Showing papers in "Indian Journal of Pharmaceutical Sciences in 2021"
TL;DR: This review throws light on recent biological expansions of pyridine along with their structure activity relationships/molecular docking to deliver association between various synthesized newer derivatives and receptor sites.
Abstract: Pyridine is an imperative pharmacophore, a privileged scaffold and an exceptional heterocyclic system in the field of drug discovery which provides many opportunities in study/explore this moiety as an anticancer agent by acting on various receptors of utmost importance. Several pyridine derivatives are reported to inhibit tubulin polymerization, androgen receptors, human carbonic anhydrase, kinase, topoisomerase enzyme and many other targets for controlling and curing global health issue of cancer. Now a days in combination with other moieties researchers are focusing for development of pyridine new entities for the treatment of cancer. This review throws light on recent biological expansions of pyridine along with their structure activity relationships/molecular docking to deliver association between various synthesized newer derivatives and receptor sites.
8 citations
TL;DR: In silico immune evaluation using C-ImmSim server showed that the peptide could concurrently elicit cell-mediated and humoral immune responses, and docking results of the multi-epitope vaccine peptide with human leukocyte antigen class I and II alleles predicted efficient binding and the resulted docked models were stable during simulation.
Abstract: Contagious human coronavirus belong to family Coronaviridae and infects human respiratory system causing the disease known as COVID-19 (WHO). To eradicate the severe acute respiratory syndrome coronavirus 2 pandemic, an effective vaccine should be developed. In the current study immunoinformatics procedures were employed to introduce a novel multi-epitope subunit vaccine. This multi-epitope vaccine can activate equally class I and II human leukocyte antigen and antibody mediated immune responses. Spike glycoprotein (PDB Id: 6VSB) of the coronavirus was selected and analysed using immune epitope database server for prediction of potential immunogenic B and T-cell epitopes. Population conservation studies of the selected protein and predicted epitopes were also performed using population conservancy analysis tool of immune epitope database resource. The two dimensional and three dimensional structure of multi-epitope vaccine were predicted and authenticated using PROCheck and Raptor-X servers. Docking results of the multi-epitope vaccine peptide with human leukocyte antigen class I and II alleles predicted efficient binding and the resulted docked models were stable during simulation. In silico immune evaluation using C-ImmSim server showed that the peptide could concurrently elicit cell-mediated and humoral immune responses. Immune simulation studies significantly anticipated high levels of IgM and IgG, T-helper, T-cytotoxic cells, INF-γ.
6 citations
TL;DR: The emergency medical services students have moderately inadequate knowledge and skills related to coronavirus disease 2019 and indicated that they are uncertain about their ability to respond adequately to, or participate satisfactorily in, pandemic-related events.
Abstract: Emergency medical services providers, including emergency medical services students are among healthcare professionals on the front line to fight coronavirus disease 2019 and are under a greater risk of exposure. Preparing emergency medical services students to safely provide healthcare during the pandemic is vital. Therefore, this study assesses the emergency medical services student’s preparedness for coronavirus disease 2019 in Saudi Arabia. A descriptive cross-sectional survey was conducted. This study was conducted at Prince Sultan Bin Abdulaziz College for Emergency Medical Services in King Saud University in Riyadh, Saudi Arabia. In this study, 198 students participated. The emergency medical services students thought they are insufficiently prepared to face situations, such coronavirus disease 2019 (2.50±1.57). Regarding knowledge, the emergency medical services students thought that they are insufficiently prepared for coronavirus disease 2019. The emergency medical services students thought that they are insufficiently contributing to local or national-level efforts associated with coronavirus disease 2019 (2.40±1.34). Among the emergency medical services students, 83 % (n=132) presented a feeling that they were not satisfactorily equipped to counter coronavirus disease 2019 situation. Furthermore, 87 % (n=138) of the emergency medical services students thought that embedding coronavirus disease 2019 related topics in the emergency medical services curriculum and theory and practical training would help prepare them. The emergency medical services students have moderately inadequate knowledge and skills related to coronavirus disease 2019. Moreover, they indicated that they are uncertain about their ability to respond adequately to, or participate satisfactorily in, pandemic-related events. The emergency medical services students have expressed the need for more knowledge and skills related to coronavirus disease 2019 to be embedded in the emergency medical services program curriculum.
6 citations
TL;DR: Overall, the precision, accuracy and reproducibility of the proposed diffuse reflectance infrared Fourier transform spectroscopy method make it appropriate for quantitative analysis of levofloxacin in solid dosage forms.
Abstract: Levofloxacin is a synthetic fluoroquinolone antibiotic available in different dosage forms for the treatment of various bacterial infections. Here in, we report the validated diffuse reflectance infrared Fourier transform spectroscopic method for quantitative analysis of levofloxacin in the solid dosage forms. This method offers the advantage of being eco-friendly that is applied for solid state samples. Appropriate quantities of levofloxacin and dry potassium bromide were mixed to get the desired concentration of samples for Fourier transform infrared spectroscopic analysis using a diffuse reflectance sampling interface. The peak in the Fourier transform infrared spectrum around 1724 cm-1 was observed for the carbonyl group of levofloxacin. The calibration curve was plotted for the area under the curve of carbonyl peak against the concentration of calibration standards. A linear calibration curve with a correlation coefficient of 0.999 was obtained in the range of 0.3-1.8 % w/w of levofloxacin. The calibration curve method was linear, precise and accurate as per guidelines. The method employed for quantification of levofloxacin in three marketed tablet dosage forms and laboratory physical mixture yielded a mean recovery of 101.32 and 98.11 percent by weight, respectively. Overall, the precision, accuracy and reproducibility of the proposed diffuse reflectance infrared Fourier transform spectroscopy method make it appropriate for quantitative analysis of levofloxacin in solid dosage forms.
