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Background An experimental design to obtain bioactive ingredients from Oroxylum indicum (L.) Kurtz was performed applying microwave-assisted extraction (MAE). Recently, tremendous research interest and benefits have been observed for extracting active constituents from plant materials using the microwave. Objectives This work aimed to develop an optimized, green, efficient, alternative procedure for extracting flavonoid and phenolic (total flavonoid content [TFC] and total phenolic content [TPC]) from leaves of Oroxylum indicum (L.) Kurtz. Materials and Methods A total of 1 g of the powdered sample was extracted using classical Soxhlet apparatus for 48 hr to ensure exhaustive extraction; simultaneously, maceration and ultrasound-assisted extraction were also carried out using 1 g of the plant sample for 12 hr and 60 min at 25˚C, respectively. The optimization of MAE was done using Taguchi L9 orthogonal design. The optimum operating conditions were microwave power (160 W), soaking time (4 min), irradiation time (4 min), and temperature (57˚C). Results The microwave method has shown 70% higher yield than other conventional techniques in a shorter time, along with increased TFC and TPC. Conclusion The TPC, TFC, and total antioxidant capacity (TAC) values are higher in the extract obtained by MAE extracts in comparison to other techniques. The extraction technique will be an ideal tool to safeguard the thermolabile plant constituents that will be more environmentally friendly.

OBJECTIVES: Olaparib is an orally active poly (ADP-ribose) PARP (polymerases) inhibitor known to destroy cancer cells with BRCA1 or BRCA2 deficiency. An authentic, fast, distinct, and reliable reverse phase-high performance liquid chromatography (RP-HPLC) method was developed and promptly validated in tablet formulations for olaparib estimation. MATERIALS AND METHODS: The proposed method focuses on the separation of olaparib in reverse phase mode using a Waters symmetry C18 (150 x 4.6 mm, 5 μm) analytical column with a flow rate of 1.0 mL/min and the injection volume was kept at 20 μL. The optimized mobile phase consists of ammonium acetate buffer (pH adjusted to 3.5 by glacial acetic acid): methanol in the ratio of 50:50 v/v. RESULTS: The eluents were measured at 254 nm and the retention time for the drug encircled was about 4.32 min. The stress degradation studies of olaparib were conducted under acidic, alkaline, oxidative, photolytic and thermal conditions to demonstrate the stability of the drug. The regression value of 0.998 showed that the developed method was linear over the range of 80 μg/mL to 120 μg/mL. The developed RP-HPLC method is accurate and precise. The method was statistically validated as per International Conference on Harmonization guidelines. CONCLUSION: The proposed method is suitable and can be applied for the quantitative estimation of olaparib without any interference of the excipients used in the drug formulations.

Relapsed and refractory (RR) acute lymphoblastic leukemia (ALL) poses unique and difficult challenges to a practicing clinician in India where access to novel immunotherapies is limited. Between 2017 and 2020, eight patients with B-cell ALL at our center received inotuzumab ozogamicin (IO) monotherapy on compassionate access, as salvage therapy after at least two lines of conventional therapy failure, and most often as outpatient infusion. Eight patients (21–60 years, three females) received IO. Three patients had morphologic relapse and five patients reported persistent measurable residual disease (MRD). The best response on IO therapy achieved was negative MRD in six of seven patients and complete response (CR) with persistent MRD in one. One patient died (intracranial hemorrhage) before completion of first cycle. All responding patients were transplant eligible and four patients (57%) underwent allogeneic hematopoietic cell transplantation (Allo-HCT). Median follow-up of this cohort is 9 months (4–29.6 months), four patients (57%) are alive as stable with negative MRD. No significant infusion reactions occurred during therapy. Three patients developed grades III and IV neutropenia, two patients showed grade III transaminitis, and two patients developed post-HCT severe sinusoidal obstruction syndrome (SOS). IO is a feasible outpatient based salvage therapy to improve the remission status in RR B-cell ALL.

The current global epidemic of the novel coronavirus (SARS-CoV-2) has been labeled a global public health emergency since it is causing substantial morbidity and mortality on daily basis. We need to identify an effective medication against SARS-CoV-2 because of its fast dissemination and re-emergence. This research is being carried out as part of a larger strategy to identify the most promising therapeutic targets using protein-protein interactions analysis. Mpro has been identified as one of the most important therapeutic targets. In this study, we did in-silico investigations to identify the target and further molecular docking, ADME, and toxicity prediction were done to assess the potential phyto-active antiviral compounds from

Background: The Arisaema (Araceae) is a genus of approximately 180 perennial herbs widely distributed in the evergreen and deciduous forests. This genus (Arisaema) has been used as a medicinal agent since ancient times. Experimental investigations have shown a promising positive correlation with its folklore claim and this encourages us to report updated medicinal review (genus Arisaema) for future research. Objective: This review aimed to summarize the ethnobotany, folklore uses, chemistry and biological activities. Conclusion: The comprehensive literature on genus Arisaema indicates the presence of terpenoids, flavonoids, and glycosphingolipids as the principal chemical constituents. Additionally, phytosterols, alkaloids, carboline derivatives and miscellaneous compounds were documented in plants of genus Arisaema. Biological investigations led to the credentials of antioxidant, anticancer, insecticidal, antimicrobial, anthelmintic and hepatoprotective activities. Following, several plant species are promising candidates for the treatment of cancer, parasitic diseases and microbial infection complications. Though, a lot of facets of this genus like phytoconstituents identification, mechanistic profile, adverse effects and clinical studies are still quite limited. Thus, this systematic review may act as a powerful tool in future studies for promoting health benefits against various health hazards.

