scholarly journals Spiculisporic Acid E, a New Spiculisporic Acid Derivative and Ergosterol Derivatives from the Marine-Sponge Associated Fungus Talaromyces trachyspermus (KUFA 0021)

2014 ◽  
Vol 9 (8) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Decha Kumla ◽  
Tida Dethoup ◽  
Suradet Buttachon ◽  
Narong Singburaudom ◽  
Artur M.S. Silva ◽  
...  
Keyword(s):  
Acid Derivative ◽  
Marine Sponge ◽  
Multidrug Resistant ◽  
Breast Adenocarcinoma ◽  
Gram Negative Bacteria ◽  
Small Cell Lung ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Mcf 7

A new spiculisporic acid derivative, spiculisporic acid E (2), and a new natural product 3-acetyl ergosterol 5, 8-endoperoxide (1), were isolated, together with ergosta-4, 6, 8 (14), 22-tetraen-3-one, glaucanic acid and glauconic acid, from the culture of the marine-sponge associated fungus Talaromyces trachyspermus (KUFA 0021). All the compounds were inactive against Gram-positive and Gram-negative bacteria, and Candida albicans, as well as multidrug-resistant isolates from the environment. Spiculisporic acid E (2), glaucanic acid and glauconic acid did not show in vitro growth inhibitory activity against the MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) and A375-C5 (melanoma) cell lines by the protein binding dye SRB method.

scholarly journals Sartoryglabrins, Analogs of Ardeemins, from Neosartorya Glabra

2011 ◽  
Vol 6 (6) ◽  
pp. 1934578X1100600
Author(s):  
Anake Kijjoa ◽  
Sonia Santos ◽  
Tida Dethoup ◽  
Leka Manoch ◽  
Ana Paula Almeida ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Human Tumor ◽  
Breast Adenocarcinoma ◽  
Moderate Activity ◽  
Growth Inhibitory ◽  
Nmr Spectrometry ◽  
Growth Inhibitory Activity ◽  
Mcf 7

Chemical investigation of a collection of the fungus Neosartorya glabra from Thailand furnished sartoryglabins A-C (1a, 1b and 2) which are analogs of the reverse prenylated indole alkaloids known as (-) ardeemins. Structures of these compounds were established by NMR spectrometry and an X-ray analysis. Sartoryglabins A-C were evaluated for their in vitro growth inhibitory activity on three human tumor cell lines: MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) and A375-C5 (melanoma). All the compounds exhibited strong to moderate activity against the MCF-7 cell line but weak or no activity against the NCI-H460 and A375-C5 cell lines. Sartoryglabin B was found to exhibit selectivity towards the MCF-7 cell line.

scholarly journals Synthesis, Molecular Docking and Anticancer Activity of Novel 1,3-Thiazolidin-4-Ones

2020 ◽  
Vol 27 (3) ◽  
pp. 345-352
Author(s):  
Ramesh Sawant ◽  
Jyoti Wadekar ◽  
Rushikesh Ukirde ◽  
Ganesh Barkade
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Cancer Cell Line ◽  
Lead Compounds ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Further Development ◽  
Mcf 7 ◽  
Clinical Strategy

Background: Cancer is a major cause of death all over the globe. Controlling cell division byinhibition of mitosis is the most successful clinical strategy for cancer treatment. The developmentof novel anticancer agents is the most important area in medicinal chemistry and drug discoveryresearch. Thiazolidine is the multifunctional nucleus which shows a number of pharmacologicalactivities like anticancer, anti-inflammatory, antioxidant, antibacterial, antifungal, antidiabetic,antihyperlipidemic and antiarthritic. Methods: In a present study series of 2-substituted-3-(1H-benzimidazole-2-yl)-thiazolidin-4-ones were designed, synthesized by the microwave-assisted system, and characterized bymelting point, IR, 1H NMR, and mass spectroscopy. All the newly synthesized compoundswere examined for their in vitro anticancer activity against breast cancer cell line MCF-7 bySulforhodamine B (SRB) assay. Results: The compounds AB-12 (GI50: 28.5 μg/ml) and AB-6 (GI50: 50.7 μg/ml) exhibitedsignificant cell growth inhibitory activity. Conclusion: These results indicate that compound AB-12 and AB-6 as related polo-like kinase1inhibitors compounds could be lead compounds for further development of anticanceragents.

