scholarly journals A Review on Diversity of Anticancer Compounds Derived from Indonesian Marine Sponges

2021 ◽  
Vol 1192 (1) ◽  
pp. 012012
Author(s):  
Tutik Murniasih ◽  
Masteria Yunovilsa Putra ◽  
Asep Bayu ◽  
Joko Tri Wibowo
Keyword(s):  
Marine Invertebrates ◽  
Multidrug Resistant ◽  
Marine Sponges ◽  
Research Trend ◽  
Cancer Drug ◽  
Anticancer Compounds ◽  
Lead Compounds ◽  
Drug Lead ◽  
New Compounds ◽  
Active Substances

Abstract As a tropical archipelago country, Indonesia has a mega diversity of marine organisms, such as sponges. About 850 species of sponges were identified from the east part of Indonesia. The uniqueness of Indonesian marine sponges attracted many researchers to explore the sponge’s potential in producing active substances. During 1995-2016, about 40 genera of Indonesian sponges were investigated for their potential in producing pharmacological activity such as antimicrobial, anticancer, antivirus, multidrug-resistant (MDR), etc. The data showed that 56.7% of 430 reported compounds were confirmed as new compounds. The research trend on Indonesian sponges was high during 2004-2013, but decreasing after 2014. However, researches in the term of active substances from marine sponges should find provide the basic skeleton of anti-cancer drug lead compounds. Chemical structure diversity plays an important role in the exploration of anticancer lead compounds. The purpose of this paper is to review the potential of anticancer diversity compounds derived from Indonesian sponges, to get comprehensive data for further investigation. As the conclusion of our review, the most anticancer compounds derived from Indonesian marine invertebrates are alkaloid groups (such as aaptamine, manzamine, and bromopyrrole derivatives), then terpenoid groups (such as diterpene, coelodiol, and coeloic acid, sesquiterpene aminoquinone, and also (+)-curcuphenol and (+)-curcudiol), and also from the other groups such as sterole, peptide, polyketide, amino acid derivatives, natural organic acid, and quinone. The most effective anticancer compounds were 5-benzoyldemethylaaptamine, isoaaptamine, 3-bromofascaplysin, hyrtioreticulins A, stylissamide X, sigmosceptrellin B, and diacarperoxide S.

scholarly journals The Isolation and Structure Elucidation of Secondary Metabolites from Tongan Marine Invertebrates

2021 ◽  
Author(s):  
◽  
Victoria Helen Woolner
Keyword(s):  
Antifungal Activity ◽  
Secondary Metabolites ◽  
Structure Elucidation ◽  
Sea Cucumber ◽  
Marine Invertebrates ◽  
Marine Sponges ◽  
Marine Organisms ◽  
New Members ◽  
Ic50 Values ◽  
New Compounds

<p>During the course of this study, Tongan marine organisms were investigated for new secondary metabolites. A combination of reversed- and normal-phase chromatographic techniques and NMR spectroscopy was employed, to aid in the isolation and structure elucidation of the five known and four new compounds isolated in this study. A brief investigation into the antifungal activity of Tongan holothurian saponins was instigated in order to compare the activity against saponins isolated from the common New Zealand sea cucumber, Australostichopus mollis. A yeast-based chemical genetics study, determined the antifungal activity, for four partially purified Tongan holothurian extracts, against Saccharomyces cerevisiae, to be similar to neothyonidioside (44), a saponin from A. mollis. This result suggested the antifungal activity to be a common characteristic to sea cucumber saponins. Further interest in secondary metabolites from Tongan marine organisms led this study towards the investigation of Tongan marine sponges. Five sponges were selected for screening, and two chosen for further study which yielded five known compounds (51–53, 61, 62) and four new fascaplysin derivatives; 7-bromoreticulatine,10-bromo-6,7-dimethoxyhomofascaplysin C,10-bromo-6, 7-dimethoxyhomofascaplysin D, and 10-bromohomofascaplysin A (63–66, respectively). Although 63 and 66 are new members of the fascaplysin family solely due to the position of the bromine, it appears that bromination on the A-ring is comparatively rare, with only three of the 24 literature examples displaying A-ring bromination. On the other hand, 64 and 65 present a new sub-class of fascaplysin derivatives due to the presence of a dimethoxy functionality. Both 7-bromoreticulatine (63) and 10-bromohomofascaplysin A (66) were found to be potently cytotoxic in the HL-60 cell line, exhibiting IC50 values of 33.8 and 498 nM, respectively. 10-Bromo-6,7-dimethoxyhomofascaplysins C (64) and D (65) were significantly less cytotoxic with respective IC₅₀ values of 2.7 and 6.0 μΜ. (Abstract continues with diagrams).</p>

scholarly journals The Isolation and Structure Elucidation of Secondary Metabolites from Tongan Marine Invertebrates

