Novel extraction technique: quantification of major phytoconstituents of arjuna in infused edible oil.

A rapid, precise, accurate, and cost-effective liquid chromatography-mass spectrometer method was developed by using a novel extraction technique for the simultaneous quantification of major oleane derivatives: arjunetin, arjungenin, arjunolic acid, and arjunic acid of Terminalia arjuna in infused edible oil. An innovative idea was implemented to extract the active phytoconstituents from the oil matrix based on the freezing point of oils and extraction solvent. The developed method was validated for all four active compounds in the linear working range of 0.47-1.72 µg/mL, 0.845-2.93 µg/mL, 1.73-5.95 µg/mL and 0.62-2.22 µg/mL with good correlations value (r2) more than 0.99 for arjunetin, arjungenin, arjunolic acid, and arjunetin, respectively. Furthermore, the HPTLC method was also developed for the quick identification of all four active markers along with other phytoconstituents infused in oil.

Exploring the Potential of Traditional Herbs in the Management of Diabetic Retinopathy: An Overview.

Diabetic retinopathy is a microvascular complication in diabetes that affects eyes and is responsible for most visual impairment in diabetic patients. Diabetic retinopathy affects up to 80% of those who have had diabetes for 20 years or more. At least 90% of new cases could be reduced with proper treatment and monitoring of the eyes. The longer a person has diabetes, the higher his or her chances of developing diabetic retinopathy. Hence, it compels need for its prevention and cure. There is an increasing interest in natural products in pharmacotherapy as the chemical diversity of natural products has better matches than the diversity of synthetic compounds. The current review summarises the potential of leading traditional herbs like Azadirachta indica, Ginkgo biloba, Anisodus tanguticus, Pinus pinaster, Salvia miltiorrhiza, Stephania tetrandra and Gymnema sylvestre in the management and potential reversal of DR-related pathogenesis. It also discusses the probable mechanism of actions, which are based on epidemiological, in-vitro and in-vivo studies carried out within past few years. Graphical Abstract.

Synthesis, Characterization of Ethyl 5-(substituted)-1H-pyrazole- 3-carboxylate Derivative as Potent Anti-inflammatory Agents.

BACKGROUND: Recently, pyrazole derivatives have shown significant antiinflammatory activity. Non-steroidal anti-inflammatory drugs have some side effects, mainly gastric irritation and gastric ulceration during the treatment of inflammation. So the current study deals with the synthesis and pharmacological evaluation of a series of novel pyrazole derivatives as anti-inflammatory agents. METHODS: A series of novel ethyl 5-(substituted)-1H-pyrazole-3-carboxylate (2a-j) were synthesized and evaluated for anti-inflammatory activity using carrageenan-induced inflammation in rat paw edema model. In the first step, diethyl oxalate react with acetophenone derivatives in presense of sodium ethoxide to form substituted ethyl-2,4-dioxo-4- phenyl butanoate derivatives as intermediate (1a-j). Further the suspension was prepared from dioxo-esters with hydrazine hydrate in glacial acetic acid yielded novel ethyl 5- (substituted)-1H-pyrazole-3-carboxylate (2a-j) derivatives. The structure of the final analogues (2a-j) has been confirmed on the basis of elemental analysis, IR, 1 H NMR and mass spectra. RESULTS: All the values of elemental analysis, FTIR, 1H NMR, and mass spectra were found to be prominent. The anti-inflammatory activity test revealed that Ethyl 5-(3,4- dimethoxyphenyl)-1H-pyrazole-3-carboxylate (2f) and ethyl 5-(2,3-dimethoxyphenyl)-1Hpyrazole- 3-carboxylate (2e) exhibited significant anti-inflammatory activity as compared to control group. CONCLUSION: The results of the current study indicate that the substitution at pyrazole scaffold could improve anti-inflammatory activity.

Adaptogenic potential of Oxitard in experimental chronic stress and chronic unpredictable stress induced dysfunctional homeostasis in rodents.

