scholarly journals Bioprospecting of Sechium spp. varieties for the selection of characters with pharmacological activity

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
María Isabel Iñiguez-Luna ◽  
Jorge Cadena-Iñiguez ◽  
Ramón Marcos Soto-Hernández ◽  
Francisco Javier Morales-Flores ◽  
Moisés Cortes-Cruz ◽  
...  

AbstractBioprospecting identifies new sources of compounds with actual or potential economic value that come from biodiversity. An analysis was performed regarding bioprospecting purposes in ten genotypes of Sechium spp., through a meta-analysis of 20 information sources considering different variables: five morphological, 19 biochemical, anti-proliferative activity of extracts on five malignant cell lines, and 188 polymorphic bands of amplified fragment length polymorphisms, were used in order to identify the most relevant variables for the design of genetic interbreeding. Significant relationships between morphological and biochemical characters and anti-proliferative activity in cell lines were obtained, with five principal components for principal component analysis (SAS/ETS); variables were identified with a statistical significance (< 0.7 and Pearson values ≥ 0.7), with 80.81% of the accumulation of genetic variation and 110 genetic bands. Thirty-nine (39) variables were recovered using NTSYSpc software where 30 showed a Pearson correlation (> 0.5) and nine variables (< 0.05), Finally, using a cladistics analysis approach highlighted 65 genetic bands, in addition to color of the fruit, presence of thorns, bitter flavor, piriform and oblong shape, and also content of chlorophylls a and b, presence of cucurbitacins, and the IC50 effect of chayote extracts on the four cell lines.

Author(s):  
Michaela Beranová ◽  
Marcela Basovníková ◽  
Dana Martinovičová

The modern indicators of the performance of business entity are based on an economic conception of profit. It means that alternative costs and risks are taken into account in construction of these indicators. Moreover, the modern indicators would also enable to clearly and digestedly identify the links on each level of management, and therefore to support the value-based management. The one of these modern indicators is Economic Value Added. This indicator has been introduced by Stewart Stern & Co. in the early nineties. As some Czech authors state (e.g. Synek, 2007), domestic alternative of the EVA indicator are the IN indexes which has been developing since the middle of the nineties as overall indexes of company’s financial health especially because the indexes coming from abroad had not a good differentiation ability with regard to specifics of the Czech economic environment. The objective of this article is to define the relations between the values of EVA indicator and the values of the index IN 99 while the analysis is focused on agricultural companies of mixed farming. The authors base their work on differences in constructions of these two indicators and on ­differences in interpretations of their results. Primarily, basic correlation of values of these indicators has been observed. The calculation of Pearson correlation coefficient has been applied on the set of fifty business entities, and the calculated result of 0.669 shows relatively stronger linear dependence. Consequent test has verified a statistical significance of this dependence. Then in this article, the authors are focused on causations of this dependence which is rather strong in spite of a different logic of these two indicators. Other consequences of overall view on company’s economic performance are discussed in the article as well.


2003 ◽  
Vol 285 (1) ◽  
pp. G12-G19 ◽  
Author(s):  
D. Sun ◽  
Y. Gong ◽  
H. Kojima ◽  
G. Wang ◽  
E. Ravinsky ◽  
...  

Increasing hepatocyte membrane potentials by augmenting GABAergic activity inhibits nonmalignant hepatocyte proliferative activity. The objectives of this study were to document 1) potential differences (PDs) of four malignant hepatocyte cell lines, 2) GABAA receptor mRNA expression in the same cell lines, and 3) effects of restoring malignant hepatocyte PDs to levels approximating those of resting, nonmalignant hepatocytes. Hepatocyte PDs were documented in nonmalignant and malignant (Chang, HepG2, HuH-7, and PLC/PRF/5) hepatocytes with a fluorescent voltage-sensitive dye and GABAA receptor expression by RT-PCR and Western blot analyses. Compared with nonmalignant human hepatocytes, all four malignant cell lines were significantly depolarized ( P < 0.0001, respectively). Only PLC/PRF/5 cells had detectable GABAA-β3 receptor mRNA expression and all cell lines were negative for GABAA-β3 receptor protein by Western blot analysis. Stable transfection of Chang cells with GABAA-β3 receptor cDNA resulted in significant increases in PD and decreases in proliferative activity as manifest by decreased [3H]thymidine and bromodeoxyurieine incorporation rates, 4-[3-(4-lodophenyl)-2-(4-nitrophenyl)-2H-5-tetrazolio]-1,3-benzene disulfonate activity, a lower mitotic index, prolongation of cell-doubling times, and attenuated growth patterns compared with cells transfected with vector alone. Colony formation in soft agar and the number of abnormal mitoses were also significantly decreased in GABAA-β3 receptor transfected cells. The results of this study indicate 1) relative to healthy hepatocytes, malignant hepatocytes are significantly depolarized, 2) GABAA-β3 receptor expression is absent in malignant hepatocyte cell lines, and 3) increasing the PD of malignant hepatocytes is associated with less proliferative activity and a loss of malignant features.


