Identification of ABA Receptor Using a Multiplexed Chemical Screening

Diseases mediated by the immune system are difficult problems to treat such as human immunodeficiency virus (HIV) and other lethal viruses. Infections that occur in normal people are generally brief and rarely leave permanent damage. Treatment of this disease requires an aggressive and innovative approach to the development of new treatments so that it requires the role of immunomodulators to improve the immune system. A substance that acts as an enhancer or immune enhancer can be obtained by using herbs that are efficacious as immunostimulants. One of the herbs used is herbal binara (Artemisia vulgaris L) which has been studied as a potential immunomodulator with high antioxidant activity. Previous research also stated that red shoots (Syzygium oleana) were studied as potential immunomodulators with high antioxidant activity. Several other species such as Syzygium samarangense have 16 flavonoida compounds which show pharmacological immunological activity. The purpose of this study was to determine the content of secondary metabolites of ethanol extract of herbal binara (Artemisia vulgaris L.) with red shoots (Syzygium oleana) and to determine the best dose of extract from the ethanol extract of herbal binara (Artemisia vulgaris L.) with red shoots (Syzygium oleana) can reduce the volume of swelling of mouse feet. Examination of the chemical content of secondary metabolites from the ethanol extract of herbal binara (Artemisia vulgaris L.) with red shoots (Syzygium oleana) is carried out by chemical screening and characterization of simplicia and extract. The method used is the slow type hypersensitivity method. In this test the independent variable is the secondary metabolite of ethanol extract of herb binara (Artemisia vulgaris L.) with red shoots (Syzygium oleana) with four concentrations (50, 100, 200 and 400 mg / kgBB). The positive control used by Stimuno dose is 32.5 mg / kgBB

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Investigation of Compounds and Biological Activity of Selected Indonesian Marine Sponges

The Natural Products Journal ◽

10.2174/2210315509666190627105237 ◽

2020 ◽

Vol 10 (3) ◽

pp. 312-321

Author(s):

Idin Sahidin ◽

Carla W. Sabandar ◽

Wahyuni ◽

Rini Hamsidi ◽

Sandra Aulia Mardikasari ◽

...

Keyword(s):

Biological Activity ◽

Antioxidant Activities ◽

Chemical Constituents ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Marine Sponges ◽

Chemical Screening ◽

Methanol Extracts ◽

Ms Analysis ◽

Antioxidant Agents

Background: Marine sponges provided a great source of natural products with promising biological activity. This study was aimed to investigate the chemical constituents of methanol extracts of selected Indonesian marine sponges (Callyspongia sp., Clathria sp., Melophlus sarasinorum, and Xestospongia sp.), collected from the Saponda Islands, Southeast Sulawesi, Indonesia as well as to evaluate their antimicrobial and antioxidant activities. Methods: LCMS/MS analysis used to identify the compounds. Agar well diffusion and DPPH assays were used to evaluate the antimicrobial and antioxidant activities. Results: Chemical screening reported alkaloids, terpenoids, steroids, and saponins from all investigated sponges. The LC-MS/MS analysis identified various compounds which mainly contained steroids. Antimicrobial activity (against Bacillus subtilis, Escherichia coli, Salmonella enterica, and Candida albicans) was only shown by the Xestospongia sp. extract. Meanwhile, extracts of M. sarasinorum, Xestospongia sp., and Callyspongia sp. exhibited potent radical scavenging activity. Conclusion: The study concluded that the selected sponges could provide various groups of compounds. Methanol extracts of these sponges could be used as sources of antimicrobial and antioxidant agents.

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Druggable Transient Pockets in Protein Kinases

Molecules ◽

10.3390/molecules26030651 ◽

2021 ◽

Vol 26 (3) ◽

pp. 651

Author(s):

Koji Umezawa ◽

Isao Kii

Keyword(s):

Drug Discovery ◽

Small Molecules ◽

Protein Kinases ◽

Binding Sites ◽

Kinase Inhibitors ◽

Screening Methods ◽

Research Attention ◽

Folding Process ◽

Chemical Screening ◽

Inhibitory Mechanisms

Drug discovery using small molecule inhibitors is reaching a stalemate due to low selectivity, adverse off-target effects and inevitable failures in clinical trials. Conventional chemical screening methods may miss potent small molecules because of their use of simple but outdated kits composed of recombinant enzyme proteins. Non-canonical inhibitors targeting a hidden pocket in a protein have received considerable research attention. Kii and colleagues identified an inhibitor targeting a transient pocket in the kinase DYRK1A during its folding process and termed it FINDY. FINDY exhibits a unique inhibitory profile; that is, FINDY does not inhibit the fully folded form of DYRK1A, indicating that the FINDY-binding pocket is hidden in the folded form. This intriguing pocket opens during the folding process and then closes upon completion of folding. In this review, we discuss previously established kinase inhibitors and their inhibitory mechanisms in comparison with FINDY. We also compare the inhibitory mechanisms with the growing concept of “cryptic inhibitor-binding sites.” These sites are buried on the inhibitor-unbound surface but become apparent when the inhibitor is bound. In addition, an alternative method based on cell-free protein synthesis of protein kinases may allow the discovery of small molecules that occupy these mysterious binding sites. Transitional folding intermediates would become alternative targets in drug discovery, enabling the efficient development of potent kinase inhibitors.

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