Background
A quantifiable method has been developed to determine the key starting material, its intermediates and known impurities in the presence of Imipramine Hydrochloride in the final API of a synthetic laboratory sample. This newly developed Reverse-Phase High-Performance Liquid Chromatography (RP-HPLC) method is, facile, specific and reliably practical.
Materials and Methods
The separation column employed was Inertsil ODS-3 C18 with a mobile phase comprised of (A) 0.1% OPA (pH adjusted to 3.2) and (B) acetonitrile. Mobile phase A is a 100% buffer solution. Acetonitrile was used as mobile phase “B” and mobile phase B was used as 100% organic Solvent. The analytes were detected at 220 nm using a UV detector where the flow rate of the mobile phase was kept at 1.0 mL min-1 and the gradient program was set as T/% B: 0/30, 5/30, 10/80, 12/80, 15/30, 20/30 with a fixed flow rate of 1.0 mL min-1.
Results
According to the regulatory standards advised by the ICH, the performance of this method is best agreed upon by all the important parameters. The approach used in the present work can be used for process development and determining the purity of associated compounds of Imipramine Hydrochloride, key starting material (2,2-dinitro-1,2-diphenylene ethane), intermediate-1 (2-2-diamino-1,2-diphenyl ethane diphosphate) and intermediate-2 (iminodibenzyl) all in a single method.
Conclusion
This newly developed and validated method will save time and create ease by preventing the development of different methods for analyzing intermediates and impurity profiling.
Aim
Broccoli fiber has enormous safety net as well as high pre-biotic value. Amoxicillin is although an effective drug against infections is equally harmful to gut microbiota and therefore the above side-effect impedes the use of amoxicillin. The present study deals with evaluating the dual benefits of the partially depolymerized fiber to deliver amoxicillin when the same is used as base fiber in lieu of Micro Crystalline Cellulose (MCC), as well as in protecting the gut microbiota by serving as transient refuge cum pre-biotic material.
Materials and Methods
Broccoli was partially depolymerized by alkali treatment and subjected to pre formulation studies such as powder microscopy, ash content analysis, particle density and angle of repose. Then using the partially depolymerized fiber formulated tablet dosage form of amoxicillin (500 mg). Using XRD and FTIR the interaction of partially depolymerized fiber with amoxicillin was studied. Release pattern of amoxicillin from the fiber and selective preference and binding of various probiotic species was studied simultaneously using different simulated gut systems.
Results
Study findings show that broccoli fiber instantaneously released amoxicillin and the space vacated by amoxicillin is being occupied rapidly by various probiotic species and thereby could survive the amoxicillin effect. The parachute effect of the fiber to probiotic is also reconfirmed by simulated gut digestion process and findings show the post gut digested fiber also exhibited significant prebiotic value. The fiber also met various physiochemical parameters that of MCC and also formulation dependent characteristics such as flow, compressibility and disintegration. Zero modification to the fiber vis-à-vis amoxicillin also established by X-ray Diffraction (XRD) and Fourier-Transform Infrared Spectroscopy (FTIR).
Conclusion
Probiotic microbes when encounter amoxicillin shows greater preference towards the partially depolymerized fiber and seek parachute effect from the fiber. Broccoli fiber is useful to deliver amoxicillin and also protect gut microbiome.
Aim/Background
The purpose of the current study is to understand the COVID-19 pandemic as the greatest psychological challenge that humankind has ever faced. COVID-19 started in China in December 2019 and has conquered the whole world today. Everyone is responding to this pandemic in their own unique way and psychologically facing a global threat in the process. This paper seeks to examine how COVID-19 has psychologically affected the education sector. The purpose of the study is to analyze the prevailing situation and to study the impact of COVID-19.
Materials and Methods
ANOVA is used as a tool to analyze the impact of school closures on different levels of students in India and to determine the effectiveness and efficiency of the education sector in India.
