New Indole Glycosides from Aesculus chinensis var. chekiangensis and Their Neuroprotective Activities

The dried seeds of Aesculus chinensis Bge. var. chekiangensis (Hu et Fang) Fang, called “Suo Luo Zi”, have been used in traditional Chinese medicine. Nevertheless, most studies have been focused on components of less polarity fractions. In this research, twelve indoles, including six new indole glycosides (1–6) as well as six known analogs were isolated from the polar portion which has been seldom studied. This is the first description of N-glucosylated indoles obtained from the genus of Aesculus. Structures of the new compounds (1–6) were elucidated based on comprehensive interpretation of HRESIMS, 1D and 2D NMR. Additionally, the neuroprotective activities of the N-glucosylated indoles were evaluated for the first time indicating that compounds 1–5 and 9–10 exhibited moderate neuroprotective activities. Further cytotoxicity tests of isolates 1–10 on three human tumor cell lines suggested that none of these compounds were cytotoxic (IC50 > 50 μM).

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A Novel Sesquiterpene Polyol Ester from the Celastrus Rosthornianus with Anti-tumor Activities

Natural Product Communications ◽

10.1177/1934578x0600100704 ◽

2006 ◽

Vol 1 (7) ◽

pp. 1934578X0600100 ◽

Cited By ~ 1

Author(s):

Kuiwu Wang ◽

Yuanjiang Pan

Keyword(s):

Tumor Cell ◽

Cell Lines ◽

Human Tumor ◽

2D Nmr ◽

Spectroscopic Techniques ◽

Tumor Cell Lines ◽

Human Tumor Cell ◽

Polyol Ester ◽

Human Tumor Cell Lines ◽

Polyol Esters

A new (1) and a known (2) β-dihydroagarofuran sesquiterpene polyol esters were isolated from Celastrus rosthornianus and their structures were established by 1D- and 2D-NMR spectroscopic techniques. The two compounds exhibited anti-tumor activities against a panel of human tumor cell lines.

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New Triterpene Glycosides from Camptosorus Sibiricus

Natural Product Communications ◽

10.1177/1934578x1000501008 ◽

2010 ◽

Vol 5 (10) ◽

pp. 1934578X1000501

Author(s):

Ning Li ◽

Wan Xiao ◽

Bailing Hou ◽

Xian Li

Keyword(s):

Human Tumor ◽

2D Nmr ◽

Spectroscopic Methods ◽

Tumor Cell Lines ◽

Human Tumor Cell ◽

Human Tumor Cell Lines ◽

Mtt Method ◽

Cycloartane Glycosides ◽

New Compounds

Two new cycloartane glycosides were isolated from the whole herbs of Camptosorus sibiricus Rupr. By means of chemical and spectroscopic methods (1D and 2D NMR, HRMS, ESIMS), the structures were established as (24 R)-3β,7β,24,25,30-pentahydroxycycloartane-30- O-coumaroyl-3- O-β-D-glucopyranosyl-24- O-β-D-glucopyranosyl-(1→6)-β-D-glucopyranoside (1) and (24 R)-3β,7β,24,25,30-pentahydroxy-1-ene-cycloartane 24- O-β-D-glucopyranoside (2). The two new compounds were inactive in vitro against A375-S2 and Hela human tumor cell lines using the MTT method.

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New Cycloartane Glycosides from Camptosorus Sibiricus Rupr

Natural Product Communications ◽

10.1177/1934578x0800300615 ◽

2008 ◽

Vol 3 (6) ◽

pp. 1934578X0800300

Author(s):

Peng Zhang ◽

Yiyu Cheng ◽

Zhongjun Ma

Keyword(s):

Human Tumor ◽

2D Nmr ◽

Spectroscopic Methods ◽

Tumor Cell Lines ◽

Human Tumor Cell ◽

Human Tumor Cell Lines ◽

Mtt Method ◽

Cycloartane Glycosides ◽

New Compounds

Two new cycloartane glycosides were isolated from the whole herbs of Camptosorus sibiricus Rupr.. By means of chemical and spectroscopic methods (IR, 1D- and 2D- NMR, HRMS, ESI-MS), the structures were established as (24 R)-3β,7β,24,25,30-pentahydroxycycloartane 3- O-β-D-glucopyranosyl-24- O-β-D-glucopyranosyl-30- O-β-D-glucopyranoside (1), and (24 R)-3β,7β,24,25,30-pentahydroxycycloartane 3- O-β-D-glucopyranosyl-(1→2)-β-D-glucopyranosyl-24- O-β-D-xylopyranosyl-(1→2)-β-D-glucopyranoside (2). The two new compounds were tested for their cytotoxicity in vitro against human tumor cell lines (A375-S2, Hela) using the MTT method, but both compounds were inactive.

