, release of inflammatory mediators, increase of adipogenesis and thus promotion of systemic dysfunction that leads to clinical manifestations of cardiovascular diseases. Seaweeds, in addition to their use as food, are now unanimously acknowledged as an invaluable source of new natural products that may hold noteworthy leads for future drug discovery and development, including in the prevention and/or treatment of the cardiovascular risk factors...
July 14, 2018: Marine Drugs
Florbela Pereira, Joao Aires-de-Sousa
Computational methodologies are assisting the exploration of marine natural products (MNPs) to make the discovery of new leads more efficient, to repurpose known MNPs, to target new metabolites on the basis of genome analysis, to reveal mechanisms of action, and to optimize leads. In silico efforts in drug discovery of NPs have mainly focused on two tasks: dereplication and prediction of bioactivities. The exploration of new chemical spaces and the application of predicted spectral data must be included in new approaches to select species, extracts, and growth conditions with maximum probabilities of medicinal chemistry novelty...
July 13, 2018: Marine Drugs
Raúl E Cian, Cristina Hernández-Chirlaque, Reyes Gámez-Belmonte, Silvina R Drago, Fermín Sánchez de Medina, Olga Martínez-Augustin
Hydrolysates of food protein sources have immunomodulatory effects, which are of interest for use as functional foods. In this study, we have characterized the immune regulatory effect on rat splenocytes, macrophages and T lymphocytes of Ulva spp. hydrolysates and their peptide fractions with or without in vitro gastrointestinal digestion and/or ultrafiltration. IL-10 was induced in almost all conditions and cell types obtained from wild type animals. The induction was in general increased by ultrafiltration and in vitro gastrointestinal digestion...
July 11, 2018: Marine Drugs
Melissa Desnoyers, Kim Gilbert, Guy Rousseau
The high-fat diet of North Americans has a major impact on cardiovascular disease occurrence. Notably, fatty acids have been identified as important factors that could modulate such diseases, especially myocardial infarction (MI). Experimentally, omega-3 polyunsaturated fatty acids (PUFA) have demonstrated positive effects on cardiovascular disorders and have also shown cardioprotection by decreasing MI size. Although many animal experiments have clearly established the benefits of omega-3 PUFA, clinical studies have not reached similar conclusions...
July 10, 2018: Marine Drugs
Ariana A Vasconcelos, Vitor H Pomin
The oceans harbor a great diversity of organisms, and have been recognized as an important source of new compounds with nutritional and therapeutic potential. Among these compounds, carbohydrate-based compounds are of particular interest because they exhibit numerous biological functions associated with their chemical diversity. This gives rise to new substances for the development of bioactive products. Many are the known applications of substances with glycosidic domains obtained from marine species. This review covers the structural properties and the current findings on the antioxidant, anti-inflammatory, anticoagulant, antitumor and antimicrobial activities of medium and high molecular-weight carbohydrates or glycosylated compounds extracted from various marine organisms...
July 9, 2018: Marine Drugs
Elena V Ivanets, Anton N Yurchenko, Olga F Smetanina, Anton B Rasin, Olesya I Zhuravleva, Mikhail V Pivkin, Roman S Popov, Gunhild von Amsberg, Shamil Sh Afiyatullov, Sergey A Dyshlovoy
Four new indole-diterpene alkaloids asperindoles A⁻D ( 1 ⁻ 4 ) and the known p -terphenyl derivative 3″-hydroxyterphenyllin ( 5 ) were isolated from the marine-derived strain of the fungus Aspergillus sp., associated with an unidentified colonial ascidian. The structures of 1 ⁻ 5 were established by 2D NMR and HRESIMS data. The absolute configurations of all stereocenters of 1 ⁻ 4 were determined by the combination of ROESY data, coupling constants analysis, and biogenetic considerations. Asperindoles C and D contain a 2-hydroxyisobutyric acid (2-HIBA) residue, rarely found in natural compounds...
July 9, 2018: Marine Drugs
Jun Zhang, Zhiqiang Yang, Yan Liang, Liping Zhong, Huiting Lin, Balian Zhong, Liangchun Li, Shihai Xu, Yonghong Liu
Four new structurally related metabolites, one γ-lactone named gliomasolide F ( 1 ), one δ-lactone named gliomasolide G ( 2 ), and two medium-chain fatty acids named gliomacids A⁻B ( 3 ⁻ 4 ), each containing nine carbons in total, were identified from the sponge-associated fungus Gliomastix sp. ZSDS1-F7-2. The planar chemical structures of these novel C9 metabolites were elucidated by nuclear magnetic resonance (NMR) spectroscopic methods, in connection with the analysis of high-resolution mass spectrometry (HRMS) and infrared (IR) data...
July 9, 2018: Marine Drugs
Qing Zhang, Beiye Yang, Fengli Li, Mengting Liu, Shuang Lin, Jianping Wang, Yongbo Xue, Hucheng Zhu, Weiguang Sun, Zhengxi Hu, Yonghui Zhang
Mycophenolic acid (MPA) is a potent inosine-5′-monophosphate dehydrogenase (IMPDH) inhibitor for immunosuppressive chemotherapy. Most importantly, as the 2-morpholinoethyl ester prodrug of MPA, mycophenolate mofetil (MMF) is a well-known immunosuppressant used to prevent rejection in organ transplantations. Nevertheless, due to its frequently occurred side effects, searching for new therapeutic agents is ongoing. In our current work, by virtue of efficient bioassay-guided fractionation and purification, eleven mycophenolic acid derivatives, including five previously unreported metabolites ( 3 ⁻ 7 ) and six known compounds ( 1 , 2 , and 8 ⁻ 11 ), were obtained from the coral-derived fungus Penicillium bialowiezense ...
