Nonpeptidic aminoquinolin-4-one derivative as a promising Alzheimer Disease therapeutic agent

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>> Sunday, August 30, 2009

Alzheimer’s disease (AD) is a serious problem worldwide especially in geriatric population. Simply, AD is typical neurodegenerative disorder characterized by the memory loss such as difficulty in remembering the things that is said or done recently. Alzheimer Wikipedia. Calpain inhibition is one of the therapeutic strategies for the treatment of AD.
What is calpain?
Calpain are calcium-dependent cytosolic proteases that play key roles in intracellular signaling cascades and calcium-induced neuronal degeneration (1).As it promotes neuronal degeneration and cell death, it has a important role in the cause and progress of neurodegenerative disorders in the elderly like AD. It is found that increased cyclin-dependent kinase (cdk5)/p25 complex were observed in the brains of AD patients. (cdk5)/p25 complex is produced by calpain-mediated cleavage of p35 to p25. The breakdown of cdk5/p35 into cdk5/p25 prolongs cdk5 kinase activity, induces mislocalization of cdk5 and increases neurotoxicity in neuronal cells via hyperphosphorylation of tau, leading to the formation of neurofibrillary tangles (2) Therefore, inhibition of calpain activity might be a promising route to discovering potent drug candidates for the treatment of AD (3)


Ferrocenophane Polyphenol: antiproliferative activity on breast and prostate cancer cells

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>> Wednesday, August 26, 2009

Ferrocenophane Polyphenol (organometallic compound) shows an exceptional antiproliferative effect on the hormone-dependent MDA-MB-231 breast and PC-3 prostate cancer cells. According to the author, one of the possible mechanisms that explain the cytotoxic effect of ferrocenyl phenols on various cancer cells is based on the in situ transformation to a reactive quinone methide (QM)
It was obtained in 28 % yield via a McMurry cross-coupling reaction with ferrocenophanone and 4, 4’-dihydroxybenzophenone.

For further details, please refer to.
J.Med.Chem, 2009, vol. 52, 4964-4967
or
Direct Link


Salinomycin: Selective inhibitor of cancer stem cells

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>> Monday, August 24, 2009

Researchers (Piyush B. Gupta et. al.,) have discovered that an ionophore antibiotic, salinomycin, selectively kills breast cancer stem cells (CSCs) better than the well known breast cancer chemotherapeutic drug, paclitaxel. It was found that salinomycin treatment results in the loss of breast CSC genes expression. (Reference: Cell 138, 645–659, August 21, 2009)


salinomycin

Synthesis of Salinomycin


Mechanism of action of Cisplatin (anticancer agents)

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>> Friday, August 21, 2009

Cisplatin, cisplatinum or cis-diamminedichloridoplatinum(II) (CDDP) is a platinum-based chemotherapy drug used to treat various types of cancers, including  sarcomas, some carcinomas (e.g.small cell lung cancer, and ovarian cancer), lymphomas and germ cell tumors. It was the first member of its class, which now also includes carboplatin and oxaliplatin. Platinum complexes are formed in cells, which bind and cause crosslinking of DNA; ultimately triggering apoptosis, or programmed cell death.
Below is the animation on mechanism of action of cisplatin:



HIV virus replication

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>> Friday, August 14, 2009

Nice animation on how the HIV virus replicates in human cell.


Cherry blossom: Not just a beautiful flower, effective antioxidant too

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cherry blossom
Cherry blossom, a beautiful flower, is not just a decorative thing but found to be good antioxidant too.


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