Results
The major findings are that due to COVID-19 the number of students affected at different levels (pre-primary students, primary students, lower secondary students and upper secondary students) whereas whether students are male or female COVID-19 have an impact on different levels of students. The experience gained during this tough period will sow seeds for both health awareness and an understanding of the importance of remaining healthy to tackle any such future impediments.
Conclusion
The paper sheds light on the psychological challenges in the Indian education sector and the various steps adopted by the Indian government to ensure the nation to survive and overcome the prevailing COVID-19 situation.
Aim
This Study aimed to develop a stable, efficient, and reproducible RP-HPLC method that indicates stability, for the simultaneous determination of Remogliflozin Etabonate and Metformin HCl.
Materials and Methods
The Separation Process By using Methanol: 0.05 M KH2PO4 (75:25%v/v) as the mobile phase and a linear gradient protocol with a detection wavelength of 240 nm, the chromatographic separation was accomplished on (Anachrom) Cosmosil C18 (250×4.6 mm, 5 μm) Column. 35°C was the column temperature, and the flow rate was 1 mL per min. For Remogliflozin Etabonate and Metformin HCl, the retention times were determined to be 8.51 and 2.63 min, respectively. Studies on forced deterioration were conducted in thermal, photolytic, oxidative, acidic, basic, oxidizing environments. According to ICH guidelines, the method’s robustness, accuracy, precision, linearity, LOD, and specificity were all verified.
Results
The regression analysis indicated a strong correlation with a linear curve in the concentration ranges 1-5 μg mL-1 for Remogliflozin Etabonate and 5-25 μg mL-1 for Metformin HCl, demonstrating the linearity of the developed method. Moreover, the approach used in the study was distinctive in that it successfully avoided degradants even after subjecting the dugs to forced degradation. The percentage recovery of REMO and MET from the pharmaceutical dosage form was in the range of 99.33%-99.73% and 99.64%-99.93% respectively. The method was characterized by high accuracy, precision, and robustness, with LOD and LOQ values of 2.218 μg mL-1 and 6.724 μg mL-1for Remogliflozin Etabonate and 0.582 μg/mL and 1.764 μg/mL for Metformin HCl, respectively.
Conclusion
The developed method can be used in routine analysis of bulk and dosage forms due to its adaptability, accuracy, and high precision.
Aim
To evaluate the pharmacokinetics and toxicity properties of Valganciclovir Hydrochloride, a potent antiviral agent, using in silico models.
Background
Valganciclovir Hydrochloride is an FDA-approved antiviral agent and understanding its pharmacokinetic and toxicological properties is critical for optimizing its use.
Objectives
To assess the pharmacokinetic properties, toxicity profile and bioactive characteristics of Valganciclovir Hydrochloride using computational in silico models.
Materials and Methods
Lipinski’s Rule of Five was applied to evaluate the compound’s solubility and intestinal absorption properties. The drug’s plasma protein binding and Blood-Brain Barrier (BBB) penetration were also assessed to understand its distribution profile. Clearance rates were calculated to evaluate how efficiently the compound is eliminated from the body. Additionally, the LD50 value of Valganciclovir Hydrochloride was estimated using a rat toxicity model to understand its toxicity threshold. Pharmacological activities were further assessed using the PASS online server to evaluate its bioactive properties and potential toxic effects on non-tumor cell lines.
Results
Valganciclovir Hydrochloride exhibited high solubility and a moderate rate of intestinal absorption. The drug showed low plasma protein binding and poor BBB penetration, suggesting that its distribution is primarily localized within the body. The compound demonstrated a low clearance rate of 5 mL/min/kg. Toxicity analysis revealed an estimated LD50 value of 3,080,000 mg/kg via the oral route, indicating a relatively high toxicity threshold. The PASS analysis highlighted various bioactive properties without any toxic effects on non-tumor cell lines, with a Probability of occurrence (Pa) value lower than 0.5, further supporting the non-toxic profile of the compound.
