scholarly journals Novel C-ring Analogs of Ursolic acid: Synthesis and Cytotoxic Evaluation

2014 ◽  
Vol 9 (12) ◽  
pp. 1934578X1400901
Author(s):  
Uppuluri V. Mallavadhani ◽  
Banita Pattnaik ◽  
Nitasha Suri ◽  
Ajit K. Saxena
Keyword(s):  
Hela Cell ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Ursolic Acid ◽  
Parent Compound ◽  
Acid Synthesis ◽  
Hela Cell Line ◽  
Hela Cell Lines ◽  
Protective Groups

Ursolic acid (1), a natural pentacyclic triterpenic acid, afforded a variety of ring-C transformed products (5–11) when treated with N-bromosuccinimide under the influence of a range of protective groups and solvents. The synthesized compounds have been evaluated for cytotoxic activity against prostate PC 3, leukemia THP 1, cervical Hela and lung A-549 cancer cell lines. Among the tested analogs, compounds 5, 8, 9 and 10 showed potent activity against PC 3, THP 1 and Hela cell lines. Especially, compound 10 showed enhanced activity against the Hela cell line than the parent compound. Compounds 5, 8 and 9 showed comparable activities against PC 3 and THP 1 cell lines.

scholarly journals Synthesis and Antiproliferative Activity of Diethylamine Mannich Base of Asymmetrical Mono-Carbonyl Curcumin Analogs against HeLa Cell Lines

2017 ◽  
Author(s):  
Pekik Wiji Prasetyaningrum ◽  
Anton Bahtiar ◽  
Hayun Hayun
Keyword(s):  
Hela Cell ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Antiproliferative Activity ◽  
Mannich Base ◽  
Parent Compound ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Curcumin Analogs ◽  
Hela Cell Lines

A series of diethylamine Mannich base of asymmetrical mono-carbonyl analogs of curcumin (AMACs) were synthesized and evaluated for cytotoxic activity against Hela Cell lines. The structures of the synthesized compounds were confirmed on the basis of FTIR, 1H-NMR, 13C-NMR and mass spectral data. Preliminary cytotoxic test using BSLT showed that all the synthesized compounds exhibited more potent cytotoxic activity than that of curcumin. While results of MTT assay showed that all the synthesized compounds exhibited more potent antiproliferative activity against HeLa cell lines than that of cisplatin. Compound 2b exhibited as the most potent compound of the series. Compound 2a, 2b, 2c, and 2f had IC50 (µM) less than that of compound 1a, 1b, 1c and 1f indicating that the addition of diethylamine Mannich base improves the antiproliferative activity of the parent compound.

Mapping the distribution of Golgi enzymes involved in the construction of complex oligosaccharides

1995 ◽  
Vol 108 (4) ◽  
pp. 1617-1627 ◽  
Author(s):  
C. Rabouille ◽  
N. Hui ◽  
F. Hunte ◽  
R. Kieckbusch ◽  
E.G. Berger ◽  
...  
Keyword(s):  
Golgi Apparatus ◽  
Hela Cell ◽  
Cell Line ◽  
Cell Lines ◽  
Hela Cells ◽  
Stable Expression ◽  
Hela Cell Line ◽  
Specific Antibodies ◽  
Hela Cell Lines ◽  
Golgi Network

The distribution of beta 1,2 N-acetylglucosaminyltransferase I (NAGT I), alpha 1,3-1,6 mannosidase II (Mann II), beta 1,4 galactosyltransferase (GalT), alpha 2,6 sialyltransferase (SialylT) was determined by immuno-labelling of cryo-sections from HeLa cell lines. Antibody labelling in the HeLa cell line was made possible by stable expression of epitope-tagged forms of these proteins or forms from species to which specific antibodies were available. NAGT I and Mann II had the same distribution occupying the medial and trans cisternae of the stack. GalT and SialylT also had the same distribution but they occupied the trans cisterna and the trans-Golgi network (TGN). These results generalise our earlier observations on the overlapping distribution of Golgi enzymes and show that each of the trans compartments of the Golgi apparatus in HeLa cells contains unique mixtures of those Golgi enzymes involved in the construction of complex, N-linked oligosaccharides.

scholarly journals CYTOTOXIC CONSTITUENTS FROM AERIAL PARTS OF HELICTERES HIRSUTA PLANT, COLLECTED IN BINH PHUOC PROVINCE

