scholarly journals Inhibitory Activity of Marine Sponge-Derived Natural Products against Parasitic Protozoa

Marine Drugs ◽  
2010 ◽  
Vol 8 (1) ◽  
pp. 47-58 ◽  
Author(s):  
Ilkay Orhan ◽  
Bilge Şener ◽  
Marcel Kaiser ◽  
Reto Brun ◽  
Deniz Tasdemir
Keyword(s):  
Natural Products ◽  
Marine Sponge ◽  
Inhibitory Activity ◽  
Parasitic Protozoa

scholarly journals Total Synthesis of Phorbazole B

Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4848
Author(s):  
Yngve Guttormsen ◽  
Magnus E. Fairhurst ◽  
Sunil K. Pandey ◽  
Johan Isaksson ◽  
Bengt Erik Haug ◽  
...  
Keyword(s):  
Natural Products ◽  
High Resolution ◽  
Secondary Metabolites ◽  
Total Synthesis ◽  
Cancer Cells ◽  
Marine Sponge ◽  
Inhibitory Activity ◽  
Late Stage ◽  
Nmr Techniques

Phorbazoles are polychlorinated heterocyclic secondary metabolites isolated from a marine sponge and several of these natural products have shown inhibitory activity against cancer cells. In this work, a synthesis of the trichlorinated phorbazole B using late stage electrophilic chlorination was developed. The synthesis relied on the use of an oxazole precursor, which was protected with an iodine in the reactive 4-position, followed by complete chlorination of all pyrrole positions. Attempts to prepare phorbazole A and C, which contain a 3,4-dichlorinated pyrrole, were unsuccessful as the desired chlorination pattern on the pyrrole could not be obtained. The identities of the dichlorinated intermediates and products were determined using NMR techniques including NOESY/ROESY, 1,1-ADEQUATE and high-resolution CLIP-HSQMBC.

scholarly journals Antiglycation potential of Indigoferin a, Indigoferin B and Indigoferin C natural products from Indigofera heterantha Brandis

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Ayesha Khan ◽  
Ajmal Khan ◽  
Manzoor Ahmad ◽  
Mumtaz Ali ◽  
Umar Farooq ◽  
...  
Keyword(s):  
Natural Products ◽  
Diabetic Complications ◽  
Inhibitory Activity ◽  
Chemical Constituents ◽  
Intramolecular Hydrogen Bonding ◽  
Glycation End Products ◽  
End Products ◽  
Serious Disease ◽  
Intramolecular Hydrogen

Abstract Background Diabetes is a long-lasting and serious disease that effect in worldwide individual lives, families, and societies. Hyperglycemia of diabetes mellitus produced Advance Glycation End Products that are associated with diabetic complications like neuropathy, nephropathy, retinopathy, and cardiovascular diseases. Methods In this study, the natural products isolated from of Indigofera heterantha Brandis, Indigoferin A (S1), Indigoferin B (S2) and Indigoferin C (S3) were evaluated for their in vitro antiglycation activity. Results The compounds exhibited a significant inhibitory activity against the formation of Advanced Glycation End-Products with IC50 values of 674.25 ± 3.2 μM, 407.03 ± 4.7 μM and 726.41 ± 2.1 μM, respectively. Here, important structure-activity relationship was observed, when the intramolecular hydrogen bonding interactions suppressed the antiglycation activity of compound S3. Thus, the study clearly demonstrates that the number and the position of substituents act as an assisting factor and directly influence the inhibitory activity of the natural product by altering the sugar or protein binding affinity. Conclusions This study explain first time the antiglycation inhibitory ability of chemical constituents isolated from I. heterantha and can be used for above late diabetic complications.

scholarly journals New Mammalian Target of Rapamycin (mTOR) Modulators Derived from Natural Product Databases and Marine Extracts by Using Molecular Docking Techniques

Marine Drugs ◽  
2018 ◽  
Vol 16 (10) ◽  
pp. 385 ◽  
Author(s):  
Verónica Ruiz-Torres ◽  
Maria Losada-Echeberría ◽  
Maria Herranz-López ◽  
Enrique Barrajón-Catalán ◽  
Vicente Galiano ◽  
...  
Keyword(s):  
Natural Products ◽  
Molecular Docking ◽  
Side Effects ◽  
Inhibitory Activity ◽  
Mammalian Target Of Rapamycin ◽  
Therapeutic Use ◽  
Cellular Growth ◽  
Target Of Rapamycin ◽  
Computational Techniques ◽  
Chemical Derivatives

Mammalian target of rapamycin (mTOR) is a PI3K-related serine/threonine protein kinase that functions as a master regulator of cellular growth and metabolism, in response to nutrient and hormonal stimuli. mTOR functions in two distinct complexes—mTORC1 is sensitive to rapamycin, while, mTORC2 is insensitive to this drug. Deregulation of mTOR’s enzymatic activity has roles in cancer, obesity, and aging. Rapamycin and its chemical derivatives are the only drugs that inhibit the hyperactivity of mTOR, but numerous side effects have been described due to its therapeutic use. The purpose of this study was to identify new compounds of natural origin that can lead to drugs with fewer side effects. We have used computational techniques (molecular docking and calculated ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity) parameters) that have enabled the selection of candidate compounds, derived from marine natural products, SuperNatural II, and ZINC natural products, for inhibitors targeting, both, the ATP and the rapamycin binding sites of mTOR. We have shown experimental evidence of the inhibitory activity of eleven selected compounds against mTOR. We have also discovered the inhibitory activity of a new marine extract against this enzyme. The results have been discussed concerning the necessity to identify new molecules for therapeutic use, especially against aging, and with fewer side effects.

