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1.
Insects ; 13(6)2022 Jun 10.
Artigo em Inglês | MEDLINE | ID: mdl-35735871

RESUMO

The guava fruit fly, Bactrocera correcta, is one of the most destructive pests in the genus Bactrocera and detects environmental odorants mainly through antennal olfactory sensilla phenotypes with nanopores. However, it is unclear whether there are naturally occurring abnormal antennal olfactory sensilla phenotypes that affect olfaction. Here, we found that there were abnormal bulges besides nanopores on the surface of trichoid and basiconic olfactory sensilla in the antennal flagellum of long-term laboratory rearing colony (LTC), and that nanopore number in these olfactory sensilla was also remarkably reduced. Notably, the electroantennogram (EAG) responses of LTC insects to methyl eugenol or ß-caryophyllene were inhibited, and their behavioral responses elicited by the same odorants were also impaired. These results revealed naturally occurring abnormal antennal olfactory sensilla phenotypes which were involved in olfactory deficit in B. correcta, providing a platform to further study nanopore-targeted pest control technologies in the future.

2.
Chinese Medical Journal ; (24): 2088-2094, 2017.
Artigo em Inglês | WPRIM (Pacífico Ocidental) | ID: wpr-338794

RESUMO

<p><b>BACKGROUND</b>Paroxysmal kinesigenic dyskinesia (PKD) is a rare movement disorder characterized by recurrent dystonic or choreoathetoid attacks triggered by sudden voluntary movements. Under the condition of psychological burden, some patients' attacks may get worsened with longer duration and higher frequency. This study aimed to assess nonmotor symptoms and quality of life of patients with PKD in a large population.</p><p><b>METHODS</b>We performed a cross-sectional survey in 165 primary PKD patients from August 2008 to October 2016 in Rui Jin Hospital, using Symptom Check List-90-Revised (SCL-90-R), World Health Organization Quality of Life-100 (WHOQoL-100), Self-Rating Depression Scale, and Self-Rating Anxiety Scale. We evaluated the differences of SCL-90-R and WHOQOL-100 scores in patients and Chinese normative data (taken from literature) by using the unpaired Student's t-test. We applied multivariate linear regression to analyze the relationships between motor manifestations, mental health, and quality of life among PKD patients.</p><p><b>RESULTS</b>Compared with Chinese normative data taken from literature, patients with PKD exhibited significantly higher (worse) scores across all SCL-90-R subscales (somatization, obsessive-compulsive, interpersonal sensitivity, depression, anxiety, hostility, phobic anxiety, paranoid ideation, and psychoticism; P= 0.000 for all) and significantly lower (worse) scores of five domains in WHOQoL-100 (physical domain, psychological domain, independence domain, social relationship domain, and general quality of life; P= 0.000 for all). Nonremission of dyskinesia episodes (P = 0.011) and higher depression score (P = 0.000) were significantly associated with lower levels of quality of life. The rates of depression and anxiety in patients with PKD were 41.2% (68/165) and 26.7% (44/165), respectively.</p><p><b>CONCLUSIONS</b>Depression, anxiety, and low levels of quality of life were prevalent in patients with PKD. Co-occurrence of depression and anxiety was common among these patients. Regular mental health interventions could set depression and anxiety as intervention targets. Considering that the motor episodes could be elicited by voluntary movements and sometimes also by emotional stress, and that symptoms may get worsened with longer duration and higher frequency when patients are stressed out, intervention or treatment of depression and anxiety might improve the motor symptoms and overall quality of life in PKD patients.</p>

