Graphisins A and B from the Lichen Graphis tetralocularis

2009 ◽  
Vol 62 (4) ◽  
pp. 389 ◽  
Author(s):  
Pattama Pittayakhajonwut ◽  
Veera Sri-indrasutdhi ◽  
Aibrohim Dramae ◽  
Sanisa Lapanun ◽  
Rapheephat Suvannakad ◽  
...  
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Cell Lines ◽  
Inhibitory Concentration ◽  
Antitubercular Activity ◽  
Antimycobacterial Activity ◽  
Chemical Investigation ◽  
Crude Extracts ◽  
Ic50 Values

Crude extracts of the lichen Graphis tetralocularis exhibited antimycobacterial activity, with minimum inhibitory concentration (MIC) values in a range of 100–200 μg mL–1. Chemical investigation of the broth led to the isolation of acremonidin E (1) and graphisins A (2) and B (3). Acremonidin E (1) displayed antitubercular activity with MIC values of 50 μg mL–1 and showed cytotoxicity against BC, KB, and NCI-H187 cell lines with IC50 values of 12.79–27.12 μg mL–1, whereas graphisins A (2) and B (3) were inactive to these tests.

Synthesis of carbohydrate-substituted isoxazoles and evaluation of their antitubercular activity

2017 ◽  
Vol 23 (3) ◽  
pp. 225-229 ◽  
Author(s):  
Khaoula Hajlaoui ◽  
Ahlem Guesmi ◽  
Naoufel Ben Hamadi ◽  
Moncef Msaddek
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Minimum Inhibitory Concentration ◽  
Bacterial Strain ◽  
Inhibitory Concentration ◽  
Cycloaddition Reaction ◽  
Antitubercular Activity ◽  
Antimycobacterial Activity ◽  
Dipolar Cycloaddition ◽  
Nitrile Oxides ◽  
Mycobacterium Tuberculosis H37rv

AbstractEight new sugar-substituted isoxazoles were synthesized by a 1,3-dipolar cycloaddition reaction of aromatic nitrile oxides with carbohydrate-substituted alkynes. Products were screened for antimycobacterial activity against the Mycobacterium tuberculosis H37Rv strain. Four compounds, 5e–h, significantly inhibit growth of the bacterial strain with a minimum inhibitory concentration (MIC) of 3.125 μg/mL.

New Groups of Potential Antituberculotics: Bis(1-aryltetrazol-5-yl) Disulfides. Structure Activity Relationship

1994 ◽  
Vol 59 (1) ◽  
pp. 234-238 ◽  
Author(s):  
Karel Waisser ◽  
Jiří Kuneš ◽  
Alexandr Hrabálek ◽  
Želmíra Odlerová
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Antimycobacterial Activity ◽  
Activity Relationship ◽  
Active Derivative ◽  
Structure Activity ◽  
Medium Activity ◽  
Substituent Constants ◽  
Atypical Strains

Oxidation of 1-aryltetrazole-5-thiols afforded bis(1-aryltetrazol-5-yl) disulfides. The compounds were tested for antimycobacterial activity against Mycobacterium tuberculosis, M. kansasii, M. avium and M. fortuitum. In the case of M. tuberculosis, the logarithm of minimum inhibitory concentration showed a parabolic dependence on hydrophobic substituent constants. Although the compounds exhibited low to medium activity, the most active derivative, bis(4-chlorophenyltetrazol-5-yl) disulfide (III) was more effective against atypical strains than are the commercial tuberculostatics used as standards.

scholarly journals New Antimalarial and Antimicrobial Tryptamine Derivatives from the Marine Sponge Fascaplysinopsis reticulata

Marine Drugs ◽  
2019 ◽  
Vol 17 (3) ◽  
pp. 167 ◽  
Author(s):  
Pierre-Eric Campos ◽  
Emmanuel Pichon ◽  
Céline Moriou ◽  
Patricia Clerc ◽  
Rozenn Trépos ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Minimum Inhibitory Concentration ◽  
Marine Sponge ◽  
Nmr Spectra ◽  
Inhibitory Concentration ◽  
Chemical Study ◽  
2D Nmr ◽  
Antimicrobial Activities ◽  
2D Nmr Spectra ◽  
Ic50 Values

Chemical study of the CH2Cl2-MeOH (1:1) extract of the sponge Fascaplysinopsis reticulata collected in Mayotte highlighted three new tryptophan derived alkaloids, 6,6′-bis-(debromo)-gelliusine F (1), 6-bromo-8,1′-dihydro-isoplysin A (2) and 5,6-dibromo-8,1′-dihydro-isoplysin A (3), along with the synthetically known 8-oxo-tryptamine (4) and the three known molecules from the same family, tryptamine (5), (E)-6-bromo-2′-demethyl-3′-N-methylaplysinopsin (6) and (Z)-6-bromo-2′-demethyl-3′-N-methylaplysinopsin (7). Their structures were elucidated by 1D and 2D NMR spectra and HRESIMS data. All compounds were evaluated for their antimicrobial and their antiplasmodial activities. Regarding antimicrobial activities, the best compounds are (2) and (3), with minimum inhibitory concentration (MIC) of 0.01 and 1 µg/mL, respectively, towards Vibrio natrigens, and (5), with MIC values of 1 µg/mL towards Vibrio carchariae. In addition the known 8-oxo-tryptamine (4) and the mixture of the (E)-6-bromo-2′-demethyl-3′-N-methylaplysinopsin (6) and (Z)-6-bromo-2′-demethyl-3′-N-methylaplysinopsin (7) showed moderate antiplasmodial activity against Plasmodium falciparum with IC50 values of 8.8 and 8.0 µg/mL, respectively.

scholarly journals Chemical Constituents and Derivatization of Melodorinol from the Roots of Melodorum fruticosum

2015 ◽  
Vol 10 (4) ◽  
pp. 1934578X1501000
Author(s):  
Siriwat Hongnak ◽  
Jongkolnee Jongaramruong ◽  
Suttira Khumkratok ◽  
Pongpun Siriphong ◽  
Santi Tip-pyang
Keyword(s):  
Cell Lines ◽  
Spectroscopic Data ◽  
Chemical Constituents ◽  
Chemical Investigation ◽  
Crude Extracts ◽  
First Time ◽  
Mcf 7

Chemical investigation of the CH2Cl2 and MeOH crude extracts of the roots of Melodorum fruticosum Lour. led to the isolation of 15 known compounds, of which 5, 10, and 12-15 are reported for the first time from this plant. In addition, melodorinol (7) was derivatized to afford six new (7a-7d and 7f-7g) analogues and one known compound (7e). Their structures were identified on the basic of spectroscopic data. Most of them were evaluated for their cytotoxicity against KB, HeLa, MCF-7 and HepG-2 cell lines. Compounds 4 and 7b were the most potent to all cell lines.

scholarly journals Antioxidant, Antimicrobial, Antidiabetic and Cytotoxic Activity of Crocus sativus L. Petals

2020 ◽  
Vol 10 (4) ◽  
pp. 1519
Author(s):  
Adil Farooq Wali ◽  
Houda Ahmed Abou Alchamat ◽  
Huda Khaled Hariri ◽  
Bushra Khaled Hariri ◽  
Godfred A. Menezes ◽  
...  
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Cytotoxic Activity ◽  
Inhibitory Concentration ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Crocus Sativus ◽  
Antidiabetic Activity ◽  
Ic50 Values ◽  
Crocus Sativus L

The purpose of this research is to examine in vitro antioxidant, antimicrobial, antidiabetic and cytotoxic efficacy of different extracts of Crocus sativus L. petals. Antioxidant activity of extracts was assessed by DPPH and ABTS (2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) assay. Among all extracts, ethanol (SPE) had the maximum radical scavenging activity with IC50 values 86.63 ± 7.53 μg/mL. The antimicrobial activity was determined by the evaluation of the minimum inhibitory concentration using the agar well plate procedure. The most effective extract was SPE with a minimum inhibitory concentration varying between 500 µg/mL, 250 µg/mL, 125 µg/mL, 62.5 µg/mL, 31.25 µg/mL, 15.63 µg/mL. Cytotoxic activity was tested against MDA-MB-231 cell lines using the MTT method whereas, antidiabetic activity was evaluated using an alpha-glucosidase inhibition assay. All extracts were found to have significant antidiabetic activity.

