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Arylation of sulfhydryl groups in vitro by the naturally occurring sesquiterpenoid benzoquinone avarone.

Avarone (AQ) is a naturally occurring sesquiterpenoid benzoquinone possessing antileukaemic activity. Its reactivity towards glutathione (GSH) and protein sulfhydryl (SH) groups was investigated. The stoichiometry of AQ reaction with GSH at [GSH]/[AQ] ratios lower than unity proved to be 1:2 (thiol:quinone), consistent with the formation of the corresponding hydroquinone (avarol) as well as a quinone-thioether in the reaction. Conversely, when the [GSH]/[AG] ratio was higher than unity, a hydroquinone-thioether was the only reaction product. AQ/protein interaction was also investigated by usin

Cyclic peroxides and analogs: Antibacterial, antimalarial, and cytotoxic marine products from Xisha sponge Diacarnus sp.

A chemical investigation of the dichloromethane extract from the Xisha sponge Diacarnus sp. revealed seven undescribed norterpene cyclic peroxides, named diacarperoxides T-Z, and five unreported related norterpenes, named diacarnoids E-I, and eleven previously reported compounds. The structures of these isolated compounds, including their absolute configurations, were elucidated based on extensive spectroscopic analyses, electronic circular dichroism (ECD) calculations, Snatzke's method, [Rh2(OCOCF3)4]-induced ECD spectra, and modified Mosher's method. Bioassays were performed to assess the an

Cloning, recombinant expression and biochemical characterisation of novel esterases from Bacillus sp. associated with the marine sponge Aplysina aerophoba.

Two novel esterases (EstB1 and EstB2) were isolated from a genomic library of Bacillus sp. associated with the marine sponge Aplysina aerophoba. EstB1 shows low identity (26-44%) with the published hydrolases of the genus Bacillus, whereas EstB2 shows high identity (73-74%) with the carboxylesterases from B. cereus and B. anthracis. Both esterases were efficiently expressed in Escherichia coli under the control of T7 promoter using the vector pET-22b(+). Recombinant EstB1 was purified in a single step to electrophoretic homogeneity by IMAC. A method for the refolding of inclusion bodies formed

Modulatory effect of bolinaquinone, a marine sesquiterpenoid, on acute and chronic inflammatory processes.

The marine metabolite bolinaquinone is a novel inhibitor of secretory phospholipase A(2) (sPLA(2)), with a potency on the human synovial enzyme (group II) higher than that of manoalide. This activity on the sPLA(2) was confirmed in vivo in the 8-h zymosan rat air pouch on the secretory enzyme accumulation in the pouch exudate. Additionally, bolinaquinone decreased potently the synthesis and release of leukotriene B(4) (LTB(4)) in calcimycin (A23187)-stimulated human neutrophils as a consequence of the inhibition of 5-lipoxygenase activity, as well as PGE(2) and NO production on zymosan-stimula

The neurologic effects of noxious marine creatures.

The concept of the sea as a source of noxious agents is perhaps not a familiar one to clinical neurologists, judging by the lack of reference to these agents in standard textbooks. Chemical, physiologic, and pharmacologic laboratories are increasingly investigating the properties of marine toxins, finding in them compounds with interesting and novel structures or unusual physiologic effects. Such substances are seen as possible agents for biologic and, more particularly, physiologic research, and as possible sources of new pharmaceuticals. These include hormone-like substances and antiviral or

Latrunculin-A causes mydriasis and cycloplegia in the cynomolgus monkey.

PURPOSE: To determine the effect of latrunculin (LAT)-A, which binds to G-actin and disassembles actin filaments, on the pupil, accommodation, and isolated ciliary muscle (CM) contraction in monkeys. METHODS: Pupil diameter (vernier calipers) and refraction (coincidence refractometry) were measured every 15 minutes from 0.75 to 3.5 hours after topical LAT-A 42 microg (approximately 10 microM in the anterior chamber [AC]). Refraction was measured every 5 minutes from 0.5 to 1.5 hours after intracameral injection of 10 microl of 50 microM LAT-A (approximately 5 microM in AC), with intramuscular

Penicillium chrysogenum DSOA associated with marine sponge (Tedania anhelans) exhibit antimycobacterial activity.

