scholarly journals Formulation, Optimization and Evaluation of Luteolin-Loaded Topical Nanoparticulate Delivery System for the Skin Cancer

Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1749
Author(s):  
Imran Kazmi ◽  
Fahad A Al-Abbasi ◽  
Muhammad Shahid Nadeem ◽  
Hisham N Altayb ◽  
Sultan Alshehri ◽  
...  
Keyword(s):  
Skin Cancer ◽  
Encapsulation Efficiency ◽  
Prediction Method ◽  
Cancer Cell Line ◽  
Drug Content ◽  
Ic50 Value ◽  
Study Results ◽  
Significant Difference ◽  
Cytotoxicity Assessment ◽  
Edge Activator

In the present study, luteolin (LT)-loaded nanosized vesicles (LT-NVs) were prepared by a solvent evaporation–hydration method using phospholipid and edge activator. The formulation was optimized using three factors at a three-level Box–Behnken design. The formulated LT-NVs were prepared using the three independent variables phospholipid (A), edge activator (B) and sonication time (C). The effect of used variables was assessed on the vesicle size (Y1) and encapsulation efficiency (Y2). The selection of optimum composition (LT-NVopt) was based on the point prediction method of the software. The prepared LT-NVopt showed the particle size of 189.92 ± 3.25 nm with an encapsulation efficiency of 92.43 ± 4.12% with PDI and zeta potential value of 0.32 and −21 mV, respectively. The formulation LT-NVopt was further converted into Carbopol 934 gel (1% w/v) to enhance skin retention. LT-NVoptG was further characterized for viscosity, spreadability, drug content, drug release, drug permeation and antioxidant, antimicrobial and cytotoxicity assessment. The evaluation result revealed optimum pH, viscosity, spreadability and good drug content. There was enhanced LT release (60.81 ± 2.87%), as well as LT permeation (128.21 ± 3.56 µg/cm2/h), which was found in comparison to the pure LT. The antioxidant and antimicrobial study results revealed significantly (p ˂ 0.05) better antioxidant potential and antimicrobial activity against the tested organisms. Finally, the samples were evaluated for cytotoxicity assessment using skin cancer cell line and results revealed a significant difference in the viability % at the tested concentration. LT-NVoptG showed a significantly lower IC50 value than the pure LT. From the study, it can be concluded that the prepared LT-NVoptG was found to be an alternative to the synthetic drug as well as conventional delivery systems.

Synthesis, Docking Study, Cytotoxicity, Antioxidant, and Anti-microbial Activities of Novel 2,4-Disubstituted Thiazoles Based on Phenothiazine

2020 ◽  
Vol 17 (2) ◽  
pp. 151-159
Author(s):  
Tran Nguyen Minh An ◽  
Pham Thai Phuong ◽  
Nguyen Minh Quang ◽  
Nguyen Van Son ◽  
Nguyen Van Cuong ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Antimicrobial Activities ◽  
Significant Activity ◽  
Thiazole Derivatives ◽  
Ligand Interaction ◽  
Ic50 Value ◽  
Mcf 7

: A series of novel 1,3-thiazole derivatives (5a-i) with a modified phenothiazine moiety were synthesized and tested against cancer cell line MCF-7 for their cytotoxicity. Most of them (5a-i) were less cytotoxic or had no activity against MCF-7 cancer cell line. Material and Methods: The IC50 value of compound (4) was 33.84 μM. The compounds (5a-i) were also evaluated for antimicrobial activities, but no significant activity was observed. The antioxidant activity was conducted for target compounds (5a-i). The IC50 value of compound (5b) was 0.151mM. Results: The total amount of energy, ACE (atomic contact energy), energy of receptor (PDB: 5G5J), and ligand interaction of structure (4) were found to be 22.448 Kcal.mol-1 , -247.68, and -91.91 Kcal.mol-1, respectively. The structure (4) is well binded with the receptor because the values of binding energy, steric energy, and the number of hydrogen bondings are -91.91, 22.448 kcal.mol-1, and 2, respectively. It shows that structure (4) has good cytotoxicity with MCF-7 in vitro. Conclusion: The increasing of docking ability of structures (5a-i) with the receptor is presented in increasing order as (5f)>(5e)>(5g)>(5a)>(5b)>(5d)>(5c)>(5i)>(5h). The structure bearing substitution as thiosemicarbazone (4), nitrogen heterocyclic (5f), halogen (5e), and azide (5g) showed good cytotoxicity activity in vitro.