2021 ◽  
Author(s):  
◽  
Victoria Helen Woolner
Keyword(s):  
Antifungal Activity ◽  
Secondary Metabolites ◽  
Structure Elucidation ◽  
Sea Cucumber ◽  
Marine Invertebrates ◽  
Marine Sponges ◽  
Marine Organisms ◽  
New Members ◽  
Ic50 Values ◽  
New Compounds

<p>During the course of this study, Tongan marine organisms were investigated for new secondary metabolites. A combination of reversed- and normal-phase chromatographic techniques and NMR spectroscopy was employed, to aid in the isolation and structure elucidation of the five known and four new compounds isolated in this study. A brief investigation into the antifungal activity of Tongan holothurian saponins was instigated in order to compare the activity against saponins isolated from the common New Zealand sea cucumber, Australostichopus mollis. A yeast-based chemical genetics study, determined the antifungal activity, for four partially purified Tongan holothurian extracts, against Saccharomyces cerevisiae, to be similar to neothyonidioside (44), a saponin from A. mollis. This result suggested the antifungal activity to be a common characteristic to sea cucumber saponins. Further interest in secondary metabolites from Tongan marine organisms led this study towards the investigation of Tongan marine sponges. Five sponges were selected for screening, and two chosen for further study which yielded five known compounds (51–53, 61, 62) and four new fascaplysin derivatives; 7-bromoreticulatine,10-bromo-6,7-dimethoxyhomofascaplysin C,10-bromo-6, 7-dimethoxyhomofascaplysin D, and 10-bromohomofascaplysin A (63–66, respectively). Although 63 and 66 are new members of the fascaplysin family solely due to the position of the bromine, it appears that bromination on the A-ring is comparatively rare, with only three of the 24 literature examples displaying A-ring bromination. On the other hand, 64 and 65 present a new sub-class of fascaplysin derivatives due to the presence of a dimethoxy functionality. Both 7-bromoreticulatine (63) and 10-bromohomofascaplysin A (66) were found to be potently cytotoxic in the HL-60 cell line, exhibiting IC50 values of 33.8 and 498 nM, respectively. 10-Bromo-6,7-dimethoxyhomofascaplysins C (64) and D (65) were significantly less cytotoxic with respective IC₅₀ values of 2.7 and 6.0 μΜ. (Abstract continues with diagrams).</p>

Antimicrobial Peptides and their Multiple Effects at Sub-Inhibitory Concentrations

2020 ◽  
Vol 20 (14) ◽  
pp. 1264-1273 ◽  
Author(s):  
Bruno Casciaro ◽  
Floriana Cappiello ◽  
Walter Verrusio ◽  
Mauro Cacciafesta ◽  
Maria Luisa Mangoni
Keyword(s):  
Antimicrobial Peptides ◽  
Inhibitory Concentration ◽  
Multidrug Resistant ◽  
Mechanisms Of Action ◽  
New Drugs ◽  
Lead Compounds ◽  
Bacterial Pathogenicity ◽  
Growth Inhibitory ◽  
Resistant Strains ◽  
Conventional Antibiotics

The frequent occurrence of multidrug-resistant strains to conventional antimicrobials has led to a clear decline in antibiotic therapies. Therefore, new molecules with different mechanisms of action are extremely necessary. Due to their unique properties, antimicrobial peptides (AMPs) represent a valid alternative to conventional antibiotics and many of them have been characterized for their activity and cytotoxicity. However, the effects that these peptides cause at concentrations below the minimum growth inhibitory concentration (MIC) have yet to be fully analyzed along with the underlying molecular mechanism. In this mini-review, the ability of AMPs to synergize with different antibiotic classes or different natural compounds is examined. Furthermore, data on microbial resistance induction are reported to highlight the importance of antibiotic resistance in the fight against infections. Finally, the effects that sub-MIC levels of AMPs can have on the bacterial pathogenicity are summarized while showing how signaling pathways can be valid therapeutic targets for the treatment of infectious diseases. All these aspects support the high potential of AMPs as lead compounds for the development of new drugs with antibacterial and immunomodulatory activities.

