1.Co-delivery of peptide-modified cisplatin and doxorubicin via mucoadhesive nanocapsules for potential synergistic intravesical chemotherapy of non-muscle-invasive bladder cancer.
Lu S1, Xu L1, Kang ET1, Mahendran R2, Chiong E2, Neoh KG3. Eur J Pharm Sci. 2016 Mar 10;84:103-15. doi: 10.1016/j.ejps.2016.01.013. Epub 2016 Jan 15.
Synergistic effect against UMUC3 bladder cancer cells was demonstrated via a "two-in-one" combination of doxorubicin (Dox) and peptide-modified cisplatin (Pt-ALy) loaded in positively charged mucoadhesive chitosan-polymethacrylic acid (CM) nanocapsules. The in vitro killing efficacy of the dual drug-loaded nanocapsules (CM-Dox-PtALy) against UMUC3 cells after 4h- and 72h-treatment is much higher (with 5-16 times lower IC50) than either Dox- or Pt-ALy-loaded nanocapsules, resulting in combination indexes of much less than 1 (i.e. obvious synergism) at fractions of affected cells ranging from 0.2 to 0.8. The dose reduction index of Pt-ALy for 72h-treatment is higher than for 4h-treatment, suggesting that Dox in CM-Dox-PtALy played a more significant role in the synergy in the former. The drug-loaded CM nanocapsules are readily taken in by the cells as shown by flow cytometry, confocal laser scanning microscopy and inductively coupled plasma mass spectrometry.
2.Palladium-catalyzed enolate arylation as a key C-C bond-forming reaction for the synthesis of isoquinolines.
Pilgrim BS1, Gatland AE, Esteves CH, McTernan CT, Jones GR, Tatton MR, Procopiou PA, Donohoe TJ. Org Biomol Chem. 2016 Jan 21;14(3):1065-90. doi: 10.1039/c5ob02320c. Epub 2015 Dec 3.
The palladium-catalyzed coupling of an enolate with an ortho-functionalized aryl halide (an α-arylation) furnishes a protected 1,5-dicarbonyl moiety that can be cyclized to an isoquinoline with a source of ammonia. This fully regioselective synthetic route tolerates a wide range of substituents, including those that give rise to the traditionally difficult to access electron-deficient isoquinoline skeletons. These two synthetic operations can be combined to give a three-component, one-pot isoquinoline synthesis. Alternatively, cyclization of the intermediates with hydroxylamine hydrochloride engenders direct access to isoquinoline N-oxides; and cyclization with methylamine, gives isoquinolinium salts. Significant diversity is available in the substituents at the C4 position in four-component, one-pot couplings, by either trapping the in situ intermediate after α-arylation with carbon or heteroatom-based electrophiles, or by performing an α,α-heterodiarylation to install aryl groups at this position.
3.Molecular and biochemical evidence on the protective effects of embelin and carnosic acid in isoproterenol-induced acute myocardial injury in rats.
Kocak C1, Kocak FE2, Akcilar R3, Isiklar OO4, Kocak H2, Bayat Z5, Simsek H3, Taser F6, Altuntas I2. Life Sci. 2016 Feb 15;147:15-23. doi: 10.1016/j.lfs.2016.01.038. Epub 2016 Jan 25.
AIMS: Acute myocardial infarction is a serious acute cardiac disorder and heart disease is still a major public health problem in adults. We investigated the effects of embelin (EMB) and carnosic acid (CA) in animals with isoproterenol (ISO)-induced myocardial injury.
4.Protective effect of fasudil hydrochloride against acute renal injury in septicopyemia rats.
Tian XH1, Jiang WS2, Li XL1, Li MF1, Liu CL3, Li XX3. Asian Pac J Trop Med. 2015 Dec;8(12):1071-5. doi: 10.1016/j.apjtm.2015.11.008. Epub 2015 Nov 12.
OBJECTIVE: To observe the protective effect of fasudil hydrochloride against acute renal injury in septicopyemia rats.