scholarly journals Radiation-induced PEGylated Ethambutol Has Low Antimycobacterial Activity in Vitro

2020 ◽  
Vol 11 (2) ◽  
pp. 8884-8894
Keyword(s):  
Antimycobacterial Activity ◽  
Multidrug Resistant ◽  
Biological Evaluation ◽  
Rapid Screening ◽  
Promising Tool ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Radiation Induced ◽  
Airborne Disease

Tuberculosis is an airborne disease caused by Mycobacterium tuberculosis and remains one of the leading causes of death worldwide. The rise in multidrug-resistant strains has prompted the search for novel strategies to produce tuberculostatic agents. This research is aimed at developing a derivative of ethambutol by gamma radiation-induced polymerization with polyethylene glycol (PEG). The synthesis was verified by Raman spectroscopy and UV–Vis spectrometry. The results show that PEG can be chemically bonded to ethambutol by amine and alcohol groups. In in vitro biological evaluation, PEGylated and neat ethambutol showed similar cell viabilities, while the modified drug lowered bacterial growth inhibitory activity. A mechanism for the polymerization is proposed. The particle size increased for PEGylated drugs concerning the starting polyether. Despite the low antimycobacterial activity in vitro, the product seems to be a promising tool for the rapid screening of hydrolase activity.

scholarly journals Synthesis and Cytotoxicity of Thieno[2,3-b]Pyridine Derivatives Toward Sensitive and Multidrug-Resistant Leukemia Cells

2021 ◽  
Vol 68 (2) ◽  
pp. 458-465
Author(s):  
Salah A. Al-Trawneh ◽  
Amer H. Tarawneh ◽  
Anastassiya V. Gadetskaya ◽  
Ean-Jeong Seo ◽  
Mohammad R. Al-Ta’ani ◽  
...  
Keyword(s):  
Multidrug Resistant ◽  
In Vitro Cytotoxicity ◽  
Leukemia Cells ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Anti Cancer ◽  
Ic50 Values ◽  
New Compounds ◽  
Potential Use

A new series of substituted ethyl 7-cyclopropyl-2-(2-aryloxo)-3-nitro-4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylates 3a–e were prepared by utilizing ethyl 2-chloro-7-cyclopropyl-3-nitro-4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylate (1) and replacing of the 2-chlorine with anions obtained from phenol (2a), salicylaldehyde derivatives 2b–d or thiophenol (2e), leading to the respective ethyl 7-cyclopropyl-2-(2-aryloxo)-3-nitro-4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylates 3a–e. The new compounds were evaluated for their in vitro cytotoxicity towards sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 leukemia cells. The screening revealed that compounds 3a, 3b, and 3e inhibited the growth of both cell lines. Compound 3b, with a phenol moiety, exhibited the highest growth inhibitory activity against CEM/ADR5000 and CCRF-CEM cells with IC50 values 4.486 ± 0.286 and 2.580 ± 0.550 μM, respectively. Collectively, the presented results demonstrate that the synthesized thieno[2,3-b]pyridines warrant further exploration for potential use as anti-cancer agents.

Synthesis, spectral, molecular modeling, biological and antitumor studies of new nifuroxazide complexes

2021 ◽  
Vol 11 (7) ◽  
pp. 1071-1083
Author(s):  
Eid H. Alosaimi ◽  
Walaa H. El-Shwiniy ◽  
Saad M. Alshahrani ◽  
Ayman A. O. Younes ◽  
Mostafa Y. Nassar ◽  
...  
Keyword(s):  
Bacterial Species ◽  
Thermal Analyses ◽  
Molar Conductance ◽  
Cancer Drug ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Anti Cancer ◽  
Hct 116 ◽  
Mcf 7

