Screening Study of Lead Compounds for Natural Product-Based Fungicides:  Antifungal Activity and Biotransformation of 6α,7α-Dihydroxy-β-himachalene byBotrytis cinerea

2005 ◽  
Vol 53 (17) ◽  
pp. 6673-6677 ◽  
Author(s):  
Mourad Daoubi ◽  
Rosario Hernández-Galán ◽  
Ahmed Benharref ◽  
Isidro G. Collado
Keyword(s):  
Antifungal Activity ◽  
Natural Product ◽  
Lead Compounds ◽  
Screening Study

Screening Study of Potential Lead Compounds for Natural Product-based Fungicides Against Phytophthora Species

2006 ◽  
Vol 154 (10) ◽  
pp. 616-621 ◽  
Author(s):  
F. J. Fernández-Acero ◽  
M. Carbú ◽  
C. Garrido ◽  
I. G. Collado ◽  
J. Cantoral ◽  
...  
Keyword(s):  
Natural Product ◽  
Phytophthora Species ◽  
Lead Compounds ◽  
Screening Study

Screening study for potential lead compounds for natural product-based fungicides: I. Synthesis and in vitro evaluation of coumarins against Botrytis cinerea

2004 ◽  
Vol 60 (9) ◽  
pp. 927-932 ◽  
Author(s):  
Mourad Daoubi ◽  
Rosa Durán-Patrón ◽  
Mohamed Hmamouchi ◽  
Rosario Hernández-Galán ◽  
Ahmed Benharref ◽  
...  
Keyword(s):  
Natural Product ◽  
Botrytis Cinerea ◽  
In Vitro Evaluation ◽  
Lead Compounds ◽  
Screening Study

scholarly journals Screening Study of Potential Lead Compounds for Natural Product Based Fungicides from Juniperus Lucayana

2008 ◽  
Vol 3 (4) ◽  
pp. 1934578X0800300
Author(s):  
Yarelis Ortíz Nuñez ◽  
Iraida Spengler Salabarria ◽  
Isidro G. Collado ◽  
Rosario Hernández-Galán
Keyword(s):  
Natural Product ◽  
Botrytis Cinerea ◽  
Fungicidal Activity ◽  
Pathogenic Fungus ◽  
Chemical Transformations ◽  
Lead Compounds ◽  
Screening Study

Based on structure and detoxification data, chemical transformations of 12-hydroxywiddrol (3) isolated from the wood of Juniperus lucayana were performed leading to hemisynthetic derivatives with improved fungicidal activity against Botrytis cinerea, a pathogenic fungus affecting commercial crops.

Synthesis and Biological Evaluation of the Antimicrobial Natural Product Lipoxazolidinone A

2018 ◽  
Author(s):  
Jonathan J. Mills ◽  
Kaylib R. Robinson ◽  
Troy E. Zehnder ◽  
Joshua G. Pierce
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Mechanism Of Action ◽  
Marine Natural Products ◽  
Biological Evaluation ◽  
Lead Compounds ◽  
Follow Up Studies ◽  
Initial Resistance ◽  
Synthesis And Biological Evaluation

The lipoxazolidinone family of marine natural products, with an unusual 4-oxazolidinone heterocycle at their core, represents a new scaffold for antimicrobial discovery; however, questions regarding their mechanism of action and high lipophilicity have likely slowed follow-up studies. Herein, we report the first synthesis of lipoxazolidinone A, 15 structural analogs to explore its active pharmacophore, and initial resistance and mechanism of action studies. These results suggest that 4-oxazolidinones are valuable scaffolds for antimicrobial development and reveal simplified lead compounds for further optimization.

scholarly journals A Novel Marine Natural Product Derived Pyrroloiminoquinone with Potent Activity against Skin Cancer Cells

Marine Drugs ◽  
2019 ◽  
Vol 17 (8) ◽  
pp. 443 ◽  
Author(s):  
Jaden Cowan ◽  
Mohammad Shadab ◽  
Dwayaja H. Nadkarni ◽  
Kailash KC ◽  
Sadanandan E. Velu ◽  
...  
Keyword(s):  
Natural Products ◽  
Side Effects ◽  
Skin Cancer ◽  
Cancer Cells ◽  
Natural Product ◽  
The United States ◽  
Marine Natural Product ◽  
Migration And Invasion ◽  
Migration Assay ◽  
Lead Compounds

