Establishment of evaluation criteria for the development of high quality ERα-targeted fluorescent probes

The Analyst ◽  
2020 ◽  
Vol 145 (18) ◽  
pp. 5989-5995
Author(s):  
Qiuyu Meng ◽  
Xiaoyu Ma ◽  
Baohua Xie ◽  
Xiaofei Deng ◽  
Jian Huang ◽  
...  
Keyword(s):  
Fluorescent Probes ◽  
Evaluation Criteria ◽  
High Quality ◽  
First Time ◽  
Mcf 7

ERα targeting fluorescent probes are important tools for ERα study. Two ERα targeting fluorescent probes were developed, which exhibited better performance in MCF-7 cells. Moreover, the probes were used for the first time to study the ERα motion.

Disability as a social phenomenon

2020 ◽  
pp. 22-38
Author(s):  
Natalia Guseva ◽  
Vitaliy Berdutin
Keyword(s):  
Social Protection ◽  
Russian Society ◽  
Stage Model ◽  
High Quality ◽  
Rehabilitation Programs ◽  
Current State ◽  
The Social ◽  
Consistent Solution ◽  
First Time

At present, the problem of establishing disability is a point at issue in Russia. Despite the fact that medical criteria for disability are being developed very actively, high-quality methods for assessing social hallmarks are still lacking. Since disability is a phenomenon inherent in any society, each state forms a social and economic policy for people with disabilities in accordance with its level of development, priorities and opportunities. We have proposed a three-stage model, which includes a system for the consistent solution of the main tasks aimed at studying the causes and consequences of the problems encountered today in the social protection of citizens with health problems. The article shows why the existing approaches to the determination of disability and rehabilitation programs do not correspond to the current state of Russian society and why a decrease in the rate of persons recognized as disabled for the first time does not indicate an improvement in the health of the population. The authors proposed a number of measures with a view to correcting the situation according to the results of the study.

Antitumoral and Anticholinesterasic Activities of the Seven Species from Rubiaceae

2019 ◽  
Vol 20 (4) ◽  
pp. 302-308 ◽  
Author(s):  
Carla R.F. Volobuff ◽  
Pedro C.O. Junior ◽  
Sidney M. dos Santos ◽  
Zefa V. Pereira ◽  
Diego C. Ferreira ◽  
...  
Keyword(s):  
Wistar Rats ◽  
Biological Activities ◽  
Brain Structures ◽  
Acetylcholinesterase Inhibition ◽  
Mato Grosso ◽  
Male Wistar Rats ◽  
First Time ◽  
Mato Grosso Do Sul ◽  
Antiproliferative Activities ◽  
Mcf 7

Background: The genus Psychotria and Palicourea are reported as a source of alkaloids and iridoids, which exhibit biological activities. This study aimed to evaluate antiproliferative and anticholinesterase activities and quantification of the alkaloids of seven species among the genus found in Mato Grosso do Sul region in Brazil. Methods: Concentrations of alkaloids were measured spectrophotometrically. The extracts were submitted to antiproliferative activity against ten cell lines. The anticholinesterase activity of the extracts was developed using brain structures of male Wistar rats: cerebral cortex, hippocampus, hypothalamus and striatum by the Ellman method. Results: Alkaloids from Psychotria and Palicourea species were quantified which showed values of 47.6 to 21.9 µg/g. Regarding the antiproliferative potential, Palicourea crocea demonstrated selectivity against the 786-0 cell line (GI50: 22.87 µg/mL). Psychotria leiocarpa inhibited cell growth against OVCAR-3 (GI50: 3.28 µg/mL), K-562 (GI50: 5.26 µg/mL), HaCaT (GI50: 27.20 µg/mL), PC-3 (GI50: 34.92 µg/mL), MCF-7 (GI50: 35.80 µg/mL) and P. capillacea showed activity against OVCAR-3 (GI50: 2.33 µg/ml) and U251 (GI50: 16.66 µg/ml). The effect of acetylcholinesterase inhibition was more effective in the hippocampus, demonstrating inhibition for Paliourea crocea, Psychotria deflexa, P. brachybotrya and P. leiocarpa of 70%, 57%, 50% and 40%, respectively, followed by P. poeppigiana and P. capillacea, inhibiting 21%, compared to the control. Conclusion: Herein, the present work showed for the first time, anticholinesterasic and antiproliferative activities of extracts of Palicourea and Psychotria seem to be mainly associated with the levels of alkaloids in the leaves of these species.