Infections caused by HSV-2 are a public health concern worldwide, and there is still a great demand for the discovery of novel anti-herpes virus agents effective against strains resistant to current antiviral agents. In this context, medicinal plants represent an alternative source of active compounds for developing efficient antiviral therapies. The aim of this study was to evaluate the antiviral activity of Arisaema tortuosum, a plant used in the traditional medicine of India. A chloroform soluble fraction of the leaves exhibited anti-HSV-2 activity with a selectivity index of 758. The extract was also active against acyclovir-resistant HSV-2 and HSV-1. The mechanism of action of the extract was investigated evidencing inhibition of both early and late events of the HSV-2 replicative cycle. A HPLC-PDA-MS/MS analysis showed the presence of flavonoids including apigenin and luteolin in the chloroform extract (CE). Apigenin and luteolin showed a high inhibitory activity with EC50 values of 0.05 and 0.41 µg/mL, respectively. Both compounds exhibited antiviral activity when added up to 6 h post infection and were able to reduce the viral progeny production. In addition, apigenin interfered with cell-to-cell virus spread.

Global competitions have made the pharmaceutical industry undergo numerous obstacles to meet up with the pace of drug discovery, growth and expansion. In order to effectively manufacture a quality product, statistical methods can be implemented for continuous improvement. Evolution in quality is accessed by determining the beneficial effects due to changes in process performance. The use of statistical tools and statistical methods have increased exponentially to meet specifications of quality during the development of pharmaceutical product. Statistical process control is a segment of industrial statistics utilized for the continuous improvement in the product quality. Statistical process control technique is a method to analyse any variation by the process of timely evaluation of the manufacturing procedure.

Any medical equipment must get a marketing authorisation from a regulatory authority before it can be sold. Obtaining authorization is a lengthy, multi-step process that requires relevant authorities to review material. After analyzing the information given by the Manufacturer, the concerned Regulatory authority provides marketing authorization. Manufacturers in the United States must apply to the US Food and Drug Administration for Marketing Authorization (USFDA). There are two types of applications in the United States: 510(k) and Pre-Market Application (PMA). The marketing of medical devices is permitted by national authorities in the EU. Notified Bodies (Third Parties) ensure Quality Assurance both before and after approval via third-party compliance. The sale and import of medical devices are approved by India’s Central Drugs Standard Control Organization (CDSCO). The CLAA scheme regulates medical devices. The central licensing authority for medical devices in India is the Drug Controller General of India (DCGI). This study aims to collect information on medical device regulations in three regions: the United States, the European Union, and India, and compare market authorization provisions in each region, as well as make this complex subject easier to understand for the readers. The medical device sector is made up of several different sorts of items that are used for a variety of purposes. Medical devices must be governed by tight rules according to the different risk categories since their safety and effectiveness are critical to human health. A common framework for medical device regulations is a comprehensive product life cycle regulatory system that includes product design, manufacture, premarket gatekeeping, and post market monitoring. Medical gadgets, on the other hand, are diverse and inventive, putting current regulatory systems to the test. As a result, competent authorities in charge of medical devices around the world are constantly updating their regulatory systems to ensure that medical devices are safe and effective. The goal of this study is to provide an overview of the regulatory regimes for medical devices in the United States.

The current global epidemic of the novel coronavirus (SARS-CoV-2) has been labeled a global public health emergency since it is causing substantial morbidity and mortality on daily basis. We need to identify an effective medication against SARS-CoV-2 because of its fast dissemination and re-emergence. This research is being carried out as part of a larger strategy to identify the most promising therapeutic targets using protein-protein interactions analysis. Mpro has been identified as one of the most important therapeutic targets. In this study, we did in-silico investigations to identify the target and further molecular docking, ADME, and toxicity prediction were done to assess the potential phyto-active antiviral compounds from Justicia adhatoda as powerful inhibitors of the Mpro of SARS-COV-2. We also investigated the capacity of these molecules to create stable interactions with the Mpro using 100 ns molecular dynamics simulation. The highest scoring compounds (taraxerol, friedelanol, anisotine, and adhatodine) were also found to exhibit excellent solubility and pharmacodynamic characteristics. We employed MMPBSA simulations to assess the stability of docked molecules in the Mpro binding site, revealing that the above compounds form the most stable complex with the Mpro. Network-based Pharmacology suggested that the selected compounds have various modes of action against SARS-CoV-2 that include immunoreaction enrichment, inflammatory reaction suppression, and more. These findings point to a promising class of drugs that should be investigated further in biochemical and cell-based studies to see their effectiveness against nCOVID-19. Communicated by Ramaswamy H. Sarma

