Background: A series of new zerumbone hydrazones 5a-f and 9a-f have been synthesized via an in situ procedure in high yields. The structure of synthesized compounds has been confirmed using 1H, 13C NMR and HR-MS. The bioassay result showed that several compounds exhibited cytotoxic effects against three human cancer cell lines including HepG-2, SK-LU-1 and MCF-7. Compound 9a showed the best cytotoxic effect against HepG-2, SK-LU-1 and MCF-7 with IC50 values of 8.20, 6.66 and 9.35 µM, respectively. Objective: This study aims at developing new zerumbone hydrazones as anticancer agents based on zerumbone, a natural compound wildly growing in Vietnam. Method: A series of new zerumbone hydrazones was designed, synthesized and evaluated for cytotoxicity against three human cancer cell lines, including HepG-2, MCF-7 and SKLu-1 using MTT method. Results: The bioassay result showed that several compounds exhibited cytotoxic effects against three human cancer cell lines including HepG-2, SK-LU-1 and MCF-7. Especially, compound 9a displayed the best cytotoxic effect against HepG-2, SK-LU-1 and MCF-7 with IC50 values of 8.20, 6.66 and 9.35 µM, respectively. Results: The bioassay result showed that several compounds exhibited cytotoxic effects against three human cancer cell lines including HepG-2, SK-LU-1 and MCF-7. Especially, compound 9a displayed the best cytotoxic effect against HepG-2, SK-LU-1 and MCF-7 with IC50 values of 8.20, 6.66 and 9.35 µM, respectively. Conclusion: The research results suggest that some compounds could be considered as a lead for future design of zerumbone hydrazones in which bio-isosteric replacements in ortho position of the phenyl ring could be performed to improve the cytotoxic activity.
Various experiments have proved that Curcuma longa (CL), the Golden Spice of our kitchen, exibits anticancer effects to inhibit the uncontrolled cell division and metastasis of carcinoma cells, by the cell cycle arrest and finally promote to programmed cell death. In particular, CL exhibits the most powerful phytocompound to affect human breast cancer, the most prevalent type of cancer among the women, throughout the world. The main compounds present in CL can be classified as Curcuminoids and Non-curcuminoids, which shows the anticancer, anti-inflamatory functions for cancer cells. It helps in powerful inhibition in low concentration on breast cancer cell lines that exhibit the estrogen receptor negative(ER) and sensitizes the cells towards the anticancer drugs in low dose. Above all, it promotes the cells towards apoptosis, which does not have hormone receptor expression. Curcuminoids and non curcuminoids inhibit the excessive cell division of breast cancer stem cells (BCSC). Prevention of BCSC proliferation is performed by suppressing metastasis and adherence of the cells with one another, ultimately limiting tumor formation. The main powerful phyto-compound present in CL, curcumin, causes the yellow coloration of it, has drawn the main interest as the chemosensitizing agent also. Different mode of cancer cell targeting and apoptosis is discussed.
Background: In recent years, great progress has been made in reducing the high level of malaria suffering worldwide. There is a great need to evaluate drug resistance reversers and consider new medicines against malaria. There are many approaches to the development of antimalarial drugs. Specific concerns must be taken in to account in these approaches, in particular there requirement for very in expensive and simple use of new therapies and the need to limit drug discovery expenses. Important ongoing efforts are the optimisation of treatment with available medications, including the use of combination therapy. The production of analogs of known agents and the identification of natural products, the use of compounds originally developed against other diseases, the assessment of overcoming drug resistance and the consideration of new therapeutic targets. Liver and spleen are the important organs which are directly associated with malarial complications. Aim: An analysis the Activity of Adenosine Triphosphatase, Aryl Hyrocarbon Hydroxylase Enzymes and Malondialdehyde in spleen Explant Culture. Objective: To determine in-Vitro Effect of Chlorquine and Picroliv on Plasmodium Berghei Induced Alterations in the Activity of Adenosine Triphosphatase, Aryl Hyrocarbon Hydroxylase Enzymes and Malondialdehyde in spleen Explant Culture. Material and method: 1-Histological preparation of spleen explants for paraplast embedding 2-Biochemicalstudies (Enzymes (Atpase, ALP&GST) and the level of protein, Malondialdehyde (MDA). Result: Splenomegalyis one of the three main diagnostic parameters of malaria infection besides fever and anaemia. Many enzymes present in the liver and spleen may also be altered or liberated under different pathological conditions. Enzymes (ATPase, ALP&GST) and the level of protein, Malondialdehyde (MDA) content was found to increase in the liver and spleen explants during malarial infection. In the liver and spleen derived from parasitized CQ treated animals, the activity of all the above enzymes (ATPase, ALP&GST) and the level of protein & MDA of liver/spleen reversed towards the normal for all the 4or3 days of incubations. Picroliv efficacy decreased with the increment of parasitaemia and at 60%parasitaemia. Conclusion: Alkalinephosphatase (ALP) was found to increase with increasing parasitaemia. After the addition of Picroliv to the medium, a decrement in the activity was observed up to day 4 of culture.A similar positive effect of Picroliv was observed on the ATPase and ALP activity of spleen explants.DNA and protein contents also increased in the parasitized liver cultured in the presence of picroliv.On the contrary, in the spleen explants DNA, protein and MDA content were found to decrease after Picroliv supplementation to the culture medium.
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