Metal complexes of Salen ligand bearing ferrocenophane

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>> Sunday, December 27, 2009

I hope you had a great Christmas time. Today, in this post, I am going to summarize the synthesis of Metal-Salen complexes bearing a ferrocenophane substituent as reported by Patti et. al. You can check out the previous post on anticancer activity of polyphenolferrocenophane.

Chiral N, N'-bis(salicylcidene)ethylendiamine (salen) compounds are a very popular ligands because of their easy formation and rich coordination chemistry with a large variety of metal ions, that has allowed their use as catalysts in different asymmetric reactions. Similarly, ferrocenyl compounds has unique electronic, steric and chemical properties which has been used to synthesize a great variety of derivatives.Interest in the preparation of chiral ferrocenes as well as development of new salen catalysts encouraged authors to synthesize novel compounds bearing both skeleton.
In this study, first ferrocenophane was synthesized and finally converted to Metal-Salen complexes.


Exploration of old drugs for new pharmacological activity

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>> Saturday, December 19, 2009

"The most fruitful basis for the discovery of a new drug is to start with an old drug"-by Pharmacologist and Nobel Laureate James Whyte Black.
Starting with the quote by J. W. Black, I would like to emphasize on ritonavir as an example of drugs being explored for new pharmacological activity. Ritonavir, a HIV protease inhibitor, was discovered in 1998 by Kemf et. al., Abott laboratories, Illinois. It is one of the drug (as protease inhibitor) used in highly active antiretroviral therapy (HAART) along with reverse transcriptase inhibitors.


Broccoli as a source of anticancer agents

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>> Saturday, December 12, 2009

Most of the people are aware of healthy benefits of broccoli but the active constituents which makes broccoli to possess anticancer property may not be well known. I hope this piece of writing, in some extent, will make familiar to active anticancer agents found in broccoli. Here, the anticancer effect of Selenium (Se)-enriched broccoli will be highlighted according to the work done by researcher from Gunma University, Japan (Abdulah, et al.).
As a member of Se-accumulator Brassica family, broccoli accumulates Se-methylselenocysteine as the major Se compound when it is germinated in Se-enriched media. Therefore, Se-enriched broccoli accumulates two active anticancer agents: sulforaphane and Se-methylselenocysteine. The anticancer property of Sulforaphane, belonging to isothiocyanates and Se-methylselenocysteine has already been reported (Nishikawa, et. al, and Kim et. al. respectively).
Recently, broccoli sprouts have received considerable attention, because they contain ten times more sulforaphane than broccoli florets. Many studies have shown that both cruciferous vegetables and selenium may reduce the incidence of prostate cancer. Thus, in this study, antiproliferative study of a control broccoli sprout extract (CSp) and a Se-enriched broccoli sprout extract (SeSp) was explored. It was found that SeSp extract contain Se in the form of Se-methylselenocysteine. It is a mono-methylated Se and is a precursor of methylselenol, an important metabolite in Se chemoprevention.


Thaspine: A promising anticancer agent from Croton Lechleri

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>> Saturday, December 05, 2009

The active alkaloid, thaspine (taspine), from the cortex of the tree Croton lechleri also known as “Sangre de grado” (blood of the dragon in Spanish) has shown to be dual topoisomerase inhibitor. It is also effective in the cells overexpressing drug efflux transporters and induces wide-spread apoptosis in multicellular spheroids. 
Using modified M30-Apoptosense method, Fayad, W., et al, has screened various natural compounds that induce apoptosis of colon carcinoma cells. They found that thaspine induced strong caspase-cleavage of cytokeratin-18 in HCT116 cells. The concentration requirement is similar to that of other cancer therapeutic drugs such as cisplatin, doxorubicin and mechlorethamine for induction of caspase activity of this cell line. Thaspine was also observed to induce tumor apoptosis in vivo. Thaspine induced the apoptosis via mitochondrial apoptosis pathway.
“Thaspine causes reduction of mitochondrial cytochrome C and an increase level in the cytosol (a hallmark of the mitochondrial apoptosis pathway). Thaspine also induced conformational activation of Bak and Bax, Bcl-2 proteins, which are key regulators of the mitochondrial apoptosis pathway.”


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