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Anti-tumor Activities of Triterpenes from Syzygium kusukusense

Natural Product Communications ◽

10.1177/1934578x1400901106 ◽

2014 ◽

Vol 9 (11) ◽

pp. 1934578X1400901 ◽

Cited By ~ 3

Author(s):

Li-Yuan Bai ◽

Wei-Yu Lin ◽

Chang-Fang Chiu ◽

Jing-Ru Weng

Keyword(s):

Tumor Cell ◽

Human Tumor ◽

Cytotoxic Activities ◽

Tumor Cell Lines ◽

Human Tumor Cell ◽

High Potency ◽

Human Tumor Cell Lines ◽

Indigenous Plant ◽

First Time ◽

Mcf 7

In this study, we report the isolation from the stem of Syzygium kusukusense of five triterpenes, 2α-hydroxybetulinic acid (1), betulinic acid (2), platanic acid (3), ursolic acid (4), and hyptatic acid A (5). All were identified for the first time from this indigenous plant of Taiwan. Assessment of the cytotoxic activities of these compounds against a panel of human tumor cell lines, including MCF-7 breast, PC-3 prostate, and SCC2095 oral squamous cell cancers, revealed the high potency of compounds 1 (IC50, 5.7 – 7.6 μM) and, especially, 4 (IC50, 1.7 – 3.7 μM) in suppressing cell viability, which warrants further mechanistic investigations.

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Differential Increases in Glutathione S-Transferase Activities in a Range of Multidrug-Resistant Human Tumor Cell Lines

Cancer Communications ◽

10.3727/095535489820875057 ◽

1989 ◽

Vol 1 (6) ◽

pp. 359-365 ◽

Cited By ~ 36

Author(s):

Richard D. H. Whelan ◽

Louise K. Hosking ◽

Alan J. Townsend ◽

Kenneth H. Cowan ◽

Bridget T. Hill

Keyword(s):

Tumor Cell ◽

Cell Lines ◽

Human Tumor ◽

Multidrug Resistant ◽

Tumor Cell Lines ◽

Glutathione S Transferase ◽

Human Tumor Cell ◽

Human Tumor Cell Lines

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Synthesis and Cytotoxicity of New Mannich Bases of 6-[3-(3,4,5-Trimetoxyphenyl)-2- propenoyl]-2(3H)-Benzoxazolone

Letters in Drug Design & Discovery ◽

10.2174/1570180816666190730164952 ◽

2020 ◽

Vol 17 (4) ◽

pp. 512-517

Author(s):

Ognyan Ivanov Petrov ◽

Yordanka Borisova Ivanova ◽

Mariana Stefanova Gerova ◽

Georgi Tsvetanov Momekov

Keyword(s):

