Aloe-emodin Quantification using HPTLC and RP-UHPLC in Extracts and Commercial Herbal Formulations: Evaluation of Antimicrobial and Antioxidant Effects.

BACKGROUND: High-performance thin-layer chromatography (HPTLC) was developed and validated for the determination of aloe-emodin in accordance with ICH guidelines. In addition, a novel RP-UHPLC method was developed, and both methods were used to analyse the herbal extract and herbal formulation. METHODS: Separation was carried out on a silica gel 60 F254 HPTLC plate using the mobile phase Toluene: Methanol (9:1). The linearity was good across the 800-4000 ng/spot range. Validation results are within acceptable limits. The percent RSD for accuracy was 0.58-1.77, and precision was 1.10-1.97 and 1.45-1.94 for intraday and interday, respectively. The percentage of aloe-emodin found in the herbal extract and aloe vera capsule was 99.83 ± 1.19 and 99.53 ± 1.29, respectively, using this method. RESULTS: Quantification of aloe-emodin in herbal extract and herbal formulation were done using a novel UHPLC method with chromatographic conditions of orthophosphoric acid Methanol (0.1 percent OPA): Water (65:35, v/v) and pH 3, a flow rate of 1.2 ml/min, and elute detection at 254 nm. At 6.32 minutes, a sharp and symmetric peak was observed. The method developed was validated in accordance with ICH guidelines. The percent RSD numerical value of accuracy was 0.304-0.576, and the inter-day and intraday precision were 0.32-3.08 and 0.51-2.78, respectively. Herbal extract and aloe vera capsule were analysed using the new UHPLC method. Aloe-emodin percentages were reported as 100.3 ± 0.89 and 99.53 ± 1.29, respectively. CONCLUSION: The antimicrobial and anti-oxidant activities of an aloe-vera herbal formulation were studied, and the results were positive.

Approaches for Ear-targeted Delivery Systems in Neurosensory Disorders to avoid Chronic Hearing Loss Mediated Neurological Diseases.

BACKGROUND AND OBJECTIVE: Hearing loss is a common audio-vestibular-related neurosensory disability of inner ears, in which patients exhibit clinical symptoms of dizziness, gait unsteadiness, and oscillopsia, at an initial stage. While, if such disorders are untreated for a prolonged duration then the progression of disease into a chronic state significantly decreases GABA level as well as an alteration in the neurotransmission of CNS systems. Hence, to control the progression of disease into a chronic approaches for timely and targeted delivery of the drugs at the site of action in the ear is now attracting the interest of neurologists for effective and safe treatment of such disorders. Among delivery systems, owing to small dimension, better penetration, rate-controlled release, higher bioavailability; nanocarriers are preferred to overcome delivery barriers, improvement in residence time, and enhanced the performance of loaded drugs. Subsequently, these carriers also stabilize encapsulated drugs while also provide an opportunity to modify the surface of carriers to favor guided direction for site-specific targeting. Contrary to this; conventional routes of drug delivery such as oral, intravenous, and intramuscular are poorer in performance because of inadequate blood supply to the inner ear and limited penetration of blood-inner ear barrier. CONCLUSION: This review summarized novel aspects of non-invasive and biocompatible nanoparticles- based approaches for targeted delivery of drugs into the cochlea of the ear to reduce the rate, and extent of the emergence of any hearing loss mediated neurological disorders.

Quality Control Standardization, Contaminant Detection and In Vitro Antioxidant Activity of Prunus domestica Linn. Fruit.