Series of Zr(IV), Ce(IV) and U(VI) complexes were synthesized with nifuroxazide ligand. Design and formulae of the complexes suggested in the light of analytical, spectral, magnetic and thermal analyses (1HNMR, IR, UV-Vis). The calculated values of molar conductance mean that, all isolated complexes were electrolytes. The data revealed the complexes formation and suggested that nifuroxazide binds as a bidentate at NO sites with metal ions. The kinetic parameters evaluated using Coats Redfern (CR) and Horowitz-Metzeger (HM) methods. The thermodynamic data reflect the thermal stability for all complexes. The calculated bond length and force constant values for UO2 bond are 1.741 Å and 459.409 Nm−1. The research investigations were related to quantum chemical calculations conducted at the theory level of DFT/B3LYP/LANL2DZ. The nifuroxazide, inorganic salts and their metal complexes were assayed against different bacterial species as well as the in vitro growth inhibitory activity against human breast carcinoma (MCF-7) and HCT-116 cell lines. Zr(IV) complex was found to have the highest activity against all the tested organisms and a powerful anti-cancer drug.

Synergistic antibacterial efficacies of the combination of bovine lactoferrin or its hydrolysate with probiotic secretion in curbing the growth of meticillin-resistant Staphylococcus aureus

2013 ◽  
Vol 62 (12) ◽  
pp. 1845-1851 ◽  
Author(s):  
Po-Wen Chen ◽  
Trista Tingyun Jheng ◽  
Ching-Ling Shyu ◽  
Frank Chiahung Mao
Keyword(s):  
Staphylococcus Aureus ◽  
Bifidobacterium Longum ◽  
Multidrug Resistant ◽  
Bovine Lactoferrin ◽  
Bifidobacterium Animalis ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Mrsa Infection ◽  
Mrsa Strains

The occurrence of multidrug-resistant or meticillin-resistant Staphylococcus aureus (MRSA) has become an important issue in clinics. This study evaluated a combinatorial treatment approach by using the well-documented antibacterial protein apo-bovine lactoferrin (apo-bLf) or its hydrolysate and specific probiotic supernatants for controlling MRSA infection. Clinical MRSA strains were isolated from different patient specimens. Apo-bLf-hydrolysate possessed stronger anti-MRSA activity than complete bLf in that it inhibited the growth of most MRSA strains tested in vitro. Otherwise, the supernatants produced by Lactobacillus fermentum (ATCC 11739), Bifidobacterium longum subsp. longum (ATCC 15707) and Bifidobacterium animalis subsp. lactis (BCRC 17394) inhibited the growth of various MRSA strains. Further, L. fermentum or B. animalis subsp. lactis supernatant plus apo-bLf or bLf-hydrolysate led to partially synergistic to synergistic growth-inhibitory activity against MRSA strains. However, L. fermentum and not B. animalis subsp. lactis or B. longum subsp. longum was observed to resist the antibacterial activity of both apo-Lf and bLf-hydrolysate. Therefore, it is suggested that L. fermentum could be the best candidate to be used with apo-bLf or bLf-hydrolysate as a live supplement against MRSA infections.

Evaluation of Cytotoxic and Tyrosinase Inhibitory Activities of 2-phenoxy(thiomethyl) pyridotriazolopyrimidines: In Vitro and Molecular Docking Studies

2020 ◽  
Vol 20 (14) ◽  
pp. 1714-1721
Author(s):  
Hatem A. Abuelizz ◽  
El Hassane Anouar ◽  
Mohamed Marzouk ◽  
Mizaton H. Hasan ◽  
Siti R. Saleh ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Kojic Acid ◽  
Docking Studies ◽  
Breast Adenocarcinoma ◽  
Amino Acid Residues ◽  
New Class ◽  
Structure Activity ◽  
Tyrosinase Inhibitors ◽  
Mcf 7

