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In silico evaluation, characterization, and in vitro anticancer activity of curcumin-nimbin loaded nanoformulation in HCT-116 cell lines.
Pub Date : 2024-12-19 eCollection Date: 2024-01-01 DOI: 10.5114/bta.2024.145256
Arumugam Madeswaran, Selvam Tamilazhagan, Sellappan Mohan

Colorectal cancer is one of the most prevalent malignancies worldwide and a leading cause of mortality. Chemotherapy medications are often limited in use due to issues like drug resistance, P-glycoprotein efflux, and relapse of chemotherapy. In this study, we formulated a nanosuspension with curcumin and nimbin to address these limitations and assessed its anticancer potential using in silico molecular docking and in vitro MTT assay.

Methods: In silico docking and ADMET analyses targeted proteins implicated in colorectal cancer, with doxorubicin as the standard. The docking studies were conducted using AutoDock 4.2, while in vitro anticancer activity was assessed through the MTT assay in HCT 116 cell lines.

Results: In silico docking of curcumin and nimbin showed significant interactions with target proteins compared to the standard. ADMET analysis indicated favorable Caco-2 permeability and intestinal absorption of the selected phytoconstituents. The MTT assay demonstrated concentration-dependent cell viability inhibition in HCT 116 cell lines treated with the nanosuspension, with an IC50 value of 30%.

Conclusion: The curcumin-nimbin loaded nanosuspension demonstrated promising anticancer activity against HCT 116 cell lines in both in silico and in vitro studies. Further studies are required to evaluate the anticancer effect of curcumin-nimbin loaded nanosupension through clinical and preclinical studies for the progress of potential formulation in the treatment of colorectal cancer.

{"title":"<i>In silico</i> evaluation, characterization, and <i>in vitro</i> anticancer activity of curcumin-nimbin loaded nanoformulation in HCT-116 cell lines.","authors":"Arumugam Madeswaran, Selvam Tamilazhagan, Sellappan Mohan","doi":"10.5114/bta.2024.145256","DOIUrl":"10.5114/bta.2024.145256","url":null,"abstract":"<p><p>Colorectal cancer is one of the most prevalent malignancies worldwide and a leading cause of mortality. Chemotherapy medications are often limited in use due to issues like drug resistance, P-glycoprotein efflux, and relapse of chemotherapy. In this study, we formulated a nanosuspension with curcumin and nimbin to address these limitations and assessed its anticancer potential using <i>in silico</i> molecular docking and <i>in vitro</i> MTT assay.</p><p><strong>Methods: </strong><i>In silico</i> docking and ADMET analyses targeted proteins implicated in colorectal cancer, with doxorubicin as the standard. The docking studies were conducted using AutoDock 4.2, while <i>in vitro</i> anticancer activity was assessed through the MTT assay in HCT 116 cell lines.</p><p><strong>Results: </strong><i>In silico</i> docking of curcumin and nimbin showed significant interactions with target proteins compared to the standard. ADMET analysis indicated favorable Caco-2 permeability and intestinal absorption of the selected phytoconstituents. The MTT assay demonstrated concentration-dependent cell viability inhibition in HCT 116 cell lines treated with the nanosuspension, with an IC<sub>50</sub> value of 30%.</p><p><strong>Conclusion: </strong>The curcumin-nimbin loaded nanosuspension demonstrated promising anticancer activity against HCT 116 cell lines in both <i>in silico</i> and <i>in vitro</i> studies. Further studies are required to evaluate the anticancer effect of curcumin-nimbin loaded nanosupension through clinical and preclinical studies for the progress of potential formulation in the treatment of colorectal cancer.</p>","PeriodicalId":94371,"journal":{"name":"Biotechnologia","volume":"105 4","pages":"355-365"},"PeriodicalIF":0.0,"publicationDate":"2024-12-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11748221/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143026191","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Biofilm architecture and dynamics of the oral ecosystem.
Pub Date : 2024-12-19 eCollection Date: 2024-01-01 DOI: 10.5114/bta.2024.145259
Rina Rani Ray

The oral cavity, being a nutritionally enriched environment, has been proven to be an ideal habitat for biofilm development. Various microenvironments, including dental enamel, supra- and subgingival surfaces, salivary fluid, and the dorsal surface of the tongue, harbor diverse microbes. These biofilms typically consist of four major layers. Depending on the food, age, clinical state, and lifestyle of the patient, the microbial growth dynamics in oral biofilm varies significantly. The presence of pathogenic bacteria that disrupt the normal floral composition of the oral cavity can lead to plaque biofilm formation, which is a precursor to various diseases. Noteworthy pathogenic bacteria, such as Porphyromonas gingivalis, Fusobacterium nucleatum, and Streptococcus mutans, often initiate biofilm formation. Undiagnosed and untreated oral biofilm can lead to severe diseases like periodontitis and eventual tooth loss. Therefore, studying the architecture and dynamics of oral biofilms is essential and can be achieved through image analysis and modern technologies, such as AI-enabled technologies and surface topography-adaptive robotic superstructures.