The increase in the use of herbal medicines has led to the implementation of more stern regulations in terms of quality variation and standardization. As medicinal plants are prone to quality variation acquired due to differences in geographical origin, collection, storage, and processing, it is essential to ensure the quality, efficacy, and biological activity of medicinal plants. This study aims to standardize the widely used fruit, i.e., Prunus domestica Linn., using evaluation techniques (microscopic, macroscopic, and physicochemical analyses), advanced instrumental (HPLC, HPTLC, and GC-MS for phytochemical, aflatoxins, pesticides, and heavy metals), biological, and toxicological techniques (microbial load and antioxidant activities). The results revealed a 6-8 cm fruit with smooth surface, delicious odor, and acidic taste (macroscopy), thin-walled epidermis devoid of cuticle and any kind of excrescences with the existence of xylem and phloem (microscopy), LOD (15.46 ± 2.24%), moisture content (13.27 ± 1.75%), the high extractive value of 24.71 ± 4.94% in water:methanol (1:1; v/v) and with ash values in the allowed limits (physicochemical properties), and the presence of numerous phytochemical classes such as alkaloids, flavonoids, carbohydrates, glycosides, saponins, etc. (phytochemical screening). Furthermore, no heavy metals (Pb, Hg, Cd, Ar), pesticides, ad microbial limits were detected beyond the permissible limits specified, as determined with AAS, GC-MS analysis, and microbial tests. The HPTLC was developed to characterize a complete phytochemical behavior for the components present in P. domestica fruit extract. The parameters utilized with the method used and the results observed for the prunus herein may render this method an effective tool for quality evaluation, standardization, and quality control of P. domestica fruit in research, industries, and market available food products of prunus.

Aegle marmelos Leaf Extract Phytochemical Analysis, Cytotoxicity, In Vitro Antioxidant and Antidiabetic Activities.

For many years, Aegle marmelos (A. marmelos) has been used medicinally and as a dietary supplement. Despite this, there are minimal research data on A. marmelos phytochemical properties and pharmacological effects. This study aimed to explore the phytoconstituents, cytotoxicity, glucose uptake, and antioxidant and antidiabetic potential of an alcoholic extract of A. marmelos leaf. The cytotoxicity of A. marmelos in HepG2 cells was tested in vitro, and the results revealed that it has strong cytocompatibility and cytoprotective properties. The extract's antioxidant activities were investigated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP) methods. Antioxidant potential was shown to be quite impressive. The enzymes α-amylase and α-glycosidase were found to be substantially inhibited by A. marmelos, with IC50 values of 46.21 and 42.07 mg/mL, respectively. In HepG2 cells, A. marmelos significantly reduced ROS levels that were elevated due to high glucose and enhanced glucose consumption (p < 0.05). These activities might be due to the enrichment of bioactive phytoconstituents analyzed chromatographically using GC/MS and HPLC. The findings of this study show that A. marmelos could be an effective restorative therapy for diabetes and related diseases.

Synthesis and anticonvulsant activity of some novel fused heterocyclic 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives.

In the present investigation, a series of 3,6-disubstituted-1,2,4-triazolo-1,3,4-thiadiazole derivatives (6a-t) were synthesized and evaluated for their anticonvulsant activity and neurotoxicity. The structures of synthesized compounds were confirmed on the basis of their elemental analysis and spectral data results. In anti-MES activity compounds 6b, 6c, 6g, 6j, 6k, 6q and 6r showed potent activity comparable to that of standard drugs: phenytoin and carbamazepine. Compounds 6c, 6k, 6n, 6p and 6s successfully passed the rotorod test without any sign of neurological deficit.

2-[3-(4-chloro/ethyl phenyl)propan-3-one]-5-(substituted phenyl)-1,3,4-oxadiazoles: synthesis and biological evaluation.

In the present investigation, two novel series of 2-[3-(4-chlorophenyl)propan-3-one]-5-(substituted phenyl)-1,3,4-oxadiazole and 2-[3-(4-ethylphenyl)propan-3-one]-5-(substituted phenyl)-1,3,4-oxadiazole were synthesized and tested for their antiinflammatory, analgesic, ulcerogenic and antibacterial actions. A fair number of compounds were found to have very good antiinflammatory activity in carrageenan induced rat paw edema test, while a few compounds showed significant analgesic activity in acetic acid induced writhing test. The newly synthesized compounds showed very low ulcerogenic action and moderate antibacterial action.