Aim
To study the Kaempferol (Kaem) on Pentetrazol (PTZ)-induced chronic epileptic rats, and to explore its effect on nucleotide-binding oligomerization domain-like receptor protein 3 (NLRP3)/ caspase-1/gasdermin D (GSDMD)-mediated pyroptosis in the cerebral cortex and its possible mechanism.
Materials and Methods
Six rats were randomly selected from 30 SPF male SD rats as the normal group, and the remaining rats were intraperitoneally injected with PTZ (35 mg/kg) for 28 d to replicate the chronic epilepsy model. The 18 successfully modeled rats were randomly divided into model, low-dose Keam (Kaem-L), Middle-dose Keam (Keam-M) and high-dose Kaem (Kaem-H) groups, with 6 rats in each group. The rats in Kaem-L, Keam-M and Kaem-H groups received 1, 2 and 10 mg/kg of Kaem by continuous lavage for 14 d, while those in normal and model groups were given equal volume of saline. The latency of Generalized Tonic-Clonic Seizures (GTCS) and Minimal Clonic Seizures (MCS) was recorded. The pathological changes of the temporal lobe cortex were observed by HE staining. Neuronal apoptosis was detected by TUNEL staining. The protein levels of NLRP3, caspase-1 and GSDMD in the cortex were detected by immunohistochemical staining and Western blot. The expression levels of TNF-α, interleukin-18 (IL-18) and IL-1β in brain tissue were detected by immunohistochemical staining. The mRNA expression levels of NLRP3, caspase-1 and GSDMD in the cerebral cortex were detected by RT-qPCR.
Results
Compared with normal group, the latency of GTCS and MCS in the rats of model group was significantly shortened (P <0.01). Compared with normal group, the number of apoptotic cortical neurons in model group was significantly increased. The protein expression levels of TNF-α, IL-18 and IL-1β in the cortical tissues were significantly increased, and the mRNA and protein expression levels of NLRP3, caspase-1 and GSDMD were also significantly increased (P <0.01). Compared with model group, the latency of GTCS and MCS in Kaem treated groups was significantly prolonged, the number of apoptotic cortical neurons in rats was significantly reduced, the protein expression levels of TNF-α, IL-18 and IL-1β in cortical tissue was reduced to varying degrees, and the mRNA and protein expression of NLRP3, caspase-1 and GSDMD also showed varying degrees of reduction (P <0.01).
Conclusion
The Kaem may reduce the secretion of inflammatory factors and inhibit the pyroptosis of nerve cells through the NLRP3/caspase-1/ GSDMD signaling pathway, thus playing a therapeutic role in chronic epileptic rats induced by PTZ.
Oxadiazoles and their derivatives represent a significant class of organic compounds, wielding profound implications in both the realms of medicinal science and heterocyclic rings housing oxygen and nitrogen atoms, has garnered attention owing to their multifaceted. Pharmacological potential. The diverse array of biological activities exhibited by oxadiazole derivatives spans antimicrobial, anti-inflammatory, anti-cancer and anti-viral effects. Beyond medicinal applications, these compounds showcase utility in agriculture, with their herbicidal, insecticidal and fungicidal properties enabling their role as effective plant protection agents. Researchers have been focusing on the synthesis and exploration of these compounds for their potential in drug development. This review article is an in-depth exploration of diverse synthetic methodologies for oxadiazole and its derivatives while highlighting their associated pharmacological activities. It offers valuable insights into this class of compounds’ versatile chemistry and potential therapeutic applications.
Background
The prime objective of the investigation is to measure the capability of expanding the enumeration of platelet in rodent model utilizing hydro-alcoholic extract of Psidium guajava L. fruit in addition with in silico modelling on Dengue Virus Protease Inhibitors.
Materials and Methods
Using a double maceration procedure with 30% water and 70% ethanol, the harvested fruit was extracted. Heparin-induced thrombocytopenic rats were used to assess the extract’s thrombocytopenic action. Prednisolone was used as the standard medication and the animals were divided into five categories. The platelet count was performed using a hemocytometer. Additionally, bleeding duration was assessed and at last in silico studies has been carried out through several softwares to identify the targeting molecule.
Results
Prednisolone, Psidium guajava L. low dosage and Psidium guajava L. high dose on the 14th day demonstrated the numbers of platelet 1732614, 874021 and 946224 respectively compared with toxicant control in the heparin-induced thrombocytopenic rat model.
Conclusion
It is clear from the results above that Psidium guajava L. significantly increased the count of platelet when equated to the toxicant control. Thus, it can be said that Psidium guajava L. plant extract significantly induces thrombocytopenia and it is found that NS2-NB3 protease is the promising target for dengue virus and in future we will try to identify the quercetin or quercetin derivatives of Psidium guajava L. responsible for producing effectiveness against the said target.
Background
Manilkara zapota, a plant with a rich history in traditional medicine, holds potential as a therapeutic agent. However, its neuroprotective properties remain largely unexplored, highlighting the need for further scientific research to understand its potential in this regard.
Objectives
This study aimed to explore the neuroprotective effects of Manilkara zapota ethanolic extract against haloperidol-induced Parkinsonism in Swiss albino mice.
Materials and Methods
The M.zapota leaf powder was extracted using 70% ethanol, followed by a qualitative and quantitative investigation. In this study, the effects of extract at 200 and 400 mg/kg (p.o.) against haloperidol in mice were assessed using various in vivo behavioural parameters including catalepsy, grid hang, horizontal bar, and parallel bar tests.
Results
The qualitative analysis of ethanolic extract identified phenols, alkaloids, carbohydrates, flavonoids, tannins, proteins, and saponins. Furthermore, the quantitative assessment indicated total flavonoid and phenol contents of 64.52 mg RTE/g and 17.6 mg GAE/g, respectively. The extract showed significant and dose-dependent enhancements in behavioural activity, motor function, muscle strength, and motor coordination. Moreover, its administration dose-dependently elevated antioxidant enzyme levels, such as glutathione, superoxide dismutase, and catalase in haloperidol-treated mice, suggesting its ability to alleviate oxidative stress. Additionally, the histopathological analysis indicated that ethanolic extract treatment restored normal architecture.
Conclusion
These findings suggest that M. zapota extract has significant neuroprotective properties against haloperidol-induced Parkinsonism, possibly via its antioxidant properties. Further research is needed to understand its mechanisms and therapeutic potential for Parkinson’s disease.
Background: Pseudomonas aeruginosa (P. aeruginosa) is the source of serious nosocomial infections, the most common of which is ventilator-associated pneumonia. P. aeruginosa infections continue to pose a substantial therapeutic problem. The expression of several virulence genes and the formation of biofilms in bacteria are caused by quorum sensing, a density-dependent cell-to-cell communication mechanism. Anti-biofilm chemicals prevent the synthesis of the polymer matrix, limit cell adhesion and attachment, reduce the generation of virulence factors, and obstruct the quorum sensing system. The present study focused on the antibiofilm activity of chrysin-fabricated silver nanoparticles (nano-chrysin) against P. aeruginosa. Materials and Methods: In our study, chrysin, which is a polyphenol, was fabricated with silver nanoparticles to make nano-chrysin. P. aeruginosa PAO1 strain was treated at sub-MIC concentrations with chrysin (50, 25, 12.5, and 6.25 μg mL-1), silver nanoparticles (6.26, 3.13, 1.56, and 0.78 μg mL-1) and formulated nano-chrysin (3.13, 1.56, 0.78, and 0.39μg mL-1) to find out the effectiveness of these compounds against biofilm formation. Results: Biofilm produced by P. aeruginosa PAO1 was found to be inhibited at sub-MIC concentrations (3.13, 1.56, 0.78, and 0.39 μg mL-1) of nano-chrysin having MIC value ranging between 50-3.13 μg mL-1 which is more potent than alone chrysin and silver nanoparticles. Conclusion: The data confirmed that nano-chrysin is effective in inhibiting biofilm formation, produced by P. aeruginosa.