scholarly journals SYNTHESIS, CHARACTERIZATION AND CYTOTOXIC ACTIVITY OF Pt(II)COMPLEX OF CAMPHOR 4-METHYL THIOSEMICARBAZONE

2018 ◽  
Vol 56 (2A) ◽  
pp. 75-80
Author(s):  
Phan Thi Hong Tuyet

The new complex of Pt(II) with camphor 4-methyl thiosemicarbazone was synthesized and characterized by means of MS, 1H-NMR and IR spectroscopes. Results show that, the molecular formula of new Pt(II) complex is [Pt(C12H20N3S))2]. The Pt(II) complex is of four coordinate. The result of in vitro anti-cancer activity of the complex has shown that the complex of Pt(II) with camphor 4-methyl thiosemicarbazone exhibit inhibitor on Hep-G2 and RD cancer cells with IC50 values of 7.74 and 7.61 µg.mL-1. These results indicated a potential of new Pt(II)complex in biomedical application.

Biomedicines ◽  
2019 ◽  
Vol 7 (4) ◽  
pp. 96 ◽  
Author(s):  
Subramani Paranthaman Balasubramani ◽  
Mohammad Atikur Rahman ◽  
Sheikh Mehboob Basha

Muscadine grape is rich in stilbenes, which include resveratrol, piceid, viniferin, pterostilbene, etc. Resveratrol has been extensively studied for its biological activities; however, the synergistic effect of stilbene compounds in berry extracts is poorly understood. The aim of this study was to evaluate the anti-cancer activity of stilbene-rich muscadine berry extract and pure resveratrol. Stilbenes were extracted from ripened berries of muscadine grape cultivars, Pineapple, and Southern Home. HPLC analysis was performed to determine quantity of stilbenes. The extracts were tested for their cytotoxic activity against A549 (lung carcinoma cells), triple negative breast cancer (HCC-1806) and HepG2 (human liver cancer) cells. The stilbene-rich extracts of the muscadine berry extracts showed cytotoxic activity against all of the cells tested. The extracts at 1 μg/mL induced death in 50–80% of cells by 72 h of treatment. About 50 μg/mL of resveratrol was required to induce a similar response in the cells. Further, modulation of genes involved in tumor progression and suppression was significantly (p < 0.0005) higher with the HepG2 cells treated with stilbene-rich berry extracts than the pure resveratrol. This shows that the synergistic activity of stilbenes present in muscadine grape berries have more potent anti-cancer activity than the resveratrol alone.


2018 ◽  
Vol 19 (3) ◽  
pp. 903 ◽  
Author(s):  
Se Byeon ◽  
Young-Su Yi ◽  
Jongsung Lee ◽  
Woo Yang ◽  
Ji Kim ◽  
...  

MedChemComm ◽  
2019 ◽  
Vol 10 (1) ◽  
pp. 116-119 ◽  
Author(s):  
Fabrizio Olivito ◽  
Nicola Amodio ◽  
Maria Luisa Di Gioia ◽  
Monica Nardi ◽  
Manuela Oliverio ◽  
...  

In this work we synthesized and tested a series of unsaturated disulfides. Two compounds showed a promising anticancer activity in vitro on A549 lung cancer cells compared to the natural analogue.


2011 ◽  
Vol 46 (10) ◽  
pp. 4957-4963 ◽  
Author(s):  
Engin Ulukaya ◽  
Ferda Ari ◽  
Konstantinos Dimas ◽  
Elif Ilkay Ikitimur ◽  
Emel Guney ◽  
...  

2019 ◽  
Vol 110 ◽  
pp. 254-264 ◽  
Author(s):  
Moniba Sajid ◽  
Chao Yan ◽  
Dawei Li ◽  
Siva Bharath Merugu ◽  
Hema Negi ◽  
...  

Marine Drugs ◽  
2020 ◽  
Vol 19 (1) ◽  
pp. 12
Author(s):  
Tao Chen ◽  
Yun Huang ◽  
Junxian Hong ◽  
Xikang Wei ◽  
Fang Zeng ◽  
...  