Non-melanoma skin cancer is one of the major ailments in the United States. Effective drugs that can cure skin cancers are limited. Moreover, the available drugs have toxic side effects. Therefore, skin cancer drugs with less toxic side effects are urgently needed. To achieve this goal, we focused our work on identifying potent lead compounds from marine natural products. Five lead compounds identified from a class of pyrroloiminoquinone natural products were evaluated for their ability to selectively kill squamous cell carcinoma (SCC13) skin cancer cells using an MTT assay. The toxicity of these compounds was also evaluated against the normal human keratinocyte HaCaT cell line. The most potent compound identified from these studies, C278 was further evaluated for its ability to inhibit cancer cell migration and invasion using a wound-healing assay and a trans-well migration assay, respectively. To investigate the molecular mechanism of cell death, the expression of apoptotic and autophagy proteins was studied in C278 treated cells compared to untreated cells using western blot. Our results showed that all five compounds effectively killed the SCC13 cells, with compound C278 being the most effective. Compound C278 was more effective in killing the SCC13 cells compared to HaCaT cells with a two-fold selectivity. The migration and the invasion of the SCC13 cells were also inhibited upon treatment with compound C278. The expression of pro-apoptotic and autophagy proteins with concomitant downregulation in the expression of survival proteins were observed in C278 treated cells. In summary, the marine natural product analog compound C278 showed promising anticancer activity against human skin cancer cells and holds potential to be developed as an effective anticancer agent to combat skin cancer.

Natural alkaloid tryptanthrin exhibits novel anticryptococcal activity

2020 ◽  
Author(s):  
Chi-Jan Lin ◽  
Ya-Lin Chang ◽  
Yu-Liang Yang ◽  
Ying-Lien Chen
Keyword(s):  
Cell Cycle ◽  
Antifungal Activity ◽  
Signaling Pathways ◽  
Natural Product ◽  
Cyclosporine A ◽  
Cryptococcal Meningitis ◽  
Synergistic Effects ◽  
Calcineurin Inhibitors ◽  
Genes Encoding ◽  
Cryptococcus Species

Abstract Cryptococcal meningitis is a prevalent invasive fungal infection that causes around 180 000 deaths annually. Currently, treatment for cryptococcal meningitis is limited and new therapeutic options are needed. Historically, medicinal plants are used to treat infectious and inflammatory skin infections. Tryptanthrin is a natural product commonly found in these plants. In this study, we demonstrated that tryptanthrin had antifungal activity with minimum inhibitory concentration (MIC) of 2 μg/ml against Cryptococcus species and of 8 μg/ml against Trichophyton rubrum. Further analysis demonstrated that tryptanthrin exerted fungistatic and potent antifungal activity at elevated temperature. In addition, tryptanthrin exhibited a synergistic effect with the calcineurin inhibitors FK506 and cyclosporine A against Cryptococcus neoformans. Furthermore, our data showed that tryptanthrin induced cell cycle arrest at the G1/S phase by regulating the expression of genes encoding cyclins and the SBF/MBF complex (CLN1, MBS1, PCL1, and WHI5) in C. neoformans. Screening of a C. neoformans mutant library further revealed that tryptanthrin was associated with various transporters and signaling pathways such as the calcium transporter (Pmc1) and protein kinase A signaling pathway. In conclusion, tryptanthrin exerted novel antifungal activity against Cryptococcus species through a mechanism that interferes with the cell cycle and signaling pathways. Lay Summary The natural product tryptanthrin had antifungal activity against Cryptococcus species by interfering cell cycle and exerted synergistic effects with immunosuppressants FK506 and cyclosporine A. Our findings suggest that tryptanthrin may be a potential drug or adjuvant for the treatment of cryptococcosis.

scholarly journals Natural Product Compounds in Alpinia officinarum and Ginger are Potent SARS-CoV-2 Papain-like Protease Inhibitors

2020 ◽  
Author(s):  
Dibakar Goswami ◽  
Mukesh Kumar ◽  
Sunil K. Ghosh ◽  
Amit Das
Keyword(s):  
Virtual Screening ◽  
Natural Product ◽  
Protease Inhibitors ◽  
In Silico ◽  
Drug Target ◽  
Homology Modelling ◽  
Protease Domain ◽  
Lead Compounds ◽  
Alpinia Officinarum ◽  
Natural Product Compounds

SARS-CoV-2 or COVID-19 has caused more than 10,00,000 infections and ~55,000 deaths worldwide spanning over 203 countries, and the numbers are exponentially increasing. Due to urgent need of treating the SARS infection, many approved, pre-clinical, anti-viral, anti-malarial and anti-SARS drugs are being administered to patients. SARS-CoV-2 papain-like protease (PLpro) has a protease domain which cleaves the viral polyproteins a/b, necessary for its survival and replication, and is one of the drug target against SARS-CoV-2. 3D structures of SARS-CoV-2 PLpro were built by homology modelling. Two models having partially open and closed conformations were used in our study. Virtual screening of natural product compounds was performed. We prepared an in house library of compounds found in rhizomes, Alpinia officinarum, ginger and curcuma, and docked them into the solvent accessible S3-S4 pocket of PLpro. Eight compounds from Alpinia officinarum and ginger bind with high in silico affinity to closed PLpro conformer, and hence are potential SARS-CoV-2 PLpro inhibitors. Our study reveal new lead compounds targeting SARS-CoV-2. Further structure based modifications or extract formulations of these compounds can lead to highly potent inhibitors to treat SARS-CoV-2 infections.<br>

