Study on enhanced serum protein protecting and anti-cathepsin activities of various curcumin formulations containing traditional excipients and bio-enhancers

• Published in: Bioorganic chemistry Vol. 104; p. 104177
• Main Authors: Raghav, Neera, Mor, Nitika
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01-11-2020
• Subjects: Animals; Anti-cathepsin; Bioavailability; Bioenhancer; Cathepsin B - antagonists & inhibitors; Cathepsin B - metabolism; Cathepsin H - antagonists & inhibitors; Cathepsin H - metabolism; Cattle; Curcumin; Curcumin - chemical synthesis; Curcumin - chemistry; Curcumin - pharmacology; Dose-Response Relationship, Drug; Drug Compounding; Enzyme Inhibitors - chemical synthesis; Enzyme Inhibitors - chemistry; Enzyme Inhibitors - pharmacology; Formulations; Goats; Milk; Models, Molecular; Molecular Structure; Protective Agents - chemical synthesis; Protective Agents - chemistry; Protective Agents - pharmacology; Serum Albumin, Bovine - metabolism; Structure-Activity Relationship; Traditional excipient; Formulations; Bioenhancer; Anti-cathepsin; Curcumin; Bioavailability; Milk; Traditional excipient
• ISSN: 0045-2068; 1090-2120
• DOI: 10.1016/j.bioorg.2020.104177

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•28 different formulations.•Bioavailability.•Anti-cathepsin activities.
Cathepsins have emerged out as significant targets in variety of tissue degenerative disorders such as inflammation, alzeimers, tumerogenesis including metastasis and invasion. Elevated levels of cathepsins and reduced cellular inhibitors at the site of these diseased conditions suggest the exploration of novel inhibitors of cathepsins. In the search of effective novel inhibitors as anti-cathepsin agents different natural products are also screened. One such molecule, curcumin has been reported as potential anti-cathepsin agent in recent past. Low solubility of curcumin makes it an important subject for screening effect of different pharmaceutical excipients toward enhanced solubility. In the present work we report serum protein protecting and anti-cathepsin activities of 28 different formulations of curcumin. The formulations have been prepared using four ingredients used in traditional medicinal system. Milk has been found to enhance solubility to a significant level. Cow milk fat, sucrose and piperine exhibited positive cooperation. The results have been explained on the basis of chemical behavior of different ingredients.