A strain of Penicillium chrysogenum was isolated from Tedania anhelans (marine sponge) collected from Indian Ocean (8°22'30″N latitude and 76°59'16″ longitude) and deposited in culture collection centers. The strain subjected to different culture conditions for production of extrolites were extracted using ethyl acetate and chloroform. When both extracts were subjected for antibacterial activity, latter had high activity. Minimum inhibitory concentration of chloroform extract ranged from 31.25-1000 μg/mL in tested microbes such as, Mycobacterium tuberculosis H37Ra, Mycobacterium avium, Mycobac

Mapacalcine protects mouse neurons against hypoxia by blocking cell calcium overload.

Stroke is one of a major cause of death and adult disability. Despite intense researches, treatment for stroke remains reduced to fibrinolysis, a technique useful for less than 10% of patients. Finding molecules able to treat or at least to decrease the deleterious consequences of stroke is an urgent need. Here, we showed that mapacalcine, a homodimeric peptide purified from the marine sponge Cliona vastifica, is able to protect mouse cortical neurons against hypoxia. We have also identified a subtype of L-type calcium channel as a target for mapacalcine and we showed that the channel has to b

Discodermolide, a cytotoxic marine agent that stabilizes microtubules more potently than taxol.

Computer-assisted structure analysis indicated (+)-discodermolide, a polyhydroxylated alkatetraene lactone marine natural product, was an antimitotic compound, and we confirmed this prediction. Previous work had shown an accumulation of discodermolide-treated cells in the G2/M portion of the cell cycle, and we have now found that discodermolide arrests Burkitt lymphoma cells in mitosis. Discodermolide-treated breast carcinoma cells displayed spectacular rearrangement of the microtubule cytoskeleton, including extensive microtubule bundling. Microtubule rearrangement that occurred with 10 nM di

Latrunculin-A increases outflow facility in the monkey.

PURPOSE: To determine the effect of Latrunculin (LAT)-A, a macrolide that binds to G-actin, which leads to the disassembly of actin filaments, on shape, junctions, and the cytoskeleton of cultured bovine aortic endothelial cells (BAECs) and on outflow facility in living monkeys. METHODS: Latrunculin-A dose-time-response relationships in BAECs were determined by immunofluorescence and phase contrast light microscopy, facility by two-level constant pressure anterior chamber perfusion. RESULTS: In BAECs, LAT-A caused dose- and incubation time- dependent destruction of actin bundles, cell separa

Олептические рецепторы в нейронной регенерации в центральной нервной системе.

Олептические рецепторы имеют решающее значение для обнаружения запахов и играют жизненно важную роль в нашем чувстве запаха, оказывая влияние на поведение, начиная от выбора пищи и кончая эмоциональными воспоминаниями. Эти рецепторы также способствуют нашему восприятию вкуса и могут применяться в медицинской диагностике и экологическом мониторинге. Способность обонятельной системы регенерировать свои сенсорные нейроны обеспечивает уникальную модель для изучения нейронной регенерации — явления, которое в основном отсутствует в центральной нервной системе. Понимание, полученное благодаря тому, к

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… Porifera and Ctenophora, which appeared later in evolutionary terms, also lack apparent orthologs of mammalian olfactory receptors (Krishnan et al., 2014). … However, evidence has not led studies aimed at confirming whether the gene in sponges (Porifera) is coding a protein able to act like olfactory receptors. …

An Updated Review on Marine Anticancer Compounds: The Use of Virtual Screening for the Discovery of Small-Molecule Cancer Drugs.

Marine secondary metabolites are a promising source of unexploited drugs that have a wide structural diversity and have shown a variety of biological activities. These compounds are produced in response to the harsh and competitive conditions that occur in the marine environment. Invertebrates are considered to be among the groups with the richest biodiversity. To date, a significant number of marine natural products (MNPs) have been established as antineoplastic drugs. This review gives an overview of MNPs, both in research or clinical stages, from diverse organisms that were reported as bein

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… They found that approximately 80% were into the phyla Porifera (47.1%) and Cnidaria (33.5%). The rest of them were in the phyla Echinodermata (7.4%), Chordata (6.0%), and Mollusca (5.0%). … They also compared the MNPs by chemical group and demonstrated that in the Porifera or Cnidaria phyla, a particular chemical group was not always prevalent through the same phylum [ 47 ]. …

Promising Activities of Marine Natural Products against Hematopoietic Malignancies.