{"title":"Biofilm architecture and dynamics of the oral ecosystem.","authors":"Rina Rani Ray","doi":"10.5114/bta.2024.145259","DOIUrl":"10.5114/bta.2024.145259","url":null,"abstract":"<p><p>The oral cavity, being a nutritionally enriched environment, has been proven to be an ideal habitat for biofilm development. Various microenvironments, including dental enamel, supra- and subgingival surfaces, salivary fluid, and the dorsal surface of the tongue, harbor diverse microbes. These biofilms typically consist of four major layers. Depending on the food, age, clinical state, and lifestyle of the patient, the microbial growth dynamics in oral biofilm varies significantly. The presence of pathogenic bacteria that disrupt the normal floral composition of the oral cavity can lead to plaque biofilm formation, which is a precursor to various diseases. Noteworthy pathogenic bacteria, such as <i>Porphyromonas gingivalis</i>, <i>Fusobacterium nucleatum</i>, and <i>Streptococcus mutans</i>, often initiate biofilm formation. Undiagnosed and untreated oral biofilm can lead to severe diseases like periodontitis and eventual tooth loss. Therefore, studying the architecture and dynamics of oral biofilms is essential and can be achieved through image analysis and modern technologies, such as AI-enabled technologies and surface topography-adaptive robotic superstructures.</p>","PeriodicalId":94371,"journal":{"name":"Biotechnologia","volume":"105 4","pages":"395-402"},"PeriodicalIF":0.0,"publicationDate":"2024-12-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11748217/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143026192","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Gliclazide protects ionizing radiation-induced intestinal injury in mice by inhibiting oxidative stress and caspase-3.
Pub Date : 2024-12-19 eCollection Date: 2024-01-01 DOI: 10.5114/bta.2024.145257
Soroush Arzani, Soghra Farzipour, Fereshteh Talebpour Amiri, Seyed Jalal Hosseinimehr

Gliclazide (GLZ), an oral antihyperglycemic medication, has additional beneficial effects, such as anti-inflammatory and antioxidant properties, besides lowering blood glucose levels. In this study, the radio-protective effect of GLZ was evaluated against ionizing radiation (IR)-induced intestinal injury in mice. Eight groups of mice were randomized as follows: control, GLZ (5, 10, and 25 mg/kg), IR (6 Gy), and IR + GLZ (at 5, 10, and 25 mg/kg). GLZ was administered to the mice for eight consecutive days, after which they were exposed to X-rays at a single dose of 6 Gy. After irradiation, biochemical parameters, immunohistochemical, and histological examinations were conducted on the ileum of the mice. IR exposure increased the levels of malondialdehyde and protein carbonyl, while glutathione levels, as oxidative stress biomarkers, decreased. Apoptosis in ileum tissues was also assessed. Furthermore, histopathological changes were observed in the irradiated mice. GLZ treatment significantly mitigated these changes. The administration of GLZ resulted in a marked decrease in caspase-3 immunoreactivity in the ileum of irradiated mice. This preclinical study exhibited that GLZ has a radioprotective effect against intestinal injury by inhibiting oxidative stress and apoptosis.

{"title":"Gliclazide protects ionizing radiation-induced intestinal injury in mice by inhibiting oxidative stress and caspase-3.","authors":"Soroush Arzani, Soghra Farzipour, Fereshteh Talebpour Amiri, Seyed Jalal Hosseinimehr","doi":"10.5114/bta.2024.145257","DOIUrl":"10.5114/bta.2024.145257","url":null,"abstract":"<p><p>Gliclazide (GLZ), an oral antihyperglycemic medication, has additional beneficial effects, such as anti-inflammatory and antioxidant properties, besides lowering blood glucose levels. In this study, the radio-protective effect of GLZ was evaluated against ionizing radiation (IR)-induced intestinal injury in mice. Eight groups of mice were randomized as follows: control, GLZ (5, 10, and 25 mg/kg), IR (6 Gy), and IR + GLZ (at 5, 10, and 25 mg/kg). GLZ was administered to the mice for eight consecutive days, after which they were exposed to X-rays at a single dose of 6 Gy. After irradiation, biochemical parameters, immunohistochemical, and histological examinations were conducted on the ileum of the mice. IR exposure increased the levels of malondialdehyde and protein carbonyl, while glutathione levels, as oxidative stress biomarkers, decreased. Apoptosis in ileum tissues was also assessed. Furthermore, histopathological changes were observed in the irradiated mice. GLZ treatment significantly mitigated these changes. The administration of GLZ resulted in a marked decrease in caspase-3 immunoreactivity in the ileum of irradiated mice. This preclinical study exhibited that GLZ has a radioprotective effect against intestinal injury by inhibiting oxidative stress and apoptosis.</p>","PeriodicalId":94371,"journal":{"name":"Biotechnologia","volume":"105 4","pages":"367-376"},"PeriodicalIF":0.0,"publicationDate":"2024-12-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11748219/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143026194","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Quercetin nanoparticles as a therapeutic approach: pharmacological actions and potential applications in therapy.
Pub Date : 2024-12-19 eCollection Date: 2024-01-01 DOI: 10.5114/bta.2024.145258
Reham Farouk El-Sayed Baiomy