scholarly journals Thiazole Analogues of the Marine Alkaloid Nortopsentin as Inhibitors of Bacterial Biofilm Formation

Molecules ◽  
2020 ◽  
Vol 26 (1) ◽  
pp. 81
Author(s):  
Anna Carbone ◽  
Stella Cascioferro ◽  
Barbara Parrino ◽  
Daniela Carbone ◽  
Camilla Pecoraro ◽  
...  
Keyword(s):  
Biofilm Formation ◽  
Bacterial Biofilm ◽  
Thiazole Derivatives ◽  
Gram Positive ◽  
Lead Compounds ◽  
New Class ◽  
Marked Selectivity ◽  
Global Threat ◽  
New Compounds ◽  
Reference Strains

Anti-virulence strategy is currently considered a promising approach to overcome the global threat of the antibiotic resistance. Among different bacterial virulence factors, the biofilm formation is recognized as one of the most relevant. Considering the high and growing percentage of multi-drug resistant infections that are biofilm-mediated, new therapeutic agents capable of counteracting the formation of biofilms are urgently required. In this scenario, a new series of 18 thiazole derivatives was efficiently synthesized and evaluated for its ability to inhibit biofilm formation against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923 and S. aureus ATCC 6538 and the Gram-negative strain Pseudomonas aeruginosa ATCC 15442. Most of the new compounds showed a marked selectivity against the Gram-positive strains. Remarkably, five compounds exhibited BIC50 values against S. aureus ATCC 25923 ranging from 1.0 to 9.1 µM. The new compounds, affecting the biofilm formation without any interference on microbial growth, can be considered promising lead compounds for the development of a new class of anti-virulence agents.

scholarly journals Antimicrobial Activities of Marine Sponge-Associated Bacteria

2021 ◽  
Vol 9 (1) ◽  
pp. 171
Author(s):  
Yitayal S. Anteneh ◽  
Qi Yang ◽  
Melissa H. Brown ◽  
Christopher M. M. Franco
Keyword(s):  
Pathogenic Bacteria ◽  
South Australia ◽  
Multidrug Resistant ◽  
Antimicrobial Activities ◽  
Marine Sponges ◽  
Bioactive Metabolites ◽  
Human Pathogens ◽  
Sponge Associated Bacteria ◽  
Microbial Symbionts ◽  
Bacteria And Fungi

The misuse and overuse of antibiotics have led to the emergence of multidrug-resistant microorganisms, which decreases the chance of treating those infected with existing antibiotics. This resistance calls for the search of new antimicrobials from prolific producers of novel natural products including marine sponges. Many of the novel active compounds reported from sponges have originated from their microbial symbionts. Therefore, this study aims to screen for bioactive metabolites from bacteria isolated from sponges. Twelve sponge samples were collected from South Australian marine environments and grown on seven isolation media under four incubation conditions; a total of 1234 bacterial isolates were obtained. Of these, 169 bacteria were tested in media optimized for production of antimicrobial metabolites and screened against eleven human pathogens. Seventy bacteria were found to be active against at least one test bacterial or fungal pathogen, while 37% of the tested bacteria showed activity against Staphylococcus aureus including methicillin-resistant strains and antifungal activity was produced by 21% the isolates. A potential novel active compound was purified possessing inhibitory activity against S. aureus. Using 16S rRNA, the strain was identified as Streptomyces sp. Our study highlights that the marine sponges of South Australia are a rich source of abundant and diverse bacteria producing metabolites with antimicrobial activities against human pathogenic bacteria and fungi.