According to the WHO classification of tumors, more than 150 typologies of hematopoietic and lymphoid tumors exist, and most of them remain incurable diseases that require innovative approaches to improve therapeutic outcome and avoid side effects. Marine organisms represent a reservoir of novel bioactive metabolites, but they are still less studied compared to their terrestrial counterparts. This review is focused on marine natural products with anticancer activity against hematological tumors, highlighting recent advances and possible perspectives. Until now, there are five commercially avai

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… Among the marine organism phyla tested, there were Annelida, Bryozoa, Chlorophyta, Chordata, Cnidaria, Cyanophyta, Echinodermata, Mollusca, Phaeophyta, Porifera, Rhodophyta, and Tracheophyta (Mangrove), and 620 of 9945 organisms were found to have anti-leukemia properties (an extract was considered “ … Even though most of the active extracts did not exhibit selectivity for the leukemia cell lines and showed varying levels of cytotoxicity against other cancer cell lines (e.g., colon, central nervous system, and breast), some Porifera demonstrated selective activity against leukemia cell lines. …

Biotechnological Innovations from Ocean: Transpiring Role of Marine Drugs in Management of Chronic Disorders.

Marine drugs are abundant in number, comprise of a diverse range of structures with corresponding mechanisms of action, and hold promise for the discovery of new and better treatment approaches for the management of several chronic diseases. There are huge reserves of natural marine biological compounds, as 70 percent of the Earth is covered with oceans, indicating a diversity of chemical entities on the planet. The marine ecosystems are a rich source of bioactive products and have been explored for lead drug molecules that have proven to be novel therapeutic targets. Over the last 70 years, m

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… Sponges belonging to the phylum Porifera , are the oldest and most prolific marine organisms on the planet. Demospongiae, a class of Porifera , account for 83% of the species with the highest number of bioactive compounds [ 8 ]. …

A Small Dibromotyrosine Derivative Purified From Pseudoceratina Sp. Suppresses TGF-β Responsiveness by Inhibiting TGF-β Type I Receptor Serine/Threonine Kinase Activity.

For clinical application, there is a great need for small-molecule inhibitors (SMIs) that could control pathogenic effects of transforming growth factor (TGF-β) and/or modulate effects of TGF-β in normal responses. Selective SMIs of the TGF-β signaling pathway developed for therapeutics will also be powerful tools in experimentally dissecting this complex pathway, especially its cross-talk with other signaling pathways. In this study, we characterized (1'R,5'S,6'S)-2-(3',5'-dibromo-1',6'-dihydroxy-4'-oxocyclohex-2'-enyl) acetonitrile (DT), a member of a new class of small-molecule inhibitors r

Potential Approaches Versus Approved or Developing Chronic Myeloid Leukemia Therapy.

Tyrosine kinase inhibitors (TKIs) have revolutionized the treatment of patients with chronic myeloid leukemia (CML). However, continued use of these inhibitors has contributed to the increase in clinical resistance and the persistence of resistant leukemic stem cells (LSCs). So, there is an urgent need to introduce additional targeted and selective therapies to eradicate quiescent LSCs, and to avoid the relapse and disease progression. Here, we focused on emerging BCR-ABL targeted and non-BCR-ABL targeted drugs employed in clinical trials and on alternative CML treatments, including antioxidan

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… Data showed that different phyla, including Annelida, Bryozoa, Chlorophyta, Chordata, Cnidaria, Cyanophyta, Echinodermata, Mollusca, Phaeophyta, Porifera, Rhodophyta and Tracheophyta (Mangrove) and 620/9945 extracts had antileukemia properties. … Among the screened organisms, Porifera showed selectivity against leukemia cell lines ( 134 ). Regarding the purified compounds from sponges with activity against CML, there are gombamide A, compound 1-8, Lembehyne B, Heteronemin, Smenospongine, Aaptamine, chujamides A and B ( 135 – 142 ). …

Полимеризация тубулинов, пропагандирующая протеины: функциональное разнообразие с последствиями в неврологических расстройствах.

Полимеризация тубулинов, пропагандирующая протеины (ПППН), в значительной степени сохраняется в различных видах, но по-прежнему недостаточно изучена. В организме человека есть три гена ТППЦ, и только один гомологический ген ТППЦ у беспозвоночных, таких как Дрософила и К. Элеган. TPPP человека (TPPP1/p25/p25α) обогащается в мозгу и имеет сходство с беспозвоночными TPPP. TPPP/p25 ассоциируется с микротубулями и играет ключевую роль в динамике микротубуля, слиянии и полимеризации, тем самым стабилизируя микротубулярную сеть. Это крайне важно для организации цитоскелета и надлежащего функционирова

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… TPPP is conserved across all major animal phyla from Porifera to vertebrates highlighting its essential biological functions during animal evolution. Multiple sequence alignment of TPPP‐family proteins across diverse species. …