scholarly journals Bufadienolides from the Skin Secretions of the Neotropical Toad Rhinella alata (Anura: Bufonidae): Antiprotozoal Activity against Trypanosoma cruzi

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4217
Author(s):  
Candelario Rodriguez ◽  
Roberto Ibáñez ◽  
Luis Mojica ◽  
Michelle Ng ◽  
Carmenza Spadafora ◽  
...  
Keyword(s):  
Vero Cells ◽  
Chemical Diversity ◽  
Hydroxyl Group ◽  
Antitrypanosomal Activity ◽  
The Family ◽  
Toad Venom ◽  
Skin Secretions ◽  
Pharmacological Potential ◽  
First Time ◽  
Mcf 7

Toads in the family Bufonidae contain bufadienolides in their venom, which are characterized by their chemical diversity and high pharmacological potential. American trypanosomiasis is a neglected disease that affects an estimated 8 million people in tropical and subtropical countries. In this research, we investigated the chemical composition and antitrypanosomal activity of toad venom from Rhinella alata collected in Panama. Structural determination using mass spectrometry (MS) and nuclear magnetic resonance (NMR) spectroscopy led to the identification of 10 bufadienolides. Compounds identified include the following: 16β-hydroxy-desacetyl-bufotalin-3-adipoyl-arginine ester (1), bufotalin (2), 16β-hydroxy-desacetyl-bufotalin-3-pimeloyl-arginine ester (3), bufotalin-3-pimeloyl-arginine ester (4), 16β-hydroxy-desacetyl-bufotalin-3-suberoyl-arginine ester (5), bufotalin-3-suberoyl-arginine ester (6), cinobufagin-3-adipoyl-arginine ester (7), cinobufagin-3-pimeloyl-arginine ester (8), cinobufagin-3-suberoyl-arginine ester (9), and cinobufagin (10). Among these, three new natural products, 1, 3, and 5, are described, and compounds 1–10 are reported for the first time in R. alata. The antitrypanosomal activity assessed in this study revealed that the presence of an arginyl-diacid attached to C-3, and a hydroxyl group at C-14 in the structure of bufadienolides that is important for their biological activity. Bufadienolides showed cytotoxic activity against epithelial kidney Vero cells; however, bufagins (2 and 10) displayed low mammalian cytotoxicity. Compounds 2 and 10 showed activity against the cancer cell lines MCF-7, NCI-H460, and SF-268.

Precursor engineering for high-quality Cs2AgBiBr6 films toward efficient lead-free double perovskite solar cells

2021 ◽  
Author(s):  
Ping Hou ◽  
Wenxiang Yang ◽  
Ning Wan ◽  
Zhi Fang ◽  
Jinju Zheng ◽  
...  
Keyword(s):  
Solar Cells ◽  
Perovskite Solar Cells ◽  
Control Sample ◽  
Double Perovskite ◽  
Lead Free ◽  
High Quality ◽  
Precursor Engineering ◽  
First Time

We report a facile BiBr3(DMSO)2 adduct process to produce high-quality Cs2AgBiBr6 films with large grains for the first time, which leads to an enhancement of over 40% on the PCE of Cs2AgBiBr6-based solar cells compared to that of the control sample.

scholarly journals Chemical Constituents of the Marine Sponge Aaptos aaptos (Schmidt, 1864) and Their Cytotoxic Activity

