Worldwide, a number of research groups are functioning towards effective treatment of colon cancer using chemotherapeutic agents. Nonsteroidal anti-inflammatory drugs are among the most potent agents discovered for the inhibition of cancer. In spite of the approval of celecoxib for adjuvant therapy in patients with familial adenomatous polyposis and precancerous disease of colon, associations of larger intensity of side effects limit its usage in cancer therapy. Combination therapy provides advantages of reduction in dose and possible reduction in toxicity and acquired drug resistance. As a consequence, targeted drug delivery and targeted molecular therapy of single or combination of anticancer agents are necessary for efficient treatment of colon cancer with reduced toxicity. In our study, combination of celecoxib and AEE788 shows growth inhibition and apoptosis in HCT 15 cells. Further, nanocarrier mediated celecoxib delivery showed high entrapment efficiency, sustained release patterns, desirable hemocompatibility and enhanced cytotoxicity and apoptosis in vitro and in vivo.
This research work was carried out to establish scientific based evidence on folkloric usage and knowledge. The aim of this work is Pharmacological evaluation of Melochia corchorifolia leaves (folkloric) for antioxidant, diuretic, antiurolithiatic, anticancer, antibacterial and anthelmintic activities. In this regard, Melochia corchorifolia leaves were extracted with chloroform and ethylalcohol. The obtained extracts were used for pharmacological activities, the antioxidant activity results, the extracts and its Phenolic content shows good averting activity. Diuretic and saluretic activity is due to altering renal sodium excretion.The antiurolithiatic activity may be due to the presence of secondary metabolites of the extract.The extracts produced good anticancer activity on HCT-116 cell line and MCF-07 cancer cell lines. The chloroform extracts of Melochia corchorifolia shows good antibacterial and anthelmintic activities. So it was concluded that this research work supports the folkloric usage of this herbal drug (Melochia corchorifolia) is a potential source for treating various ailments.
The original work of the present book consists of three research projects: In the first part: Synthesis, cytotoxicity evaluation, molecular docking and utility of novel chalcones as precursors for heterocycles incorporating pyrazole moiety.In the second part: Synthesis and antimicrobial activity of novel azolopyrimidines and pyrido-triazolo-pyrimidinones incorporating pyrazole moiety.In the third part: Synthesis of new pyrazolyl-pyridines as antitumor agents. The assigned structures for all the newly synthesized compounds were confirmed on the basis of elemental analyses and spectral data and the mechanisms of their formation were also discussed. In addition, some of the newly synthesized chalcones were tested for their cytotoxicity against human colon carcinoma cell line (HCT-116) and against human hepatocellular carcinoma (HEPG2) cell lines and the results revealed that some compounds have promising activities compared with the standard drug Doxorubicin. Molecular docking was also carried out for the high potent compounds.
Phytic acid is extensively known for its anti-nutritional properties. The wide notion about this compound is to be changed totally. Hence, the study is focused on bringing out its potential as a drug molecule. The knowledge gained by understanding the binding efficacy of phytic acid and its analogues can help in the development of a new lead molecule. The antibacterial studies and cell line studies using HCT-15 confirmed the drugability. The potency of cancer drug targets can also be screened using docking studies. The entire work can bring out an effective lead molecule which maybe subjected to clinical trials. It is hypothesized that phytic acid and its derivatives having one or more of the following chemical functional groups such as the number of phosphates, phospho-diesters, charged phosphates, halogens, heavy atoms, steriocentred atoms, hydoxyl groups, hydrogen donors and acceptors, have an effect on the binding affinity towards the selected targets. Although, there are few reports to suggest the anticancer activity of PA, there is no work on its structure-activity relationship.