The utilization of quercetin nanoparticles as a novel therapeutic strategy has garnered significant attention in recent years. These nanoparticles offer a unique approach to enhancing delivery and effectiveness while overcoming the drawbacks of quercetin. By exploiting the advantages of nanotechnology, such as increased stability and improved bioavailability, quercetin nanoparticles hold significant potential for developing innovative treatments across various medical fields. Quercetin nanoparticles have emerged as an indispensable component in numerous pharmaceutical and medicinal formulations. They are recognized for their anticancer, antitumor, anti-inflammatory, and antidiabetic properties, making them valuable in addressing allergic reactions, metabolic disorders, inflammatory disorders, cardiovascular diseases, and arthritis. From a pharmacological perspective, quercetin nanoparticles have demonstrated beneficial effects against Alzheimer's disease, primarily through their inhibitory impact on acetylcholinesterase. Furthermore, these nanoparticles have been scientifically documented to possess antioxidant, anticarcinogenic, hepatoprotective, and cytotoxic activities. This comprehensive review aims to explore the pharmacokinetics and biological activities associated with quercetin nanoparticles. It also highlights their potential as therapeutic agents in treating a wide range of diseases, including Alzheimer's disease, cancer, and neurodegenerative disorders.

{"title":"Quercetin nanoparticles as a therapeutic approach: pharmacological actions and potential applications in therapy.","authors":"Reham Farouk El-Sayed Baiomy","doi":"10.5114/bta.2024.145258","DOIUrl":"10.5114/bta.2024.145258","url":null,"abstract":"<p><p>The utilization of quercetin nanoparticles as a novel therapeutic strategy has garnered significant attention in recent years. These nanoparticles offer a unique approach to enhancing delivery and effectiveness while overcoming the drawbacks of quercetin. By exploiting the advantages of nanotechnology, such as increased stability and improved bioavailability, quercetin nanoparticles hold significant potential for developing innovative treatments across various medical fields. Quercetin nanoparticles have emerged as an indispensable component in numerous pharmaceutical and medicinal formulations. They are recognized for their anticancer, antitumor, anti-inflammatory, and antidiabetic properties, making them valuable in addressing allergic reactions, metabolic disorders, inflammatory disorders, cardiovascular diseases, and arthritis. From a pharmacological perspective, quercetin nanoparticles have demonstrated beneficial effects against Alzheimer's disease, primarily through their inhibitory impact on acetylcholinesterase. Furthermore, these nanoparticles have been scientifically documented to possess antioxidant, anticarcinogenic, hepatoprotective, and cytotoxic activities. This comprehensive review aims to explore the pharmacokinetics and biological activities associated with quercetin nanoparticles. It also highlights their potential as therapeutic agents in treating a wide range of diseases, including Alzheimer's disease, cancer, and neurodegenerative disorders.</p>","PeriodicalId":94371,"journal":{"name":"Biotechnologia","volume":"105 4","pages":"377-393"},"PeriodicalIF":0.0,"publicationDate":"2024-12-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11748223/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143026264","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Investigation of antioxidant, antimicrobial, and enzymatic properties of thermophilic cyanobacteria extracts.
Pub Date : 2024-12-19 eCollection Date: 2024-01-01 DOI: 10.5114/bta.2024.145253
Aytan Fataliyeva, Meral Yilmaz Cankilic, Nalan Yilmaz Sariozlu

Background: The present study investigated the antioxidant, antimicrobial, and partial enzymatic properties of 52 thermophilic cyanobacteria isolates in vitro.