Rotundic Acid Regulates the Effects of Let-7f-5p on Caco2 Cell Proliferation

2020 ◽  
Vol 20 ◽  
Author(s):  
Yuan Feng ◽  
Xinran Liu ◽  
Yueqing Han ◽  
Mantian Chen ◽  
Lin Zhang ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Colony Formation ◽  
Cancer Cell Line ◽  
Human Colon ◽  
Colon Cancer Cell Line ◽  
Inhibitory Effect ◽  
Human Colon Cancer ◽  
Caco2 Cell ◽  
Study Results ◽  
Rotundic Acid

Background & Objective: Nowadays, the interaction between natural products and microRNAs provides a promising field for exploring the chemo preventive agents for various cancers.As a member of microRNAs, the expression of let-7f-5p is universally down regulated in colorectal cancer (CRC). The present study aimed to uncover the function of let-7f-5p in the proliferation of human colon cancer cell line Caco2 and explored chemo preventive agents from natural resources that can prevent the development of CRC. Methods: Herein, Caco2 cells were transfected with let-7f-5p mimic and inhibitor to manipulate let-7f-5p levels, and the expression of let-7f-5p wasper formed by RT‑qPCR. Next, we determined how let-7f-5p regulates Caco2 cell proliferation by using MTT, wound-healing, cell cycle,and colony formation assays.Besides, to further understand the effect of let-7f-5p, we evaluated the protein level of AMER3 and SLC9A9 by using western blotting assays. Results: The results showed a suppressive function of let-7f-5p on Caco2 cell proliferation and then put forward a triterpenoid (rotundic acid, RA) which significant antagonized the effect of cell proliferation, restitution after wounding,and colony formation caused by let-7f-5p. Moreover, the western blot results further indicated that the inhibitory effect of RA might be due to its suppressive role in let-7f-5p-targeted AMER3 and SLC9A9 regulation. Conclusion: Our validation study results confirmed that let-7f-5p was a potent tumor suppressor gene of Caco2 cell proliferation,and RA showed as a regulator of the effect oflet-7f-5p on cell proliferation and then could be a potential chemo preventive agent for CRC treatment.

scholarly journals Ayurveda Body–Mind Constitutional Types and Role of Yoga Intervention Among Type 2 Diabetes Mellitus Population of Chandigarh and Panchkula Regions

2021 ◽  
pp. 097275312110000
Author(s):  
Madhava Sai Sivapuram ◽  
Vinod Srivastava ◽  
Navneet Kaur ◽  
Akshay Anand ◽  
Raghuram Nagarathna ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Lipid Profiles ◽  
Control Groups ◽  
Yoga Intervention ◽  
Positive Effects ◽  
Study Results ◽  
Significant Difference ◽  
And Control

Background: Type 2 diabetes needs a better understanding of etiological factors and management strategies based on lifestyle and constitutional factors, given its high association rate with many cardiovascular, neurological disorders, and COVID-19 infection. Purpose: The present study was undertaken to investigate the effect of Diabetes-specific integrated Yoga lifestyle Protocol (DYP) on glycemic control and lipid profiles of diabetic adults. Along with the DYP intervention, the individuals residing in Chandigarh and Panchkula union territories in the northern part of India were assessed for Ayurveda-based body–mind constitutional type. Ayurveda describes body–mind constitution as “ prakriti,” which has been discussed from two angles, namely physiological and psychological as body and mind are correlated. Methods: Cluster sampling of waitlist control study subjects was used as the sampling method for the study. A total of 1,215 registered subjects (81 diabetic) responded in randomly selected clusters in Chandigarh and Panchkula. Ayurveda physicians did Ayurveda body–mind constitutional assessment called prakriti assessment (physiological body–mind constitution assessment) in 35 participants (23 diabetic, 12 prediabetic) as a part of the study. Results: A group of 50 subjects was randomly selected for yoga intervention out of 81 diabetes mellitus adults, and 31 subjects were enrolled as waitlist controls. A significant decrease in the glycosylated hemoglobin levels from 8.49 ± 1.94% to 7.97 ± 2.20% in the intervention group was noticed. The lipid profiles of the DYP intervention and control groups were monitored. Three-month follow-up results of lipid profile diagnostic tests in intervention and control groups showed a significant difference between the two groups ( P < 0.05). Most diabetic and prediabetic individuals were found to have pitta dosha ( pitta controls all heat, metabolism, and transformation in the mind and body) as dominant constitution type. Conclusion: The study results demonstrated significant positive effects of yoga in diabetic individuals. This study has indicated the evidence for the safety and efficacy of the validated DYP for community-level interventions to prevent maladies like brain damage and stroke.