Synthesis and Crystal Chemistry of New Transition Metal Tellurium Oxides in Compounds Containing Lead and Barium

2000 ◽  
Vol 658 ◽  
Author(s):  
Boris Wedel ◽  
Katsumasa Sugiyama ◽  
Kimio Itagaki ◽  
Hanskarl Müller-Buschbaum
Keyword(s):  
Solid State ◽  
Transition Metal ◽  
Solid State Reactions ◽  
Solid State Chemistry ◽  
Wide Field ◽  
Synthesis Conditions ◽  
Lead Compounds ◽  
Alkaline Transition ◽  
New Compounds ◽  
Channel Structures

ABSTRACTDuring the past decades the solid state chemistry of tellurium oxides has been enriched by a series of quaternary metallates. Interest attaches not only to the chemical and physical properties of these compounds, but also to their structure, which have been studied by modern methods. The partial similarity of earth alkaline metals and lead in solid state chemistry and their relationships in oxides opens a wide field of investigations. Eight new compounds in the systems Ba-M-Te-O (M= Nb, Ta) and Pb-M-Te-O (M = Mn, Ni, Cu, Zn) were prepared and structurally characterized: Ba2Nb2TeO10, Ba2M6Te2O21 (M = Nb, Ta) and the lead compounds PbMnTeO3, Pb3Ni4.5Te2.5O15, PbCu3TeO7, PbZn4SiTeO10 and the mixed compound PbMn2Ni6Te3O18. The structures of all compounds are based on frameworks of edge and corner sharing oxygen octahedra of the transition metal and the tellurium. Various different channel structures were observed and distinguished. The compounds were prepared by heating from mixtures of the oxides, and the single crystals were grown by flux method or solid state reactions on air. The synthesis conditions were modified to obtained microcrystalline material for purification and structural characterizations, which were carried out using a variety of tools including powder diffraction data and refinements of X-ray data. Relationships between lead transition metal tellurium oxides and the earth alkaline transition metals tellurium oxides are compared.

scholarly journals Derivatives of 2-Aminopyridines as Inhibitors of Multidrug Resistant Staphylococcus Aureus Strains

2018 ◽  
Vol 10 (1) ◽  
pp. 153
Author(s):  
Iniobong E. Ante ◽  
Sherifat A Aboaba ◽  
Hina Siddiqui ◽  
Muhammad A Bashir ◽  
Muhammad I Choudhary
Keyword(s):  
Staphylococcus Aureus ◽  
Mass Spectra ◽  
Multidrug Resistant ◽  
Drug Resistant ◽  
Acid Chlorides ◽  
Alamar Blue ◽  
Standard Drug ◽  
Starting Point ◽  
New Compounds ◽  
Derivatives Of

A new series of 2-aminopyridine derivatives were synthesised. N-acylation of 2-amino-3-chloro-5-(trifluoromethyl) pyridine and 2-amino-5-(trifluoromethyl) pyridine with series of acid chlorides afforded a total of fourteen (14) amide compounds. The structures of the new compounds have been established by their IR, NMR and mass spectra data. All the compounds were tested for their activity against four (4) multi-drug resistant (MDR) bacteria Staphylococcus aureus strains using microplate alamar blue assay. The MDR-Staphylococcus aureus strains employed for this study were Epidermic Methicilin Resistant Staphylococcus aureus (EMRSA-17), Methicilin Resistant Staphylococcus aureus (MRSA-252), Epidermic Methicilin Resistant Staphylococcus aureus (EMRSA-16) and Pakistani Drug resistant clinical isolate of Staphylococcus aureus (PRSA). Other bacteria strains also used include Escherichia coli (ATCC 2592), Shigella flexenari (ATCC 12022), Staphylococcus aureus (NCTC 6571) and Pseudomonas aeruginosa (NCTC 10662). The synthesised compounds exhibited very good activity against the four MDR-Staphylococcus aureus strains of which most of the compounds showed higher potencies for inhibiting the growth of the strains than vancomycin, the standard drug employed. The compounds reported here may serve as the starting point for the design and development of MDR-S.aureus inhibitors as antibacterial agents.

scholarly journals Cytotoxic activity of marine sponge extracts from the sub-Antarctic Islands and the Southern Ocean