Natural products as modulators of the cyclic-AMP pathway: evaluation and synthesis of lead compounds

2018 ◽  
Vol 16 (35) ◽  
pp. 6372-6390 ◽  
Author(s):  
Saumitra Sengupta ◽  
Goverdhan Mehta
Keyword(s):  
Natural Products ◽  
Cyclic Amp ◽  
Total Synthesis ◽  
Natural Product ◽  
Lead Compounds ◽  
Camp Pathway

Natural product modulators of the cAMP pathway have been evaluated and their total synthesis campaign is described in detail.

scholarly journals Natural Product Compounds in Alpinia officinarum and Ginger are Potent SARS-CoV-2 Papain-like Protease Inhibitors

2020 ◽  
Author(s):  
Dibakar Goswami ◽  
Mukesh Kumar ◽  
Sunil K. Ghosh ◽  
Amit Das
Keyword(s):  
Virtual Screening ◽  
Natural Product ◽  
Protease Inhibitors ◽  
In Silico ◽  
Drug Target ◽  
Homology Modelling ◽  
Protease Domain ◽  
Lead Compounds ◽  
Alpinia Officinarum ◽  
Natural Product Compounds

SARS-CoV-2 or COVID-19 has caused more than 10,00,000 infections and ~55,000 deaths worldwide spanning over 203 countries, and the numbers are exponentially increasing. Due to urgent need of treating the SARS infection, many approved, pre-clinical, anti-viral, anti-malarial and anti-SARS drugs are being administered to patients. SARS-CoV-2 papain-like protease (PLpro) has a protease domain which cleaves the viral polyproteins a/b, necessary for its survival and replication, and is one of the drug target against SARS-CoV-2. 3D structures of SARS-CoV-2 PLpro were built by homology modelling. Two models having partially open and closed conformations were used in our study. Virtual screening of natural product compounds was performed. We prepared an in house library of compounds found in rhizomes, Alpinia officinarum, ginger and curcuma, and docked them into the solvent accessible S3-S4 pocket of PLpro. Eight compounds from Alpinia officinarum and ginger bind with high in silico affinity to closed PLpro conformer, and hence are potential SARS-CoV-2 PLpro inhibitors. Our study reveal new lead compounds targeting SARS-CoV-2. Further structure based modifications or extract formulations of these compounds can lead to highly potent inhibitors to treat SARS-CoV-2 infections.<br>

scholarly journals Antifungal Activity of Metabolites from the Marine Sponges Amphimedon sp. and Monanchora arbuscula against Aspergillus flavus Strains Isolated from Peanuts (Arachis hypogaea)

2014 ◽  
Vol 9 (1) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Cynthia Arevabini ◽  
Yasmin D. Crivelenti ◽  
Mariana H. de Abreu ◽  
Tamires A. Bitencourt ◽  
Mário F. C. Santos ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Arachis Hypogaea ◽  
Aspergillus Flavus ◽  
Biosynthetic Pathway ◽  
Its Region ◽  
Marine Sponges ◽  
Marine Alkaloids ◽  
Lead Compounds ◽  
Arachis Hypogaea L ◽  
Aflatoxigenic Fungi

Contamination of preharvest and stored peanuts ( Arachis hypogaea L.) by aflatoxigenic strains of Aspergillus flavus is an important economical and food safety problem in many tropical and subtropical areas of the world. The present investigation reports the antifungal activity of a halitoxins/amphitoxins enriched extract obtained from the sponge Amphimedon sp. (HAEEAsp), and of batzelladine L isolated from the sponge Monanchora arbuscula on Aspergillus flavus isolated from stored peanuts. A PCR system directed against the ITS region and aflatoxin biosynthetic pathway genes of A. flavus was applied for identification of aflatoxin producing strains. The HAEEAsp extract and batzelladine L showed minimal inhibitory concentration (MIC) in the range between 1.9 to 15.6 μg/mL and between 1.9 to 7.8 μg/mL, respectively. The minimal fungicide concentration (MFC) of HAEEAsp extract and batzelladine L was in the range between 3.9 to 31.3 μg/mL and 3.9 to 15.6 μg/mL, respectively. These results indicate that these marine alkaloids may be further explored for the development of potential lead compounds active against aflatoxigenic fungi.

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