5 citations
TL;DR: Berberine loaded solid lipid nanoparticle is successful drug delivery system demonstrating its effectiveness in controlling hyperlipidemia due to the improved bioavailability of berberine.
Abstract: Berberine is an isoquinoline alkaloid possesses multitude of biological effects. However, quaternary amine cation of berberine causes poor water solubility, resulting in low bioavailability which limits its pharmacological purpose. The aim of this study was to prepare and optimize berberine loaded solid lipid nanoparticle and to evaluate its pharmacokinetic and antihyperlipidemic activity. The solid lipid nanoparticles were prepared by solvent injection method and 32 full factorial design was used to study the effect of concentration of polyvinyl alcohol (X1) and amount of lipid (X2) on particle size (Y1) and entrapment efficiency (Y2). The formulation was optimized using desirability function and evaluated for physicochemical, morphological, in vitro drug release and in vivo pharmacokinetic study. In vivo antihyperlipidemic activity of the formulation was also studied using high fat diet induced hyperlipidemia model. The formulation optimized by validated experimental design comprise of 1 % w/v polyvinyl alcohol, 279 mg lipid (stearic acid) to achieve particle size of 395 nm with 82.44 % entrapment efficiency. In vitro release study of berberine loaded solid lipid nanoparticle showed an initial burst release followed by slow and continuous release. Berberine loaded solid lipid nanoparticle also showed 4.13 folds improvement in relative bioavailability compared to Berberine suspension. Furthermore, Berberine loaded solid lipid nanoparticle ameliorate the levels of total cholesterol (-41 %), TG (-49 %), lipoprotein cholesterol-C (-80 %) and high-density lipoprotein cholesterol(+119 %) compared to hyperlipidemic control and also found to be better than pure drug. The prepared berberine loaded solid lipid nanoparticle are successful drug delivery system demonstrating its effectiveness in controlling hyperlipidemia due to the improved bioavailability of berberine.
5 citations
TL;DR: It could be concluded that selected parts of Terminalia catappa have immune stimulatory as well as anti-inflammatory properties, thereby proving their efficacy as true immunomodulators.
Abstract: Modulation of immunity is the most sought therapeutic effect as many human ailments arise because of imbalance in immune mechanisms. In the current corona virus disease scenarios also, the role of immunity to combat the dreadful virus has been well emphasized. Hence the present study aims at evaluating the immunomodulatory potential of aqueous extract obtained from the different parts such as bark, fruit and wood of Terminalia catappa. Based on the results obtained in acute oral toxicity and dose fixation studies, medium dose (250 mg/kg body weight) of selected plant extracts were administered for 14 d to swiss albino mice to evaluate nonspecific (Neutrophil adhesion, Phagocytic index) and specific (Hemagglutination antibody titer, Delayed type hypersensitivity) immunomodulatory properties. The results obtained for plant extract treated groups were compared with cyclophosphamide (immunosuppressant) treated and levamisole (immunostimulant) treated mice. From the data of the results obtained it could be concluded that selected parts of Terminalia catappa have immune stimulatory as well as anti-inflammatory properties, thereby proving their efficacy as true immunomodulators. Among the parts selected, fruits exhibited significant immunomodulatory potential followed by bark and wood.
5 citations
TL;DR: The present study was aimed to evaluate the anti-ferlility activity of Caesalpinia pulcherrima Linn in rats and found that there is a significant increase in antiimplantation and resorption in a dose dependent manner.
Abstract: The present study was aimed to evaluate the anti-ferlility activity of Caesalpinia pulcherrima Linn in rats. The plant Caesalpinia pulcherrima is a shrub or small tree. The plant is normally considered to be an ornamental shrub which is planted in gardens and parks for its beautiful red or yellow flowers. The phytochemical screening of the plant has shown the presence of various chemical constituents like alkaloids, flavonoids, steroids and triterpenes. The bark extracts of Caesalpinia pulcherrima have exhibited significant estrogenic activity. Both the aqueous and alcoholic extracts have produced reduction in ovarian and increase in uterine weight in a dose dependent manner. Also there is a significant increase in antiimplantation and resorption in a dose dependent manner. The activity shown can be attributed to the presence of phytochemical constituents.
5 citations
TL;DR: In this paper, a grafted polymer of polyacrylamide with gum arabica was synthesized as Gum acacia-g-polyacrylide using microwave assisted synthesis with ceric ammonium nitrate as a reaction initiator.
Abstract: In the present work, a grafted polymer of polyacrylamide with gum arabica was synthesized as Gum acacia-g-polyacrylamide using microwave-assisted synthesis with ceric ammonium nitrate as a reaction initiator. The polymer was utilized in combination with sodium alginate to prepare interpenetrating polymer network hydrogel beads to effectively deliver gabapentin in gastrointestinal tract. The formulated interpenetrating polymer network microbeads showed pH-responsive release in a different medium. The interpenetrating polymer network hydrogel beads were processed for different analytical characterization like Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray powder diffraction and scanning electron microscopy. The Fourier transform infrared spectroscopy study confirms the formation of gum acacia-g-polyacrylamide whereas differential scanning calorimetry, X-ray powder diffraction studies confirm the appearance of gabapentin in the interpenetrating polymer network microbead formulations. The release of the drug from the interpenetrating polymer network structured hydrogel beads was found higher in pH 6.8 as compared to pH 1.2 and pH 7.4 indicating the effective delivery of gabapentin from the interpenetrating polymer network beads to upper duodenum for better absorption.
4 citations
TL;DR: It is recommended that iron nanoparticles from mushrooms have great potential to act as safe alternative to antibiotics to fight the challenges of drug discovery.