Background: Laccifer lacca (Kerr) produces a mixture of polyhydroxy anthraquinones (laccaic acid) known as lac dye. Literature suggests that these laccaic acids have a structural resemblance with the anticancer drug Adriamycin (ADR). Hence, they may possess potential anticancer activity. Method: This study was designed to explore the in vitro anticancer activity of the three fractions of lac dye, i.e., chloroform (C), methanol (M), and water (W) fractions, and isolation of constituents from bioactive fraction. Results: SRB (Sulforhodamine B) assay method was employed to evaluate the inhibitory action of all three fractions. However, only methanolic showed promising inhibitory action with GI50 Conclusion: Conclusively, only the methanol fraction (M) showed promising anticancer activity against in vitro MDAMB- 231 and SiHa cell lines compared to the standard adriamycin.

Green synthesis of gold nanoparticles (GNPs) has received substantial attention, because nanoparticles are produced in an eco-friendly way using biomolecules present in plant extracts in a single step reaction. This research article highlights GNPs obtained using shade-dried leaf extracts of Millettia pinnata (L.) with aqueous auric chloride (HAuCl4) at ambient temperature. In the present study, GNPs with average particle size 37 nm in size were fabricated. Furthermore, the synthesis method to obtain stable and monodispersed GNPs was advanced by optimising enzyme concentration 100 μg/ml, pH 5.4, substrate concentration 0.45 mM and 12 h time of reaction. The confirmation of GNPs formation and characterisation was followed by UV-vis-absorption spectroscopy, dynamic light scattering (DLS), and zeta potential (ZP) for the analysis of shape, size, and stability, respectively. TEM images and powder XRD revealed the GNPs synthesis of spherical-shaped nanoparticles in the face-centred cubic arrangement. Cytotoxicity of GNPs was studied against A549 lung cancer cells with IC50 14.76 μg/ml and found lower as compared to doxorubicin IC50 11.23 μg/ml but significant enough to be used as a vehicle GNPs produced using green source can be used as significant therapeutic agents and drug delivery carriers.

In December 2019, the Coronavirus disease-2019 (COVID-19) virus emerged in Wuhan, China. The first resolved COVID-19 crystal structure (main protease) has been developed and various repurposing activities are in process. In this study, a knowledge gap in relation to COVID-19, with the previously known fatal Coronavirus (CoV) epidemics, Severe acute respiratory syndrome (SARS) and Middle East respiratory syndrome (MERS) CoVs, is covered by the investigation of sequence statistics, molecular modelling, virtual screening, docking, and sequence comparison statistics of the COVID-19 main protease. COVID-19 main protease Mpro formed a sequence similarity group with SARS CoV that was distant from MERS CoV. The identity % was 96 and 51 for COVID-19/SARS and COVID-19/MERS CoV sequence comparisons, respectively. We used molecular docking and a molecular interaction approach to identify small-molecules that bind to the isolated Viral S-protein at its host receptor region. These molecules have good solubility and pharmacodynamics properties. They also obey Lipinski’s rule, which makes them promising compounds to pursue further biochemical and cell-based assays to explore their potential for use against COVID-19. We hypothesize that the top score identified molecules that may be used to limit viral recognition of host cells and/or disrupt host-virus interactions. A ranked list of selected compounds is given that can be tested experimentally.

Ethnopharmacological relevance Vachellia (Acacia) nilotica and other plants of this genus have been used in traditional medicine of Asian and African countries to treat many disorders, including sexually transmitted diseases, but few studies were performed to validate their anti-microbial and anti-viral activity against sexually transmitted infections. Aim of the study The present study was undertaken to explore whether the ethnomedical use of V.nilotica to treat genital lesions is substantiated by its antiviral activity against the human immunodeficiency virus (HIV), the herpes simplex virus (HSV) and the human papillomavirus (HPV). Materials and methods The antiviral activity of V.nilotica was tested in vitro by virus-specific inhibition assays using HSV-2 strains, sensible or resistant to acyclovir, HIV-1IIIb strain and HPV-16 pseudovirion (PsV). The potential mode of action of extract against HSV-2 and HPV-16 was further investigated by virus inactivation and time-of-addition assays on cell cultures. Results V.nilotica chloroform, methanolic and water bark extracts exerted antiviral activity against HSV-2 and HPV-16 PsV infections; among these, methanolic extract showed the best EC50s with values of 4.71 and 1.80 µg/ml against HSV-2 and HPV-16, respectively, and it was also active against an acyclovir-resistant HSV-2 strain with an EC50 of 6.71 µg/ml. By contrast, no suppression of HIV infection was observed. Investigation of the mechanism of action revealed that the methanolic extract directly inactivated the infectivity of the HPV-16 particles, whereas a partial virus inactivation and interference with virus attachment (EC50 of 2.74 µg/ml) were both found to contribute to the anti-HSV-2 activity. Conclusions These results support the traditional use of V.nilotica applied externally for the treatment of genital lesions. Further work remains to be done in order to identify the bioactive components.