July 7, 2018: Marine Drugs
Dong-Lan Wu, Hou-Jin Li, Duncan R Smith, Janejira Jaratsittisin, Xia-Fu-Kai-Ti Xia-Ke-Er, Wen-Zhe Ma, Yong-Wei Guo, Jun Dong, Juan Shen, De-Po Yang, Wen-Jian Lan
In our continuous chemical investigation on the marine-derived fungus Dichotomomyces cejpii F31-1, two new polyketides dichocetides B-C ( 1 , 2 ), two new alkaloids dichotomocejs E-F ( 3 , 4 ), and three known fumiquinozalines: scequinadoline A ( 5 ), quinadoline A ( 6 ), and scequinadoline E ( 7 ) were discovered from the culture broth and the mycelium in the culture medium, by the addition of l-tryptophan and l-phenylalanine. Their chemical structures were established by one dimensional (1D), two dimensional (2D) nuclear magnetic resonance (NMR) and high resolution mass spectrometry (HR-MS) data...
July 6, 2018: Marine Drugs
Junde Chen, Ying Liu, Guangyu Wang, Shanshan Sun, Rui Liu, Bihong Hong, Ran Gao, Kaikai Bai
Hypertension can cause coronary heart disease. Synthetic angiotensin-converting enzyme (ACE) inhibitors are effective antihypertensive drugs but often cause side effects. The aim of this study was to prepare potential ACE inhibitors from scales. Gelatin was extracted from lizardfish scales. Then, scale gelatin was enzymolyzed to prepare ACE inhibitory peptides using response surface methodology. Proteolytic conditions after optimization were as follows: pH 7.0, enzyme substrate ratio 3.2%, temperature 47 °C, and proteolysis lasting 2 h and 50 min...
July 4, 2018: Marine Drugs
Ignacio Abreu Castilla, David F Woods, F Jerry Reen, Fergal O'Gara
In a demanding commercial world, large-scale chemical processes have been widely utilised to satisfy consumer related needs. Chemical industries are key to promoting economic growth and meeting the requirements of a sustainable industrialised society. The market need for diverse commodities produced by the chemical industry is rapidly expanding globally. Accompanying this demand is an increased threat to the environment and to human health, due to waste produced by increased industrial production. This increased demand has underscored the necessity to increase reaction efficiencies, in order to reduce costs and increase profits...
July 4, 2018: Marine Drugs
Junjun Meng, Wei Cheng, Hajar Heydari, Bin Wang, Kui Zhu, Belma Konuklugil, Wenhan Lin
Antibacterial activity assessment and high performance liquid chromatography associated with nuclear magnetic resonance (HPLC/NMR) data revealed that the EtOAc extract of the fermented endophytic fungus Trichoderma saturnisporum DI-IA, obtained from the marine sponge Dictyonella incisa , contained conjugated olefinic metabolites with antibacterial activity. Chemical examination of the fungal strain resulted in the isolation of eight new sorbicillinoid-based compounds, namely saturnispols A⁻H ( 1 ⁻ 8 ). Their structures were determined on the basis of extensive spectroscopic analysis, including the experimental and calculated electronic circular dichroism (ECD) data for the configurational assignments...
July 4, 2018: Marine Drugs
Innocent J Macha, Besim Ben-Nissan
Musculoskeletal disorders in the elderly have significantly increased due to the increase in an ageing population. The treatment of these diseases necessitates surgical procedures, including total joint replacements such as hip and knee joints. Over the years a number of treatment options have been specifically established which are either permanent or use temporary natural materials such as marine skeletons that possess unique architectural structure and chemical composition for the repair and regeneration of bone tissue...
July 2, 2018: Marine Drugs
Mari Yotsu-Yamashita, Yuuma Nagaoka, Koji Muramoto, Yuko Cho, Keiichi Konoki
Pufferfish saxitoxin and tetrodotoxin (TTX) binding protein (PSTBP) is a glycoprotein that we previously isolated from the blood plasma of the pufferfish Takifugu pardalis ; this protein was also detected in seven species of the genus Takifugu . We proposed that PSTBP is a carrier protein for TTX in pufferfish; however, PSTBP had not yet been found in genera other than Takifugu . In this study, we investigated the presence of PSTBP-like proteins in the toxic pufferfish Arothron nigropunctatus , A. hispidus , A...
June 29, 2018: Marine Drugs
Takeshi Yamada, Tetsuya Kajimoto, Takashi Kikuchi, Reiko Tanaka
As part of research to search for antitumor agents in fungi originating from marine organisms, cephalimysins E⁻L were isolated from a culture broth of Aspergillus fumigatus that was separated from the marine fish Mugil cephalus . One- and two-dimensional nuclear magnetic resonance spectra revealed their planar structures, which are diastereomers of each other. Their absolute stereostructures were established by epimerization at C-8 with acidic methanol, nuclear Overhauser effect spectroscopy (NOESY), and circular dichroism (CD) spectroscopy...
June 29, 2018: Marine Drugs
Yunping Tang, Shujie Jin, Xiaoyan Li, Xiaojuan Li, Xuyang Hu, Yan Chen, Fangfang Huang, Zuisu Yang, Fangmiao Yu, Guofang Ding
Collagen and collagen peptides are widely used as cosmetic ingredients. In the present study, acid-solubilized collagen (ASC) and pepsin-solubilized collagen (PSC) were extracted from giant croaker ( Nibea japonica ) skin. The proline hydroxylation rates of ASC and PSC were 38.1% and 39.3%. The denaturation temperatures (Td ) were approximately 34.5 °C for both ASC and PSC. The results of sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) and fourier transform infrared spetroscopy (FTIR) demonstrated that ASC and PSC were mainly type I collagen...
June 29, 2018: Marine Drugs
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