A Meta-Analysis of Extracorporeal Anticoagulants in Pediatric Continuous Kidney Replacement Therapy

2021 ◽  
pp. 088506662199275
Author(s):  
Rupesh Raina ◽  
Nirav Agrawal ◽  
Kirsten Kusumi ◽  
Avisha Pandey ◽  
Abhishek Tibrewal ◽  
...  
Keyword(s):  
Replacement Therapy ◽  
Meta Analysis ◽  
Kidney Injury ◽  
Electrolyte Imbalance ◽  
Therapeutic Modality ◽  
Regional Citrate Anticoagulation ◽  
Increased Risk ◽  
Study Results ◽  
Significant Difference ◽  
Kidney Replacement Therapy

Objective: Continuous kidney replacement therapy (CKRT) is the primary therapeutic modality utilized in hemodynamically unstable patients with severe acute kidney injury. As the circuit is extracorporeal, it poses an increased risk of blood clotting and circuit loss; frequent circuit losses affect the provider’s ability to provide optimal treatment. The objective of this meta-analysis is to evaluate the safety and efficacy of the extracorporeal anticoagulants in the pediatric CKRT population. Data Sources: We conducted a literature search on PubMed/Medline and Embase for relevant citations. Study Selection: Studies were included if they involved patients under the age of 18 years undergoing CKRT, with the use of anticoagulation (heparin, citrate, or prostacyclin) as a part of therapy. Only English articles were included in the study. Data Extraction: Initial search yielded 58 articles and a total of 24 articles were included and reviewed. A meta-analysis was performed focusing on the safety and effectiveness of regional citrate anticoagulation (RCA) vs unfractionated heparin (UFH) anticoagulants in children. Data Synthesis: RCA had statistically significantly longer circuit life of 50.65 hours vs. UFH of 42.10 hours. Two major adverse effects metabolic alkalosis and electrolyte imbalance seen more commonly in RCA compared to UFH. There was not a significant difference in the risk of systemic bleeding when comparing RCA vs. UFH. Conclusion: RCA is the preferred anticoagulant over UFH due to its significantly longer circuit life, although vigilant circuit monitoring is required due to the increased risk of electrolyte disturbances. Prostacyclin was not included in the meta-analysis due to the lack of data in pediatric patients. Additional studies are needed to strengthen the study results further.

scholarly journals Reproductive Performance Following Hysteroscopic Surgery for Uterine Septum: Results from a Single Surgeon Data

2021 ◽  
Vol 10 (1) ◽  
pp. 130
Author(s):  
Ertan Saridogan ◽  
Mona Salman ◽  
Lerzan Sinem Direk ◽  
Ali Alchami
Keyword(s):  
Reproductive Performance ◽  
Observational Studies ◽  
Patient Characteristics ◽  
Reproductive Outcomes ◽  
Hysteroscopic Surgery ◽  
High Quality Evidence ◽  
Study Results ◽  
Significant Difference ◽  
Uterine Septum