The Role of Aromatase Enzyme in Hormone Related Diseases and Plant-Based Aromatase Inhibitors as Therapeutic Regimens

2021 ◽  
Vol 21 ◽  
Author(s):  
Kevser Taban Akça ◽  
Murside Ayşe Demirel ◽  
Ipek Süntar
Keyword(s):  
Natural Products ◽  
Aromatase Inhibitors ◽  
Inhibitory Activity ◽  
Chemical Compounds ◽  
Synthesis Methods ◽  
Herbal Drugs ◽  
Drug Discovery And Development ◽  
History Of ◽  
History Of Use

: Medicinal plants have a long history of use as food and remedy in traditional and modern societies, as well as have been used as herbal drugs and sources of novel bioactive compounds. They provide a wide array of chemical compounds, many of which can not be synthesized via current synthesis methods. Natural products may provide aromatase inhibitory activity through various pathways and may act clinically effective for treating pathologies associated with excessive aromatase secretion including breast, ovarian and endometrial cancers, endometriosis, uterine fibroid, benign prostatic hyperplasia (BPH), prostate cancer, infertility, and gynecomastia. Recent studies have shown that natural products with aromatase inhibitory activity, could also be good options against secondary recurrence of breast cancer by exhibiting chemopreventive effects. Therefore, screening for new plant-based aromatase inhibitors may provide novel leads for drug discovery and development, particularly with increased clinical efficacy and decreased side effects.

Acetylcholinesterase Inhibitory Activity of Scopolin and Scopoletin Discovered by Virtual Screening of Natural Products†

2004 ◽  
Vol 47 (25) ◽  
pp. 6248-6254 ◽  
Author(s):  
Judith M. Rollinger ◽  
Ariane Hornick ◽  
Thierry Langer ◽  
Hermann Stuppner ◽  
Helmut Prast
Keyword(s):  
Natural Products ◽  
Virtual Screening ◽  
Inhibitory Activity ◽  
Acetylcholinesterase Inhibitory Activity

scholarly journals Multi-Omic Profiling of Melophlus Sponges Reveals Diverse Metabolomic and Microbiome Architectures that Are Non-overlapping with Ecological Neighbors

Marine Drugs ◽  
2020 ◽  
Vol 18 (2) ◽  
pp. 124 ◽  
Author(s):  
Ipsita Mohanty ◽  
Sheila Podell ◽  
Jason S. Biggs ◽  
Neha Garg ◽  
Eric E. Allen ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Natural Products ◽  
Candidate Gene ◽  
Marine Sponge ◽  
Gene Clusters ◽  
Marine Sponges ◽  
Quantitative Comparison ◽  
Filter Feeding ◽  
Chemical Structures ◽  
Ecological Relevance

Marine sponge holobionts, defined as filter-feeding sponge hosts together with their associated microbiomes, are prolific sources of natural products. The inventory of natural products that have been isolated from marine sponges is extensive. Here, using untargeted mass spectrometry, we demonstrate that sponges harbor a far greater diversity of low-abundance natural products that have evaded discovery. While these low-abundance natural products may not be feasible to isolate, insights into their chemical structures can be gleaned by careful curation of mass fragmentation spectra. Sponges are also some of the most complex, multi-organismal holobiont communities in the oceans. We overlay sponge metabolomes with their microbiome structures and detailed metagenomic characterization to discover candidate gene clusters that encode production of sponge-derived natural products. The multi-omic profiling strategy for sponges that we describe here enables quantitative comparison of sponge metabolomes and microbiomes to address, among other questions, the ecological relevance of sponge natural products and for the phylochemical assignment of previously undescribed sponge identities.

scholarly journals Biological and Chemical Diversity of Marine Sponge-Derived Microorganisms over the Last Two Decades from 1998 to 2017

Molecules ◽  
2020 ◽  
Vol 25 (4) ◽  
pp. 853 ◽  
Author(s):  
Mei-Mei Cheng ◽  
Xu-Li Tang ◽  
Yan-Ting Sun ◽  
Dong-Yang Song ◽  
Yu-Jing Cheng ◽  
...  
Keyword(s):  
Natural Products ◽  
Secondary Metabolites ◽  
Natural Product ◽  
Marine Sponge ◽  
Marine Sponges ◽  
Chemical Diversity ◽  
Comprehensive Overview ◽  
Bioactive Secondary Metabolites ◽  
The Relationship ◽  
Product Chemistry

Marine sponges are well known as rich sources of biologically natural products. Growing evidence indicates that sponges harbor a wealth of microorganisms in their bodies, which are likely to be the true producers of bioactive secondary metabolites. In order to promote the study of natural product chemistry and explore the relationship between microorganisms and their sponge hosts, in this review, we give a comprehensive overview of the structures, sources, and activities of the 774 new marine natural products from sponge-derived microorganisms described over the last two decades from 1998 to 2017.

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