The Arisaema (Araceae) is a genus of approximately 180 perennial herbs widely distributed in the evergreen and deciduous forests. This genus (Arisaema) has been used as a medicinal agent since ancient times. Experimental investigations have shown a promising positive correlation with its folklore claim and this encourages us to report updated medicinal review (genus Arisaema) for future research.This review aimed to summarize the ethnobotany, folklore uses, chemistry and biological activities.The comprehensive literature on genus Arisaema indicates the presence of terpenoids, flavonoids, and glycosphingolipids as the principal chemical constituents. Additionally, phytosterols, alkaloids, carboline derivatives and miscellaneous compounds were documented in plants of genus Arisaema. Biological investigations led to the credentials of antioxidant, anticancer, insecticidal, antimicrobial, anthelmintic and hepatoprotective activities. Following, several plant species are promising candidates for the treatment of cancer, parasitic diseases and microbial infection complications. Though, a lot of facets of this genus like phytoconstituents identification, mechanistic profile, adverse effects and clinical studies are still quite limited. Thus, this systematic review may act as a powerful tool in future studies for promoting health benefits against various health hazards.

Deltamethrin, a well-known type 2 synthetic pyrethroid insecticide, is a widespread environmental toxicant. It has potential to accumulate in body fluids and tissues due to its lipophilic characteristics. The immune system is among the most sensitive targets regarding toxicity of environmental pollutants. Various methods are available in the literature to analyze deltamethrin (DLM) concentration in plasma and tissues, but regarding the immune organs, only one gas chromatography–tandem mass spectrometry (GC–MS/MS) method (on spleen tissues) has been reported. In the present investigation, a rapid and sensitive high-performance liquid chromatography (HPLC) method has been developed and validated to determine DLM concentration in plasma, thymus, and spleen using zaleplone as an internal standard. Liquid chromatography (LC) separation is performed on an Agilent Zorbax® C8 column (250 mm × 4.6 mm, i.d., 5 μm) with isocratic elution using a mobile phase consisting of acetonitrile–5 mM KH2PO4 (70:30, v/v) at a f...

A simple, rapid, precise and accurate High-Performance Thin Layer Chromatography (HPTLC) method was developed and validated for the estimation of Nintedanib, a novel tyrosine kinase inhibitor used in idiopathic pulmonary fibrosis, in bulk drug. Chromatography was carried out using silica gel 60 F254 Thin Layer Chromatography (TLC) plate and mobile phase Chloroform: Methanol in the ratio 7:3 v/v. The densitometric determination was done at 386 nm. Regression analysis data for the calibration plot were indicative of a good linear relationship between response and concentration over the range of 800–3200 ng/band. The variance (r) was found to be 0.999. The Limit of Detection (LOD) and Limit of Quantitation (LOQ) were found to be 83.357 ng/band and 252.599 ng/band respectively. The method was validated according to the International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use [ICH Q2(R1)] guideline. The method was precise and accurate with %RSD 0.5323 (intraday) and 0.6939 (interday) respectively and percentage recoveries in the range 99.65–101.43%.

Nateglinide (NAT) and Pioglitazone (PIO) are an antidiabetic drugs combination and currently under clinical trial in countries like Japan. In this study, an alternative, a simple, sensitive high-performance liquid chromatography method has been developed (limit of detection: 15 ng/mL and limit of quantification: 50 ng/mL) for simultaneous estimation of this drug combination in rat plasma. Most remarkably, bioavailability of NAT has been increased markedly on coadministration with PIO, than when it was administered alone. Thus, PIO is assumed to retard the catabolism of NAT by inhibiting metabolic liver-microsomal enzyme, especially CYP2C9. Using a Waters Nova-Pak C 18 column (150 × 3.9 mm, 4 μm) and a mobile phase of acetonitrile: 10 mM KH2PO4 (60: 40, V/V (volume by volume)) pH 3.5, the analysis was performed at 210 nm with a flow rate of 1.5 mL/min. In silico docking via molecular dynamics simulation revealed that NAT-CYP2C9 binding affinity may be reduced after PIO attachment, presumably due to the binding site overlapping of the two drugs. Thus, it has been proposed that NAT and PIO may be an efficient synergistic fixed dose combination against diabetes mellitus, and the above method can foster a simple but highly sensitive bioanalytical estimation for routine analysis.

