scholarly journals A New Ellagic Acid Glycoside and DNA Topoisomerase IB Inhibitory Activity of Saponins from Putranjiva roxburghii

2014 ◽  
Vol 9 (5) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Ashish Kumar ◽  
Somenath Roy Chowdhury ◽  
Tulika Chakrabarti ◽  
Hemanta K Majumdar ◽  
Tarun Jha ◽  
...  
Keyword(s):  
Spectral Analysis ◽  
Methyl Ester ◽  
Ellagic Acid ◽  
Inhibitory Activity ◽  
Stem Bark ◽  
Chemical Investigation ◽  
Dna Topoisomerase ◽  
Topoisomerase Ib ◽  
Putranjiva Roxburghii ◽  
First Time

Chemical investigation of the stem bark and leaves of Putranjiva roxburghii has resulted in the isolation of a new ellagic acid glycoside (5) along with four saponins (1-4). The structures of the isolated compounds were established by detailed spectral analysis. Incidentally putranoside-A methyl ester (4) has been isolated for the first time from this species and the saponins (1-4) exhibited potent DNA topoisomerase IB inhibitory activity.

scholarly journals Saracoside: A New Lignan Glycoside from Saraca indica, a Potential Inhibitor of DNA Topoisomerase IB

2012 ◽  
Vol 7 (6) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Tulika Mukherjee ◽  
Sayan Chowdhury ◽  
Ashish Kumar ◽  
Hemanta K Majumder ◽  
Parasuraman Jaisankar ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Stem Bark ◽  
Chemical Investigation ◽  
Dna Topoisomerase ◽  
Potential Inhibitor ◽  
Topoisomerase Ib ◽  
Lignan Glycoside ◽  
Lignan Glycosides ◽  
First Time

Chemical investigation of the stem bark of Saraca indica has resulted in the isolation of a new lignan glycoside, saracoside, along with four known lignan glycosides lyoniside, icariside E3, (+)5′methoxyisolarciresinol-9′- O-β-D-glucopyranoside and nudiposide, and a phenolic glucopyranoside, 3,4,5– trimethoxyphenyl-β-D-glucopyranoside, which has been isolated for the first time from this species. The isolated lignan glycosides exhibit potent DNA topoisomerase IB inhibitory activity.

scholarly journals Anthocephaline, a New Indole Alkaloid and Cadambine, a Potent Inhibitor of DNA Topoisomerase IB of Leishmania donovani (LdTOP1LS), Isolated from Anthocephalus cadamba

2015 ◽  
Vol 10 (2) ◽  
pp. 1934578X1501000
Author(s):  
Ashish Kumar ◽  
Somenath Roy Chowdhury ◽  
Kumar Kalyan Jatte ◽  
Tulika Chakrabarti ◽  
Hemanta K Majumder ◽  
...  
Keyword(s):  
Spectral Analysis ◽  
Inhibitory Activity ◽  
Leishmania Donovani ◽  
Potent Inhibitor ◽  
Indole Alkaloid ◽  
2D Nmr ◽  
Stem Bark ◽  
Dna Topoisomerase ◽  
Topoisomerase Ib ◽  
Anthocephalus Cadamba

Chemical investigation of the stem bark of Anthocephalus cadamba has resulted in the isolation of anthocephaline (1), a new indole alkaloid, along with strictosamide (2), vincosamide (3) and cadambine (4). The structures of the isolated alkaloids (1-4) were established by detailed 2D NMR spectral analysis. Cadambine (4) exhibited potent DNA topoisomerase IB inhibitory activity.

scholarly journals An Ellagic Acid Derivative and Its Antioxidant Activity of Stem Bark Extracts of Syzygium polycephalum Miq. (Myrtaceae)

2018 ◽  
Vol 18 (1) ◽  
pp. 26
Author(s):  
Tukiran Tukiran ◽  
Andika Pramudya Wardana ◽  
Nurul Hidayati ◽  
Kuniyoshi Shimizu
Keyword(s):  
Antioxidant Activity ◽  
Acid Derivative ◽  
Ellagic Acid ◽  
Methanol Extract ◽  
Stem Bark ◽  
Spectroscopic Studies ◽  
Chloroform Fraction ◽  
Ic50 Value ◽  
Isolated Compound ◽  
First Time

The investigation of the Syzygium polycephalum Miq. (Myrtaceae) aimed to assess the phytochemical contents and antioxidant activity of the chloroform fraction. In this study, the fraction was obtained from methanol extract of S. polycephalum stem bark partitionated by chloroform. An ellagic acid derivative was successively isolated from the chloroform fraction. The molecular structure of isolated compound was elucidated and established as 3,4,3’-tri-O-methylellagic acid through extensive spectroscopic studies including UV-Vis, FTIR, NMR and LC-MS analyses and by comparison with literature data. The finding of the isolated compound is the first time from the plant, although the isolated compound previously have been found in the other Syzygium species such as S. cumini together with ellagic acid and 3,3’-di-O-methylellagic acid. The chloroform fraction, isolated compound, and vitamin C showed antioxidant activity against 2,2’-diphenyl-1-picrylhydrazyl (DPPH) with IC50 value of 163.6, 72.1, and 11.5 μg/mL, respectively.

scholarly journals A Bioactive Diterpene from Entada Abyssinica

2007 ◽  
Vol 2 (1) ◽  
pp. 1934578X0700200 ◽  
Author(s):  
Alembert T. Tchinda ◽  
Victorine Fuendjiep ◽  
Yalemtsehay Mekonnen ◽  
Bernadette B. Ngo ◽  
Ermias Dagne
Keyword(s):  
Methyl Ester ◽  
Stem Bark ◽  
Acetone Extract ◽  
Clerodane Diterpenoids ◽  
Antileishmanial Activities ◽  
First Time

Three clerodane diterpenoids, 8S-kolavic acid 18-methyl ester (1), 8S-kolavic acid 15-methyl ester (2) and 8S-kolavenol (3) were isolated from the acetone extract of the stem bark of Entada abyssinica along with trans-communic acid (4) and 1-octacosanol. Their structures were established mainly based on 1D (1H, 13C and DEPT) and 2D (1H-1H COSY, HSQC and HMBC) NMR experiments. Compound 1, described here for the first time, showed strong antimicrobial and moderate antileishmanial activities.

scholarly journals α-Glucosidase Inhibitory Activity of Resin From Sakhalin fir Tree (Abies sachalinensis) and its Bioactive Compounds

2019 ◽  
Vol 14 (6) ◽  
pp. 1934578X1985846
Author(s):  
Toshinori Nakagawa ◽  
Ahmed Ashour ◽  
Yhiya Amen ◽  
Yurie Koba ◽  
Koichiro Ohnuki ◽  
...  
Keyword(s):  
Methyl Ester ◽  
High Activity ◽  
Inhibitory Activity ◽  
Point Of View ◽  
Functional Health ◽  
Abies Sachalinensis ◽  
Dioic Acid ◽  
Glucosidase Inhibitors ◽  
First Time

This study investigated in vitro the α-glucosidase inhibitory activity of resin from the Sakhalin fir tree ( Abies sachalinensis). The resin showed extremely high activity (IC50 of 17.3 µg/mL). We isolated 8 compounds from the resin and identified them. All of the compounds isolated from A. sachalinensis resin are reported for the first time in the present study. In an α-glucosidase inhibitory assay, 6 compounds—(holophyllane C (1), (−) -(24 E)-23-oxo-3,4- seco-9β H-lanosta-4(28),6,8(14),24-tetraen-3,26-dioic acid (2), abiesonic acid (3), (−) -(24 E)-23-oxo-3,4- seco-9β H-lanosta-4(28),7,24-triene-3,26-dioic acid (4), 3,4- seco-4(28),6,8(14),22Z,24-mariesapentaen-26,23-olide-3-oic acid (5), and (−) -abiesonic acid 3-methyl ester (6))—showed high activity (their IC50 values were 25.1, 20.9, 82.4, 20.5, 27.3, and 20.5 µg/mL, respectively). These compounds should contribute to the resin’s α-glucosidase inhibitory activity. From an industrial point of view, these findings provide new data to support that the resin of A. sachalinensis is a rich source of α-glucosidase inhibitors, which are highly valuable for their potential to be developed as functional health foods.

scholarly journals In Vitro and In Silico Characterization of an Antimalarial Compound with Antitumor Activity Targeting Human DNA Topoisomerase IB

2021 ◽  
Vol 22 (14) ◽  
pp. 7455
Author(s):  
Bini Chhetri Soren ◽  
Jagadish Babu Dasari ◽  
Alessio Ottaviani ◽  
Beatrice Messina ◽  
Giada Andreotti ◽  
...  
Keyword(s):  
Enzyme Reaction ◽  
Dna Topoisomerase ◽  
Human Dna ◽  
Topoisomerase Ib ◽  
Topological State ◽  
Cleavage Step ◽  
Dynamics Simulations ◽  
In Silico Characterization ◽  
Dna Complex