Materials and methods: The DPPH scavenging method was applied to test the antioxidant potential of isolates' methanol extracts. Agar block diffusion and agar well diffusion methods were used to evaluate the antimicrobial activity and measured in milimeters. The measurement of enzyme activity was carried out by a modification of the agar block method by the growth of the cyanobacteria.

Results: Among the cyanobacterial extracts, strain 37 (0.78 ± 0.055 mg/ml) showed an IC50 value close to ascorbic acid (0.22 ± 0.04 mg/ml), indicating that it has a specific antioxidant source. Isolate G13 was shown to have the strongest antimicrobial activity against Micrococcus luteus NRRL B-4375 in the agar well diffusion method. In addition, the ability to produce enzymes was determined in isolate G1 (25 ± 5.66 mm), which had the highest cellulase activity at pH 8, and isolate K42 (22 ± 0.71 mm), which had the highest lipase activity at pH 7.

Conclusion: When percent inhibition and IC50 values were examined, it was found that cyanobacterial methanol extracts had moderate and low scavenging activity in comparison to the standard antioxidant ascorbic acid. In a study using the agar well diffusion method, the activity of cyanobacterial extracts against test bacteria was observed. In light of the results obtained, it is believed that the isolates exhibited lipase and cellulase (pH 7 and 8) enzyme activity at both pH levels and have potential for industrial use.

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引用次数: 0
First identification report for amino acid composition of red algae Gracilaria spp. obtained from Central Java, Indonesia.
Pub Date : 2024-12-19 eCollection Date: 2024-01-01 DOI: 10.5114/bta.2024.145254
Klara Kharisma Bunga Chandra, Tri Rini Nuringtyas, Tri Joko Raharjo

Gracilaria is a genus of red algae found mainly in Asia. Various species of Gracilaria are distributed throughout Indonesia's marine waters, especially in coastal areas, and are cultivated for research and economic purposes. Gracilaria mainly consists of polysaccharides and pigments, which have hindered protein identification. The unique protein expressions have never been analyzed using a proteomic approach, and no reports are available on Gracilaria spp. amino acid sequences in Central Java. Based on this background, we aimed to explore Gracilaria protein characterization using unique peptide sequence analysis via LC-HRMS. The usage of liquid chromatography coupled with high-resolution mass spectrometry (LC-HRMS) has been growing in biomedical and environmental sciences, offering high accuracy in protein detection. We followed the LC-HRMS standard protocol with an optimized precipitation procedure. TCA/acetone precipitation was used for protein purification, after which the precipitate was subjected to protein digestion to obtain small peptide fractions. Protein analysis results are presented as protein concentrations, molecular models, and peptide sequences. This experiment identified four sequences derived from the Rhodophyta database: TKKILDK (845.5455 Da), TVKSLLTK (889.5717 Da), ILVKTLK (814.5761 Da), and TGcGRSKR (921.4683 Da). This study reveals peptide sequences for Gracilaria spp., showing similarities with other red algae species, along with the functions of the peptide sequences. Furthermore, amino acid models of secondary structures were provided to support our findings.

{"title":"First identification report for amino acid composition of red algae <i>Gracilaria</i> spp. obtained from Central Java, Indonesia.","authors":"Klara Kharisma Bunga Chandra, Tri Rini Nuringtyas, Tri Joko Raharjo","doi":"10.5114/bta.2024.145254","DOIUrl":"10.5114/bta.2024.145254","url":null,"abstract":"<p><p><i>Gracilaria</i> is a genus of red algae found mainly in Asia. Various species of <i>Gracilaria</i> are distributed throughout Indonesia's marine waters, especially in coastal areas, and are cultivated for research and economic purposes. <i>Gracilaria</i> mainly consists of polysaccharides and pigments, which have hindered protein identification. The unique protein expressions have never been analyzed using a proteomic approach, and no reports are available on <i>Gracilaria</i> spp. amino acid sequences in Central Java. Based on this background, we aimed to explore <i>Gracilaria</i> protein characterization using unique peptide sequence analysis via LC-HRMS. The usage of liquid chromatography coupled with high-resolution mass spectrometry (LC-HRMS) has been growing in biomedical and environmental sciences, offering high accuracy in protein detection. We followed the LC-HRMS standard protocol with an optimized precipitation procedure. TCA/acetone precipitation was used for protein purification, after which the precipitate was subjected to protein digestion to obtain small peptide fractions. Protein analysis results are presented as protein concentrations, molecular models, and peptide sequences. This experiment identified four sequences derived from the Rhodophyta database: TKKILDK (845.5455 Da), TVKSLLTK (889.5717 Da), ILVKTLK (814.5761 Da), and TGcGRSKR (921.4683 Da). This study reveals peptide sequences for <i>Gracilaria</i> spp., showing similarities with other red algae species, along with the functions of the peptide sequences. Furthermore, amino acid models of secondary structures were provided to support our findings.</p>","PeriodicalId":94371,"journal":{"name":"Biotechnologia","volume":"105 4","pages":"325-335"},"PeriodicalIF":0.0,"publicationDate":"2024-12-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11748218/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143026193","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Newly developed genomic SSR markers revealed the population structure and genetic characteristics of abaca (Musa textilis Nee).
Pub Date : 2024-12-19 eCollection Date: 2024-01-01 DOI: 10.5114/bta.2024.145255
Mariecris Rizalyn R Mendoza, Antonio C Laurena, Maria Genaleen Q Diaz, Eureka Teresa M Ocampo, Tonette P Laude, Antonio G Lalusin