2021 ◽  
Vol 16 (2) ◽  
pp. 1934578X2199334
Author(s):  
Do Thi Trang ◽  
Bui Huu Tai ◽  
Dan Thuy Hang ◽  
Pham Hai Yen ◽  
Phan Thi Thanh Huong ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Spectral Data ◽  
Absolute Configuration ◽  
Marine Sponge ◽  
Chemical Constituents ◽  
2D Nmr ◽  
Extensive Analysis ◽  
First Time ◽  
Tddft Method ◽  
Mcf 7

Seven compounds (1-7) were isolated from the marine sponge Aaptos aaptos living in the Vietnamese sea. Their structures were determined as 2 hours, 5 H,7 H,9 H-9 S-hydroxy-imidazo[1,5- α]pyridine-1,3-dione (1), 3-([9-methylhexadecyl]oxy)propane-1,2-diol 2, 2,3-dihydro-2,3-dioxoaaptamine (3), indol-3-aldehyde (4), methyl indole-3-carboxylate (5) 4-hydroxy-5-(indole-3-yl)−5-oxo-pentan-2-one (6), and thymidine (7) by extensive analysis of HR-ESI-MS, 1D, and 2D NMR spectral data, as well as by comparison of the spectral data with those reported in the literature. In addition, the absolute configuration of 1 was determined from the experimental ECD spectrum and comparison of this with the theoretical ECD calculations using the TDDFT method. Compounds 1 and 2 were isolated from nature for the first time. Compound 3 induced cytotoxic activity against SK-LU-1, MCF-7, HepG2, and SK-Mel-2 cell lines with IC50 values of 41.27 ± 2.63, 40.70 ± 2.65, 34.31 ± 3.43, and 36.63 ± 1.40 µM, respectively.

scholarly journals A Novel and Efficient High-Yield Method for Preparing Bacterial Ghosts

Toxins ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 420
Author(s):  
Yi Ma ◽  
Liu Cui ◽  
Meng Wang ◽  
Qiuli Sun ◽  
Kaisheng Liu ◽  
...  
Keyword(s):  
Large Scale ◽  
Expression System ◽  
High Yield ◽  
Wild Type ◽  
High Quality ◽  
Efficient Protection ◽  
Bacterial Ghosts ◽  
Cell Envelopes ◽  
Extracellular Structures ◽  
First Time

Bacterial ghosts (BGs) are empty cell envelopes possessing native extracellular structures without a cytoplasm and genetic materials. BGs are proposed to have significant prospects in biomedical research as vaccines or delivery carriers. The applications of BGs are often limited by inefficient bacterial lysis and a low yield. To solve these problems, we compared the lysis efficiency of the wild-type protein E (EW) from phage ΦX174 and the screened mutant protein E (EM) in the Escherichia coli BL21(DE3) strain. The results show that the lysis efficiency mediated by protein EM was improved. The implementation of the pLysS plasmid allowed nearly 100% lysis efficiency, with a high initial cell density as high as OD600 = 2.0, which was higher compared to the commonly used BG preparation method. The results of Western blot analysis and immunofluorescence indicate that the expression level of protein EM was significantly higher than that of the non-pLysS plasmid. High-quality BGs were observed by SEM and TEM. To verify the applicability of this method in other bacteria, the T7 RNA polymerase expression system was successfully constructed in Salmonella enterica (S. Enterica, SE). A pET vector containing EM and pLysS were introduced to obtain high-quality SE ghosts which could provide efficient protection for humans and animals. This paper describes a novel and commonly used method to produce high-quality BGs on a large scale for the first time.

scholarly journals Unraveling the long-pursued Au144 structure by x-ray crystallography

2018 ◽  
Vol 4 (10) ◽  
pp. eaat7259 ◽  
Author(s):  
Nan Yan ◽  
Nan Xia ◽  
Lingwen Liao ◽  
Min Zhu ◽  
Fengming Jin ◽  
...  
Keyword(s):  
Metal Nanoparticles ◽  
Weak Interactions ◽  
Gold Nanoclusters ◽  
Atomic Level ◽  
High Quality ◽  
X Ray ◽  
X Ray Crystallography ◽  
Quantum Size ◽  
First Time

