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Chitosan (CS) and phloroglucinol (PhG), two extracts abundantly found in marine life, were investigated for their ability to biomodify demineralized dentin by enhancing collagen crosslinks and improving dentin extracellular matrix (ECM) mechanical and biochemical stability. Dentin obtained from non-carious extracted human molars were demineralized with phosphoric acid. Baseline Fourier-transform infrared (FTIR) spectra, apparent flexural elastic modulus (AE) and dry mass (DM) of each specimen were independently acquired. Specimens were randomly incubated for 5 min into either ultrapure water (no-treatment), 1% glutaraldehyde (GA), 1% CS or 1% PhG. Water and GA were used, respectively, as a negative and positive control for collagen crosslinks. Specimens' post-treatment FTIR spectra, AE, and DM were obtained and compared with correspondent baseline measurements. Additionally, the host-derived proteolytic activity of dentin ECM was assessed using hydroxyproline assay (HYP) and spectrofluorometric analysis of a fluorescent-quenched substrate specific for matrix metalloproteinases (MMPs). Finally, the bond strength of an etch-and-rinse adhesive was evaluated after application of marine compounds as non-rinsing dentin primers. Dentin specimens FTIR spectral profile changed remarkably, and their AE increased significantly after treatment with marine compounds. DM variation, HYP assay and fluorogenic substrate analysis concurrently indicated the biodegradation of CS- and PhG-treated specimens was significantly lesser in comparison with untreated specimens. CS and PhG treatments enhanced biomechanical/biochemical stability of demineralized dentin. These novel results show that PhG is a primer with the capacity to biomodify demineralized dentin, hence rendering it less susceptible to biodegradation by host-proteases.

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BACKGROUND/AIM: A series of experiments on HeLa cells were conducted to provide new information concerning the anti-cancer properties of jaspine B hydrochloride (JBH). MATERIALS AND METHODS: HeLa cells treated with 0.5 µmol/l JBH for 24, 48, and 72 h underwent flow cytometric analysis of the cell cycle, and measurement of phosphatidylserine externalization, mitochondrial membrane potential (MMP), casp-3 activation, cleavage of PARP, ceramide levels, aSMase activity, and Bcl-2 release. nSMase activity was measured by a colorimetric assay. Gene expression was determined by qRT-PCR. Immunocytochemistry was performed to detect p21 and p27 expression. RESULTS: JBH-induced apoptosis in HeLa cells associated with externalization of phosphatidylserine, reduced MMP, activation of casp-3, and cleavage of PARP as well as up-regulation of TNF-α, FasL, and casp-8. Significant increase in nSMase activity, ceramide levels, Bcl-2 release (predominantly in the inactive form), and pro-apoptotic nuclear localization of p21 and p27 were also detected. CONCLUSION: JBH-induced apoptosis in HeLa cells is associated with disrupted sphingolipid homeostasis resulting in increased ceramide levels.

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Marine derivatives are of great pharmaceutical interest as inhibitory compound and search of bioactive compounds from Marine organism which is relatively new to medicinal chemistry. Our main aim in the study is to screen possible inhibitors against CCR5 which acts as co-receptor M-tropic HIV-1, through virtual screening of 122 Marine derived compounds from various organisms known to have biological activity. Homology Model of CCR5 was constructed using MODELLER and the Model was energy minimized and validated using PROCHECK to obtain a stable structure, which was further used for virtual screening of Marine derived compounds through molecular Docking studies using GOLD. The Docked complexes were validated and Enumerated based on the GOLD Scoring function to pick out the best Marine inhibitor based on GOLD score. Thus from the entire 122 Marine compounds which were Docked, we got best 4 of them with optimal GOLD Score. (LAMIVUDINE: 45.0218, BATZELLINE-D: 44.3852.ACYCLOVIR: 43.1362 and THIIOACETAMIDE: 42.7412) Further the Complexes were analyzed through LIGPLOT for their interaction for the 4 best docked Marine compounds. Thus from the Complex scoring and binding ability its deciphered that these Marine compounds could be promising inhibitors for M-tropic HIV-1 using CCR5 as Drug target yet pharmacological studies have to confirm it.