Author(s):  
Novikova ◽  
SP Romanenko ◽  
MA Lobkis

Introduction: In the Russian Federation, much attention is traditionally paid to military education and training. A special place in its structure is occupied by the system of cadet classes and corps. A distinctive feature of the learning mode in such institutions is a combined effect of standard and specific factors of indoor school environment and intensive physical activity owing to sports, applied military and drill training. No evidence-based methods of establishing nutrient requirements of children in modern conditions of cadet corps have been developed so far, which predetermines the potential of transforming nutrition from a health-saving factor into a health risk factor. Our objective was to provide a scientific substantiation of the model of healthy nutrition for students of cadet-type educational establishments. Methods: The statistical significance of the correlation was evaluated using the Student’s t-test. Correlation and regression analyses were used to assess cause-and-effect relationships. The Pearson correlation coefficient (rxy) was used as an indicator of the strength of the relationship between quantitative indicators x and y, both having a normal distribution. Correlation coefficient (rxy) values were interpreted in accordance with the Chaddock scale. For the purpose of statistical modeling, the method of multiple linear regressions was used. Conclusions: We substantiated the innovative model of organizing healthy nutrition for students of cadet-type schools based on the correlation and regression analyses with determination of statistical significance of the studied characteristics. Its efficiency indicators include an increase in average functional capabilities of students by more than 10 % and a reduction in the probability of developmental disorders by more than 25 %.


2020 ◽  
Vol 17 (5) ◽  
pp. 563-573 ◽  
Author(s):  
Chandrakant Dhondiram Pawar ◽  
Dattatraya Navnath Pansare ◽  
Devanand Baburao Shinde

Background: Thiophene ring forms important building block in medicinal chemistry. Literature reveals that thiophene ring in combination with different groups shows different activity. By keeping these things in mind we have designed and synthesized a new series of amide and sulfonamide coupled thiophene. A series of novel substituted 3-sulfamoylbenzo[b]thiophene-4- carboxamide molecules containing sulfonamide and amide group were designed, synthesized and used for anti-proliferative activity study. Methods: The final compounds 16-36 were synthesized by using series of reactions comprising sulfonation, sulfonamide coupling, hydrolysis and peptide coupling. The yields of compounds 16- 36 are in the range of 90-98%. The structures of the synthesized compounds were elucidated and confirmed by 1H NMR, 13C NMR, LCMS and the purity was checked through HPLC analysis. The compounds were further tested for their in vitro anticancer activity against a series of cell lines A549, HeLa, MCF-7 and Du-145. Results: The intermediates 8-13, 15 and final compounds 16-36 were synthesized in good yields. The synthesized compounds were further tested for their anticancer activity and most of compounds showed moderate to good anticancer activity against all four cell lines. Conclusion: We have synthesized 21 compounds and were screened for anticancer activity against MCF-7, HeLa, A-549 and Du-145 cancer cell lines. Most of the compounds were active for tested cell lines with IC50 value in the range of 1.81 to 9.73 μM. The compounds 18, 19, 21, 25, 30, 31 and 33 are most active in cell line data with IC50 value in the range of 1.81 to 2.52 μM.


2020 ◽  
Vol 20 (10) ◽  
pp. 1209-1220
Author(s):  
Rafat M. Mohareb ◽  
Ensaf S. Alwan