Tumor Cell ◽

Cell Lines ◽

Biological Activities ◽

Human Tumor ◽

Mannich Bases ◽

In Vitro Cytotoxicity ◽

Tumor Cell Lines ◽

Human Tumor Cell ◽

Human Tumor Cell Lines

Background: Chemotherapy is one of the mainstays of cancer treatment, despite the serious side effects of the clinically available anticancer drugs. In recent years increasing attention has been directed towards novel agents with improved efficacy and selectivity. Compounds with chalcone backbone have been reported to possess various biological activities such as anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, etc. It was reported that aminomethylation of hydroxy chalcones to the corresponding Mannich bases increased their cytotoxicity. In this context, our interest has been focused on the design and synthesis of the so-called multi-target molecules, containing two or more pharmacophore fragments. Methods: A series of Mannich bases were synthesized by the reaction between 6-[3-(3,4,5- trimethoxyphenyl)-2-propenoyl]-2(3Н)-benzoxazolone, formaldehyde, and a secondary amine. The structures of the compounds were confirmed by elemental analysis, IR and NMR spectra. The new Mannich bases were evaluated for their in vitro cytotoxicity against a panel of human tumor cell lines, including BV-173, SKW-3, K-562, HL-60, HD-MY-Z and MDA-MB-231. The effects of selected compounds on the cellular levels of glutathione (GSH) were determined. Results: The new compounds 4a-e exhibited concentration-dependent cytotoxic effects at micromolar concentrations in MTT-dye reduction assay against a panel of human tumor cell lines, similar to those of starting chalcone 3. The tested agents led to concentration - dependent depletion of cellular GSH levels, whereby the effects of the chalcone prototype 3 and its Mannich base-derivatives were comparable. Conclusion: The highest chemosensitivity to the tested compounds was observed in BV- 173followed by SKW-3 and HL-60 cell lines.

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Anticancer activity of pyrimidodiazepines based on 2-chloro-4-anilinoquinazoline: synthesis, DNA binding and molecular docking

RSC Advances ◽

10.1039/d1ra03509f ◽

2021 ◽

Vol 11 (38) ◽

pp. 23310-23329

Author(s):

Viviana Cuartas ◽

Alberto Aragón-Muriel ◽

Yamil Liscano ◽

Dorian Polo-Cerón ◽

Maria del Pilar Crespo-Ortiz ◽

...

Keyword(s):

Molecular Docking ◽

Dna Binding ◽

Tumor Cell ◽

Anticancer Activity ◽

Cell Lines ◽

Human Tumor ◽

Tumor Cell Lines ◽

Human Tumor Cell ◽

Human Tumor Cell Lines

A new series of quinazoline-based chalcones and pyrimidodiazepines were tested against 60 human tumor cell lines.

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Pharmacoinformatics and Preclinical Studies of NSC765690 and NSC765599, Potential STAT3/CDK2/4/6 Inhibitors with Antitumor Activities against NCI60 Human Tumor Cell Lines

Biomedicines ◽

10.3390/biomedicines9010092 ◽

2021 ◽

Vol 9 (1) ◽

pp. 92

Author(s):

Bashir Lawal ◽

Yen-Lin Liu ◽

Ntlotlang Mokgautsi ◽

Harshita Khedkar ◽

Maryam Rachmawati Sumitra ◽

...

Keyword(s):

Tumor Cell ◽

Cell Lines ◽

Cancer Cell ◽

Human Tumor ◽

Cancer Cell Lines ◽

Tumor Cell Lines ◽

Human Tumor Cell ◽

Human Tumor Cell Lines ◽

Anti Cancer

Signal transducer and activator of transcription 3 (STAT3) is a transcriptional regulator of a number of biological processes including cell differentiation, proliferation, survival, and angiogenesis, while cyclin-dependent kinases (CDKs) are a critical regulator of cell cycle progression. These proteins appear to play central roles in angiogenesis and cell survival and are widely implicated in tumor progression. In this study, we used the well-characterized US National Cancer Institute 60 (NCI60) human tumor cell lines to screen the in vitro anti-cancer activities of our novel small molecule derivatives (NSC765690 and NSC765599) of salicylanilide. Furthermore, we used the DTP-COMPARE algorithm and in silico drug target prediction to identify the potential molecular targets, and finally, we used molecular docking to assess the interaction between the compounds and prominent potential targets. We found that NSC765690 and NSC765599 exhibited an anti-proliferative effect against the 60 panels of NCI human cancer cell lines, and dose-dependent cytotoxic preference for NSCLC, melanoma, renal, and breast cancer cell lines. Protein–ligand interactions studies revealed that NSC765690 and NSC765599 were favored ligands for STAT3/CDK2/4/6. Moreover, cyclization of the salicylanilide core scaffold of NSC765690 mediated its higher anti-cancer activities and had greater potential to interact with STAT3/CDK2/4/6 than did NSC765599 with an open-ring structure. NSC765690 and NSC765599 met the required safety and criteria of a good drug candidate, and are thus worthy of further in-vitro and in-vivo investigations in tumor-bearing mice to assess their full therapeutic efficacy.

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