The latest research has indicated that anti-tumor agents with COX-2 inhibitory activity may benefit their anti-tumor efficiency. A series of sclerotiorin derivatives have been synthesized and screened for their cytotoxic activity against human lung cancer cells A549, breast cancer cells MDA-MB-435 using the MTT method. Among them, compounds 3, 7, 12, 13, 15, 17 showed good cytotoxic activity with IC50 values of 6.39, 9.20, 9.76, 7.75, 9.08, and 8.18 μM, respectively. In addition, all compounds were tested in vitro the COX-2 inhibitory activity. The results disclosed compounds 7, 13, 25 and sclerotiorin showed moderate to good COX-2 inhibition with the inhibitory ratios of 58.7%, 51.1%, 66.1% and 56.1%, respectively. Notably, compound 3 displayed a comparable inhibition ratio (70.6%) to the positive control indomethacin (78.9%). Furthermore, molecular docking was used to rationalize the potential of the sclerotiorin derivatives as COX2 inhibitory agents by predicting their binding energy, binding modes and optimal orientation at the active site of the COX-2. Additionally, the structure-activity relationships (SARS) have been addressed.


2019 ◽  
Vol 43 (45) ◽  
pp. 17891-17901 ◽  
Author(s):  
Daina Kalniņa ◽  
Aviva Levina ◽  
Alexander Pei ◽  
Kārlis Agris Gross ◽  
Peter A. Lay

Nanocrystalline V(v)-doped hydroxyapatite and its reduced analogue (V(v) and V(iv) mixture) show promising in vitro cytotoxicity against cultured human bone cancer cells.


2018 ◽  
Vol 50 (1) ◽  
pp. 79-91 ◽  
Author(s):  
Wei Yan ◽  
Mingyue Tao ◽  
Baofei Jiang ◽  
Mengchu Yao ◽  
Yali Jun ◽  
...  

Background/Aims: Multidrug resistance (MDR) is the most common cause of chemotherapy failure. Upregulation of P-glycoprotein (P-gp) is one of the main mechanisms underlying MDR. Methods: In this study, we developed a targeted drug and small interfering (si)RNA co-delivery system based on specific aptamer-conjugated grapefruit-derived nanovectors (GNVs) that we tested in MDR LoVo colon cancer cells. The internalization of nanovectors in cancer cells was tested by fluorescence microscopy and flow cytometry. The anti-cancer activity in vitro was determined by colony formation and cell apoptosis assays. The biodistribution of nanovectors was analyzed by live imaging and the anti-cancer activity in vivo was observed. Results: GNVs loaded with aptamer increased doxorubicin (Dox) accumulation in MDR LoVo cells, an effect that was abolished by pretreatment with DNase. The LA1 aptamer effectively promoted nanovector internalization into cells at 4°C and increased the targeted delivery of Dox to tumors. Constructs harboring Dox, LA1, and P-gp siRNA more effectively inhibited proliferation and enhanced apoptosis in cultured MDR LoVo cells while exhibiting more potent anti-tumor activity in vivo than free Dox or GNVs loaded with Dox alone or in conjunction with LA1, an effect that was associated with downregulation of P-gp expression. Conclusion: This GNV-based system may be an effective strategy for overcoming MDR in clinical settings.


2015 ◽  
Vol 1 (01) ◽  
pp. 17-21
Author(s):  
P. Ethalsha Robert ◽  
A. Malar Retna

The present study evaluates in-vitro cytotoxic activity of active extracts of medicinal plants. It evaluates anti-cancer activity of most active extracts of I. pes-caprae and C. roseus. This study focuses on the total phenol content and the total flavanoid content of the plant and searches into its medicinal potency based on the total phenol and total flavanoid content. The anti-cancer activity of the extract is found to be more significant than one another.The cytotoxic activity of Ipomoea pes-caprae and C. roseus showed better results. Methanol extracts of aerial and root of Ipomoea pes-caprae possess maximum anticancer activity is found to be 61.77% and 65.55%. Chloroform extract of Catharanthus roseus root was also active against MCF- 7 cells by exhibiting 64.34% of activity. These plants may be a source of new antibiotic compounds.These findings enriches our knowledge of the chemical constituents that are responsible for the medicinal uses of the plant and the anti-cancer potential of selected plants.


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