Background: Recently tetrahydrobenzo[b]thiazole derivatives acquired a special attention due to their wide range of pharmacological activities especially the therapeutic activities. Through the market it was found that many pharmacological drugs containing the thiazole nucleus were known. Objective: This work aimed to synthesize target molecules not only possess anti-tumor activities but also kinase inhibitors. The target molecules were obtained starting from the arylhydrazonocyclohexan-1,3-dione followed by their heterocyclization reactions to produce anticancer target molecules. Methods: The arylhydrazone derivatives 3a-c underwent different heterocyclization reactions to produce thiophene, thiazole, pyrazole and 1,2,4-triazine derivatives. The anti-proliferative activity of twenty six compounds among the synthesized compounds toward the six cancer cell lines namely A549, H460, HT-29, MKN-45, U87MG, and SMMC-7721 was studied. Results: Anti-proliferative evaluations, tyrosine and Pim-1 kinase inhibitions were perform for most of the synthesized compounds where the varieties of substituent through the aryl ring and the thiophene moiety afforded compounds with high activities. Conclusion: The compounds with high anti-proliferative activity towards the cancer cell lines showed that compounds 3b, 3c, 5e, 5f, 8c, 9c, 11c, 12c, 14e, 14f and 16c were the most cytotoxic compounds. Further tests of the latter compounds toward the five tyrosine kinases c-Kit, Flt-3, VEGFR-2, EGFR, and PDGFR and Pim-1 kinase showed that compounds 3c, 5e, 5f, 8c, 9c, 12c, 14e, 14f and 16c were the most potent of the tested compounds toward the five tyrosine kinases and compounds 6d, 11a, 20b and 21e were of the highest inhibitions towards Pim-1 kinase. Pan Assay Interference Compounds (PAINS) for the most cytotoxic compounds showed zero PAINS alert and can be used as lead compounds.


2021 ◽  
Vol 20 (1) ◽  
Author(s):  
Yuan-Yuan Gong ◽  
Hai-Ying Peng

Abstract Background To investigate the correlation between the thickness of epicardial adipose tissue (EAT), C-reactive protein (CRP), interleukin (IL) -6, visfatin, juxtaposed with another zinc finger protein 1 (JAZF1) and type 2 diabetic mellitus (T2DM) macroangiopathy. Methods The study enrolled 82 patients with T2DM with macroangiopathy (the Complication Group), and 85 patients with T2DM (the Diabetes Group) who were admitted to Shandong Provincial Third Hospital from February 2018 to February 2020. In addition, 90 healthy people who underwent physical examination at the same hospital during the same period were enrolled (the Healthy Control Group). Age, gender, height, weight, waist circumference (WC), hip circumference (HC), diabetic course and therapeutic drugs, waist hip ratio (WHR), and body mass index (BMI) were recorded and calculated. Results The baseline characteristics of the three groups were comparable, and the diabetic course of the Complication Group and the Diabetes Group was not significantly different (P > 0.05). The WHR of the Complication Group was higher than that of the Diabetes Group and the Healthy Control Group, with statistical significance (P < 0.05). The FPG, 2hPG, HbA1C, CRP, IL-6, Visfatin, JAZF1, HOMA-IR, EAT thickness, and baPWV of the Complication Group were all higher than those of the Diabetes Group and the Healthy Control Group (P < 0.05, respectively). The JAZF1 and FIns of the Complication Group and Diabetes Group were lower than those of the Healthy Control Group, and JAZF1 of the Complication Group was lower than the Diabetes Group with statistical significance (P<0.05, respectively). Pearson correlation analysis showed that the EAT thickness was positively correlated with CRP, IL-6, visfatin, and JAZF1 (r = 0.387, 0.451, 0.283, 0.301, respectively, all P<0.001). Pearson correlation analysis showed that baPWV was positively correlated with EAT thickness, CRP, IL-6, visfatin, and JAZF1 (r = 0.293, 0.382, 0.473, 0.286, respectively, all P < 0.001). Multivariate stepwise regression analysis showed that FPG, 2hPG, HbA1C, CRP, IL-6, visfatin, JAZF1, and EAT thickness were independent risk factors that affected T2DM macroangiopathy. Conclusions Clinical monitoring and treatment of T2DM macroangiopathy can use CRP, IL-6, Visfatin, JAZF1, and EAT thickness as new targets to delay the progression of the disease. Further research on the relationship between the above factors and the pathogenesis of T2DM macroangiopathy may be helpful provide new treatment strategies.


Vascular ◽  
2021 ◽  
pp. 170853812199127
Author(s):  
Lixin Wang ◽  
Enci Wang ◽  
Fei Liu ◽  
Wei Zhang ◽  
Xiaolong Shu ◽  
...  