Abstract: In the present investigation, iron nanoparticles were synthesized by using mushroom extract. The production of iron nanoparticles from P. florida was initially confirmed by color changes from brown to dark brown within 30 min at 60° and further characterized by Ultraviolet-Visible spectroscopy and scanning electron microscope with Edax. The biosynthesized iron nanoparticles were subjected to antimicrobial activities and showed higher zone of inhibition against Candida glabrata followed by Micrococcus mucilaginosus, Pseudomonas aeruginosa, Candida albicans, Klebsiella terrigena, K. pneumoniae, Escherichia coli, Candida sp., Bacillus cereus and Staphylococcus aureus. This extract was confirmed as effective against microorganisms which was well comparable with standard antibiotics. The present study has recommended that iron nanoparticles from mushrooms have great potential to act as safe alternative to antibiotics to fight the challenges of drug discovery.
4 citations
TL;DR: In this paper, a three-dimensional Box-Behnken design at three levels (33) was developed to study how selected independent variables affect dependent responses, and three different levels were established as the lowest, highest and middle variables tested.
Abstract: Current research has been done to develop statistically and optimized immediate release tablets for eslicarbazepine. Nineteen formulations of eslicarbazepine acetate immediate release tablets are prepared by wet granulation. The three-dimensional Box-Behnken design at three levels (33) was developed to study how selected independent variables affect dependent responses. After the initial test, three independent items were selected as follows; polyvinylpyrrolidone (A), tapioca starch (B) and galbanum gum (C). Responses to measure were the time of disintegration (Y1) and in vitro drug release at 45 min (Y2). In accordance with the independent variables, three different levels were established as the lowest, highest and middle variables tested. The predicted formula formulated with the Box-Behnken statistical design consisted of polyvinylpyrrolidone, tapioca starch and galbanum gum at the optimum levels of 2.49, 2.77 and 3 respectively.
4 citations
TL;DR: It was concluded that the simplex lattice design is suitable for efficiently optimizing the floating matrix tablet of glipizide and shows the possibility of the formulation to remain in the stomach of human being for the desired period.
Abstract: The aim of the present study was to prepare the floating matrix tablet of glipizide by applying Simplex lattice design using kappa carrageenan, Hydroxypropylmethylcellulose K15M and sodium bicarbonate as independent variable. The similarity factor (f2), time to release 50 % of drug and time to release 90 % of drug were taken as dependent factors. A total of 14 batches were prepared as given by Design-Expert® Software (version- 9.0.6, Stat-Ease) and the response obtained for the dependent variables was statistically evaluated. Radiological study was performed on healthy albino rabbits for checking the gastroretention for optimized floating tablet of glipizide. The results indicated that the formulation G-simplex lattice design 8 with 50 mg of Hydroxypropylmethylcellulose, 30 mg of kappa carrageenan and 10 mg of sodium alginate is the optimized formulation with highest desirability. The in vivo X-ray imaging study clearly revealed that the optimized formulations remained afloat in gastric fluid up to 12 h in the stomach of rabbit, which shows the possibility of the formulation to remain in the stomach of human being for the desired period. It was concluded that the simplex lattice design is suitable for efficiently optimizing the floating matrix tablet of glipizide.
TL;DR: The observational group was found to have improved oxygen saturation levels during frequent evaluation with the saturation probes when compared with control group, as well the recovery time was also improved and the quality of life in the observation group was significantly better than that in the control group.
Abstract: To explore the effect of clinical pharmacist intervention on the treatment of viral pneumonia with intravenous methyl prednisolone and others. The clinical data of 112 patients from July 2020 to September 2020 were categorized into observational group (n=56) and random group (n=56) according to the randomized double blind method. The control group with routine nursing intervention and the observational group was treated with comprehensive clinical pharmacist and nursing intervention. Quality of life, recovery time and saturation levels were assessed frequently and on a weekly basis. The observational group was found to have improved oxygen saturation levels during frequent evaluation with the saturation probes when compared with control group, as well the recovery time was also improved. The quality of life in the observation group was significantly better than that in the control group. Incorporating a clinical pharmacist as an integral member of the health care team, brings numerous benefits, one among them is significant improvement in the delay drug administration to the patient. It is undeniable that a clinical pharmacist is a drug information resource for all the health professionals working in a hospital setting.
TL;DR: In silico molecular docking study was executed to estimate the efficacy of phytochemicals along with the two Food and drug administration approved hepatitis C virus non-structural protein3-4A inhibitors-Grazoprevir and simeprevir as reference compounds against the selected target.
Abstract: Hepatitis C virus infection is the leading cause of chronic liver disease and hepatocellular carcinoma. There is no effective vaccine for hepatitis C virus prevention despite the fact that severalvaccinesare under development. Currently, the Unites States Food and drug administration approved combination drugs for all genotypes that would help to cure the infection more quickly and efficiently than ever before. However, the high costs, development of various side effects and emergence of drug resistant strains demand the need for new anti-viral to treat different stages of the hepatitis C virus life cycle. Focussing drug candidate from herbal ingredients is the novel approach of pharmaceutical science over the past few decades. In this perspective, the present study aimed to investigate the phytochemicals present in Acacia nilotica (L.) Delile against hepatitis C virus non-structural protein3-4A serine protease. The N-terminal Protease domain of non-structural protein3 along with non-structural protein4A protein is responsible for the cleavage of four polypeptide junctions’ viz., non-structural protein3-4A, non-structural protein4A-non-structural protein4B, non-structural protein4B-non-structural protein5A and non-structural protein5A-5B that are essential for viral genome replication. Hence targeting non-structural protein3-4A blocks the replication process. Here, in silico molecular docking study was executed to estimate the efficacy ofphytochemicals along with the two Food and drug administration approved hepatitis C virus non-structural protein3-4A inhibitors-Grazoprevir and simeprevir as reference compoundsagainst the selected target. Docking results revealed that about six phytochemicals (+)-Catechin 5-Gallate, Acacetin, (+)-Mollisacacidin, Catechin, Acalinol A and Chlorogenic acid are better than the reference compounds and hence selected as hits. Further, the hit molecules were filtered through analysing druglikeness properties, pharmacokinetics, medicinal chemistry friendliness including pan assay interference compounds and Brenk structural alerts, leadlikeness and finally prediction of potential toxicity and toxic substructure to ascertain a lead molecule. The results obtained in the current study propose Acacetin as the lead molecule for further in vitro and in vivo study.
