Council of Scientific and Industrial Research

Mayo Foundation for Medical Education and Research

Rajkumar Banerjee

Arabinda Chaudhuri

Nalam Madhusudhana Rao

Prasanta Kumar Das

Gollapudi Venkata Srilakshmi

Badari Narayana Prasad Rachapudi

Debabrata Mukhopadhyay

Pradosh Prasad Chakrabarti

Amarnath Mukherjee

Surendar Reddy Bathula

Sujan Kumar Mondal

Sayantani Roy

Sudhakar Jinka

The present invention relates to the development of the cationic progesterone compounds as a novel anti-tumor agent. The present invention provides a method for the preparation of novel series of progesterone derivatives. The invention also provides information related to highly selective anti-cancer activities of these compounds in wide range of cancer cell irrespective of their progesterone receptor status. Thus, the presently disclosed cationic progesterone compounds offer a viable option as anti-cancer therapeutics.

Progesterone-cationic lipid hybrid as anticancer agent and the process of synthesis thereof

The present invention provides an anti-cancer lipid-based composition that kills very aggressive pancreatic cancer cells and breast cancer stem cell (CSC)-like cells. This composition is a concoction of an anti-cancer agent, ESC8 and a glucocorticoid receptor (GR)-targeting cationic lipid delivery system, DX which is further complexed with plasmid DNA. This composition shows anti-cancer effect and initiates killing of cancer cells and CSC-like cells within 3 h. When anti-cancer gene encoded plasmid is used, residual cancer cells were also significantly eradicated after 2 days of exposure. The formulation-free naked ESC8 requires at least ten-fold more concentration and 3 days of continuous treatment to get a similar level of killing. The composition could also inhibit the tumor growth in mice orthotopically implanted with very aggressive mouse breast cancer cell, ANV-1. This cell is known to produce breast CSC-like cells that show phenotype of advanced cancer relapsing. There is no visible toxic effect of this composition when injected in mice, indicating that it has minimum to no toxic effect to normal homeostasis. The present invention is likely to find specific application in developing potential therapeutic treatment for aggressive cancers and CSC-like cancers.

Synergistic anti-cancer composition and a process for the preparation thereof

The present invention relates to a formulation in which glycolipids and phospholipids, isolated from rice bran gum samples, were used in conjunction with gene carrying lipids to test its efficacy in delivering genes to cancer cells selectively. This formulation did not mediate efficient delivery of genes to non-cancerous cells, thus, showing potential use of this formulation to deliver anticancer therapeutics to cancer cells without eliciting treatment related toxicity to normal cells.

Rice bran-lipids based formulation and process for preparation thereof for selective delivery of genes to cancer cells

The present invention relates to a cationic lipid based aqueous formulation comprising cationic lipid, dexamethasone and a neutral co-lipid, wherein the said formulation is useful for selective targeting and delivering gene to glucocorticoid receptor expressing cancer cells. Glucorticoid receptors (GR) express in various normal and cancer cells. A lot of ligand activated physiological functions are known involving GR but its role in cancer progression (if any) is not clearly understood. Synthetic GR antagonist, dexamethasone (Dex) finds use as anti-inflammatory drug and is known to induce apoptosis in cancer cells. This Dex is included in a cationic lipid-based formulation as a co-lipid to deliver to and express genes specifically in cancer cells possibly through expressed GR. Gene delivery to cancer cells is independent of the gene construct, and tumor cell line. Normal transformed cells expressing GR but with no cancer lineage show much smaller level of transfection. The composition of the formulation is optimized. The formulation may have particular application to the enhanced delivery of anticancer genetic constructs to cancer, with the synergistic effect of Dex in inducing apoptosis as such.

Aqueous formulation for selective targeting and delivering gene to cancer cells

The present invention provides a novel series of cationic, lipid-based, 17&#x3b1;-substituted-estradiol derivatives. The present invention further provides a process for the preparation of a novel series of 17&#x3b1;-substituted-estradiol derivatives. The invention also provides information about highly selective anticancer activities of these molecules in estrogen responsive cell lines. The compound elicits high level of toxicity to gynecological cancer cell lines such as MCF-7, T47D (estrogen receptor positive cell lines), MDA-MB-468 (estrogen receptor knock-out cell line), HeIa (cervical cancer). The present class of cationic lipid-based, estradiol derivatives is likely to find specific use in developing target specifically deliverable anticancer drugs for the treatment of gynecological cancers that are most prevalent in women population irrespective of ethnicity.

Cationic 17 &#x3b1;-substituted-estradiol derivatives useful as anti-cancer agent

The present invention provides processes for the synthesis of novel cationic amphiphiles capable of facilitating transport of biologically active molecules into cells wherein the said amphiphiles contain N-hydroxyalkyl group and have at least one hydroxyalkyl group containing 1-3 carbon atoms directly linked to the positively charged nitrogen atom.

Process for synthesis of novel cationic amphiphiles containing N-hydroxyalkyl group for intracellular delivery of biologically active molecules

The present invention provides novel cationic amphiphiles containing novel N-hydroxyalkyl group and therapeutic formulations containing the said amphiphiles that are capable of facilitating transport of biologically active molecules into cells. The said novel cationic compounds having the following structural formula:

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Hyderabad Telangana, India

Rajkumar Banerjee