An attempt toward screening of phytoconstituents (Arisaema genus) against herpes viruses (HSV-1 and HSV-2) was carried out using in silico approaches. Human HSV-1 and HSV-2 are accountable for cold sores genital herpes, respectively. Two drug targets, namely thymidine kinase (TK; PDB: 2ki5) serine protease (PDB: 1at3) were selected for HSV-1 and HSV-2. Initially, molecular docking tool was employed to screened apex hits phytoconstituents against herpes infections. ADME-T studies of top ranked were also further highlighted to achieve their effectiveness. Following, molecular dynamics studies were also examined to further optimize the stability of ligands. Glide scores and binding interactions of phytoconstituents were compared with Acyclovir, the main drug used in treatment of HSV, the screened top hits exhibited more glide scores and better binding for both HSV-1 and HSV-2 receptors. Additionally, ADME-T showed an ideal range for top hits while molecular dynamics results also illustrated stability of models. Ultimately, the whole efforts reveal to top three most promising hits for HSV-1 (39, 21, 19) and HSV-2 (20, 51, 19) receptors which can be explored further in wet lab experiments as promising agents against HSV infections.

Ethnopharmacological relevance Ficus religiosa L. is one of the most relevant members of the family of Moraceae . It is the most sacred tree of South Asia, and it is used in traditional Ayurvedic and Unani medicine to cure respiratory disorders like cough, wheezing and asthma. Some studies were performed to investigate the anti-asthmatic potential of F. religiosa bark, leaves and fruit extracts but none of them tested their antiviral activity against viruses responsible for the exacerbation of wheezing and asthma. Aim of the study The present study was undertaken to investigate the antiviral activity of F. religiosa L. extracts against respiratory viruses such as human respiratory syncytial virus (RSV) and human rhinovirus (HRV). Materials and methods The antiviral activity of F. religiosa L. was tested in vitro by plaque reduction and virus yield assays and the major mechanism of action was investigated by virus inactivation and time-of-addition assays. Results F. religiosa L. methanol bark extract was the most active against HRV with an EC 50 of 5.52 µg/mL. This extract likely inhibited late steps of replicative cycle. Water bark extract was the most active against RSV with an EC 50 between 2.23 and 4.37 µg/mL. Partial virus inactivation and interference with virus attachment were both found to contribute to the anti-RSV activity. Replication of both viruses was inhibited in viral yield reduction assays. Conclusions The results of the present study demonstrate that F. religiosa L. is endowed with antiviral activity against RSV and HRV in vitro . Further work remains to be done to identify the active components and to assess the therapeutic potential in vivo .

For the first time, we developed and validated a highly sensitive, selective and rapid HPLC-ESI-MS-MS method for simultaneous quantification of metolazone (MET), losartan (LOS) and its metabolite losartan carboxylic acid (LCA) in rat plasma. After solid-phase extraction, the analytes and internal standard (irbesartan) were extracted from 100 µL plasma sample on an Agilent Poroshell 120, EC-C18 (50 × 4.6 mm, i.d., 2.7 µm) column using 5 µL injection volume with a total run time of 3 min. Acidified methanol/water mixture was used as a mobile phase. The parent → product ion transitions for MET (m/z 366.0 → 258.9), LOS (m/z 423.2 → 207.0), LCA (m/z 437.0 → 235.1) and IS (m/z 429.2 → 207.0) were monitored on a triple quadrupole mass spectrometer, operating in the multiple reaction monitoring and positive ion mode. The method was found to be linear in the range of 0.05-250 for MET, 2-3,000 for LOS and 4-3,500 ng/mL for LCA. The method was validated with respect to selectivity, linearity, accuracy, precision, recovery and stability according to accepted regulatory guidelines. The described method was successfully applied to preclinical pharmacokinetic studies of analytes after an oral administration of mixture of MET (1 mg/kg) and LOS (10 mg/kg) in rats.

A highly sensitive, accurate and robust LC-MS/MS method was developed and validated for determination of nimorazole (NMZ) in rat plasma using metronidazole (MNZ) as internal standard (IS). The analyte and IS were extracted from plasma by precipitating protein with acetonitrile and were chromatographed using an Agilent Poroshell 120, EC-C18 column. The mobile phase was composed of a mixture of acetonitrile and 0.1 % formic acid (85:15 v/v). The total run time was 1.5 min and injection volume was 5 μL. Multiple reaction monitoring mode using the transitions of m/z 227.1 → m/z 114.0 for MNZ and m/z 172.10 → m/z 128.1 for IS were monitored on a triple quadrupole mass spectrometer, operating in positive ion mode. The calibration curve was linear in the range of 0.25–200 ng/mL (r2 > 0.9996) and the lower limit of quantification was 0.25 ng/mL in the rat plasma samples. Recoveries of NMZ ranged between 88.05 and 95.25%. The precision (intra-day and inter-day) and accuracy of the quality control samples were 1.25–8.20% and −2.50–3.10, respectively. The analyte and IS were found to be stable during all sample storage and analysis procedures. The LC-MS/MS method described here was validated and successfully applied to pharmacokinetic study in rats. Copyright © 2015 John Wiley & Sons, Ltd.