The transition from nanocluster to nanocrystal is a central issue in nanoscience. The atomic structure determination of metal nanoparticles in the transition size range is challenging and particularly important in understanding the quantum size effect at the atomic level. On the basis of the rationale that the intra- and interparticle weak interactions play critical roles in growing high-quality single crystals of metal nanoparticles, we have reproducibly obtained ideal crystals of Au144(SR)60 and successfully solved its structure by x-ray crystallography (XRC); this structure was theoretically predicted a decade ago and has long been pursued experimentally but without success until now. Here, XRC reveals an interesting Au12 hollow icosahedron in thiolated gold nanoclusters for the first time. The Au–Au bond length, close to that of bulk gold, shows better thermal extensibility than the other Au–Au bond lengths in Au144(SR)60, providing an atomic-level perspective because metal generally shows better thermal extensibility than nonmetal materials. Thus, our work not only reveals the mysterious, long experimentally pursued structure of a transition-sized nanoparticle but also has important implications for the growth of high-quality, single-crystal nanoparticles, as well as for the understanding of the thermal extensibility of metals from the perspective of chemical bonding.

scholarly journals Labdane and Abietane Diterpenoids from Juniperus oblonga and Their Cytotoxic Activity

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1561 ◽  
Author(s):  
Qiao ◽  
Khutsishvili ◽  
Alizade ◽  
Atha ◽  
Borris
Keyword(s):  
Cell Lines ◽  
Human Tumor ◽  
2D Nmr ◽  
Human Tumor Cell Lines ◽  
Abietane Diterpenoids ◽  
Whole Plant ◽  
Phytochemical Investigation ◽  
Ic50 Values ◽  
First Time ◽  
Mcf 7

A phytochemical investigation of the whole plant of Juniperus oblonga led to the isolationof one previously undescribed labdane diterpenoid, (4R,5S,9S,10R)‐13‐des‐ethyl‐13‐oxolabda‐8(17),11E‐dien‐19‐oic acid (1), together with nine known diterpenoids (2–3, 6–12), two lignans (4, 5),and a coumarin (13). The structures of all the compounds were elucidated on the basis ofspectrometric data, primarily one‐dimensional (1D)‐ and two‐dimensional (2D)‐NMR and massspectrometry. Electronic circular dichroism (ECD) calculations determined the absoluteconfiguration of 1. In addition, the isolated compounds were evaluated for their cytotoxic activityagainst three human tumor cell lines (HepG2, MCF‐7, and HeLa). 6,12‐Dihydroxyabieta‐5,8,11,13‐tetraen‐7‐one (6) showed moderate cytotoxicity against all three cell lines with IC50 values rangingfrom 24.41 μM to 58.39 μM and trilobinone (10) showed weaker activity with IC50 values rangingfrom 56.93 μM to 79.98 μM. None of the isolated diterpenoids have been previously reported fromJuniperus oblonga, and five compounds are here reported from the genus Juniperus for the first time.

scholarly journals PHYTOCHEMICAL SCREENING AND BIOLOGICAL EVALUATION OF DYPSIS LEPTOCHEILOS LEAVES EXTRACT AND MOLECULAR DOCKING STUDY OF THE ISOLATED COMPOUNDS

2020 ◽  
pp. 106-113
Author(s):  
HAITHAM ALI IBRAHIM ◽  
FATEHIA SAYED ELSHARAWY ◽  
MAHMMOUD ELHASSAB ◽  
SAMAH SHABANA ◽  
EMAN GABER HAGGAG
Keyword(s):  
Antioxidant Activity ◽  
Phenolic Compounds ◽  
Ethyl Acetate ◽  
Chromatographic Separation ◽  
Ethyl Acetate Fraction ◽  
Docking Study ◽  
Separation Techniques ◽  
Reference Drug ◽  
First Time ◽  
Mcf 7