scholarly journals SYNTHESIS AND ANTITUBERCULAR ACTIVITY OF PIPERIDINE AND MORPHOLINE 1, 8 NAPHTHYRIDINE ANALOGUES

2016 ◽  
Vol 8 (12) ◽  
pp. 252 ◽  
Author(s):  
Muwaffag Badawneh ◽  
Jalal Aljamal
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Inhibitory Concentration ◽  
Antitubercular Activity ◽  
Antimycobacterial Activity ◽  
Significant Activity ◽  
Reference Drug ◽  
Novel Drugs ◽  
Elemental Analyses ◽  
Antimycobacterial Agents

<p><strong>Objective: </strong>The search for new, potentially useful antimycobacterial agents. In continuation with our previous screening for the discovery of novel drugs for tuberculosis, a new series of 1,8-naphthyridines derivatives were synthesized and evaluated <em>in vitro </em>for antimycobacterial activity against <em>Mycobacterium tuberculosis </em>H37Rv.</p><p><strong>Methods: </strong>Several 4-morpholinomethyl-1.8-naphthyridine derivatives have been synthesized in excellent yields. The synthesized compounds were characterized by spectroscopic methods as well as elemental analyses. They were screened for their antimycobacterial activity. The growth was monitored radiometrically in 7H12 broth with the BACTEC 460 TB system. The minimum inhibitory concentration (MIC) was determined for compounds that demonstrated ≥ 90% growth inhibition in the primary screening.</p><p><strong>Results: </strong>The obtained data suggested that all compounds showed significant activity against <em>Mycobacterium tuberculosis </em>H37Rv<em> </em>compared to the standard reference drug. Analogues (6-11) having heterocyclic groups in position 7 were the most potent of those we tested.</p><p><strong>Conclusion: </strong>These findings clearly identify the 1,8-naphthyridine analogue (10) with a 6-amino-2-(4'-methoxy benzylamine-4-morpholinomethyl-7-morpholino-substituent as promising anti-tubercular agents possessing significant activity against <em>Mycobacterium tuberculosis </em>H37Rv</p>

scholarly journals Investigation of Copaifera genus as a new source of antimycobaterial agents

2020 ◽  
Vol 6 (7) ◽  
pp. FSO587
Author(s):  
Jéssica Aparecida Alves ◽  
Fariza Abrão ◽  
Thaís da Silva Moraes ◽  
Jaqueline Lopes Damasceno ◽  
Marcos Fernando dos Santos Moraes ◽  
...  
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Plant Extracts ◽  
Concentration Index ◽  
Inhibitory Concentration ◽  
Antimycobacterial Activity ◽  
Synergistic Action ◽  
Fractional Inhibitory Concentration ◽  
Fractional Inhibitory Concentration Index ◽  
Copaifera Langsdorffii

Aim: This paper reports on the antimycobacterial activity of the oleoresins and extracts obtained from Copaifera spp. Materials & methods: The minimum inhibitory concentration (MIC) and fractional inhibitory concentration index techniques helped to evaluate the effect of these oleoresins and extracts against six strains of mycobacteria that cause tuberculosis. Results & conclusion: Among the assayed oleoresins and plant extracts, the Copaifera langsdorffii, Copaifera duckei, Copaifera reticulata and Copaifera trapezifolia oleoresins provided the lowest MIC values against some of the tested strains. The combination of Copaifera spp. samples with isoniazid did not evidence any synergistic action. Some Copaifera spp. oleoresins may represent a future source for the discovery of new antimycobacterial drugs due to their low MIC values.

scholarly journals Antitubercular and antibacterial activities of isoxazolines derived from natural products: Isoxazolines as inhibitors of Mycobacterium tuberculosis InhA

2021 ◽  
pp. 174751982110478
Author(s):  
Anuchit Phanumartwiwath ◽  
Chatchai Kesornpun ◽  
Sanya Sureram ◽  
Poonpilas Hongmanee ◽  
Pornpan Pungpo ◽  
...  
Keyword(s):  
Natural Products ◽  
Mycobacterium Tuberculosis ◽  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Hydrophobic Interactions ◽  
Acyl Carrier Protein ◽  
Antitubercular Activity ◽  
Antibacterial Activities ◽  
Key Residues ◽  
Derivatives Of