3.
Arch Pharm Res ; 33(6): 807-11, 2010 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-20607484

RESUMO

A novel mixed NH(3)/NH(2)OH platinum(II) complex cis-[Pt(NH(3))(NH(2)OH)Cl(2)] was synthesized and characterized by elemental analysis, FAB-MS, FT-IR and (1)H NMR spectroscopy. This complex was determined to have a good water-solubility and satisfactory stability. The pertinent complex was evaluated for its in vitro cytotoxicity against 3AO, HCT-116, LNcap, A549/ATCC and SGC-7901 human carcinoma cell lines. It shows appreciable cytotoxic activity that is comparable with cisplatin and is much more active than carboplatin.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Cisplatino/análogos & derivados , Hidroxilaminas/química , Antineoplásicos/química , Linhagem Celular Tumoral , Cisplatino/síntese química , Cisplatino/química , Cisplatino/farmacologia , Desenho de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Estabilidade de Medicamentos , Humanos , Concentração Inibidora 50 , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Solubilidade , Espectrometria de Massas de Bombardeamento Rápido de Átomos , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier
4.
Chem Pharm Bull (Tokyo) ; 57(4): 424-7, 2009 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-19336943

RESUMO

Diiodo-, dibromo- and dichloro-platinum(II) complexes containing L-histidine ligand were prepared. Their spectra and X-ray crystal structure of the dibromo-platinum(II) complex were described. Only the dichloro-platinum(II) complex showed comparable cytotoxic activity with carboplatin against A549/ATCC, HT-29, and LNcap cell lines. Nevertheless the complexes with COOH-substituted ligands histidine may be good starting materials to synthesize targeting platinum complexes since they could be easily linked to suitable carrier molecules via esterification.


Assuntos
Antineoplásicos/síntese química , Histidina/química , Compostos Organoplatínicos/síntese química , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Cristalografia por Raios X , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Ligantes , Modelos Moleculares , Estrutura Molecular , Compostos Organoplatínicos/química , Compostos Organoplatínicos/farmacologia
5.
Acta Crystallogr Sect E Struct Rep Online ; 65(Pt 10): m1264, 2009 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-21577775

RESUMO

In the crystal structure of the title compound, [Ir(C(5)H(7)O(2))(3)(H(2)O)], the Ir(III) atom is six-coordinated and situated in a slightly distorted octa-hedral environment. The complex contains both Ir-O and Ir-C bonds and was isolated from a reaction mixture of IrCl(3)(H(2)O)(x), pentane-2,5-dione and NaHCO(3). O-H⋯O hydrogen bonding between the water molecules and the carbonyl O atoms of adjacent molecules leads to a layered motif extending parallel to (010).

6.
J Pharm Pharmacol ; 60(10): 1335-40, 2008 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-18812026

RESUMO

Previous studies showed that bis(alpha-furancarboxylato)oxovanadium(IV) (BFOV), an orally active anti-diabetic organic vanadium complex, could improve insulin resistance in animals with type 2 diabetes. The present study has been carried out to evaluate the effects of BFOV on insulin-resistant glucose metabolism using dexamethasone-treated 3T3-L1 adipocytes as an in-vitro model of insulin resistance. The results showed that BFOV, similar to vanadyl sulfate and rosiglitazone, caused a concentration-dependent increase in glucose consumption by insulin-resistant adipocytes. Moreover, BFOV enhanced the action of insulin and completely prevented the development of insulin resistance induced by dexamethasone, leading to glucose consumption equal to that by normal cells. In addition, dexamethasone reduced the mRNA expression of insulin receptor substrate 1 (IRS-1) and glucose transporter 4 (GLUT4) in 3T3-L1 adipocytes, while BFOV normalized the expression of IRS-1 and GLUT4. These findings suggest that BFOV prevents and improves dexamethasone-induced insulin resistance in 3T3-L1 adipocytes by enhancing expression of IRS-1 and GLUT4 mRNA.


Assuntos
Adipócitos/efeitos dos fármacos , Dexametasona/farmacologia , Insulina/farmacologia , Compostos Organometálicos/farmacologia , Células 3T3-L1 , Adipócitos/citologia , Adipócitos/metabolismo , Animais , Relação Dose-Resposta a Droga , Glucocorticoides/farmacologia , Glucose/metabolismo , Glucose/farmacologia , