scholarly journals Nine new compounds from the root bark of Lycium chinense and their α-glucosidase inhibitory activity

RSC Advances ◽  
2017 ◽  
Vol 7 (2) ◽  
pp. 805-812 ◽  
Author(s):  
Ya-Nan Yang ◽  
Ya-Wen An ◽  
Zhi-Lai Zhan ◽  
Jing Xie ◽  
Jian-Shuang Jiang ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Root Bark ◽  
Lycium Chinense ◽  
New Compounds ◽  
Solanaceae Family ◽  
Deciduous Shrub

Lycium chinense Mill. is a deciduous shrub in the Solanaceae family that is known for its fruits (Lycii fructus) and root bark (Lycii cortex).

scholarly journals Modifications on the Tetrahydroquinoline Scaffold Targeting a Phenylalanine Cluster on GPER as Antiproliferative Compounds against Renal, Liver and Pancreatic Cancer Cells

2021 ◽  
Vol 14 (1) ◽  
pp. 49
Author(s):  
David Méndez-Luna ◽  
Loreley Araceli Morelos-Garnica ◽  
Juan Benjamín García-Vázquez ◽  
Martiniano Bello ◽  
Itzia Irene Padilla-Martínez ◽  
...  
Keyword(s):  
Binding Site ◽  
Cell Lines ◽  
Cancer Cell ◽  
Inhibitory Activity ◽  
In Silico ◽  
Cancer Cell Lines ◽  
Pancreatic Cancer Cells ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
New Compounds

The implementation of chemo- and bioinformatics tools is a crucial step in the design of structure-based drugs, enabling the identification of more specific and effective molecules against cancer without side effects. In this study, three new compounds were designed and synthesized with suitable absorption, distribution, metabolism, excretion and toxicity (ADME-tox) properties and high affinity for the G protein-coupled estrogen receptor (GPER) binding site by in silico methods, which correlated with the growth inhibitory activity tested in a cluster of cancer cell lines. Docking and molecular dynamics (MD) simulations accompanied by a molecular mechanics/generalized Born surface area (MMGBSA) approach yielded the binding modes and energetic features of the proposed compounds on GPER. These in silico studies showed that the compounds reached the GPER binding site, establishing interactions with a phenylalanine cluster (F206, F208 and F278) required for GPER molecular recognition of its agonist and antagonist ligands. Finally, a 3-(4,5-dimethylthiazol-2-yl)2,5-diphenyltetrazolium bromide (MTT) assay showed growth inhibitory activity of compounds 4, 5 and 7 in three different cancer cell lines—MIA Paca-2, RCC4-VA and Hep G2—at micromolar concentrations. These new molecules with specific chemical modifications of the GPER pharmacophore open up the possibility of generating new compounds capable of reaching the GPER binding site with potential growth inhibitory activities against nonconventional GPER cell models.

Two Ceramides from Tanacetum artemesioides

2004 ◽  
Vol 59 (3) ◽  
pp. 329-333 ◽  
Author(s):  
Viqar U. Ahmad ◽  
Javid Hussain ◽  
Hidayat Hussain ◽  
Umar Farooq ◽  
Erum Akber ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Structure Elucidation ◽  
2D Nmr ◽  
Nmr Analysis ◽  
New Compounds

Two new ceramides have been isolated from Tanacetum artemisioides, besides the known constituents β -sitosterol and β -sitosterol glycoside. The structure elucidation of the isolated new compounds was based primarily on 1D and 2D NMR analysis, including COSY, HMQC, HMBC correlations. The compound 1 and 2 showed inhibitory activity against acetylcholinesterase

Jatrophainolides A–C, new cembrane-type diterpenoids with PTP1B inhibitory activity from the root bark of Jatropha integerrima

2020 ◽  
Vol 36 ◽  
pp. 166-170
Author(s):  
Dong-Bo Zhang ◽  
Zheng Wang ◽  
Yan-Ni Liang ◽  
Jin-Gao Yu ◽  
Zhen Zhang ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Root Bark

New 2-arylbenzofurans from the root bark of Artocarpus gomezianus and their α-glucosidase inhibitory activity

2017 ◽  
Vol 33 (10) ◽  
pp. 1436-1441 ◽  
Author(s):  
Poomraphie Nuntawong ◽  
Virunh Kongkatitham ◽  
Kittisak Likhitwitayawuid ◽  
Wanwimon Mekboonsonglarp ◽  
Suchada Sukrong ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Root Bark

Nano-cuprous oxide catalyzed one-pot synthesis of a carbazole-based STAT3 inhibitor: a facile approach via intramolecular C–N bond formation reactions

RSC Advances ◽  
2016 ◽  
Vol 6 (43) ◽  
pp. 36775-36785 ◽  
Author(s):  
C. P. Baburajeev ◽  
Chakrabhavi Dhananjaya Mohan ◽  
Govindagouda S. Patil ◽  
Shobith Rangappa ◽  
Vijay Pandey ◽  
...  
Keyword(s):  
Cuprous Oxide ◽  
Inhibitory Activity ◽  
Bond Formation ◽  
One Pot ◽  
Carbazole Derivatives ◽  
One Pot Synthesis ◽  
The One ◽  
New Compounds ◽  
Bond Formation Reactions

In this study, we report the one-pot synthesis of substituted carbazole derivatives using nano cuprous oxide as a catalyst and demonstrated the STAT3 inhibitory activity of new compounds.

scholarly journals Propolis Components and Biological Activities from Stingless Bees Collected on South Sulawesi, Indonesia

2020 ◽  
Vol 27 (1) ◽  
pp. 82
Author(s):  
Ryo Miyata ◽  
Muhamad Sahlan ◽  
Yoshinobu Ishikawa ◽  
Hiroshi Hashimoto ◽  
Sari Honda ◽  
...  
Keyword(s):  
Abscisic Acid ◽  
Inhibitory Activity ◽  
Stingless Bees ◽  
Spectroscopic Analysis ◽  
Biological Activities ◽  
X Ray ◽  
X Ray Crystallography ◽  
South Sulawesi ◽  
Ic50 Value ◽  
New Compounds

Three new compounds, namely sulabiroins A (1) and B (2), and 2',3'-dihydro-3'-hydroxypapuanic acid (3), were isolated from the propolis of stingless bees (Tetragonula aff. biroi) collected on South Sulawesi, Indonesia. In addition, ten known compounds, (–)-papuanic acid (4), (–)-isocalolongic acid (5), isopapuanic acid (6), isocalopolyanic acid (7), glyasperin A (8), broussoflavonol F (9), (2S)-5,7-dihydroxy-4'-methoxy-8-prenylflavanone (10), isorhamnetin (11), (1'S)-2-trans,4-trans-abscisic acid (12), and (1'S)-2-cis,4-trans-abscisic acid (13) were identified. The structures of the new and known compounds were determined by spectroscopic analysis. The absolute configurations of sulabiroins A (1) and B (2) were determined by X-ray crystallography analysis and ECD calculation, respectively. The propolis from stingless bee (Tetragonula aff. biroi) collected on South Sulawesi contained compounds not present in propolis from other regions. Sulabiroin A (1) and isorhamnetin (11) were examined for xanthine oxidase (XO) inhibitory activity as one of biological activities; isorhamnetin (11) exhibited potent XO inhibitory activity, with an IC50 value of 3.9 µm.

scholarly journals Novel Thiosemicarbazone Derivatives: In Vitro and In Silico Evaluation as Potential MAO-B Inhibitors

Molecules ◽  
2021 ◽  
Vol 26 (21) ◽  
pp. 6640
Author(s):  
Derya Osmaniye ◽  
Berkant Kurban ◽  
Begüm Nurpelin Sağlık ◽  
Serkan Levent ◽  
Yusuf Özkay ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Active Sites ◽  
Docking Study ◽  
Fluorometric Method ◽  
Mao B ◽  
Micromolar Concentration ◽  
Ic50 Value ◽  
Competitive Inhibitors ◽  
New Compounds

MAO-B inhibitors are frequently used in the treatment of neurodegenerative diseases such as Parkinson’s and Alzheimer’s. Due to the limited number of compounds available in this field, there is a need to develop new compounds. In the recent works, it was shown that various thiosemicarbazone derivatives show hMAO inhibitory activity in the range of micromolar concentration. It is thought that benzofuran and benzothiophene structures may mimic structures such as indane and indanone, which are frequently found in the structures of such inhibitors. Based on this view, new benzofuran/benzothiophene and thiosemicarbazone hybrid compounds were synthesized, characterized and screened for their hMAO-A and hMAO-B inhibitory activity by an in vitro fluorometric method. The compounds including methoxyethyl substituent (2b and 2h) were found to be the most effective agents in the series against MAO-B enzyme with the IC50 value of 0.042 ± 0.002 µM and 0.056 ± 0.002 µM, respectively. The mechanism of hMAO-B inhibition of compounds 2b and 2h was investigated by Lineweaver–Burk graphics. Compounds 2b and 2h were reversible and non-competitive inhibitors with similar inhibition features as the substrates. The Ki values of compounds 2b and 2h were calculated as 0.035 µM and 0.046 µM, respectively, with the help of secondary plots. The docking study of compound 2b and 2h revealed that there is a strong interaction between the active sites of hMAO-B and analyzed compound.

scholarly journals New Fluorene Derivatives from Dendrobium gibsonii and Their α-Glucosidase Inhibitory Activity

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 4931
Author(s):  
May Thazin Thant ◽  
Nutputsorn Chatsumpun ◽  
Wanwimon Mekboonsonglarp ◽  
Boonchoo Sritularak ◽  
Kittisak Likhitwitayawuid
Keyword(s):  
Kinetic Study ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Enzyme Kinetic ◽  
Whole Plant ◽  
Noncompetitive Inhibitor ◽  
Inhibitory Activities ◽  
New Compounds ◽  
Enzyme Kinetic Study

Two new compounds, dihydrodengibsinin (1) and dendrogibsol (2), were isolated from the whole plant of Dendrobium gibsonii, together with seven known compounds (3–9). The structures of the new compounds were elucidated by their spectroscopic data. All these isolates were evaluated for their α-glucosidase inhibitory activities. Dendrogibsol (2) and lusianthridin (7) showed strong α-glucosidase inhibitory activity when compared with acarbose. An enzyme kinetic study revealed that dendrogibsol (2) is a noncompetitive inhibitor of α-glucosidase.

scholarly journals Cytotoxic Prenylated Polyphenolic Compounds from Maackia amurensis Root Bark

2017 ◽  
Vol 12 (7) ◽  
pp. 1934578X1701200
Author(s):  
Marina V. Veselova ◽  
Sergey A. Fedoreyev ◽  
Darya V. Tarbeeva ◽  
Nadezda I. Kulesh ◽  
Anatoliy I. Kalinovskiy ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Hela Cells ◽  
Human Cancer ◽  
Polyphenolic Compounds ◽  
Root Bark ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Maackia Amurensis ◽  
New Compounds

Two new prenylated flavanones, isomaackiaflavanone A (1), isomaackiaflavanone B (2) and a new prenylated stilbene maackiastilbene (3), along with five known flavanones were isolated from the root bark of Maackia amurensis using repeated column chromatography on silica gel, Sephadex LH-20 and octadecyl silica (ODS-A) sorbents. The structures of the new compounds were elucidated by HPLC–PDA–MS, HR-ESI-MS, 1H, 13C, 1H–1H COSY, HSQC, ROESY and HMBC NMR analyses. The cytotoxicity of compounds 1–2, 4–8 against two human cancer cell lines HeLa and SK-MEL-5 was tested using the MTS method. Compounds 4, 6 and 8 showed the strongest cytotoxic activity among the compounds tested with IC50 values of 6.5, 8.8 and 7.7 μM, against SK-MEL-5 cells and 8.2, 18.8 and 12 μM against HeLa cells, respectively.

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