Uterine septum can negatively affect reproductive outcomes in women. Based on evidence from retrospective observational studies, hysteroscopic incision has been considered a solution to improve reproductive performance, however there has been recent controversy on the need for surgery for uterine septum. High quality evidence from prospective studies is still lacking, and until it is available, experts are encouraged to publish their data. We are therefore presenting our data that involves analysis of the patient characteristics, surgical approach and long-term reproductive outcomes of women who received treatment for uterine septum under the care of a single surgeon. This includes all women (99) who underwent hysteroscopic surgery for uterine septum between January 2001 and December 2019. Of those 99 women treated for intrauterine septum who were trying to conceive, 91.4% (64/70) achieved pregnancy, 78.6% (55/70) had live births and 8.6% (6/70) had miscarriages. No statistically significant difference was found in the live birth rates when data was analyzed in subgroups based on age, reason for referral/aetiology and severity of pathology. Our study results support the view that surgical treatment of uterine septa is beneficial in improving reproductive outcomes.

scholarly journals Transformation and functional verification of Cry5Aa in cotton

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Shihao Zhao ◽  
Feng Wang ◽  
Qiuping Zhang ◽  
Jiayi Zou ◽  
Zhangshu Xie ◽  
...  
Keyword(s):  
Resistance Gene ◽  
Insect Resistance ◽  
Expression Patterns ◽  
Instar Larva ◽  
Cotton Bollworm ◽  
Pcr Analysis ◽  
Functional Verification ◽  
Study Results ◽  
Significant Difference ◽  
Transgenic Strains

AbstractMost of the cotton bollworm-resistant genes applied in cotton are more than 20 years and they all belong to Cry1Ab/c family, but the insect-resistant effects of Cry5Aa on cotton were rarely reported. The possible risk of resistance is increasing. The study synthesized a novel bollworm-resistant gene Cry5Aa artificially based on preferences of cotton codon. The new gene was transferred to cotton through the method of pollen tube pathway. The transgenic strains were identified by kanamycin test in field and laboratory PCR analysis. Meanwhile, an insect resistance test was conducted by artificial bollworm feeding with transgenic leaves and GK19 was used as a control in this study. Results showed that rate of positive transgenic strains with kanamycin resistance in the first generation (T1), the second generation (T2) and the third generation (T3) respectively were 7.76%, 73.1% and 95.5%. However, PCR analysis showed that the positive strain rate in T1, T2 and T3 were 2.35%, 55.8% and 94.5%, respectively. The resistant assay of cotton bollworm showed that the mortality rate of the second, third and fourth instar larva feed by the transgenic cotton leaves, were 85.42%, 73.35% and 62.79%, respectively. There was a significant difference between transgenic plant of Cry5Aa and GK19 in insect resistance. Finally, we also conducted the further analysis of gene expression patterns, gene flow and the effect on non-target pest in the study. The results showed that Cry5Aa gene had less environmental impact, and Cry5Aa has been transferred successfully and expressed stably in cotton. Therefore, the novel bollworm resistance gene can partially replace the current insect-resistance gene of Lepidoptera insects.

scholarly journals Formulation of Piperine–Chitosan-Coated Liposomes: Characterization and In Vitro Cytotoxic Evaluation

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3281
Author(s):  
Syed Sarim Imam ◽  
Sultan Alshehri ◽  
Mohammad A. Altamimi ◽  
Afzal Hussain ◽  
Wajhul Qamar ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Breast Cancer Cell Line ◽  
Therapeutic Efficacy ◽  
Cancer Cell Line ◽  
Permeation Study ◽  
Study Results

