O-Glucoside of natural cleomiscosin-A: An attenuator of pro-inflammatory cytokine production
Publication date: August 2018 Source:Phytochemistry Letters, Volume 26 Author(s): Ahil Sajeli Begum, S. Santhosh Kumar, Suryanarayana Gottapu, Kirti Hira The study was aimed to improve the hydrophilic property and pro-inflammatory cytokine inhibitory effect of cleomiscosin-A (CA), a naturally occurring coumarinolignan in plants. In view of this, O-, N- and S-glucosides of cleomiscosin-A was designed and docking studies were performed for TNF-α protein. All derivatives showed considerable docking scores in the range of −8.433 to −9.401 kcal/mol compared to a standard TNF-α inhibitor. The O-glucoside of cleomiscosin-A (CAG) was synthesized by reacting natural cleomiscosin-A (CA) with acetobromo-α-d-glucose and pyridine. The formed product was confirmed through APCI-MS and proton NMR analysis. Inhibition effect of CA and CAG against TNF-α, IL-6 and IL-1β secretions was determined on lipopolysaccharide-induced RAW 264.7 cells using ELISA kits. CAG was potentially inhibitory against IL-6 and IL-1β secretions exhibiting IC50 values of 7.94 and 45.76 μM, respectively. Also, in-vivo (mouse endotoxemia model) performance of CAG (oral administration) in inhibiting TNF-α expression was significant (52.03% and 29.23% at 50 and 25 mg/kg body weight, respectively), demonstrating five-fold increase in activity compared to CA. In addition, CAG reduced LPS-induced NO levels and was found to be weakly cytotoxic (IC50 > 150 ...
Conclusions: Results reveals that developed nitrendipine nanoemulsion gel overcomes the limitation of low penetration and accentuate permeation through albino Wistar rat skin. It was concluded that nanoemulsion gel could be utilized as a potential carrier for transdermal delivery of nitrendipine. PMID: 31976777 [PubMed - as supplied by publisher]
Authors: Rezaie Shirmard L, Ghofrani M, Bahari Javan N, Bayrami S, Tavassoli A, Rezaie A, Amini M, Kebriaee-Zadeh A, Rouini MR, Dinarvand R, Rafiee-Tehrani M, Dorkoosh FA Abstract Uncontrolled distribution of nanoparticles (NPs) within the body can significantly decrease the efficiency of drug therapy and is considered among the main restrictions of NPs application. The aim of this study was to develop a depot combination delivery system (CDS) containing fingolimod loaded poly (3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) NPs dispersed into a matrix of oleic acid-grafted-aminated alginate (OA-g-AAlg) to minimize ...
Authors: Yoshida T, Sako K, Kondo H Abstract High consumption of oil formulations has been reported to reduce the blood exposure of drugs like tacrolimus. Consumption of oil formulations has also been shown to inhibit T-cell production of interleukin-2 (IL-2) compared to solid dispersion formulations (SDFs). However, a large amount of oil causes gastrointestinal side effects such as diarrhea and low compliance. Here, we investigated the feasibility of reducing the amount of oil and substitution of chemically synthetized oils for natural oils in these formulations. Reducing the amount of sunflower oil increased bloo...
CONCLUSIONS: In conclusion, the potential for supersaturation in LBDDS, and the risk of precipitation, was found to be highly drug dependent. The apparent degree of supersaturation was considered a major factor impacting the ability to maintain drug supersaturation upon storage. PMID: 31975613 [PubMed - as supplied by publisher]
Authors: Mailhot Vega RB, Hoppe BS PMID: 31976780 [PubMed - as supplied by publisher]
With a second case of a deadly Chinese virus confirmed in the United States, and four cases under investigation in New York, Buffalo-area hospitals are on alert and preparing as best as they can. The novel coronavirus was first identified in Wuhan, China, in December. More than 850 cases have since been reported worldwide, with more than 40 deaths in China. Transportation has been shutdown with travel restricted for millions in that country as international officials work to contain the di sease. In…
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