scholarly journals Antitumor Trans Platinum Adducts of GMP and AMP

2000 ◽  
Vol 7 (4) ◽  
pp. 169-176 ◽  
Author(s):  
Yangzhong Liu ◽  
Maria F. Sivo ◽  
Giovanni Natile ◽  
Einar Sletten

Recently it has been shown that several analogues of the clinically ineffective trans-DDP exhibit antitumor activity comparable to that of cis-DDP. The present paper describes the binding of antitumor trans-[PtCl2(E-iminoether)2] (trans-EE) to guanosinemonophosphate (GMP) and adenosinemonophosphate (AMP). We have used HPLC and H1 and N15 NMR to characterize the different adducts. In the case of a 1:1 mixture of trans-EE and GMP, at an early stage of the reaction, a monofunctional adduct is formed which, subsequently, is partly converted into a monosolvated monofunctional species. After about 70 hours an equilibrium is established between chloro and solvato monofunctional adducts at a ratio of 30/70. In the presence of excess GMP (4:1) the initially formed monofunctional adducts react further to give two bifunctional adducts, one with the iminoether ligands in their original E configurations and the other with the iminoether ligands having one E and the other, Z configurations. The coordination geometry obtained by energy minimization calculations is in qualitative agreement with 2D NMR data.

Biochemistry ◽  
1990 ◽  
Vol 29 (19) ◽  
pp. 4723-4734 ◽  
Author(s):  
Mukti H. Sarma ◽  
Goutam Gupta ◽  
Angel E. Garcia ◽  
Kimiko Umemoto ◽  
Ramaswamy H. Sarma

2002 ◽  
Vol 57 (11-12) ◽  
pp. 976-982 ◽  
Author(s):  
Sabine Glasl ◽  
Pavel Mucaji ◽  
Ingrid Werner ◽  
Armin Presser ◽  
Johann Jurenitsch

The investigation of a dichloromethane extract of flower heads of a Hungarian taxon of the Achillea millefolium group led to the isolation of three flavonoid aglycones, one triterpene, one germacranolide and five guaianolides. Their structures were elucidated by UV-VIS, EI- and CI-MS, 1H NMR and 13C NMR spectroscopic methods as well as by 2D-NMR studies and by selective 1D-NOE experiments. Besides apigenin, luteolin and centaureidin, β-sitosterol, 3β-hydroxy-11α,13-dihydro-costunolide, desacetylmatricarin, leucodin, achillin, 8α-angeloxy-leucodin and 8α-angeloxy-achillin were isolated. Both latter substances are reported here for the first time. Their NMR data were compared with those of the other guaianolides. The stereochemistry of 3β-hydroxy-11α,13-dihydro-costunolide was discussed and compared with data of the literature.


Author(s):  
Carmen García-Alba

This study is part of a larger research study (doctoral dissertation), in which a comparative study with adolescent samples is done: 50 anorexic restricting patients (ANP), 50 patients diagnosed with depression (DP) and 50 non patients (NP). The proposed objective is two-fold: 1) To try to clarify the existing relationship between Anorexia (AN) and Depression (D), investigated from diverse disciplines but without conclusive results. 2) To detect in the ANP personality different traits from those of other groups, which should, if possible, allow to detect them at an early stage for an adequate prognosis. The current article presents the Rorschach findings in relation to the cognitive functioning of the ANP. In them, the following has been detected: (1) An information processing similar to that of the other groups, even with a more complete (L ≤ .99), more complex (DQ+↑) and better discriminated (Zd↑) grasp of the stimulus; (2) Mediating processes very similar to those of the other groups, sharing with them the perceptive maladjustments (X–%↑) and an excessive individualism (Xu%↑); (3) A clearly differentiating ideation disorder. Definitely, the ANP use predominantly ideation (M↑), but their thought, usually well-adjusted (MQo↑), presents eventual operations of delusional type (MQnone↑). Above that, their thinking is marked by a great passivity (Mp↑), which makes them more vulnerable to accept ideas without criticizing them and it results in a very inefficient thinking, which spins around these concepts without finding solutions, entering into a sort of ruminating which is completely unproductive. The differences toward the obsessive pathology are established. The discriminant analysis conducted with all the Rorschach variables that resulted as significant throughout the research, provides quite a consistent function which discriminates the ANP: MQnone↑, Mp↑, FD↓, Ma↑, MQo↑, AdjD↑, Sum H↑, (H)↑. Based on this we can understand that these adolescents, being in a developmental period of big changes and disorientations in relation with their own image, confronted with life events, and possibly starting off with some biologic vulnerability: (1) Due to the alterations of their ideation, accept without criticism (Mp) irrational ideas dominating in our culture, in which slimness appears as the only model, synthesis of intelligence, beauty and success; remaining captured in this type of mental activity (MQnone), which they cannot escape nor criticize (Mp), despite they reason adequately on other topics (MQo); (2) Their alterations of self-perception [(H)] make them hide themselves in a fantasized image, which is the axis of their interests and the only thing that really matters to them; (3) The resources they have to decide on behaviors and to finish these deliberately (AdjD), and their scarce tendency to the introspection (FD) lead to their decision of not eating, based on distorted and passively accepted thinking, which has great power and thus, so difficult to modify. Finally, based on the Rorschach data obtained, the hypothesis of a personality disorder as underlying pathology is pointed out.


Author(s):  
Menghan TAO ◽  
Ning XIAO ◽  
Xingfu ZHAO ◽  
Wenbin LIU

New energy vehicles(NEV) as a new thing for sustainable development, in China, on the one hand has faced the rapid expansion of the market; the other hand, for the new NEV users, the current NEVs cannot keep up with the degree of innovation. This paper demonstrates the reasons for the existence of this systematic challenge, and puts forward the method of UX research which is different from the traditional petrol vehicles research in the early stage of development, which studies from the user's essence level, to form the innovative product programs which meet the needs of users and being real attractive.