Background: The use of tyrosinase has confirmed to be the best means of recognizing safe, effective, and potent tyrosinase inhibitors for whitening skin. Twenty-four 2-phenoxy(thiomethyl)pyridotriazolopyrimidines were synthesized and characterized in our previous studies. Objective: The present work aimed to evaluate their cytotoxicity against HepG2 (hepatocellular carcinoma), A549 (pulmonary adenocarcinoma), MCF-7 (breast adenocarcinoma) and WRL 68 (embryonic liver) cell lines. Methods: MTT assay was employed to investigate the cytotoxicity, and a tyrosinase inhibitor screening kit was used to evaluate the Tyrosinase (TYR) inhibitory activity of the targets. Results: The tested compounds exhibited no considerable cytotoxicity, and nine of them were selected for a tyrosinase inhibitory test. Compounds 2b, 2m, and 5a showed good inhibitory percentages against TYR compared to that of kojic acid (reference substance). Molecular docking was performed to rationalize the Structure-Activity Relationship (SAR) of the target pyridotriazolopyrimidines and analyze the binding between the docked-selected compounds and the amino acid residues in the active site of tyrosinase. Conclusion: The target pyridotriazolopyrimidines were identified as a new class of tyrosinase inhibitors.

scholarly journals Semi-Synthesis of Harringtonolide Derivatives and Their Antiproliferative Activity

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1380
Author(s):  
Xiutao Wu ◽  
Lijie Gong ◽  
Chen Chen ◽  
Ye Tao ◽  
Wuxi Zhou ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Normal Cell ◽  
Selectivity Index ◽  
Cytotoxic Activities ◽  
Structure Activity ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Hct 116 ◽  
Systematic Structure

Harringtonolide (HO), a natural product isolated from Cephalotaxus harringtonia, exhibits potent antiproliferative activity. However, little information has been reported on the systematic structure−activity relationship (SAR) of HO derivatives. Modifications on tropone, lactone, and allyl positions of HO (1) were carried out to provide 17 derivatives (2–13, 11a–11f). The in vitro antiproliferative activity against four cancer cell lines (HCT-116, A375, A549, and Huh-7) and one normal cell line (L-02) was tested. Amongst these novel derivatives, compound 6 exhibited comparable cell growth inhibitory activity to HO and displayed better selectivity index (SI = 56.5) between Huh-7 and L-02 cells. The SAR results revealed that the tropone and lactone moieties are essential for the cytotoxic activities, which provided useful suggestions for further structural optimization of HO.

scholarly journals Plasmodium falciparum Line-Dependent Association ofIn VitroGrowth-Inhibitory Activity and Risk of Malaria

2012 ◽  
Vol 80 (5) ◽  
pp. 1900-1908 ◽  
Author(s):  
Josea Rono ◽  
Anna Färnert ◽  
Daniel Olsson ◽  
Faith Osier ◽  
Ingegerd Rooth ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Inhibitory Activity ◽  
Content Type ◽  
Phenotypic Differences ◽  
Erythrocyte Invasion ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Control Study

ABSTRACTPlasmodium falciparum's ability to invade erythrocytes is essential for its survival within the human host. Immune mechanisms that impair this ability are therefore expected to contribute to immunity against the parasite. Plasma of humans who are naturally exposed to malaria has been shown to have growth-inhibitory activity (GIA)in vitro. However, the importance of GIA in relation to protection from malaria has been unclear. In a case-control study nested within a longitudinally followed population in Tanzania, plasma samples collected at baseline from 171 individuals (55 cases and 116 age-matched controls) were assayed for GIA using threeP. falciparumlines (3D7, K1, and W2mef) chosen based on their erythrocyte invasion phenotypes. Distribution of GIA differed between the lines, with most samples inhibiting the growth of 3D7 and K1 and enhancing the growth of W2mef. GIA to 3D7 was associated with a reduced risk of malaria within 40 weeks of follow-up (odds ratio, 0.45; 95% confidence interval [CI], 0.21 to 0.96;P= 0.04), whereas GIA to K1 and W2mef was not. These results show that GIA, as well as its association with protection from malaria, is dependent on theP. falciparumline and can be explained by differences in erythrocyte invasion phenotypes between parasite lines. Our study contributes knowledge on the biological importance of growth inhibition and the potential influence ofP. falciparumerythrocyte invasion phenotypic differences on its relationship to protective immunity against malaria.

Sign in / Sign up

Export Citation Format

Share Document