Objective This systematic review and meta-analysis evaluated the published data on the efficacy and safety of therapies for superior mesenteric venous thrombosis (SMVT), aiming to provide a reference and set of recommendations for clinical treatment. Methods Relevant databases were searched for studies published from 2000 to June 2020 on SMVT treated with conservative treatment, surgical treatment, or endovascular approach. Different treatment types were grouped for analysis and comparison, and odds ratios with corresponding 95% confidence intervals were calculated. The outcomes were pooled using meta-analytic methods and presented by forest plots. Results Eighteen articles, including eight on SMVT patients treated with endovascular therapies, were enrolled. The treatment effectiveness was compared between different groups according to the change of symptoms, the occurrence of complications, and mortality as well. The conservative treatment group had better efficacy compared to the surgery group (89.0% vs. 78.6%, P <0.05), and the one-year survival rate was also higher (94.4% vs. 80.0%, P >0.05), but without statistical significance. As for endovascular treatment, the effectiveness was significantly higher than the surgery group (94.8% vs. 75.2%, P <0.05), and the conservative treatment group as well (93.3% vs. 86.3%, P >0.05), which still requires further research for the lack of statistical significance. Conclusions Present findings indicate that anticoagulation, as conservative treatment should be the preferred clinical option in the clinic for SMVT, due to its better curative effect compared to other treatment options, including lower mortality, fewer complications, and better prognosis. Moreover, endovascular treatment is a feasible and promising approach that is worth in-depth research, for it is less invasive than surgery and has relatively better effectiveness, thus can provide an alternative option for SMVT treatment and may be considered as a reliable method in clinical.


2021 ◽  
Vol 13 (12) ◽  
pp. 6910
Author(s):  
Adil Dilawar ◽  
Baozhang Chen ◽  
Arfan Arshad ◽  
Lifeng Guo ◽  
Muhammad Irfan Ehsan ◽  
...  

Here, we provided a comprehensive analysis of long-term drought and climate extreme patterns in the agro ecological zones (AEZs) of Pakistan during 1980–2019. Drought trends were investigated using the standardized precipitation evapotranspiration index (SPEI) at various timescales (SPEI-1, SPEI-3, SPEI-6, and SPEI-12). The results showed that droughts (seasonal and annual) were more persistent and severe in the southern, southwestern, southeastern, and central parts of the region. Drought exacerbated with slopes of −0.02, −0.07, −0.08, −0.01, and −0.02 per year. Drought prevailed in all AEZs in the spring season. The majority of AEZs in Pakistan’s southern, middle, and southwestern regions had experienced substantial warming. The mean annual temperature minimum (Tmin) increased faster than the mean annual temperature maximum (Tmax) in all zones. Precipitation decreased in the southern, northern, central, and southwestern parts of the region. Principal component analysis (PCA) revealed a robust increase in temperature extremes with a variance of 76% and a decrease in precipitation extremes with a variance of 91% in the region. Temperature and precipitation extremes indices had a strong Pearson correlation with drought events. Higher temperatures resulted in extreme drought (dry conditions), while higher precipitation levels resulted in wetting conditions (no drought) in different AEZs. In most AEZs, drought occurrences were more responsive to precipitation. The current findings are helpful for climate mitigation strategies and specific zonal efforts are needed to alleviate the environmental and societal impacts of drought.


2021 ◽  
Vol 11 (7) ◽  
pp. 677
Author(s):  
Jeong Yee ◽  
Hamin Kim ◽  
Yunhee Heo ◽  
Ha-Young Yoon ◽  
Gonjin Song ◽  
...  

Purpose: Cytochrome P450 (CYP) is involved in the metabolism of statins; CYP3A5 is the main enzyme responsible for lipophilic statin metabolism. However, the evidence of the association between CYP3A5*3 polymorphism and the risk of statin-induced adverse events remains unclear. Therefore, this study aimed to perform a systematic review and meta-analysis to investigate the relationship between the CYP3A5*3 polymorphism and the risk of statin-induced adverse events. Methods: The PubMed, Web of Science, and EMBASE databases were searched for qualified studies published until August 2020. Observational studies that included the association between statin-induced adverse events and the CYP3A5*3 polymorphism were reviewed. The odds ratios (ORs) and 95% confidence intervals (CIs) were evaluated to assess the strength of the relationship. The Mantel–Haenszel method was used to provide the pooled ORs. Heterogeneity was estimated with I2 statistics and publication bias was determined by Begg’s and Egger’s test of the funnel plot. Data analysis was performed using Review Manager (version 5.4) and R Studio (version 3.6). Results: In total, data from 8 studies involving 1614 patients were included in this meta-analysis. The CYP3A5*3 polymorphism was found to be associated with the risk of statin-induced adverse events (*3/*3 vs. *1/*1 + *1/*3: OR = 1.40, 95% CI = 1.08–1.82). For myopathy, the pooled OR was 1.30 (95% CI: 0.96–1.75). The subgroup analysis of statin-induced myopathy revealed a trend, which did not achieve statistical significance. Conclusions: This meta-analysis demonstrated that the CYP3A5*3 polymorphism affected statin-induced adverse event risk. Therefore, CYP3A5 genotyping may be useful to predict statin toxicity.


Sign in / Sign up

Export Citation Format

Share Document