scholarly journals Two groups of copperII pyridine–triazole complexes with “open or close” pepper rings and their in vitro antitumor activities

RSC Advances ◽  
2020 ◽  
Vol 10 (11) ◽  
pp. 6297-6305
Author(s):  
ZhaoGuo Hong ◽  
Chu Zheng ◽  
Bi Luo ◽  
Xin You ◽  
HeDong Bian ◽  
...  

The pepper ring-modified complexes (Group II, C4–C6) exhibited significant antitumor activity than veratrole-modified complexes (Group I, C1–C3) towards several cancer cells with IC50 ranging from 3.45 to 8.59 μM.

1997 ◽  
Vol 36 (08) ◽  
pp. 259-264
Author(s):  
N. Topuzović

Summary Aim: The purpose of this study was to investigate the changes in blood activity during rest, exercise and recovery, and to assess its influence on left ventricular (LV) volume determination using the count-based method requiring blood sampling. Methods: Forty-four patients underwent rest-stress radionuclide ventriculography; Tc-99m-human serum albumin was used in 13 patients (Group I), red blood cells was labeled using Tc-99m in 17 patients (Group II) in vivo, and in 14 patients (Group III) by modified in vivo/in vitro method. LV volumes were determined by a count-based method using corrected count rate in blood samples obtained during rest, peak exercise and after recovery. Results: In group I at stress, the blood activity decreased by 12.6 ± 5.4%, p <0.05, as compared to the rest level, and increased by 25.1 ± 6.4%, p <0.001, and 12.8 ± 4.5%, p <0.05, above the resting level in group II and III, respectively. This had profound effects on LV volume determinations if only one rest blood aliquot was used: during exercise, the LV volumes significantly decreased by 22.1 ± 9.6%, p <0.05, in group I, whereas in groups II and III it was significantly overestimated by 32.1 ± 10.3%, p <0.001, and 10.7 ± 6.4%, p <0.05, respectively. The changes in blood activity between stress and recovery were not significantly different for any of the groups. Conclusion: The use of only a single blood sample as volume aliquot at rest in rest-stress studies leads to erroneous estimation of cardiac volumes due to significant changes in blood radioactivity during exercise and recovery.


2019 ◽  
Vol 16 (6) ◽  
pp. 462-467
Author(s):  
Songtao Li ◽  
Hongling Zhao ◽  
Zhifeng Yin ◽  
Shuhua Deng ◽  
Yang Gao ◽  
...  

A series of new phenanthrene-based tylophorine derivatives (PBTs) were synthesized in good yield and their structures were characterized by 1H-NMR spectroscopy and ESI MS. In vitro antitumor activity of these compounds against five human carcinoma cell lines, including HCT116 (colorectal), BGC-823 (gastric), HepG-2 (hepatic), Hela (cervical) and H460 (lung) cells, was evaluated by MTT assay. Among these PBTs, compound 6b showed the highest antitumor activities against HCT116 and HepG-2 cell lines with IC50 values of 6.1 and 6.4 μM, respectively, which were comparable to that of adriamycin hydrochloride. The structure-activity relationship of these compounds was also discussed based on the results of their antitumor activity.


Cancers ◽  
2021 ◽  
Vol 13 (16) ◽  
pp. 3975
Author(s):  
Marco A. De Velasco ◽  
Yurie Kura ◽  
Naomi Ando ◽  
Noriko Sako ◽  
Eri Banno ◽  
...  

Significant improvements with apalutamide, a nonsteroidal antiandrogen used to treat patients suffering from advanced prostate cancer (PCa), have prompted evaluation for additional indications and therapeutic development with other agents; however, persistent androgen receptor (AR) signaling remains problematic. We used autochthonous mouse models of Pten-deficient PCa to examine the context-specific antitumor activity of apalutamide and profile its molecular responses. Overall, apalutamide showed potent antitumor activity in both early-stage and late-stage models of castration-naïve prostate cancer (CNPC). Molecular profiling by Western blot and immunohistochemistry associated persistent surviving cancer cells with upregulated AKT signaling. While apalutamide was ineffective in an early-stage model of castration-resistant prostate cancer (CRPC), it tended to prolong survival in late-stage CRPC. Molecular features associated with surviving cancer cells in CRPC included upregulated aberrant-AR, and phosphorylated S6 and proline-rich Akt substrate of 40 kDa (PRAS40). Strong synergy was observed with the pan-AKT inhibitor GSK690693 and apalutamide in vitro against the CNPC- and CRPC-derived cell lines and tended to improve the antitumor responses in CNPC but not CRPC in vivo. Upregulation of signal transducer and activator of transcription 3 (STAT3) and proviral insertion in murine-1 (PIM-1) were associated with combined apalutamide/GSK690693. Our findings show that apalutamide can attenuate Pten-deficient PCa in a context-specific manner and provides data that can be used to further study and, possibly, develop additional combinations with apalutamide.