Isoxazoline derivatives of the natural products eugenol, 1’- S-acetoxychavicol acetate and sclareol are prepared through 1,3-dipolar cycloaddition reactions in an aqueous buffered system. The compounds are evaluated for their antitubercular and antibacterial activities. Compounds 2, 2a and 3f display strong antitubercular activity with minimum inhibitory concentration values of 26.68, 17.89 and 14.58 µM, respectively. Furthermore, derivative 3f exhibits antibacterial activity against Bacillus cereus (minimum inhibitory concentration value of 29.16 µM). Isoxazoline derivatives of 1’- S-acetoxychavicol acetate demonstrate improvements in cytotoxicity, and derivative 3f of sclareol demonstrates improved antitubercular and antibacterial activities. Isoxazolines derived from natural products exhibit Mycobacterium tuberculosis enoyl-acyl carrier protein reductase (InhA) inhibitory activity, and molecular modelling predicts that they form hydrogen bonding and hydrophobic interactions with NADH and with the key residues of the InhA binding site.

scholarly journals Bioactive Secondary Metabolites from the Culture of the Mangrove-Derived Fungus Daldinia eschscholtzii HJ004

Marine Drugs ◽  
2019 ◽  
Vol 17 (12) ◽  
pp. 710 ◽  
Author(s):  
Hai-Xia Liao ◽  
Tai-Ming Shao ◽  
Rong-Qing Mei ◽  
Guo-Lei Huang ◽  
Xue-Ming Zhou ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Minimum Inhibitory Concentration ◽  
Secondary Metabolites ◽  
Inhibitory Concentration ◽  
Etoac Extract ◽  
Bioactive Secondary Metabolites ◽  
Ic50 Values ◽  
Mic Value ◽  
Potent Inhibitory Activity

Two new polyketides, 8-O-methylnodulisporin F (1) and nodulisporin H (2), two new naphthoquinones, 5-hydroxy-2-methoxy-6,7-dimethyl-1,4-naphthoquinone (3) and 5-hydroxy-2-methoxynaphtho[9–c]furan-1,4-dione (4), and a new naphthofuran 1,3,8-trimethoxynaphtho[9–c]furan (5), along with five known compounds 4-O-methyl eleutherol (6), 2-acetyl-7-methoxybenzofuran (7), (-)-orthosporin (8), diaporthin (9), and 6-hydroxymellein (10), were obtained from the EtOAc extract of the mangrove-derived fungus Daldinia eschscholtzii HJ004. The structures of the isolated compounds were elucidated by extensive NMR and MS analyses, while the absolute configurations of the stereogenic carbons were established based on experimental and calculated electronic circular dichroism spectra. Compounds 4 and 7 displayed a potent inhibitory activity against α-glucosidase with the IC50 values of 5.7 and 1.1 μg/mL, respectively. Compounds 1 and 2 showed a moderate antibacterial activity against Staphylococcus aureus, methicillin-resistant S. aureus (MRSA) and Bacillus cereus, with minimum inhibitory concentration (MIC) values ranging from 6.25 to 12.5 μg/mL. Compound 3 exhibited antibacterial activity against B. cereus with the MIC value of 12.5 μg/mL.

One New C21 Steroidal Glycosides from the Leaves of Cynanchum hancockianum

2019 ◽  
Vol 16 (7) ◽  
pp. 556-559
Author(s):  
Shubei Yu ◽  
Xixi Lin ◽  
Yi Zheng ◽  
Zheng Wu ◽  
Wei Zheng ◽  
...  
Keyword(s):  
Cell Lines ◽  
Chemical Investigation ◽  
Cytotoxic Activities ◽  
First Report ◽  
Steroidal Glycosides ◽  
Ic50 Values ◽  
Mcf 7

C21 steroids glycosides of various deoxysugars have been emerging from genus of Cynanchum. Besides classical C21 glycosides, many C21 glycosides with seco-ring aglycones attracted the extensive attention of many researchers. We conducted a systematic chemical investigation on Cynanchum hancockianum, which led to the isolation of one new seco-ring C21 steroidal glycosides. The new compound was identified as cynaascyriogenin 3-O-&#946;-D-glucopyranosyl-(1-4)-&#945;-L-cymaropyranosy-(1-4)- &#946;-D-cymaropyranosyl-(1-4)-&#946;-D-cymaropyranoside. The cytotoxic activities of the compound were evaluated using the A549 and MCF-7 cell lines, respectively. The IC50 values of the compound were 41.3 and 67.1&#181;M, respectively. This is the first report on the isolation of seco-ring C21 steroidal glycosides from Cynanchum hancockianum.

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