In recent years, natural edible products have been found to be important therapeutic agents for the treatment of chronic human diseases including cancer, cardiovascular disease, and neurodegeneration. Curcumin is a well-known diarylheptanoid constituent of turmeric which possesses anticancer effects under both pre-clinical and clinical conditions. Moreover, it is well known that the anticancer effects of curcumin are primarily due to the activation of apoptotic pathways in the cancer cells as well as inhibition of tumor microenvironments like inflammation, angiogenesis, and tumor metastasis. In particular, extensive studies have demonstrated that curcumin targets numerous therapeutically important cancer signaling pathways such as p53, Ras, PI3K, AKT, Wnt-β catenin, mTOR and so on. Clinical studies also suggested that either curcumin alone or as combination with other drugs possess promising anticancer effect in cancer patients without causing any adverse effects. In this article, we critically review the available scientific evidence on the molecular targets of curcumin for the treatment of different types of cancer. In addition, we also discuss its chemistry, sources, bioavailability, and future research directions.
Context: Naturally occurring polyphenols including olive oil (OO) and its constituents hydroxytyrosol (HT) and tyrosol (TY), consumed in the Mediterranean diet, have shown to treat various ailments due to their remarkable antioxidant properties. Objective: The present study investigates the hepatoprotective effects of OO and its phenolic compounds HT and TY against TCDD-induced hepatotoxicity in male Wistar rats. Materials and methods: TCDD was administered at a dose of 100 ng/kg p.o. for 20 d. Administration of OO (10 ml/kg; oral), HT (0.5 mg/kg; oral), and TY (30 mg/kg; i.p) was started 5 d prior to TCDD administration, and continued for 25 d with or without TCDD administration. At the end of the experiment (25 d), blood was taken for biochemical analyses and liver for the measurement of macromolecular damages, antioxidant status, expressions of CYP1A1, and apoptotic factors. Results: TCDD administration resulted in significant (p50.05) increase in the level of hepatic stress markers ALT (101.6 ± 3.07 IU/l), AST (295.0 ± 3.0 IU/l), and ALP (266.66 ± 3.7 IU/l). Also, biochemical analyses of liver reported elevation in nitrite and protein carbonyl content and depletion of NQO1 and HO. However, OO, HT, and TY restored the antioxidant status. Protein expressions by Western Blot technique showed an increase in the level of CYP1A1 and Bax and a decreased level of Bcl-2 on TCDD treatment, and vice versa on OO, HT, and TY treatment. Discussion and conclusion: Our work concludes that dietary supplementation of OO, HT, and TY could serve as a potential preventive drug for TCDD-induced hepatotoxicity.
Dementia is a chronic progressive mental disorder, which adversely affects memory, thinking, comprehension, calculation and language. Some of the commonest forms of dementia are Alzheimer's disease, Parkinsonism, Dementia with Lewy Bodies and Myasthenia gravis. All these disorders are related to abnormalities in the central cholinergic system, which shows a decline in acetylcholine level. Cholinesterase (ChE) inhibitors are one of the novel strategies used for the symptomatic treatment of neurological disorders like dementia. In the course of screening new ChE inhibitors from marine sources, about 11 seaweeds, which have wide pharmaceutical applications, were collected from Hare Island, Gulf of Mannar, Tamilnadu, India. Methanolic extracts of the seaweeds were assessed for ChE inhibitory activity under in vitro conditions. Kinetic parameters IC(50), K(i) and V(max) were also analysed. The results showed that 3/11 seaweeds showed 50% inhibition for both ChEs (using acetylthiocholine iodide and butyrylthiocholine iodide as substrate) at concentrations of 2 mg mL(-1) (Gracilaria gracilis, Sargassum, Cladophora fasicularis for ChE with acetylthiocholine iodide as substrate and Gracilaria gracilis, Gracilaria edulis, Sargassum for ChE with butyrylthiocholine iodide as substrate) and 4/11 showed no inhibitory activity. Inhibitory activity of seaweed extracts was compared with standard drug donepezil. Enzyme kinetic analysis showed that algal extracts exhibited mixed type inhibition (partially non-competitive inhibition).
Context: Sargassum has been used in traditional Chinese medicine since the eighth century AD to treat goiter. Sargassum wightii Greville (Sargassaceae) is a major source of alginic acid used widely in food and drug industries. Objective: To evaluate the anti-Alzheimer potential of S. wightii through evaluation of antioxidant and cholinesterase inhibitory activities. Materials and methods: Successive extraction was done using solvents of varying polarity. Solvent extracts (100-500 mg/mL) were employed for all the antioxidant assays. Free radical scavenging activity was evaluated by 2,2-diphenyl-1-picrylhydrazyl, OH. , H 2 O 2 radical scavenging assay. The reducing power of the seaweed was evaluated by ferric reducing antioxidant power and reducing power assay. Cholinesterase (ChE) inhibitory activity was evaluated and the Km, Vmax and Ki were calculated. Further, compound characterization was done by GC-MS analysis. Results: The non-polar extracts were found to possess significant antioxidant activity. At 100 mg/mL, petroleum ether, hexane, benzene and dichloromethane extracts showed significant ChE inhibitory activity with IC 50 values of 19.33 AE 0.56, 46.81 AE 1.62, 27.24 AE 0.90, 50.56 AE 0.90 mg/mL, respectively, for AChE, and 17.91 AE 0.65, 32.75 AE 1.00, 12.98 AE 0.31, 36.16 AE 0.64 mg/mL, respectively, for BuChE. GC-MS reveals that 1,2-benzenedicarboxylic acid, diisooctyl ester is the major compound present in dichloromethane extract of S. wightii. The mode of inhibition exhibited by dichloromethane extract against the cholinesterases was found to be competitive type. Discussion and conclusion: The presence of high amount of terpenoids could be the possible reason for its potential antioxidant and ChE inhibitory activity.
Biofilm formation, quorum sensing (QS)-regulated virulence and emergence of antibiotic resistance in bacterial pathogens lead to major health problems. In this perspective, antibiofilm agents and QS inhibitors have gained much attention to treat infections caused by antibiotic-resistant pathogens. For the first time, this investigation reports the antibiofilm and QS inhibitory potential of the brown macroalga Padina gymnospora against the nosocomial pathogen Serratia marcescens. The methanolic extract of P. gymnospora inhibited biofilm formation and the production of prodigiosin and protease. Successive solvent extraction, bioassay-guided fractionation of chloroform extract and GC-MS analysis of active fractions showed the presence of alphabisabolol with a relative abundance of 69 %. In vitro assays with alpha-bisabolol evidenced the potent inhibition of biofilm and QS-controlled prodigiosin, protease and swarming in S. marcescens, without exerting deleterious effect on its growth and metabolic activity. The results of this study exemplify the use of P. gymnospora and alpha-bisabolol as promising alternatives to antibiotics.
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