Abaca (Musa textilis Nee) is the primary source of manila hemp fiber, a vital industrial product for the country. Previous studies have relied on molecular markers designed for other Musa species or distant genera like rice, limiting accurate genetic characterization and germplasm conservation. To address this, we developed 50 genome-specific molecular markers based on the recently released whole genome sequence assembly of Abaca var. Abuab by Galvez et al. (2021). Among these markers, 28 showed high polymorphism, with an average PIC value of 0.78. Population analysis revealed a heterozygosity of 0.428, indicating moderate genetic diversity, supported by an alpha value of 0.0735 and an F stp value of 0.0815, which suggests moderate genetic differentiation among abaca accessions. Cluster analyses, generated by DARwin and STRUCTURE software with 91% similarity, identified four clusters. The new markers were also able to distinguish six Musa accessions exhibiting morphological traits of both abaca and banana. Discrepancies in sample identification due to identical or inverted names were resolved using population structure analysis. Molecular variance analysis showed a 12% variance among the four abaca subpopulations and 88% within populations, suggesting recent divergence. Our study highlights the diversity, identity, and genetic variation within the abaca collection using accurate, robust, cost-effective, and computationally simple genome-specific markers. These markers are pivotal for genetic studies of abaca, including traitmarker mapping and the differentiation of accessions even in the juvenile stage, when phenotypic differences may be subtle.

{"title":"Newly developed genomic SSR markers revealed the population structure and genetic characteristics of abaca (<i>Musa textilis</i> Nee).","authors":"Mariecris Rizalyn R Mendoza, Antonio C Laurena, Maria Genaleen Q Diaz, Eureka Teresa M Ocampo, Tonette P Laude, Antonio G Lalusin","doi":"10.5114/bta.2024.145255","DOIUrl":"10.5114/bta.2024.145255","url":null,"abstract":"<p><p>Abaca (<i>Musa textilis</i> Nee) is the primary source of manila hemp fiber, a vital industrial product for the country. Previous studies have relied on molecular markers designed for other <i>Musa</i> species or distant genera like rice, limiting accurate genetic characterization and germplasm conservation. To address this, we developed 50 genome-specific molecular markers based on the recently released whole genome sequence assembly of Abaca var. <i>Abuab</i> by Galvez et al. (2021). Among these markers, 28 showed high polymorphism, with an average PIC value of 0.78. Population analysis revealed a heterozygosity of 0.428, indicating moderate genetic diversity, supported by an alpha value of 0.0735 and an <i>F</i> <sub>stp</sub> value of 0.0815, which suggests moderate genetic differentiation among abaca accessions. Cluster analyses, generated by DARwin and STRUCTURE software with 91% similarity, identified four clusters. The new markers were also able to distinguish six <i>Musa</i> accessions exhibiting morphological traits of both abaca and banana. Discrepancies in sample identification due to identical or inverted names were resolved using population structure analysis. Molecular variance analysis showed a 12% variance among the four abaca subpopulations and 88% within populations, suggesting recent divergence. Our study highlights the diversity, identity, and genetic variation within the abaca collection using accurate, robust, cost-effective, and computationally simple genome-specific markers. These markers are pivotal for genetic studies of abaca, including traitmarker mapping and the differentiation of accessions even in the juvenile stage, when phenotypic differences may be subtle.</p>","PeriodicalId":94371,"journal":{"name":"Biotechnologia","volume":"105 4","pages":"337-353"},"PeriodicalIF":0.0,"publicationDate":"2024-12-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11748220/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143026263","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Investigation of CNS depressant and muscle relaxant effects of the ethnomedicinal plant Macropanax dispermus on Swiss Albino mice and its effect against oxidative stress. 民族药用植物大戟对瑞士白化小鼠中枢神经系统抑制和肌肉松弛作用的研究及其对氧化应激的影响
Pub Date : 2024-09-30 eCollection Date: 2024-01-01 DOI: 10.5114/bta.2024.141804
Syeda Rubaiya Afrin, Mohammad Rashedul Islam, Md Ashraful Alam, Ummah Tasnim Nisat, Bakul Akter, Mohammed Kamrul Hossain