Objective: phytochemical investigation of the ethyl acetate fraction (EAF) of 80% aqueous methanol extract (AME) of Dypsis leptocheilos leaves, in addition to evaluation of the antioxidant, cytotoxic and antimicrobial activities of the AME and EAF. Docking was used to predict and understand cytotoxicity of the isolated compounds. Methods: The ethyl acetate fraction (EAF) of Dypsis leptocheilos leaves was subjected to different chromatographic separation techniques. Structures of the isolated compounds were established by different spectroscopic techniques (1H/13C NMR). Antioxidant activity was evaluated by DPPH assay, while cytotoxicity was evaluated by MTT cell viability assay. Antimicrobial activity was evaluated by agar diffusion method. The docking study was conducted using Auto Dock Vina; the estrogen receptor (PDB 5t92) was used as a receptor for the docking. Results: Chromatographic separation techniques were led to the isolation of five phenolic compounds; these compounds were identified to be apigenin 8-C-β-D-glucopyranoside (Vitexin) (1), apigenin 6-C-β-D-glucopyranoside (Isovitexin) (2), luteolin 7-O-β-D-glucopyranoside (3), luteolin 8-C-β-D-glucopyranoside (Orientin) (4), luteolin 6-C-β-D-glucopyranoside (Isoorientin) (5). They were isolated and identified for the first time from this plant species. The AME and EAF showed moderate activity against Gram positive and Gram negatvie bacteria, while both of them showed similar and powerful antioxidant activity with SC50 = 12.8±0.56 µg/ml and SC50 = 17±0.77 µg/ml respectively, compared to ascorbic (reference drug) SC50 = 14.2±0.35 µg/ml. The EAF showed higher cytotoxic activity on the MCF-7 cells (human breast cancer cell line), with IC50 = 12.3 ± 1.82 µg/ml, compared to Vinblastine Sulfate (reference drug). All isolated compounds showed good binding affinity to the estrogen receptors existed in the MCF-7 cell. Conclusion: Five phenolic compounds were isolated for the first time from the EAF of Dypsis leptocheilos leaves. The AME and EAF extracts showed variable antioxidant, antimicrobial and cytotoxic activities.

scholarly journals REPRODUCING QUALITIES OF RAMS OF THE MOLDOVAN TYPE KARAKUL BREED

2020 ◽  
Vol 59 ◽  
pp. 92-96
Author(s):  
D. Rotari
Keyword(s):  
Sperm Count ◽  
Sperm Concentration ◽  
Animal Husbandry ◽  
Sperm Production ◽  
Livestock Farming ◽  
High Quality ◽  
Average Percentage ◽  
Reproductive Ability ◽  
First Time

Issues related to the reproduction of animals have been and remain one of the most complex and relevant problems of biology and are constantly finding a direct and effective way out into livestock farming practice. The rational use of breeding sheep as producers is limited by the lack of standard, objective methods and methods for the timely assessment of their reproductive ability. The article presents the results of evaluating the sperm production of rams-producers. For the first time, the freshly obtained sperm of rams of Moldavian type producers of the Karakul breed was evaluated using the macroscopic method - ejaculate volume, color and smell, as well as the microscopic method - motility, sperm concentration in the ejaculate, total sperm count in the ejaculate sperm movements (VAP; VSL and VCL) as well as the percentage of abnormal forms of sperm. The experiments were carried out on sheep producers grown on a pedigree farm of the experimental farm of the Moldavian Scientific and Practical Institute of Biotechnology in Animal Husbandry and Veterinary Medicine. As a result of the studies, it was found that the ejaculate volume on average was 0.99 ± 0.04 ml, motility was 0.95 ± 0.02 and sperm concentration 1.51 ± 0.14 billion/ml. The percentage of pathological forms in sperm averaged 13.72 ± 0.61, an indicator that characterizes the high quality of sperm. The average quality indicator of ejaculates obtained from ram-producers of the Moldavian type of the Karakul breed corresponds to physiological standards for the Karakul breed. The average percentage of pathological forms of sperm found in ejaculates indicates that the rams were in good conditions of feeding and keeping. According to research, we can say that the Moldovan type of Karakul rams can be successfully used to obtain high quality ejaculates suitable for freezing sperm at 196°C.

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