Zygote ◽  
2021 ◽  
pp. 1-5
Author(s):  
H. Debbarh ◽  
N. Louanjli ◽  
S. Aboulmaouahib ◽  
M. Jamil ◽  
L. Ahbbas ◽  
...  

Summary Maternal age is a significant factor influencing in vitro fertilization (IVF) outcomes. Oxidative stress (OS) is one of the major causes of age-related cellular and molecular damage. The purpose of this work was to investigate the correlation between maternal age with intrafollicular antioxidants and OS markers in follicular fluid (FF), and also to determine the OS status in patients of advanced age. This study was a prospective study including 201 women undergoing IVF whose age was between 24 and 45 years old. FF samples were obtained from mature follicles at the time of oocyte retrieval. After treatment of FF, lipid peroxidation levels (MDA) and enzyme activities such as superoxide dismutase (SOD), catalase (CAT), glutathione reductase (GR) and glutathione (GSH) level were evaluated using spectrophotometry. The results indicated that the age cutoff point for increasing the MDA level was fixed at 37 years, allowing the study to be differentiated into two age groups. Group I included patients whose age was less than 37 years, and group II included patients whose age was greater than or equal 37 years. Statistical analysis revealed that MDA and GSH levels and GR activity were significantly higher in group II compared with group I. The SOD and CAT activities were significantly less in group II compared with group I. We concluded that from 37 years old a reproductive ageing was accompanied by a change in the antioxidant pattern in FF that impaired reactive oxygen species scavenging efficiency.


2021 ◽  
Vol 99 (Supplement_3) ◽  
pp. 172-173
Author(s):  
Xiaoge Sun ◽  
Yitong Su ◽  
YangYi Hao ◽  
Gaokun Liu ◽  
Yue Gong ◽  
...  

Abstract To improve the efficiency of whole cottonseed (WCS) on dairy cattle, crush and alkali treatment were combined (Table 1) in this study. The gastrointestinal tract digestibility of WCS were measured by in situ ruminal incubation and in vitro fermentation, respectively. Finally, animal feeding experiment was conducted to evaluate the effect of processed WCS on dairy cattle. A total of 30 Holstein dairy cows with similar physiological status were allocated to three groups (CON, Group I, and Group II). Ration for the CON group was a basic ration with no WCS, ration with about 8% non-processed WCS was for Group I (DM basis), while the Group II was provided by the ration added with 8% Crush-Alkali (4% mixed alkali solids with NaOH/CaO ratio at 1:1) treated WCS. Results of the in situ and in vitro experiments showed that, compared with non-treated WCS, Crushing-Alkali treatment groups significantly improved WCS ruminal effective degradation rate of dry matter (DM), crude protein (CP), ether extract (EE), and neutral detergent fiber (NDF) (P &lt; 0.05). Furthermore, Crush-Alkali (4% mixed alkali solids with NaOH/CaO ratio at 1:1) was the most beneficial to improve WCS gastrointestinal degradation of DM, CP and NDF, as well as enhance WCS rumen-bypass of EE. With the lowest free gossypol content (P&lt; 0.05). Results of animal feeding experiment showed that DMI, 4% fat corrected milk production (4% FCM), milk protein, milk fat, and content of short-chain saturated fatty acids in milk in Group II significantly increased (P &lt; 0.05) compared with CON group. DMI, ω-6 polyunsaturated fatty acids (PUFA) in milk, and the ratio of ω-6 to ω-3 PUFA were significantly higher in Group II than that in Group I (P &lt; 0.05). Additionally, free gossypol concentration in serum and milk, as well as parameters reflecting liver function were not notably different among the three groups (P &gt; 0.05).


2017 ◽  
Vol 7 (1) ◽  
Author(s):  
Kim Rouven Liedtke ◽  
Sander Bekeschus ◽  
André Kaeding ◽  
Christine Hackbarth ◽  
Jens-Peter Kuehn ◽  
...  

2012 ◽  
Vol 17 (4) ◽  
pp. 1-7 ◽  
Author(s):  
Roberto Hideo Shimizu ◽  
Karlos Giovani Grando ◽  
Isabela Almeida Shimizu ◽  
Augusto Ricardo Andriguetto ◽  
Ana Cláudia Moreira Melo ◽  
...  