A simple, sensitive and easy high-performance liquid chromatographic [HPLC] method has been developed and validated for the simultaneous estimation of albendazole [ABZ] and praziquantel [PRQ] using diazepam as an internal standard in rat plasma. Extraction of ABZ, PRQ and Diazepam in rat plasma was carried out by a process which involves precipitation of proteins called protein precipitation. Protein precipitation method was done by using 8.25% v/v perchloric acid. Chromatographic separations were performed using an Enable C18 column [250 mm × 4.6 mm, 5 μm: Spinco Biotech Pvt. Ltd]. The mobile phase consisted of acetonitrile: water [60:40, v/v] at a flow rate of 1.0 mL min-1 at an ambient temperature for plasma samples. The above method was developed and validated over the range from 50-8000 ng mL-1 for both ABZ and PRQ in the rat plasma. The recovery of ABZ was found to be 97.81 to 105.28%, whereas PRQ recoveries ranged from 96.80 to 102.63% in the rat plasma. Acceptable Intra-day and inter-day assay precision [

A simple, sensitive, selective and reproducible method based on a reversed-phase chromatography was developed for the determination of Praziquantel in rat plasma using internal standard as Diazepam. Praziquantel & Diazepam was separated on a C18 column Enable (250 mm × 4.6 mm, 5 µm particle size: Spinco Biotech Pvt Ltd), with retention times of 6.4 & 8.5 min. Ultraviolet detection was set at 225 nm. The mobile phase consisted of acetonitrile and water (60:40, v/v), running through the column at a flow rate of 1.0 mL min-1. The chromatographic analysis was operated at an ambient temperature. Sample preparation (200 µl plasma) was done by protein precipitation using perchloric acid. Calibration curve in plasma was plotted at different concentration level 5, 50, 100, 500, 1000, 2000, 3000 & 5000 ng mL-1 were found to be linear with correlation coefficients (r) is 0.9989. The precision of the method based on within-day repeatability and reproducibility (day-to-day variation) was within 15% (relative standard deviation: R.S.D. should be less than 15 according to CDER guidance for Bio-analytical Method Validation). Good accuracy was observed for both the intra-day or inter-day assays, as indicated by the minimal deviation of mean values. Limit of quantitation (LOQ) was accepted as 5 ng mL-1 using 200 µl samples. The mean recovery was found to be greater than 90% for praziquantel. The method appears to be robust and has been applied for pharmacokinetic study of praziquantel, in three different groups of rats following a single oral dose of 40 mg kg-1 body weight of praziquantel.

Treatment of breast cancer is not easy because of the complexity in molecular physiology. Surgery, chemotherapy and radiation therapy includes different sources of treating breast cancer. The systemic chemotherapy faces lot of challenges, mainly adverse effects. So, there is a need of newer drugs to be developed against breast cancer. The present work tries to justify the folklore claims of Tabernaemontana divaricata (L.) R. Br. ex Roem. & Schult. through a sound scientific background using modern analytical tools. It was found that phytoconstituents of the plant showed good docking score against 3ERT protein. The petroleum ether extract and chloroform extract showed anticancer activity. Petroleum ether extract was found to have GI50 value of 18.7µg/ml. Phytochemical Studies lead to the isolation of two compounds, 1 and 2. These compounds, isolated from the leaves were studied and characterized tentatively with the help of modern analytical tools like FTIR, 1H NMR and MS. Based upon spectral studies, compound 1 was characterized as 2-(1,6a,6b,9,9,12a,14b-heptamethyl 1, 2, 4a, 5, 6, 6a, 6b, 7, 9, 10, 11, 12, 12a, 12b, 13, 14b-hexadecahydropicen-3-yl) propan-2-yl nonanoate. Compound 2 was found to be not pure enough to be characterized. The isolated compounds were also tested for their anti-proliferative activity against breast cancer.

Introduction: Aerva lanata (Linn) of family Amaranthaceae is an important and commonly used plant for its medicinal and pharmacological properties and proving the traditional uses of flowers of A. lanata Linn. Objective: All extracts of A. lanata were further evaluated for antioxidant, antimicrobial, and antiurolithiatic potential to scientifically prove the traditional uses. Materials and Methods: In the present investigation, different solvent extracts of flowers were obtained using a Soxhlet extractor. Microorganisms were obtained from IMTECH, Chandigarh. Antiurolithiatic study was carried out in Albino Research and Training Centre, Hyderabad. Results: Regardless of the antioxidant studied, the methanolic extract presented the highest antioxidant activity and the aqueous extracts offered the lowest, following the order: methanolic extract > ethyl acetate > chloroform > aqueous. The results of this antimicrobial study indicate that methanolic extract of A. lanata could be used as antimicrobial agents. Overall, the methanolic flower extract of A. lanata (Linn) was significantly more promising as antiurolithiatic spectrum. This result also suggested the potential usefulness of the methanolic extract as an antiurolithiatic agent. Conclusion: Henceforward, this research can be acknowledged as a prime new report that focuses on the application of A. lanata (Linn) as an antioxidant, antimicrobial, and antiurolithiatic agent. SUMMARY Overall, methanolic flower extract of Aerva lanata Linn showed promising antioxidant activityAdditionally, methanolic flower extract of A. lanata Linn exhibited remarkable antimicrobial and antiurolithiatic potential. Abbreviations used: IMTECH Chandigarh: Institute of Microbial Technology, Chandigarh; IMMT: Institute of Mineral and Material Technology; CSIR: Council of Scientific & Industrial Research; DPPH: 1,1-diphenyl-2-picrylhydrazyl; MTCC: Microbial Type Culture Collection; BHT: Butylated Hydroxyl Toluene.