Background and objective: Since plant-based natural drugs are widely accepted in modern times and possess numerous pharmacological effects with an extensive therapeutic range, an ethnomedicinal plant native to Bangladesh was selected to investigate for investigation of its various pharmacological effects. Macropanax dispermus has been traditionally used and has demonstrated numerous pharmacological effects in preclinical investigations. Therefore, this research aimed to assess the central nervous system (CNS) depressant and antioxidant activities of the crude methanol extracts of the stem barks (MDMS), leaves (MDML), and their different fractions.

Methods: The CNS depressant activity was assessed using the hole cross, rota-rod, and elevated plus maze tests on Swiss Albino mice, while the antioxidant activity was evaluated using the 2,2-diphenyl-1-picrylhydrazyl free radical, hydrogen peroxide (H2O2) nonradical scavenging, and ferric reducing power assays.

Results: The conducted assays successfully demonstrated that the chloroform fraction of MDML is a significantly (P < 0.001) effective CNS depressant, muscle relaxant, and anxiolytic agent with excellent antioxidative effects compared to standard and control. The aqueous fraction of MDML also acted as a significantly (P < 0.001) active CNS depressant and muscle relaxant, and it was a highly active ferric-reducing agent. All effects were dose and concentration-dependent.

Conclusion: The presence of various phytochemicals might contribute to these activities. However, further research is suggested to isolate their active compounds and evaluate their mechanisms of action.

背景和目的:由于以植物为基础的天然药物在现代已被广泛接受,并且具有多种药理作用和广泛的治疗范围,因此我们选择了一种原产于孟加拉国的民族药用植物来研究其各种药理作用。Macropanax dispermus 是一种传统的药用植物,在临床前研究中已证明其具有多种药理作用。因此,本研究旨在评估茎皮(MDMS)、叶片(MDML)及其不同馏分的粗甲醇提取物的中枢神经系统(CNS)抑制和抗氧化活性:中枢神经系统抑制活性通过对瑞士白化小鼠进行的孔十字试验、rota-rod试验和高架加迷宫试验进行评估,而抗氧化活性则通过2,2-二苯基-1-苦基肼自由基、过氧化氢(H2O2)非自由基清除和铁还原力试验进行评估:实验结果表明,与标准品和对照品相比,MDML 的氯仿馏分是一种有效的中枢神经系统抑制剂、肌肉松弛剂和抗焦虑剂,具有极佳的抗氧化效果(P < 0.001)。MDML 的水馏分也具有明显(P < 0.001)的中枢神经系统抑制和肌肉松弛活性,并且是一种高活性的铁还原剂。所有作用都与剂量和浓度有关:结论:各种植物化学物质的存在可能是产生这些活性的原因。结论:各种植物化学物质的存在可能是产生这些活性的原因之一,但还需要进一步研究,以分离其活性化合物并评估其作用机制。
{"title":"Investigation of CNS depressant and muscle relaxant effects of the ethnomedicinal plant <i>Macropanax dispermus</i> on Swiss Albino mice and its effect against oxidative stress.","authors":"Syeda Rubaiya Afrin, Mohammad Rashedul Islam, Md Ashraful Alam, Ummah Tasnim Nisat, Bakul Akter, Mohammed Kamrul Hossain","doi":"10.5114/bta.2024.141804","DOIUrl":"https://doi.org/10.5114/bta.2024.141804","url":null,"abstract":"<p><strong>Background and objective: </strong>Since plant-based natural drugs are widely accepted in modern times and possess numerous pharmacological effects with an extensive therapeutic range, an ethnomedicinal plant native to Bangladesh was selected to investigate for investigation of its various pharmacological effects. <i>Macropanax dispermus</i> has been traditionally used and has demonstrated numerous pharmacological effects in preclinical investigations. Therefore, this research aimed to assess the central nervous system (CNS) depressant and antioxidant activities of the crude methanol extracts of the stem barks (MDMS), leaves (MDML), and their different fractions.</p><p><strong>Methods: </strong>The CNS depressant activity was assessed using the hole cross, rota-rod, and elevated plus maze tests on Swiss Albino mice, while the antioxidant activity was evaluated using the 2,2-diphenyl-1-picrylhydrazyl free radical, hydrogen peroxide (H<sub>2</sub>O<sub>2</sub>) nonradical scavenging, and ferric reducing power assays.</p><p><strong>Results: </strong>The conducted assays successfully demonstrated that the chloroform fraction of MDML is a significantly (<i>P</i> < 0.001) effective CNS depressant, muscle relaxant, and anxiolytic agent with excellent antioxidative effects compared to standard and control. The aqueous fraction of MDML also acted as a significantly (<i>P</i> < 0.001) active CNS depressant and muscle relaxant, and it was a highly active ferric-reducing agent. All effects were dose and concentration-dependent.</p><p><strong>Conclusion: </strong>The presence of various phytochemicals might contribute to these activities. However, further research is suggested to isolate their active compounds and evaluate their mechanisms of action.</p>","PeriodicalId":94371,"journal":{"name":"Biotechnologia","volume":"105 3","pages":"249-261"},"PeriodicalIF":0.0,"publicationDate":"2024-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11492893/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142515776","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Investigation of the new substitution glycine to alanine within the Kringle-2 domain of reteplase: a molecular dynamics study. 研究网状血小板酶 Kringle-2 结构域中甘氨酸到丙氨酸的新取代:分子动力学研究。
Pub Date : 2024-09-30 eCollection Date: 2024-01-01 DOI: 10.5114/bta.2024.141801
Kaveh Haji-Allahverdipoor, Habib Eslami, Koosha Rokhzadi, Mokhtar Jalali Javaran, Sajad Rashidi Monfared, Mohamad Bagher Khademerfan