2016 ◽  
Vol Volume 112 (Number 11/12) ◽  
Author(s):  
Elisabeth K. Olsen ◽  
Christopher K. de Cerf ◽  
Godwin A. Dziwornu ◽  
Eleonora Puccinelli ◽  
Isabelle J. Ansorge ◽  
...  
Keyword(s):  
Natural Products ◽  
Southern Ocean ◽  
Cytotoxic Activity ◽  
Marine Invertebrates ◽  
Cold Water ◽  
Research Effort ◽  
Benthic Invertebrate ◽  
Marine Sponges ◽  
Bioactive Natural Products ◽  
Prince Edward Islands

Abstract Over the past 50 years, marine invertebrates, especially sponges, have proven to be a valuable source of new and/or bioactive natural products that have the potential to be further developed as lead compounds for pharmaceutical applications. Although marine benthic invertebrate communities occurring off the coast of South Africa have been explored for their biomedicinal potential, the natural product investigation of marine sponges from the sub-Antarctic Islands in the Southern Ocean for the presence of bioactive secondary metabolites has been relatively unexplored thus far. We report here the results for the biological screening of both aqueous and organic extracts prepared from nine specimens of eight species of marine sponges, collected from around Marion Island and the Prince Edward Islands in the Southern Ocean, for their cytotoxic activity against three cancer cell lines. The results obtained through this multidisciplinary collaborative research effort by exclusively South African institutions has provided an exciting opportunity to discover cytotoxic compounds from sub-Antarctic sponges, whilst contributing to our understanding of the biodiversity and geographic distributions of these cold-water invertebrates. Therefore, we acknowledge here the various contributions of the diverse scientific disciplines that played a pivotal role in providing the necessary platform for the future natural products chemistry investigation of these marine sponges from the sub- Antarctic Islands and the Southern Ocean.

Search for new compounds and biologically active substances from Chinese marine organisms

1999 ◽  
Vol 71 (6) ◽  
pp. 1147-1151 ◽  
Author(s):  
L. Zeng ◽  
J. Su ◽  
Yongli Zhong ◽  
Xiong Fu ◽  
T. Peng ◽  
...  
Keyword(s):  
Marine Organisms ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
New Compounds ◽  
Active Substances ◽  
Chinese Marine

scholarly journals A Program for Automated Data Mining of PubChem to Screen a Billion Compounds and Generate by Machine Learning Based AutoQSAR Algorithm Anti-Corona Viral Drug Leads (Replicase Polyprotein 1ab Inhibitors) and in Silico Study of the Top Drug Lead Compounds

2020 ◽  
Author(s):  
Ben Geoffrey A S ◽  
Akhil Sanker ◽  
Host Antony Davidd ◽  
Judith Gracia
Keyword(s):  
Machine Learning ◽  
Data Mining ◽  
In Silico ◽  
Drug Target ◽  
Data Set ◽  
Lead Compounds ◽  
Pubchem Database ◽  
Drug Lead ◽  
Lead Generation ◽  
Drug Leads

Our work is composed of a python program for automatic data mining of PubChem database to collect data associated with the corona virus drug target replicase polyprotein 1ab (UniProt identifier : POC6X7 ) of data set involving active compounds, their activity value (IC50) and their chemical/molecular descriptors to run a machine learning based AutoQSAR algorithm on the data set to generate anti-corona viral drug leads. The machine learning based AutoQSAR algorithm involves feature selection, QSAR modelling, validation and prediction. The drug leads generated each time the program is run is reflective of the constantly growing PubChem database is an important dynamic feature of the program which facilitates fast and dynamic anti-corona viral drug lead generation reflective of the constantly growing PubChem database. The program prints out the top anti-corona viral drug leads after screening PubChem library which is over a billion compounds. The interaction of top drug lead compounds generated by the program and two corona viral drug target proteins, 3-Cystiene like Protease (3CLPro) and Papain like protease (PLpro) was studied and analysed using molecular docking tools. The compounds generated as drug leads by the program showed favourable interaction with the drug target proteins and thus we recommend the program for use in anti-corona viral compound drug lead generation as it helps reduce the complexity of virtual screening and ushers in an age of automatic ease in drug lead generation. The leads generated by the program can further be tested for drug potential through further In Silico, In Vitro and In Vivo testing <div><br></div><div><div>The program is hosted, maintained and supported at the GitHub repository link given below</div><div><br></div><div>https://github.com/bengeof/Drug-Discovery-P0C6X7</div></div><div><br></div>

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