TL;DR: Femoral head replacement in the treatment of intertrochanteric fracture of femur has shorter postoperative weight bearing time and hospitalization time, which is more conducive to the recovery of hip joint function and improvement of bone metabolism indexes.
Abstract: To explore the clinical efficacy of proximal femoral nail antirotation and femoral head replacement in the treatment of intertrochanteric fracture of femur and to explore the effect of tartrate resistant acid phosphatase 5b and bone alkaline phosphatase. 100 patients with intertrochanteric fracture of femur from January 2017 to January 2020 in our hospital were selected and randomly divided into proximal femoral nail antirotation group (n=50) and femoral head replacement group (n=50). The operation time, intraoperative blood loss, postoperative weight bearing time, length of hospital stay, Harris score, tartrate resistant acid phosphatase 5b, bone alkaline phosphatase level and complications were compared between the two groups. Compared with femoral head replacement group, the operation time, intraoperative blood loss, postoperative weight bearing time and hospitalization time of proximal femoral nail antirotation group were significantly increased (p<0.05). Compared with before operation, Harris score of two groups were significantly increased after operation and the increase of femoral head replacement group was significantly greater than that of proximal femoral nail antirotation group (p<0.05). Compared with before operation, tartrate resistant acid phosphatase 5b was significantly lower, bone alkaline phosphatase was significantly higher and femoral head replacement was significantly higher in the two groups after operation (p<0.05). Compared with femoral head replacement group (16.00 %), the incidence of complications in proximal femoral nail antirotation group (6.00 %) was significantly lower (p<0.05). Compared with proximal femoral nail antirotation, femoral head replacement in the treatment of intertrochanteric fracture of femur has shorter postoperative weight bearing time and hospitalization time, which is more conducive to the recovery of hip joint function and improvement of bone metabolism indexes. However, femoral head replacement has longer operation time, more bleeding and higher risk of postoperative complications, which has a good reference value for clinical treatment of intertrochanteric fracture of femur.
TL;DR: In this article, the effect of partially hydrolyzed ginsenoside on transdermal permeation and retention of loaded liquid crystalline nanoparticles was investigated, and it was shown that the skin permeation of the peptide was significantly increased when loaded onto liquid crystal nanoparticles with ginsenide (p < 0.01).
Abstract: Although palmitoyl lysine threonine threonine lysine serine is claimed to be a useful bioactive peptide molecule to arrest skin aging, literature on transdermal permeation and retention of the peptide has rarely been reported. Aim of this study was to investigate the effect of partially hydrolyzed ginsenoside on transdermal permeation and retention of palmitoyl lysine threonine threonine lysine serine loaded liquid crystalline nanoparticles. Palmitoyl lysine threonine threonine lysine serine was loaded onto liquid crystalline nanoparticles using a hot melting and sonication method. Particle size of the liquid crystalline nanoparticles was reduced to <300 nm after addition of partially hydrolyzed ginsenoside into the constitution of the liquid crystalline nanoparticles and the polydispersity index indicated a monodisperse state. Transmission electron microscopy showed multilayered spherical liquid crystalline nanoparticles with dense core and corona like surface. Franz diffusion cell study demonstrated that skin permeation of palmitoyl lysine threonine threonine lysine serine was significantly increased when loaded onto liquid crystalline nanoparticles comprising partially hydrolyzed ginsenoside (p<0.01), and that this was proportional to the amount of the ginsenoside added. The steady state flux of palmitoyl lysine threonine threonine lysine serine in liquid crystalline nanoparticles comprising 2.84 % ginsenoside increased 4.60 fold and 2.36 fold compared to that of control (solubilized in propylene glycol) and liquid crystalline nanoparticles without ginsenoside, respectively. Partially hydrolyzed ginsenoside may be useful as a novel material to improve skin permeation of peptide molecules suffering from low transdermal absorption.
TL;DR: The following article will review the application progress of rapid rehabilitation surgery in clinical anesthesia in recent years.
Abstract: Rapid rehabilitation surgery, also known as accelerated rehabilitation surgery, is a series of perioperative optimal management measures based on evidence-based medicine, in order to minimize the perioperative stress reaction of patients and reduce the risk of various complications, so as to achieve the goal of improving prognosis and promoting rapid recovery of patients. The concept of rapid rehabilitation surgery plays an important role in clinical anesthesia. It runs through the whole anesthetic work, such as preoperative anesthetic health education, preoperative fasting, selection of anesthetic scheme, intraoperative fluid therapy, intraoperative body temperature monitoring, postoperative analgesia and perioperative anesthetic management. The following article will review the application progress of rapid rehabilitation surgery in clinical anesthesia in recent years.
TL;DR: Professional case management based on the WeChat mobile platform helps to improve the effectiveness of out-of-hospital care for breast cancer and adapt to the rapidly developing medical model.