Human DNA topoisomerase IB controls the topological state of supercoiled DNA through a complex catalytic cycle that consists of cleavage and religation reactions, allowing the progression of fundamental DNA metabolism. The catalytic steps of human DNA topoisomerase IB were analyzed in the presence of a drug, obtained by the open-access drug bank Medicines for Malaria Venture. The experiments indicate that the compound strongly and irreversibly inhibits the cleavage step of the enzyme reaction and reduces the cell viability of three different cancer cell lines. Molecular docking and molecular dynamics simulations suggest that the drug binds to the human DNA topoisomerase IB-DNA complex sitting inside the catalytic site of the enzyme, providing a molecular explanation for the cleavage-inhibition effect. For all these reasons, the aforementioned drug could be a possible lead compound for the development of an efficient anti-tumor molecule targeting human DNA topoisomerase IB.

scholarly journals Cyclic Lipopeptides with Herbicidal and Insecticidal Activities Produced by Bacillus clausii DTM1

2015 ◽  
Vol 10 (12) ◽  
pp. 1934578X1501001 ◽  
Author(s):  
Da-Le Guo ◽  
Bo Wan ◽  
Shi-Ji Xiao ◽  
Sarah Allen ◽  
Yu-Cheng Gu ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Natural Product ◽  
Fermentation Broth ◽  
Cyclic Lipopeptides ◽  
Bacillus Clausii ◽  
Cyclic Lipopeptide ◽  
Lipopeptide Biosurfactants ◽  
First Time ◽  
Insecticidal Activities

Seven cyclic lipopeptide biosurfactants (1–7) were isolated for the first time from the fermentation broth of endophytic Bacillus clausii DTM1 and were identified as anteisoC13[Val7] surfactin-(L-Glu)-O-methyl-ester (1), anteisoC12[Val7] surfactin (2), anteisoC15[Val7] surfactin (3), isoC14[Leu7] surfactin (4), anteisoC12[Leu7] surfactin (5), nC13[Leu7] surfactin (6), and anteisoC14[Leu7] surfactin-(L-Glu)-O-methyl-ester (7); 1 has not been isolated before as a natural product from any source. Plate-based herbicide and insecticide bioassays showed that all compounds exhibited interesting insecticidal and herbicidal activities.

scholarly journals First total synthesis of the (±)-2-methoxy-6-heptadecynoic acid and related 2-methoxylated analogs as effective inhibitors of the Leishmania topoisomerase IB enzyme

2012 ◽  
Vol 84 (9) ◽  
pp. 1867-1875 ◽  
Author(s):  
Néstor M. Carballeira ◽  
Michelle Cartagena ◽  
Fengyu Li ◽  
Zhongfang Chen ◽  
Christopher F. Prada ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Fatty Acid ◽  
Total Synthesis ◽  
Leishmania Donovani ◽  
Dna Topoisomerase ◽  
Triple Bonds ◽  
Weak Intermolecular Interactions ◽  
Topoisomerase Ib ◽  
Effective Inhibition ◽  
Acetylenic Fatty Acid

The fatty acids (±)-2-methoxy-6Z-heptadecenoic acid, (±)-2-methoxy-6-hepta-decynoic acid, and (±)-2-methoxyheptadecanoic acid were synthesized and their inhibitory activity against the Leishmania DNA topoisomerase IB enzyme (LdTopIB) determined. Both 2-OMe-17:1 fatty acids were synthesized from 4-bromo-1-pentanol, the olefinic fatty acid in 10 steps and in 7 % overall yield, while the acetylenic fatty acid in 7 steps and in 14 % overall yield. The 2-OMe-17:0 acid was prepared in 6 steps and in 42 % yield from 1-hexa-decanol. The 2-OMe-17:1 acids inhibited LdTopIB, with the acetylenic acid displaying an EC50 = 16.6 ± 1.1 μM, but the 2-OMe-17:0 acid did not inhibit LdTopIB. The (±)-2-methoxy-6Z-heptadecenoic acid preferentially inhibited LdTopIB over the human TopIB enzyme. Unsaturation seems to be a prerequisite for effective inhibition, rationalized in terms of weak intermolecular interactions between the active site of LdTopIB and either the double or triple bonds of the fatty acids. Toxicity toward Leishmania donovani promastigotes was also investigated, resulting in the order acetylenic > olefinic > saturated with the (±)-2-methoxy-6-heptadecynoic acid displaying an EC50 = 74.0 ± 17.1 μM. Our results indicate that α-methoxylation decreases the toxicity of C17:1 fatty acids toward L. donovani promastigotes, but improves their selectivity index.

scholarly journals Gimatecan and other camptothecin derivatives poison Leishmania DNA-topoisomerase IB leading to a strong leishmanicidal effect

2013 ◽  
Vol 85 (10) ◽  
pp. 1433-1440 ◽  
Author(s):  
Christopher F. Prada ◽  
Raquel Álvarez-Velilla ◽  
Rafael Balaña-Fouce ◽  
Carlos Prieto ◽  
Estefania Calvo-Álvarez ◽  
...  
Keyword(s):  
Dna Topoisomerase ◽  
Topoisomerase Ib
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