BACKGROUND: Oxitard, a polyherbal formulation comprising the extracts of Withania somnifera, Mangifera indica, Glycyrrhiza glabra, Daucus carota, Vitis vinifera, powders of Syzygium aromaticum, Yashada bhasma and Emblica officinalis; and oils of Triticum sativum. OBJECTIVE: Current study deals with the assessment of Oxitard (a marketed polyherbal formulation) for its adaptogenic potential in chronic unpredictable stress (CUS) and chronic stress (CS) induced dysfunctional homeostasis in rodents. MATERIALS & METHODS: Animals were immobilized for 2 h every day for ten days to induce CS. In order to induce CUS, animals were employed in a battery of stressors of variable value and duration for ten days. Following administration of Oxitard, stress was induced in the animals. Stress-induced efficient changes were evaluated by assessing organ (adrenal gland) weights, ulcer index, hematological parameters and biochemical levels of reduced glutathione (GSH), thiobarbituric acid reactive substances (TBARS) and catalase (CAT). RESULTS: CS and CUS significantly modified the oxidative stress parameters (increased MDA and decreased GSH). Furthermore, CS and CUS lead to weight reduction, adrenal hypertrophy and gastric ulceration. Pre-treatment with Oxitard (200 and 400 mg/kg, p.o.) significantly modified CS and CUS induced hematological changes, oxidative stress parameters and pathological effects. CONCLUSION: In conclusion, Oxitard-intervened antioxidant actions are accountable for its adaptogenic effects in stress-induced dysfunctional homeostasis.

Synthesis, Characterization & Screening for Anti-Inflammatory & Analgesic Activity of Quinoline Derivatives Bearing Azetidinones Scaffolds.

BACKGROUND: Non-steroidal anti-inflammatory drugs (NSAIDS) are clinically used as anti-inflammatory, analgesic and antipyretic agents but they have the drawbacks such as gastric irritation and gastric ulceration. Recently, quinoline derivatives have shown significant anti-inflammatory and less ulcerogenic activity. The present study deals with the synthesis and pharmacological assessment of a series of novel quinoline derivatives bearing azetidinones scaffolds as anti-inflammatory and analgesic agents. METHODS: A series of newer 3-chloro-1-(substituted)-4-(tetrazolo [1,5-a]quinolin-4- yl)azetidin-2-one derivatives (6a-l) was synthesized starting with acetanilide (1). Initially, acetanilide (1) was allowed to react with Vilsmeier-Haack reagent (DMF + POCl3) to form 2- chloro-3-formyl quinoline (2). The 2-chloro-3-formyl quinoline (2) was further treated with p-toluenesulphonic acid and sodium azide which yielded Tetrazolo [1,5-1] quinoline-4- carbaldehyde (3). The reaction of formyl group with various substituted amines (4a-l) formed corresponding Schiff base intermediates (5a-l), which were further allowed to react with chloroacetyl chloride to produce 3-chloro-1-(substituted)-4-(tetrazolo [1,5-a]quinolin-4-yl) azetidin-2-one derivatives (6a-l). The structure of the final analogues (6a-l) has been confirmed on the basis of elemental analysis, IR, 1H NMR, 13C NMR and mass spectra. All the synthesized compounds were evaluated for their anti-inflammatory and analgesic activities by using carrageenan induced rat paw model and Eddy's hot plate method respectively. RESULTS: All the values of elemental analysis, IR, 1H NMR, 13C NMR and mass spectra were found to be prominent. The anti-inflammatory activity test revealed that 3-chloro-1-(4-methoxyphenyl)- 4-(tetrazolo[1,5-a] quinolin-4-yl)azetidin-2-one (6b), 3-chloro-1-(2-methoxyphenyl)- 4-(tetrazolo[1,5-a]quinolin-4-yl)azetidin-2-one (6a) exhibited significant anti-inflammatory and analgesic activity as compared to control group. CONCLUSION: The results of the current study indicate that substitution at quinoline derivatives bearing azetidinones scaffolds showed potent analgesic and anti-inflammatory activities.

Fractal growth kinetics and electric potential oscillations during electropolymerization of pyrrole.

Fractal growth, growth kinetics, and electrical conductivity of aggregates obtained during electropolymerization in the systems (A) pyrrole-4-toluene sulfonic acid silver salt (4-TSS)-acetonitrile, (B) pyrrole-4-TSS-ZnSO(4)-acetonitrile, and (C) pyrrole-4-TSS-aniline-acetonitrile were investigated. In the case of system (A), effect of [4-TSS], [pyrrole], field intensity, and solvents H(2)O and CH(3)OH on morphology, fractal character, and growth kinetics was also studied. Fractal growth data were examined in detail. During studies on system (A), electric potential oscillations were observed and subjected to detailed study. The results indicate that fractal growth pattern and electric potential oscillations are inter-related. The mechanism of development of fractal growth, dendritic structure, and electric potential oscillations is discussed in terms of diffusion-limited aggregation and modified Diaz's mechanism, which explains the random movement of radical cations.