Abstract: To explore the effects of extended care based on the WeChat platform on self-efficacy and quality of life of postoperative breast cancer patients. 126 patients who underwent modified radical breast cancer surgery in our hospital from January 2018 to March 2019 were divided into a control group (n=63) and an observation group (n=63) according to a randomly generated numerical table. The control group was given regular nursing care, and the observation group was given extended nursing care using the WeChat public platform on the basis of the control group. The Hospital Anxiety and Depression Scale was used to assess the anxiety and depression of the two groups; the Breast Cancer Treatment Discomfort Rating Scale was developed with reference to the National Cancer Society’s Common Symptom Assessment Criteria and the American Cancer Treatment Collaborative’s classification criteria; and the Generic Quality of Life Inventory-74 was used to assess the quality of life of the postoperative patients and to conduct a patient satisfaction survey. The results showed that there were no significant differences in hospital anxiety and depression scores and anxiety status between the two groups before the intervention care, and the differences in hospital anxiety and depression scores, anxiety status and depression status were statistically significant after the treatment care. After the nursing intervention, the time effect, group effect, and interaction effect were statistically significant when comparing the discomfort scores of the two groups. After the nursing intervention, patients self-efficacy scores and quality of life scores were significantly higher in the observation group than in the control group. Before the intervention, there was no statistically significant difference in nursing satisfaction between the two groups; after the intervention, the satisfaction of the observation group was higher than that of the control group, and the difference was statistically significant. Professional case management based on the WeChat mobile platform helps to improve the effectiveness of out-of-hospital care for breast cancer and adapt to the rapidly developing medical model.
TL;DR: A liquid chromatographic method has been established for the separation of metformin, glipizide, gliclazide, glibenclamide and glimepiride using experimental design as discussed by the authors.
Abstract: A liquid chromatographic method has been established for the separation of metformin, glipizide, gliclazide, glibenclamide and glimepiride using experimental design. The main intention of this method is to optimize suitable chromatographic conditions for the proper elution of the drug molecules with minimal analysis time. The relationship between the individual and combined effect of critical process parameters and chromatographic efficiency was made clear and was achieved with the aid of experimental design methodology. Waters Sunfire C18 type column (150×4.6 mm, 5 µm particle size) was employed and 0.1 % acetic acid in water: acetonitrile mixture was adopted as mobile phase (flow rate: 0.469 ml/min) for the separation of analytes. The developed method was validated and has been extended for the assay of marketed formulations.
TL;DR: The results strongly support the use of Schinus molle aqueous extracts in topical formulations to promote wound healing.
Abstract: This study aims to investigate the cytotoxicity of Andrographis paniculata, Ziziphus spina-christi and Gymnanthemum extensum crude extracts and their combination with low piperine fractional Piper nigrum extract. All plants were extracted with water and five organic solvents (methanol, ethanol, dichloromethane, ethyl acetate and hexane). Cytotoxicity was assessed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay on three cancer types (breast, colorectal and ovarian cancers) and two non-cancerous cells. The combination among extracts with low piperine fractional Piper nigrum extract was separately conducted in several tests including cytotoxicity, apoptosis and multi caspase activity. We found that, the dichloromethane crude extract of Andrographis paniculata, Ziziphus spina-christi and Gymnanthemum extensum exhibited the strongest cytotoxicity on colorectal cancer cells SW-620 (7.49±0.04 µg. ml-1), breast cancer cells Michigan Cancer Foundation-7 (13.35±0.30 µg. ml-1) and ovarian cancer cells A2780 (15.58±1.81 µg. ml-1), respectively. Gas chromatography mass spectrometry study of dichloromethane crude extract of Andrographis paniculata, Ziziphus spina-christi and Gymnanthemum extensum identified major compounds including 1-heptatriacotanol (60.29 %) and palmitic acid (26.92 % for dichloromethane crude extract of Ziziphus spina-christi and 21.40 % for dichloromethane crude extract of Gymnanthemum extensum), respectively. The combination of dichloromethane crude extract of Ziziphus spina-christi and low piperine fractional Piper nigrum extract at ratio IC50:0.5IC50 showed a moderate synergistic effect on Michigan Cancer Foundation-7 cells. Interestingly, the mixture of dichloromethane crude extract of Gymnanthemum extensum with low piperine fractional Piper nigrum extract at ratio IC50:IC50, 0.5 IC50:IC50 and IC50:0.5 IC50 exhibited a synergistic effect on Michigan Cancer Foundation-7 cells. Moreover, combination of dichloromethane crude extract of Gymnanthemum extensum with low piperine fractional Piper nigrum extract induced the apoptosis and multi caspase activity in a time dependent manner. In conclusion, dichloromethane crude extract of Andrographis paniculata, Ziziphus spina-christi and Gymnanthemum extensum displayed potent anticancer activities and the combination of dichloromethane crude extract of Gymnanthemum extensum with low piperine fractional Piper nigrum extract can be a promising regimen for an alternative cancer treatment
TL;DR: It can be known that small incision fenestration enjoys significant clinical effect for lumbar disc herniation complicated with lumbars spinal stenosis is with important clinical promotion value.
Abstract: The paper aims to assess clinical effect of small incision fenestration for lumbar disc herniation complicated with lumbar spinal stenosis and provide more adequate scientific guiding basis for clinical treatment. In this paper, clinical data of 1200 lumbar disc herniation patients with lumbar spinal stenosis who were hospitalized during June 2014 and June 2015 were retrospectively analyzed. Depending on their different treatment options, the patients were divided into two groups: 550 cases of control group patients underwent conventional surgery, 650 cases of observation group patients received small incision fenestration. The two groups of patient’s operation time, intraoperative blood loss and postoperative hospital stay were recorded in detail. Clinical results of the two groups of surgical treatment were evaluated and compared with visual analog scale pain grade score and lower back pain Japanese orthopaedic association scoring system. The treatment results showed that operation time, postoperative hospital stay and intraoperative blood loss of observation group were significantly less than those of control group. Comparison between groups, p<0.05, statistically significant; visual analog scale score and Japanese orthopaedic association score result showed significant superiority of observation group therapy compared to control group. Statistical difference of p<0.05 is statistically significant. It can thus be known that small incision fenestration enjoys significant clinical effect for lumbar disc herniation complicated with lumbar spinal stenosis is with important clinical promotion value.
