Cortisone is a naturally-occurring corticosteroid metabolite that is also used as a pharmaceutical prodrug. The corticosteroids market is expected to witness a CAGR of 4.3%, during the period 2020-2025. Cortisone is very well known for its therapeutic effects but due to its numerous side effects, especially in prolonged and high-dose therapies, the development of the pharmaceutical industry is currently aimed at finding new compounds with similar activities but with minor or no side effects so the main aim of the research has been to develop new drugs with better therapeutic activities while trying to obtain a decrease in the side effects that derive from their use. Biotransformations are an important methodology toward more sustainable industrial processes according to the principles of “green chemistry”.

In this work we have focused the attention on the biotransformation of cortisone with Rhodococcus rhodnii strain as two completely new compounds were obtained.

Studies on in vitro biological activity of these molecules have shown that both compounds were not cytotoxic to human keratinocyte cells and can be considered as non-genotoxic for Ames test, furthermore, studies on antioxidant properties have shown that both compounds presented a very high antioxidant activity.

Regarding the anti-inflammatory activity both compounds inhibited the TNFα-stimulated espression and secretion of NFkB target cytokines, inhibited also COX activity and can activate the glucocorticoid receptor. Finally both compounds display neuroprotective propertiesCortisone is a naturally-occurring corticosteroid metabolite that is also used as a pharmaceutical prodrug. The corticosteroids market is expected to witness a CAGR of 4.3%, during the period 2020-2025. Cortisone is very well known for its therapeutic effects but due to its numerous side effects, especially in prolonged and high-dose therapies, the development of the pharmaceutical industry is currently aimed at finding new compounds with similar activities but with minor or no side effects so the main aim of the research has been to develop new drugs with better therapeutic activities while trying to obtain a decrease in the side effects that derive from their use. Biotransformations are an important methodology toward more sustainable industrial processes according to the principles of “green chemistry”.

In this work we have focused the attention on the biotransformation of cortisone with Rhodococcus rhodnii strain as two completely new compounds were obtained.

Studies on in vitro biological activity of these molecules have shown that both compounds were not cytotoxic to human keratinocyte cells and can be considered as non-genotoxic for Ames test, furthermore, studies on antioxidant properties have shown that both compounds presented a very high antioxidant activity.

Regarding the anti-inflammatory activity both compounds inhibited the TNFα-stimulated espression and secretion of NFkB target cytokines, inhibited also COX activity and can activate the glucocorticoid receptor. Finally both compounds display neuroprotective properties

Background: Bile acids (BAs) are a family of steroids synthesized from cholesterol in the liver. Amongbile acids, ursode oxycholic acid (UDCA) is the drug of choice for treating primary biliary cirrhosis and dissolving cholesterol gallstones. The clinical effectiveness of UDCA includes its choleretic activity, the capability to inhibit hydrophobic bile acid absorption by the intestine under cholestatic conditions, reducing cholangiocyte injury, stimulation of impaired biliary output, and inhibition of hepatocyte apoptosis. Despite its clinical effectiveness, UDCA is poorly soluble in the gastro-duo- deno-jejunal contents, and pharmacological doses of UDCA are not readily soluble in the stomach and intestine, resulting in incomplete absorption. Indeed, the solubility of 20 mg/L greatly limits the bioavailability ofUDCA.

Objective: Since the bioavailability of drug products plays a critical role in the design of oraladministration dosages, we investigated the enzymatic esterification of UDCA as a strategy of hydrophilization. This work proposes an enzymatic strategy for the covalent attack of highly hydrophilic molecules using acidic functions of commercially available bioactive compounds.

Methods: We decided to enzymatically synthesize a glyceric ester of UDCA bile acid to produce a more water-soluble molecule. The esterification reactions between UDCA and glycerol were performed with an immobilized lipase B from Candida antarctica (Novozym 435) in solvent-free and solvent-assisted systems.

Results: The optimization of the processes, such as lipase and compounds concentrations, solvents amount, temperatures, stirring speed, and times is reported.

Conclusion: N435 demonstrated itself to be a suitable enzyme for the effective production of UDCA monoglyceride. The characterization of the UDCA-monoglyceride, enzymatically synthesized, has been performed by 1 H-NMR, 13C-NMR, COSY, HSQC, HMBC, IR, and MS spectroscopy.

Introduction: Prevalence of oral squamous carcinoma (OSCC) is increasing in developing countries and represents complex pharmacotherapy with poor prognosis which results in higher rate of mortality. Therefore, it is needed to perform drug utilization pattern of palliative chemotherapeutic agents to rationalize the drug therapy in OSCC to inhibit disease.

Aim: The aim was to study of drug-utilization pattern and effectiveness of palliative   chemotherapy in OSCC patients at tertiary care hospital.

Methodology: A prospective longitudinal study was conducted in the Kailash Cancer Hospital & Research Centre, Gujarat, India to study the patient characteristics, their treatment profile, recurrence profile, palliative treatment and quality of life. Data collection was done by case record form and Quality of life (QoL) questionnaire.

Result: Out of total 104 patients of OSCC attaining the palliative care treatment, 97 (9.3%) patients were male and 7 (6.7%) were female. In the present study, 83 patients had recurrent cancer  while 21 patients were newly diagnosed with Metastatic disease. In this work all 104 patients had Stage 4 malignancy. We used Methotrexate as monotherapy  while Ci in combination with methotrexate, 5-Fluorouracil (5-FU) and docetaxel observed to be 38%; 42% and 49%, respectively- so this has to be changed  The subjective assessment of therapy by questionnaire revealed a statically significant (p=0.05) improvement in patient symptoms.

Conclusion: It was concluded that tailored drug therapy approach for palliative chemotherapy with clinically potential intervention for management of terminal oral cancer patients with less incidence of toxicity.