OBJECTIVE: This in vitro study was designed to evaluate the shear bond strength (SBS) of orthodontic metal brackets bonded by direct and indirect techniques. METHODS: Thirty healthy human maxillary premolar teeth were used. The teeth were divided into three groups of 10 teeth each: Group I - indirect bonding with SondhiTM Rapid-Set system (3M/Unitek), Group II - indirect bonding with TransbondTM XT adhesive system (3M/Unitek) and Group III - direct bonding with TransbondTM XT adhesive system (3M/Unitek). After bonding and obtaining the specimens for the study, the specimens were subjected to SBS testing in a universal testing machine (Emic, model DL-500). The Kolmogorov-Smirnov test was applied to ascertain that the data had a normal distribution and the Bartlett test to check whether there was homogeneity of variance. One-factor analysis of variance was performed and, subsequently, Tukey's test for paired means. A 5% significance level was adopted. RESULTS: The results of Group I were 67.6 (N) and 5.9 (MPa); Group II, 68.9 (N) and 6.1 (MPa) and Group III (control), 92.5 (N) and 8.1 (MPa). CONCLUSION: It can therefore be concluded that the means for Group III were significantly higher compared with Groups I and II in both Newton (N) and Megapascal (MPa) values. The means attained by the indirect bonding technique used in Groups I and II, however, exhibited no statistically significant differences.


2009 ◽  
Vol 66 (1) ◽  
pp. 57-62 ◽  
Author(s):  
Drenka Turjacanin-Pantelic ◽  
Dragana Bojovic-Jovic ◽  
Biljana Arsic ◽  
Eliana Garalejic

Background/Aim. A modern approach to surgical treatment of tuboperitoneal infertility is based on laporascopic techniques. The aim of this study was to compare results of tuboperitoneal infertility treatment by the use of laparoscopy and classical laparotomy. Methods. A retrospectiveprospective study on 66 women treated operatively form tuboperitoneal infertility was performed. Data from patient's anamnesis and those related to the surgical treatment results, obtained by the use of an inquiry, were used in retrospective and prospective analysis, respectively. Chi-square test was used in statistical analysis. P value < 0.05 was considered significant. Results. Classical laparotomy was used on 34 women in a period from 1996 to 1997, while 32 women were operated laparoscopically in a period from 1999 to 2000. The results were as follows: a total number of conceived women was 16 (24%), seven in the group I (20.6%) and nine in the group II (28.1%); 13 women were with one pregnancy, six in the group I (17.6%) and seven in the group II (22%). Twice pregnant were three women, one in the group I (2.9%) and two in the group II (6.2%). The resulting pregnancies were: five women with abortion spontaneous, two in the group I (5.9%) and three in the group II (9.4%); two women with extrauterine pregnancy in the group I (5.9%); three with pretemporal birth, one in the group I (2.9%) and two in the group II (6.2%), while six women were with the temporal birth, two in the group I (5.9%) and four in the group II (12.5%). Statistical analysis showed that there was no significant difference in the results between these two groups. Conclusion. Surgical treatment of tubeperitoneal infertility, regardless of the used methods (classical laparotomy or laparoscopy) was successful in a great number of women. These methods have a great advantage over in vitro fertilization, and they should not be ignored.


Author(s):  
Nandita Bansal

Introduction: Intracoronal bleaching is the simplest, least invasive, and least expensive means available to lighten non-vital discolored teeth. The objective of the study: To evaluate the intra coronal bleaching efficacy of 35% Carbamide peroxide relative to 35% Hydrogen peroxide and Sodium perborate using artificially stained extracted human teeth. Materials and Methods: Eighty extracted human permanent maxillary and mandibular anterior teeth and single-rooted premolars were artificially stained using whole human blood and root canal treatment was completed. They were bleached twice 7 days apart using: Group I (n=20) – 35% Carbamide peroxide gel, Group II (n=20) – 35% Hydrogen peroxide gel, Group III (n=20) – 2 gm Sodium perborate mixed with per ml of distilled water, Group IV (n=20)– Distilled water only (control). Evaluation of shade was performed on day 0,7,14. Results: On day 7, In Groups I and Group II, there was a reduction in the shade by 2 vita tab positions, whereas Group IIIlightened by 1-tab position only. On day 14, CP and HP lightened by overall 3-tab positions and SP by 2-tab positions. There were no statistical differences between the groups on day 7 and day 14. Conclusion: 35% Carbamide peroxide, 35% Hydrogen peroxide and Sodiumperborate were equally effective for Intra coronal bleaching.


2019 ◽  
Vol 43 (9-10) ◽  
pp. 437-442 ◽  
Author(s):  
Shou De Xu ◽  
Xiang Hua Wu

A series of bimetallic dppfM(II) (dppf = 1,1’-bis (diphenyphosphino) ferrocene; M = Pt and Pd) dithiocarbamate complexes is synthesized and characterized by spectroscopic methods and single-crystal X-ray diffraction. Their antitumor activities in vitro are investigated by MTT assays against four cancer cell lines. The anticancer studies indicate most of the complexes display good to excellent antitumor activity. Remarkably, the platinum complex with a pyrrolidinyl substituent (3b) was identified as the most promising candidate due to its high potency and broad spectrum of activity.


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