2018 ◽  
Vol 127 (1A) ◽  
pp. 111
Author(s):  
Pham Huu Dien
Keyword(s):  
Hela Cell ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Folk Medicine ◽  
Hep G2 ◽  
Aerial Parts ◽  
Hela Cell Lines ◽  
Human Prostate Carcinoma ◽  
Pure Compounds ◽  
Human Lung Carcinoma

<p><em>Helicteres hirsuta</em> plant is a member of <em>Helicteres </em>genus<em> </em>of the plant family Sterculiaceae and widely found in countries of South Asia such as Vietnam, Lao, Thailand etc. In recent years, it is known as a new folk medicine protecting and securing people against human lung carcinoma, hormone - dependent human prostate carcinoma and human liver. In this paper, from aerial parts of <em>Helicteres hirsuta</em> plant, collected in Binhphuoc province (October, 2016) three pure compounds <strong>1</strong>-<strong>3</strong> were isolated and structurally elucidated, such as <em>b</em>-stigmasterol (<strong>1</strong>), protosta-17(20), 24-dien-3<em>b</em>-ol (<strong>2</strong>) and icosanoic acid (<strong>3</strong>). Among them, compound <strong>2</strong> has a remarkable cytotoxic activity against SK-LU-1, Hep-G2, and Hela cell lines with IC<sub>50</sub> values from 32.86 to 77.31 mg/mL, meanwhile compound <strong>3</strong> shows a moderable cytotoxic activity against SK-Mel-2, AGS, SK-LU-1, Hep-G2, and Hela cell lines with IC<sub>50</sub> values from 59.02 to 80.87 mg/mL.  </p>

scholarly journals Evaluation of Cytotoxicity and Apoptotic behavior of Cerium Oxide/Zinc Oxide/ Graphene Oxide in HeLa and VERO cell Lines

2021 ◽  
Author(s):  
saranya J ◽  
BS Sre ◽  
M Arivanandan ◽  
K Bhuvaneswari ◽  
S Sherin ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Zinc Oxide ◽  
Graphene Oxide ◽  
Hela Cell ◽  
Cell Line ◽  
Cerium Oxide ◽  
Cell Lines ◽  
Morphological Properties ◽  
Hela Cell Lines ◽  
Anti Cancer

Abstract Using the ultrasonic approach, we produced a morphology involving cerium oxide/ Zinc oxide/graphene oxide (CeO2/ZnO/GO) nanocomposite-based system. The developed nanocomposite was examined using X-Ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and field emission scanning electron microscopy (FESEM). The average crystallite size was found to be 11.44 nm, as determined by XRD. FTIR analysis was used to confirm the existence of functional groups. FESEM was used to verify the morphological properties of CeO2/ZnO/GO. The micromorphology of CeO2/ZnO/GO nanocomposite reveals a smoother sheet-like structure. In addition, using an antiproliferative assay test, the developed nanosystem was evaluated for its scavenging anti-cancer capability against HeLa cell lines at various doses and incubation intervals. In our investigation, the effective IC50 concentration was reported to be 62.5 µg/ml at 72 h. Further, the developed nanosystem was evaluated for its killing efficacy against normal cell line. To identify apoptosis-associated alterations of cell membranes throughout the apoptosis process, a dual acridine orange/ethidium bromide (AO/EB) fluorescent staining was done using CeO2/ZnO/GO nanocomposite at three specific concentrations. The quantitative analysis was carried out using flow cytometry (FACS study) to determine the cell cycle during which the greatest number of HeLa cells were destroyed. According to the results of the FACS investigation, maximum cell cycle has taken place in P2, P4.As a result, the newly designed CeO2/ZnO/GO hybrid has demonstrated improved anti-cancer efficacy against the HeLa cell line, making it a better therapeutic agent for cervical cancer detection.

scholarly journals Methylation of 2-Aryl-2-(3-indolyl)acetohydroxamic Acids and Evaluation of Cytotoxic Activity of the Products

Molbank ◽  
10.3390/m1307 ◽  
2021 ◽  
Vol 2022 (1) ◽  
pp. M1307
Author(s):  
Dmitrii A. Aksenov ◽  
Alexander V. Aksenov ◽  
Lidiya A. Prityko ◽  
Nicolai A. Aksenov ◽  
Liliya V. Frolova ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Hela Cell ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Hydroxamic Acid ◽  
Methyl Esters ◽  
Hydroxamic Acids ◽  
Hela Cell Line ◽  
Lead Compounds