TL;DR: In this article, the platelet stimulating activity of carpaine extracted from papaya leaves was investigated in the treatment of thrombocytopenia associated with diseases and drugs and the results showed that bioavailability enhanced carpaine exhibits potent activity of increasing platelet count.
Abstract: Carica papaya leaves are used in folklore medicine for the treatment of different types of thrombocytopenia associated with diseases and drugs. There are several scientific studies carried out on humans and animal models to confirm the efficacy of papaya leaves extract for the treatment of thrombocytopenia. In the present study, the alkaloid, carpaine extracted from papaya leaves was found to have platelet stimulating activity. Papaya leaves powder was extracted by microwave with a mixture of methanol: glacial acetic acid: water (180:2:1.6 v/v/v). The extract was treated with suitable solvent to obtain alkaloid fraction. From the total alkaloids, carpaine was further separated by preparative thin layer chromatography, purified and analyzed. Carpaine was complexed with beta-cyclodextrin and mixed with piperine. The complex was administered in thrombocytopenia induced rats. The results showed that bioavailability enhanced carpaine exhibits potent activity of increasing platelet count.
TL;DR: Different kinetics model were used to analyze in vitro drug release and results indicated that the drug release follows Korsemeyer-Peppa’s model.
Abstract: Biopolymeric nanoparticles were synthesized using Gellan Gum and loaded with Atenolol, an antihypertensive drug by ionotropic gelation (an easy and ecofriendly system) induced by BaCl2 as an ionic crosslinking agent to improve absorption and bioavailability of drug. These nanoparticles were characterized by scanning electron microscope, fourier-transform infrared spectroscopy, X-ray diffraction analysis and dynamic light scattering techniques. Mean particle size obtained was 85.61 nm by X-ray diffraction, Zeta potential -19.4 mV with fibrous morphology. In order to optimize conditions for in vitro drug release various physicochemical parameters were studied. Different kinetics model were used to analyze in vitro drug release and results indicated that the drug release follows Korsemeyer-Peppa’s model.
TL;DR: The present in silico study explores the comparative efficacy of these drugs to inhibit 3-chymotrypsin like protease and RNA dependent RNA polymerase, to plan therapeutic options for patients based on their disease severity.
Abstract: Favipiravir and remdesivir are investigational drugs for coronavirus disease 2019 that is caused by severe acute respiratory syndrome coronavirus 2. The active forms of these drugs are reported to target and inhibit viral RNA dependent RNA polymerase, which is derived from 3-chymotrypsin like protease, a viral replicase enzyme. The present in silico study explores the comparative efficacy of these drugs to inhibit 3-chymotrypsin like protease and RNA dependent RNA polymerase, to plan therapeutic options for patients based on their disease severity. Active favipiravir and remdesivir molecules bind to 3-chymotrypsin like protease with energies of 6.18 and -6.52 kcal/mol in contrast to -5.62 and -3.91 kcal/mol for RNA dependent RNA polymerase. Further, hydrophobic interactions and salt bridge formations cement drug bindings with 3-chymotrypsin like protease, but not with RNA dependent RNA polymerase. Molecular dynamic simulation experiments, performed under certain experimental constraints reveal that the root mean square flexibilities of active residues in drug complexes with 3-chymotrypsin like protease are lower than in free 3-chymotrypsin like protease making the former more stable than the latter because of their rigidity and stabilities. Both drugs may hence serve as good therapeutic options for early stages of coronavirus disease 2019. However, more severe symptoms may be treated better with favipiravir due to its better binding with RNA dependent RNA polymerase, as compared to remdesivir. The “one drug does not fit all” concept is true for coronavirus disease 2019 as it is being currently realized by clinicians all around the world. Hence precise knowledge about critical interactions of these drugs with the viral enzymes will help medicos make vital therapeutic decisions on interventional options for patients who report to hospitals without over symptoms or with varying degrees of disease severity.
TL;DR: Age, income, occupation, whether suffering from chronic diseases, whether they are willing to use information technology to detect and manage diseases and other factors, all affect the demand of the elderly for basic medical services and rehabilitation guidance services in medical service institutions.
Abstract: There are clinics around nursing homes in foreign countries or family doctors for every elderly. When a disease occurs, doctors can provide door to door service to help patients. Since the epidemic of coronavirus disease 2019, the elderly have been a high risk group of people infected with coronavirus disease 2019. In both the United States and Canada, the first recorded coronavirus disease 2019 deaths and outbreaks occurred in nursing homes with case fatality rates in these settings reported to be as high as 33.7 %. Due to the lack of adequate medical facilities and adequate medical staff to provide services, the elderly are more likely to be infected with the virus as a result of social interaction. All these show that foreign models can no longer meet the medical needs of the elderly. Therefore, we should take a different perspective and combine pension services with medical care. At present, China is exploring the mode of combination of medical and nursing services. In this study, we investigated the current situation of integrated medical and nursing services in China, exploring the transformation of primary medical institutions into medical and nursing service providers. The integrated eldercare services with medical care is that we make use of the existing medical resources to provide care services, which can meet the health needs of the elderly and reduce the infection rate of the elderly. Using a self-administered or interview questionnaire survey, we conducted t-test and one-way analysis of variance. It was found that the elderly are most satisfied with the geographical location (90.84 %) and medical services (90.82 %), and the most dissatisfied with consultation (87.66 %) and institutional fees (87.23 %). The elderly with the older age, the higher the monthly income of more than 3000 yuan, marriage and chronic diseases, are highly satisfied with their community health service institutions (p<0.05). Through one-way analysis of variance, there were significant differences in medical and health service demand among the groups with different monthly income (f=5.289 and 5.312, p<0.05), different occupation (f=5.574 and 2.325, p<0.05), and different ideal mode of providing for the aged (f=5.237, p=0.002<0.05). By independent sample t test, it was found that there were significant differences in basic medical service demand and health guidance service demand between people with chronic diseases and those without chronic diseases (p<0.05), and those who were willing and unwilling to use information technology for disease management (p<0.05). Through regression analysis, we can see that age (t=4.411, p<0.05) and income (t=2.061, p<0.05) have significant influence on basic medical service among the three variables of age, education and monthly income, and the coefficient is positive. Age (t=2.508, p<0.05) and income (t=3.143, p<0.05) had significant influence on rehabilitation guidance service, and the coefficient was positive. In summary, age, income, occupation, whether suffering from chronic diseases, whether they are willing to use information technology to detect and manage diseases and other factors, all affect the demand of the elderly for basic medical services and rehabilitation guidance services in medical service institutions. Through the research on the current situation of the integrated medical and nursing services in China, this study enriches the relevant evidence of the integrated medical and nursing services, and has a certain reference value for the relevant management departments to formulate policiesis.
TL;DR: Traditional Chinese medicine continuous nursing has positive effects on improving the cognitive function, neural function, social function, motor function of elderly patients with stroke.
Abstract: To evaluate the effect of traditional Chinese medicine continuous nursing on the functional improvement of elderly stroke patients. A total of 85 cases of elderly stroke patients admitted to the department of neurology of our hospital from January 2019 to January 2020 were selected as the research objects. According to the random number table method, the selected cases were divided into two groups, the control group (42 cases) received routine discharge nursing and the study group (43 cases) received traditional Chinese medicine continuous nursing on the basis of the control group. The cognitive function, neurological function, social function and motor function were compared between the two groups. Compared with those before intervention, the scores of Montreal cognitive assessment scale in the two groups were significantly increased after the intervention (p<0.05) and Montreal cognitive assessment scale score of the study group was higher than that of the control group (p<0.05). Compared with those before the intervention, the National Institutes of Health Stroke Scale scores of the two groups were significantly decreased after the intervention (p<0.05) and the National Institutes of Health Stroke Scale score of the study group was lower than that of the control group (p<0.05). Compared with those before the intervention, the Social Functional Rafing Scale scores of the two groups were significantly decreased after the intervention (p<0.05) and the Social Functional Rafing Scale score of the study group was lower than that of the control group (p<0.05). Compared with those before the intervention, the scores of Fugl-Meyer assessment (upper limb) and Fugl-Meyer assessment (lower limb) of the two groups were significantly increased after the intervention (p<0.05) and the scores of Fugl-Meyer assessment (upper limb) and Fugl- Meyer assessment (lower limb) of the study group were higher than those of the control group (p<0.05). Traditional Chinese medicine continuous nursing has positive effects on improving the cognitive function, neural function, social function, motor function of elderly patients with stroke.
TL;DR: In this article, mesoporous silica nanoparticles of tamoxifen are prepared to deal with the problem of solubility of anti-cancerous drugs because of their complicated structures.
Abstract: Breast cancer is a cancer which has significant societal impact because it generally affects the young age people. Tamoxifen is Biopharmaceutical Classification System class II drug. This active pharmaceutical ingredient have problem with solubility. Most of the anti-cancerous drugs have problem with solubility because of their complicated structures. To deal with this problem mesoporous silica nanoparticles of tamoxifen are prepared. Drug entrapped in mesoporous structure which is having size less than 200 nm. It leads to improvement in solubility and further bioavailability. Various studies after formulation show improvement in solubility and decrease in particle size. Further fast dissolving tablet is prepared to improve bioavailability. Pre compression studies and post compression studies show tablet dissolve within 30 s. Hence mesoporous silica nanoparticles are best way to improve solubility.
TL;DR: In the intensive hypoglycemic treatment of patients with type 2 diabetes mellitus using an insulin pump, the application of flash glucose monitoring system can effectively control blood glucose, accelerate blood glucose control and reduce insulin dosage and hypoglycemia reaction, which is helpful to raise the comfort level of patients, ameliorate the psychological and sleep states and improve the quality of life.
Abstract: To explore the role of flash glucose monitoring system combined with insulin pump in the blood glucose treatment of patients with type 2 diabetes mellitus. Eighty patients with type 2 diabetes mellitus treated in our hospital from September 2019 to September 2020 were randomly divided into two groups (n=40) using a random number table. Both groups received hypoglycemic treatment using an insulin pump. During treatment, blood glucose level was measured by collecting the fingertip blood of control group, while dynamic blood glucose monitoring was carried out for observation group using the flash glucose monitoring system. Blood glucose indices, time of controlling blood glucose to target level, insulin dosage, incidence rate of hypoglycemia, comfort score; mental state scores, sleep quality score and quality of life score were compared. After treatment, fasting blood glucose and 2 h postprandial blood glucose were lower, time of controlling blood glucose to target level was shorter and insulin dosage was smaller in observation group than those in control group (p<0.05). Observation group had lower incidence rate of hypoglycemia, Self-rating Anxiety Scale, Self-rating Depression Scale and Pittsburgh Sleep Quality Index scores, as well as higher comfort and quality of life scores than those of control group (p<0.05). In the intensive hypoglycemic treatment of patients with type 2 diabetes mellitus using an insulin pump, the application of flash glucose monitoring system can effectively control blood glucose, accelerate blood glucose control and reduce insulin dosage and hypoglycemia reaction, which is helpful to raise the comfort level of patients, ameliorate the psychological and sleep states and improve the quality of life.