Inductively Coupled Plasma - Optical Emission Spectrometry (ICP-OES) was used to estimate and evaluate the levels of heavy metals in vegetables collected from various sites of Ranchi city (tribal dominated population) followed by health risk assessment by determining Metal Pollution Index (MPI), Daily intake of metal (DIM) and Health Risk Index (HRI). The concentration levels of Pb, Cd and Ni in vegetables were found to contain beyond than the permissible PFA limit. All sites showed quite a few higher concentrations of Lead (Pb), than the permissible PFA limit. Among thirteen vegetables, Beet, Cucumber, Pea, Beans, Lady's finger, Corriender leaves and Tomato showed high levels of Pb in vegetables collected from all sites. Health Risk Index was also found > 1 for Cd, Co and Pb. Health Risk Index for Cadmium was 1.64 and 2.38 in Cucumber from Site-6 and Site-8 respectively. In Spinach it was 2.19 and 2.15 respectively for Site-6 and Site-8. Health Risk Index for Pb was > 1 in Cucumber (All sites; 3.54 in Site-8), Pea (All sites except Site10; 2.45 in Site-7), Beans (All sites; 1.38 in Site-9), Lady's finger (All sites; 2.03 in Site-7), and Tomato (All sites except Site-10; 2.79 in Site-8). Lead and cadmium were among the most abundant heavy metals in the selected vegetables. The excessive content of these heavy metals in food may causes number of diseases. HRI more than 1 is considered to be not safe for human health. In present study, HRI indicates considerable risk and negative impact on human health.

Human rhino viruses (HRVs) serve as an imperative precursor for frequent cases of the common cold among children worldwide. An in-silico molecular docking attempt was made of some chief phytochemical entities (Arisaema plant species) as inhibitors of HRVs with selective therapeutic target action and minimal side effects. Around 60 phytoconstituents of different Arisaema species were docked against HRV receptor (PDB: 2XYA). Binding conformers of test ligands were compared with internal ligand. Finally, Syringaresinol 4'-O-β-D-glucopyranoside (glide score: -10.86), Rutin (glide score: -9.04) & Apigenin-6,8-di-C-β-D-glucopyranoside (glide score: -7.88) have resulted in most promising hits which can be further act as an effective template to experimentally validate or further designed their choosy and budding analogue agents against HRVSs.

Molecular docking study was performed using Maestro Schrodinger suite 8.5 mainly on twenty nine phytoconstituents reported from the plant Aerva lanta for their antimicrobial potential. The crystal structure of protein data bank (PDB-ID: 3SRW) was obtained from RCSB (Research Collaboratory for Structural Bioinformatics) website. The ligands were obtained from the reported literature search of Aerva lanta plant. The top hits were analyzed for their binding affinity with the dihydrofolate reductase enzyme. The docking results revealed that rutin (Glide score: -11.75) exhibited better binding interaction to dihydrofolate reductase receptor.

Pyrethrin; derived from natural source (Chrysanthemum cinerariifolium) confirmed as a fundamental nucleus for the development of pyrethroids which ultimately resulted in the outstanding insecticidal activity by targeting the nervous systems of insects. To date, the binding and entry mechanism by which RSV infects respiratory epithelial cells is not still well understood and need to be explored. Notably, pyrethrins have exhibited considerable antiviral potential & thus an effort was made computationally to evaluate the pyrethroids as hopeful inhibitors of Respiratory Syncytial Virus (RSV). Type 1 & type 2 Pyrethroids were subjected to docking simulations by using Maestro 9.2 version (Schrodinger LLC). Cyfluthrin showed better binding interactions against RSV (Glide score: -4.54). Remarkably, it showed two hydrogen bonding interactions with Lys46 (1.82 A) & Hie151 (2.19 A) of RSV protein receptor. The decrease in glide score is evidence for greater bond stability with protein. Based on the current findings, these studies in future may act as effective predecessor tool to further validate pyrethroids with wet lab experiments as capable antiviral agents for RSV.

Ficus religiosa extracts have been used in traditional Indian medicine to treat sexually transmitted infections such as gonorrhea and genital ulcers. The aim of this study was to investigate the antiviral activity of F. religiosa extracts against herpes simplex virus type 2 (HSV-2), the main causative agent of genital ulcers and sores. Water and chloroform bark extracts were the most active against HSV-2, and also against an acyclovir-resistant strain. We demonstrate that the water extract has a direct virus-inactivating activity. By contrast, the chloroform extract inhibits viral attachment and entry and limits the production of viral progeny.

Introduction: Aerva lanata (Linn) of family Amaranthaceae is an important and commonly used plant for its medicinal and pharmacological properties and proving the traditional uses of flowers of A. lanata Linn. Objective: All extracts of A. lanata were further evaluated for antioxidant, antimicrobial, and antiurolithiatic potential to scientifically prove the traditional uses. Materials and Methods: In the present investigation, different solvent extracts of flowers were obtained using a Soxhlet extractor. Microorganisms were obtained from IMTECH, Chandigarh. Antiurolithiatic study was carried out in Albino Research and Training Centre, Hyderabad. Results: Regardless of the antioxidant studied, the methanolic extract presented the highest antioxidant activity and the aqueous extracts offered the lowest, following the order: methanolic extract > ethyl acetate > chloroform > aqueous. The results of this antimicrobial study indicate that methanolic extract of A. lanata could be used as antimicrobial agents. Overall, the methanolic flower extract of A. lanata (Linn) was significantly more promising as antiurolithiatic spectrum. This result also suggested the potential usefulness of the methanolic extract as an antiurolithiatic agent. Conclusion: Henceforward, this research can be acknowledged as a prime new report that focuses on the application of A. lanata (Linn) as an antioxidant, antimicrobial, and antiurolithiatic agent. Abbreviations used: IMTECH Chandigarh: Institute of Microbial Technology, Chandigarh; IMMT: Institute of Mineral and Material Technology; CSIR: Council of Scientific & Industrial Research; DPPH: 1,1-diphenyl-2-picrylhydrazyl; MTCC: Microbial Type Culture Collection; BHT: Butylated Hydroxyl Toluene.

The sensation of pain is initiated in peripheral pain receptors (nociceptors) and its purpose is to draw attention to tissue damage. In order to test analgesic activity, it is obviously necessary to induce pain in the subject and then modify the response to, or perception of, this pain. Analgesic studies of the methanol (90% v/v) extract (MELP) of Litsea polyantha Juss. bark (Yield: 11.79% w/w) was carried out using healthy adult Swiss albino mice of either sex weighing between 20 to 25 g respectively. The experiment protocols were approved by the Institutional Animal Ethical Committee (621/02/ac/CPCSEA) prior to the conduct of the animal experiments. The animals were divided into 6 groups (n=6). Group I and II were used as control, received 10% v/v propylene glycol (PG) and distilled water (DW) at the dose of 10 ml/kg b.w. Group III, IV & V were treated with MELP (50, 75 and 100 mg/kg b.w., i.p.), respectively; Group VI received Morphine sulphate (10 mg/kg b.w., s.c.) an opioid analgesic as standard drug. A reduction in the tail withdrawal as compared to the control group was considered as evidence for the presence of analgesia. Tail flick latency was measured 30 min after the drug administration and Pain Inhibition Percentage (PIP) was calculated. MELP given by intraperitoneal route in mice showed significant and dose-dependent central analgesic activity (P

Pyrethroids have shown promising potential to induce apoptogenic signaling pathways in various cells. Therefore, present study on pyrethroids was designed to unlock better alternative agents against cancer disease. Different targets such as estrogen (PDB: 3ERT), androgens (PDB: 2PIT) & cervix (PDB: 3F81) cancer receptors were used in the study. Type 1 & type 2 pyrethroids were subjected to docking simulations using Maestro 9.2 version (Schrodinger’s LLC). Pyrethroids (Type 1 & type 2) docking studies have revealed varying glide score to cancer receptors. Resmethrin exhibited better binding interaction to estrogen (Glide Score: -7.32) & androgens (Glide Score: -7.47) while fluvalinate against cervix (Glide Score: -4.54) protein receptors. Decrease in glide score be evidence for greater bond stability with protein. Based on the current finding from docking studies, these preliminary results may act as effective precursor tool for development of pyrethroids as promising anticancer agents. However, furthermore experimental validation using in-vitro & in-vivo studies is needed to explore their therapeutic & toxic effects.

A highly sensitive, accurate and robust LC-MS/MS method was developed and validated for determination of nimorazole (NMZ) in rat plasma using metronidazole (MNZ) as internal standard (IS). The analyte and IS were extracted from plasma by precipitating protein with acetonitrile and were chromatographed using an Agilent Poroshell 120, EC-C18 column. The mobile phase was composed of a mixture of acetonitrile and 0.1 % formic acid (85:15 v/v). The total run time was 1.5 min and injection volume was 5 μL. Multiple reaction monitoring mode using the transitions of m/z 227.1 → m/z 114.0 for MNZ and m/z 172.10 → m/z 128.1 for IS were monitored on a triple quadrupole mass spectrometer, operating in positive ion mode. The calibration curve was linear in the range of 0.25-200 ng/mL (r(2) 0.9996) and the lower limit of quantification was 0.25 ng/mL in the rat plasma samples. Recoveries of NMZ ranged between 88.05 and 95.25%. The precision (intra-day and inter-day) and accuracy of the quality control samples were 1.25-8.20% and -2.50-3.10, respectively. The analyte and IS were found to be stable during all sample storage and analysis procedures. The LC-MS/MS method described here was validated and successfully applied to pharmacokinetic study in rats.