Pathogens ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 752
Author(s):  
Chung-Guei Huang ◽  
Avijit Dutta ◽  
Ching-Tai Huang ◽  
Pi-Yueh Chang ◽  
Mei-Jen Hsiao ◽  
...  

A total of 15 RT-PCR confirmed COVID-19 patients were admitted to our hospital during the in-itial outbreak in Taiwan. The average time of virus clearance was delayed in seven patients, 24.14 ± 4.33 days compared to 10.25 ± 0.56 days post-symptom onset (PSO) in the other eight pa-tients. There was strong antibody response in patients with viral persistence at the pharynx, with peak values of serum antibody 677.2 ± 217.8 vs. 76.70 ± 32.11 in patients with delayed versus rapid virus clearance. The patients with delayed viral clearance had excessive antibodies of compromised quality in an early stage with the delay in peak virus neutralization efficacy, 34.14 ± 7.15 versus 12.50 ± 2.35 days PSO in patients with rapid virus clearance. Weak antibody re-sponse of patients with rapid viral clearance was also effective, with substantial and comparable neutralization efficacy, 35.70 ± 8.78 versus 41.37 ± 11.49 of patients with delayed virus clearance. Human Cytokine 48-Plex Screening of the serial sera samples revealed elevated concentrations of proinflammatory cytokines and chemokines in a deceased patient with delayed virus clear-ance and severe disease. The levels were comparatively less in the other two patients who suf-fered from severe disease but eventually survived.


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.


1997 ◽  
Vol 467 ◽  
Author(s):  
Fumio Yoshizawa ◽  
Kunihiro Shiota ◽  
Daisuke Inoue ◽  
Jun-ichi Hanna

ABSTRACTPolycrystalline SiGe (poly-SiGe) film growth by reactive thermal CVD with a gaseous mixture of Si2H6 and GeF4 was investigated on various substrates such as Al,Cr, Pt, Si, ITO, ZnO and thermally grown SiO2.In Ge-rich film growth, SEM observation in the early stage of the film growth revealed that direct nucleation of crystallites took place on the substrates. The nucleation was governed by two different mechanisms: one was a heterogeneous nucleation on the surface and the other was a homogeneous nucleation in the gas phase. In the former case, the selective nucleation was observed at temperatures lower than 400°C on metal substrates and Si, where the activation of adsorbed GeF4 on the surface played a major role for the nuclei formation, leading to the selective film growth.On the other hand, the direct nucleation did not always take place in Si-rich film growth irrespective of the substrates and depended on the growth rate. In a growth rate of 3.6nm/min, the high crystallinity of poly-Si0.95Ge0.05in a 220nm-thick film was achieved at 450°C due to the no initial deposition of amorphous tissue on SiO2 substrates.


2006 ◽  
Vol 16 (1-2) ◽  
pp. 69-73 ◽  
Author(s):  
Yoshinari Takai ◽  
Toshihisa Murofushi ◽  
Munetaka Ushio ◽  
Shinichi Iwasaki

The time course of the recovery of subjective visual horizontal (SVH) after unilateral vestibular deafferentation by intratympanic instillation of gentamicin was studied. Six patients who underwent intratympanic gentamicin instillation therapy for Meniere's disease (1 man and 5 women, 32 to 69 years of age) were enrolled in this study. For comparison, SVH in 23 healthy subjects (12 men and 11 woman, 23 to 48 years of age) was also measured. The mean ± SD of SVH in healthy subjects was 0.0 ± 1.1 deg. All of the 6 patients showed significantly deviated SVH toward the injected side-down at the early stage after the therapy. Although one patient showed recovery of SVH to the normal range 25 days after the injection, the other patients required more time for recovery. Three patients did not show recovery to the normal range after 1 year. On the other hand, spontaneous nystagmus observed using an infrared CCD camera in total dark disappeared after 35 days (median). Patients who had normal vestibular evoked myogenic potentials before the therapy showed a tendency of delay of recovery of SVH. The reasons why the recovery of SVH took longer than the disappearance of spontaneous nystagmus are discussed in this report.


Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2481
Author(s):  
Anita M. Sutedja ◽  
Emiko Yanase ◽  
Irmanida Batubara ◽  
Dedi Fardiaz ◽  
Hanifah N. Lioe

Although the intake of jack bean (Canavalia ensiformis (L.) DC.), an underutilized tropical legume, can potentially decrease the risk of several chronic diseases, not much effort has been directed at profiling the polyphenolics contained therein. Hence, this work aimed to identify and quantify the dominant jack bean polyphenolics, which are believed to have antioxidant and other bioactivities. Four major compounds were detected and identified as kaempferol glycosides with three or four glycoside units. Their structures were established based on UV-visible, 1D, 2D NMR, and HR-ESI-MS analyses. Specifically, kaempferol 3-O-α-l-rhamnopyranosyl (1→6)- β-d-glucopyranosyl (1→2)-β-d-galactopyranosyl-7-O-[3-O-o-anisoyl]-α-l-rhamnopyranoside was detected for the first time, while the other three compounds have already been described in plants other than jack bean. This new compound was found to have a higher α-glucosidase inhibition activity compared to acarbose.


1989 ◽  
Vol 111 (4) ◽  
pp. 1484-1491 ◽  
Author(s):  
Thomas G. Pagano ◽  
Paulos G. Yohannes ◽  
Benjamin P. Hay ◽  
Jerry R. Scott ◽  
Richard G. Finke ◽  
...  

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