Background: Recombinant plasminogen activator (r-PA) consists of the Kringle-2 and protease domains of human tissue-type plasminogen. It is used clinically to treat coronary artery thrombosis and acute myocardial infarction. However, the expression and production of reteplase (r-PA) are limited due to its susceptibility to proteolysis during manufacturing processes. Therefore, efforts have been made to address this limitation.

Materials and methods: To enhance the conformational stability of r-PA and increase its resistance to proteolysis, we used Gly 6 Ala substitutions in the Kringle-2 domain through in silico . We created an in silico mutant collection with eight structures, incorporating four designated mutations (R103S, G39A, G53A, and G55A). Using MODELLER software and homology modeling, we developed three-dimensional structures for two Kringle-2 and tissue plasminogen activator protease domains, including the wild noncleavable form (R103S) and mutants with all four designated mutations. We assessed protein stability using a dynamic cross-correlation matrix by extracting global properties such as Root Mean Square Deviation (RMSD) and Root Mean Square Fluctuation (RMSF) from trajectory files.

Results: The findings revealed that a single glycine-alanine substitution (G39A) enhanced the conformational stability of r-PA, as evidenced by improvements in RMSD, RMSF, radius of gyration, surface accessibility, hydrogen bond formation, eigenvector projection, and density analysis.

Conclusion: The conformational stability of r-PA conferred by glycine replacement with alanine may decrease the propensity for proteolysis in protease - rich environments across various recombinant systems and potentially enhance its production and expression levels.