The present research work is designed to prepare and evaluate piperine liposomes and piperine–chitosan-coated liposomes for oral delivery. Piperine (PPN) is a water-insoluble bioactive compound used for different diseases. The prepared formulations were evaluated for physicochemical study, mucoadhesive study, permeation study and in vitro cytotoxic study using the MCF7 breast cancer cell line. Piperine-loaded liposomes (PLF) were prepared by the thin-film evaporation method. The selected liposomes were coated with chitosan (PLFC) by electrostatic deposition to enhance the mucoadhesive property and in vitro therapeutic efficacy. Based on the findings of the study, the prepared PPN liposomes (PLF3) and chitosan coated PPN liposomes (PLF3C1) showed a nanometric size range of 165.7 ± 7.4 to 243.4 ± 7.5, a narrow polydispersity index (>0.3) and zeta potential (−7.1 to 29.8 mV). The average encapsulation efficiency was found to be between 60 and 80% for all prepared formulations. The drug release and permeation study profile showed biphasic release behavior and enhanced PPN permeation. The in vitro antioxidant study results showed a comparable antioxidant activity with pure PPN. The anticancer study depicted that the cell viability assay of tested PLF3C2 has significantly (p < 0.001)) reduced the IC50 when compared with pure PPN. The study revealed that oral chitosan-coated liposomes are a promising delivery system for the PPN and can increase the therapeutic efficacy against the breast cancer cell line.

scholarly journals The Combined Effects of Sports Smart Bracelet and Multi-Component Exercise Program on Exercise Motivation among the Elderly in Macau

Medicina ◽  
2021 ◽  
Vol 57 (1) ◽  
pp. 34
Author(s):  
Cheuk Kei Lao ◽  
Bing Long Wang ◽  
Richard S. Wang ◽  
Hsiao Yun Chang
Keyword(s):  
Artificial Intelligence ◽  
Exercise Training ◽  
Training Programs ◽  
Exercise Program ◽  
The Elderly ◽  
Control Group ◽  
Exercise Motivation ◽  
Sport Training ◽  
Study Results ◽  
Significant Difference

Background and objectives: Faced with the serious problem of an aging population, exercise is one of the most effective ways to maintain the health of the elderly. In recent years, with the popularization of smartphones, the elderly have increasingly accepted technological products that incorporate artificial intelligence (AI). However, there is not much research on using artificial intelligence bracelets to enhance elders’ motivation and participation in exercise. Therefore, the purpose of this study is to evaluate the effectiveness of the combination of sports smart bracelets and multi-sport training programs on the motivation of the elderly in Macau. Materials and Methods: The study was conducted with a randomized trial design in a 12 week multi-sport exercise training intervention. According to the evaluation, a total of sixty elders’ pre- and post-test data were included in this study. Results: After 12 weeks of multi-sport exercise training, the evaluation scores on the exercise motivation scale (EMS) increased significantly in the group wearing exercise bracelets and those taking part in the multi-component exercise program, and the degree of progress reached a statistically significant level, but the control group did not show any statistically significant difference. The influence of the combination of sports smart bracelets and multi-sport training programs on elders’ motivation is clearer. Conclusions: The use of sports smart bracelets by elderly people in conjunction with diverse exercise training can effectively enhance elders’ motivation and increase their participation in regular exercise. The combination of sports smart bracelets and multi-sport training programs is worth promoting in the elderly population.

Combining Webduino Programming With Situated Learning to Promote Computational Thinking, Motivation, and Satisfaction Among High School Students

2021 ◽  
pp. 073563312110399
Author(s):  
Ting-Ting Wu ◽  
Jian-Ming Chen
Keyword(s):  
High School ◽  
High School Students ◽  
Programming Languages ◽  
Situated Learning ◽  
Learning Strategy ◽  
Computational Thinking ◽  
Learning Motivation ◽  
School Students ◽  
Study Results ◽  
Significant Difference

Many countries have incorporated computational thinking (CT) and programming languages into their science and technology courses. Students can improve their CT ability by learning programming languages. Moreover, situated learning enables students to generate knowledge and master problem-solving skills through interaction with situations. This study incorporated Webduino learning and the situated learning strategy into a programming course and analyzed its impact on high school students’ CT ability, learning motivation, and course satisfaction. A quasi-experimental research method was adopted, wherein the experimental group was subjected to the situated learning strategy and the control group was subjected to a traditional teaching method. The study results revealed that integrating Webduino programming with situated learning could effectively improve five categories of CT skills; moreover, the activity models of situated learning enhanced the value and expectation dimensions of learning motivation. In addition, satisfaction with the course content and self-identity slightly improved. However, because teachers were required to elaborate on stories to promote learner engagement with life situations, the time available for programming was limited. Thus, no significant difference was observed in teaching satisfaction.

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