2-Aryl-2-(3-indolyl)acetohydroxamic acids demonstrate promising antitumor activity, but quickly metabolize in vivo via glucuronidation of hydroxamic acid residue. In an attempt to improve their pharmacokinetics, methyl esters were synthesized via a newly developed protocol for chemoselective mono-methylation of hydroxamic acids. The cytotoxicity of these derivatives against the HeLa cell line was evaluated and found to be inferior compared to the parent lead compounds.

scholarly journals Total synthesis and anticancer activity of the natural oleanolic acid bidesmoside saponin, albidoside A, isolated from the roots of Acacia albida

2019 ◽  
Vol 44 (1-2) ◽  
pp. 42-49
Author(s):  
Tiantian Guo ◽  
Yiming Song ◽  
Yinghui Lu ◽  
Guolin Li ◽  
Tian Liu ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Hela Cell ◽  
Anticancer Activity ◽  
Cell Line ◽  
Oleanolic Acid ◽  
Triterpenoid Saponin ◽  
Hela Cell Line ◽  
Hela Cell Lines ◽  
Acacia Albida ◽  
Mcf 7

The first synthesis of a natural triterpenoid saponin bearing N-acetylglucosamine, albidoside A, which is isolated from the roots of Acacia albida, is concisely achieved in a convergent strategy. Preliminary pharmacological research shows anticancer activity against HL-60, MCF-7, MDA-MB-231, Hep-2, and Hela cell lines. In particular, it exhibited good selectivity, which is five times more cytotoxic toward Hep-2 cells (IC50 = 8.91 μM) than the Hela cell line.

scholarly journals Synthesis and Biological Activity Studies of Methyl-5-(Hydroxymethyl)-2-Furan Carboxylate and Derivatives

2019 ◽  
Vol 35 (3) ◽  
pp. 080-1085 ◽  
Author(s):  
Weerachai Phutdhawong ◽  
Siwaporn Inpang ◽  
Thongchai Taechowisan ◽  
Waya S. Phutdhawong
Keyword(s):  
Biological Activity ◽  
Hela Cell ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Furfuryl Alcohol ◽  
Methyl Acetate ◽  
Biological Activities ◽  
Hela Cell Line ◽  
Amine Derivative

Methyl-5-(hydroxymethyl)-2-furan carboxylate and derivatives were prepared from furfuryl alcohol and their biological activities were studied for cytotoxicity against cancer cell lines HeLa, HepG2 and Vero, and Gram (+) and Gram (-) bacteria. The amine derivative, (5-(((2-(1H-indol-3-yl)ethyl)amino)methyl) furan-2-yl)methyl acetate, was found to have the most potent biological activity with IC50 62.37 µg/mL against the HeLa cell line and MIC 250 µg/mL against the photogenic bacteria.

Evaluation of photodynamic therapy and nuclear imaging potential of subphthalocyanine integrated TiO2 nanoparticles in mammary and cervical tumor cells

2019 ◽  
Vol 23 (07n08) ◽  
pp. 908-915 ◽  
Author(s):  
Fatma Yurt ◽  
Kasim Ocakoglu ◽  
Ozge Er ◽  
Hale Melis Soylu ◽  
Mine Ince ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
Hela Cell ◽  
Cell Line ◽  
Cell Lines ◽  
Nuclear Imaging ◽  
Target Tissue ◽  
Hela Cell Lines ◽  
Wi38 Cell

This study, subphthalocyanines (SubPc) and SubPc integrated TiO2 nanoparticles (SubPc-TiO[Formula: see text] were synthesized as novel photosensitizers. Their PDT effects were evaluated. Furthermore, nuclear imaging potential of [Formula: see text]I-labelled SubPc/SubPc-TiO2 were examined in mouse mammary carcinoma (EMT6) and cervix adenocarcinoma (HeLa) cell lines. The uptake results show that SubPc labelled with [Formula: see text]I radionuclide ([Formula: see text]I-SubPc) in EMT6 and HeLa cell lines was found to be approximately the same as in the WI38 cell line. However, the uptake values of SubPc-TiO2 labelled with [Formula: see text]I ([Formula: see text]I-SubPc-TiO[Formula: see text] in EMT6 and HeLa cell lines were determined to be two times higher than in the WI38 cell line. In other words, the target/non-target tissue ratio was identified as two in the EMT6 and HeLa cell lines. [Formula: see text]I-SubPc-TiO2 is promising for imaging or treatment of breast and cervix tumors. In vitro photodynamic therapy studies have shown that SubPc and SubPc-TiO2 are suitable agents for PDT. In addition, SubPc-TiO2 has higher phototoxicity than SubPc. As a future study, in vivo experiments will be held and performed in tumor-bearing nude mice.

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