背景:重组纤溶酶原激活剂(r-PA)由人类组织型纤溶酶原的 Kringle-2 和蛋白酶结构域组成。它在临床上用于治疗冠状动脉血栓和急性心肌梗死。然而,由于其在生产过程中易被蛋白水解,再普酶(r-PA)的表达和生产受到限制。因此,人们一直在努力解决这一局限性:为了增强 r-PA 的构象稳定性并提高其抗蛋白酶解的能力,我们在 Kringle-2 结构域中使用了 Gly 6 Ala 的硅代。我们创建了一个具有八个结构的硅突变体集合,其中包含四个指定的突变(R103S、G39A、G53A 和 G55A)。利用 MODELLER 软件和同源建模,我们开发出了两个 Kringle-2 和组织纤溶酶原激活物蛋白酶结构域的三维结构,包括野生的不可裂解形式(R103S)和所有四个指定突变的突变体。通过从轨迹文件中提取均方根偏差(RMSD)和均方根波动(RMSF)等全局属性,我们利用动态交叉相关矩阵评估了蛋白质的稳定性:研究结果表明,单个甘氨酸-丙氨酸取代(G39A)增强了r-PA的构象稳定性,这体现在RMSD、RMSF、回旋半径、表面可及性、氢键形成、特征向量投影和密度分析等方面:用丙氨酸取代甘氨酸可赋予 r-PA 构象稳定性,这可能会降低各种重组系统在蛋白酶丰富的环境中的蛋白水解倾向,并有可能提高其生产和表达水平。
{"title":"Investigation of the new substitution glycine to alanine within the Kringle-2 domain of reteplase: a molecular dynamics study.","authors":"Kaveh Haji-Allahverdipoor, Habib Eslami, Koosha Rokhzadi, Mokhtar Jalali Javaran, Sajad Rashidi Monfared, Mohamad Bagher Khademerfan","doi":"10.5114/bta.2024.141801","DOIUrl":"https://doi.org/10.5114/bta.2024.141801","url":null,"abstract":"<p><strong>Background: </strong>Recombinant plasminogen activator (r-PA) consists of the Kringle-2 and protease domains of human tissue-type plasminogen. It is used clinically to treat coronary artery thrombosis and acute myocardial infarction. However, the expression and production of reteplase (r-PA) are limited due to its susceptibility to proteolysis during manufacturing processes. Therefore, efforts have been made to address this limitation.</p><p><strong>Materials and methods: </strong>To enhance the conformational stability of r-PA and increase its resistance to proteolysis, we used Gly 6 Ala substitutions in the Kringle-2 domain through <i>in silico</i> . We created an <i>in silico</i> mutant collection with eight structures, incorporating four designated mutations (R103S, G39A, G53A, and G55A). Using MODELLER software and homology modeling, we developed three-dimensional structures for two Kringle-2 and tissue plasminogen activator protease domains, including the wild noncleavable form (R103S) and mutants with all four designated mutations. We assessed protein stability using a dynamic cross-correlation matrix by extracting global properties such as Root Mean Square Deviation (RMSD) and Root Mean Square Fluctuation (RMSF) from trajectory files.</p><p><strong>Results: </strong>The findings revealed that a single glycine-alanine substitution (G39A) enhanced the conformational stability of r-PA, as evidenced by improvements in RMSD, RMSF, radius of gyration, surface accessibility, hydrogen bond formation, eigenvector projection, and density analysis.</p><p><strong>Conclusion: </strong>The conformational stability of r-PA conferred by glycine replacement with alanine may decrease the propensity for proteolysis in protease - rich environments across various recombinant systems and potentially enhance its production and expression levels.</p>","PeriodicalId":94371,"journal":{"name":"Biotechnologia","volume":"105 3","pages":"201-213"},"PeriodicalIF":0.0,"publicationDate":"2024-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11492890/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142515777","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Nanotechnology in cancer therapeutics, diagnosis, and management. 癌症治疗、诊断和管理中的纳米技术。
Pub Date : 2024-09-30 eCollection Date: 2024-01-01 DOI: 10.5114/bta.2024.141807
Disha Hazarika, Sumit Sarma, Priyanka Shankarishan

Nanotechnology presents an exciting opportunity in cancer research by offering significant advancements in therapies, diagnosis, and management. It possesses unparalleled potential to enhance the accuracy and effectiveness of cancer therapy while simultaneously reducing adverse effects, owing to its distinctive capability to manipulate matter at a molecular level. Using nanoparticle carriers has facilitated the precise administration of therapeutic agents to afflicted areas within the human body through customized drug delivery systems, resulting in improved treatment accuracy and efficacy while reducing adverse effects. These techniques improve drug solubility and stability, leading to elevated levels of biochemical availability and improved efficacy outcomes for patients with minimal negative effects during treatment cycles. Another use case for nanoparticles includes tumor imaging; functionalized with targeting ligands containing diagnostic agents, they foster early detection, making quicker remedial action plans possible. Overall, the incorporation of nanotechnology ensures a promising future, although it stresses the need to address regulatory hurdles and safety concerns before widespread clinical implementation. Despite the complexity of cancer research and patient care, nanotechnology shows promise in transforming both fields.

纳米技术在治疗、诊断和管理方面取得了重大进展,为癌症研究带来了令人振奋的机遇。由于纳米技术具有在分子水平操纵物质的独特能力,它在提高癌症治疗的准确性和有效性,同时减少不良反应方面具有无与伦比的潜力。使用纳米粒子载体有助于通过定制的给药系统将治疗药物精确地输送到人体内的患病部位,从而提高治疗的准确性和有效性,同时减少不良反应。这些技术提高了药物的溶解度和稳定性,从而提高了生化可用性水平,改善了患者的疗效,并将治疗周期中的负面影响降至最低。纳米粒子的另一个用途包括肿瘤成像;纳米粒子与含有诊断剂的靶向配体功能化,可促进早期检测,使更快的补救行动计划成为可能。总之,纳米技术的应用前景广阔,但在广泛临床应用之前,还需要解决监管障碍和安全问题。尽管癌症研究和病人护理工作十分复杂,但纳米技术有望改变这两个领域。
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引用次数: 0
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