TL;DR: It is confirmed that Bardet-Biedl syndrome 4 can be used as an independent prognostic factor for the prognosis of breast cancer, which provides a basis for exploring a new target for the treatment of Breast cancer.
Abstract: Bardet-Biedl syndrome 4 is the key protein to control cilia formation. In this study, bioinformatics method was used to screen the core genes related to the prognosis of breast cancer by analyzing the gene chip data of gene expression omnibus and the cancer genome atlas database, so as to provide a new candidate target for the treatment of breast cancer. Data were downloaded from the cancer genome atlas, gene expression omnibus to evaluate Bardet-Biedl syndrome 4 expression levels in breast cancer. Differentially expressed genes were screened by R package. Gene ontology and Kyoto encyclopedia of Genes and Genomes pathway enrichment analysis was used to explore the biological functions of differentially expressed genes. The correlation of differentially expressed genes used was, “corrplot” for visual analysis. The proteinprotein interaction relationship was constructed based on search tool for the retrieval of interacting genes/ proteins database and Cytoscape software and the key genes were obtained by module analysis with Cytoscape software molecular complex detection plugin and the prognostic value and survival of Bardet- Biedl syndrome 4 were evaluated by R package. Finally, the correlation between Bardet-Biedl syndrome 4 and clinicopathological parameters was also visualized by R package. These differentially expressed genes were mainly involved in response to peptide hormone, nuclear division, hormone secretion and transport and extracellular matrix. Genes were mainly involved in the Kyoto encyclopedia of genes and genomes pathway called Interleukin-17 signaling pathway. Bardet-Biedl syndrome 4 levels were found to be down regulated in breast cancer tissues compared with normal tissues. Survival analysis showed that low Bardet-Biedl syndrome 4 expression was associated with poor prognosis. These results were verified in clinical specimens, where in the Bardet-Biedl syndrome 4 protein levels were significantly down regulated in breast cancer tissues compared with non-breast cancer tissues. This study confirmed that Bardet-Biedl syndrome 4 can be used as an independent prognostic factor for the prognosis of breast cancer, which provides a basis for exploring a new target for the treatment of breast cancer.
TL;DR: Results suggest possible partial contribution of Aspergillus neoniger to the reported activity of the host plant and suggest potential protective role of this endophyte on its host plant.
Abstract: Endophytes are considered as a rich source of bioactive natural products. Many plants have not been investigated for their endophytic content yet, such as the medicinal plant Ficus carica. Recent studies confirmed antimicrobial and anticancer activities for the plant extract. To find out if its endophytes contribute to its reported activities, the bioactive endophyte Aspergillus neoniger was selected for investigation of its metabolites since it exerted antimicrobial and anticancer activities in preliminary screening assays. The fungal extract was subjected to bioactivity guided chromatographic fractionation for isolation of its bioactive metabolites. This resulted in the identification of four aurasperones (asperpyrone D, aurasperone D, dianhydroaurasperone C, aurasperone A) through spectroscopic analysis. Aurasperone D and asperpyrone D were found to be cytotoxic against human cervical cancer cells (50 % cytotoxic concentration=4.4 μg ml-1 and 3.0 μg ml-1 respectively). Aurasperone D exerted strong antiproliferative effect against human immortal erythroleukaemia cells 562 and human umbilical vein endothelial cells (concentration at which 50 % growth inhibition achieved is 5.3 and 4.7 μg ml-1) as well as asperpyrone D (concentration at which 50 % growth inhibition achieved is 4.9 and 5.4 μg ml-1). Dianhydroaurasperone C and aurasperone A, on the contrary, showed weak cytotoxic and antiproliferative effects. All compounds were tested for antimicrobial activity against several test strains including the plant pathogen Fusarium oxysporum. Results revealed that aurasperone D and asperpyrone D to be most active which suggests potential protective role of this endophyte on its host plant. These results suggest possible partial contribution of Aspergillus neoniger to the reported activity of the host plant
TL;DR: Results suggest a protective effect against carbon tetrachloride induced acute liver injury by inhibiting the activation of nucleotide binding leucine rich repeat receptors family pyrin domain containing 3 inflammasome, which suggest a promising avenue for the exploration of Smilax glabra Roxb.
Abstract: The experiment was conducted to investigate the protective effect of Smilax glabra Roxb. aqueous extract on carbon tetrachloride induced acute liver injury in rats by regulating the nucleotide binding leucine rich repeat receptors family pyrin domain containing 3 inflammasome. In this study, a rat acute liver injury model was established by a single intraperitoneal injection of 50 % carbon tetrachloride oil solution (1 ml/kg body weight). A total of 50 rats were randomly divided into control group, model group and 3 Smilax glabra Roxb. aqueous extract intervention groups (0.75, 1.5 and 3 g/kg body weight/d). Smilax glabra Roxb. aqueous extract or distilled water was orally administered by gavage once daily for seven consecutive days. Then the blood and liver samples were collected. The results showed that in the 3 intervention Smilax glabra Roxb. aqueous extract groups, the levels of serum aspartate aminotransferase and Alanine aminotransferase, the content of malondialdehyde in rat liver tissues significantly reduced and superoxide dismutase, catalase and glutathione increased significantly, the liver lobule structures were repaired and the liver cells were aligned in an orderly manner, the expressions of nucleotide binding leucine rich repeat receptors family pyrin domain containing 3 inflammasome, apoptosis associated speck like protein containing and caspase-1 proteins, Interleukin 1 beta messenger ribonucleic acid was decreased. Smilax glabra Roxb. aqueous extract exerted a protective effect against carbon tetrachloride induced acute liver injury by inhibiting the activation of nucleotide binding leucine rich repeat receptors family pyrin domain containing 3 inflammasome, which suggest a promising avenue for the exploration of Smilax glabra Roxb. aqueous extract in improving acute liver injury.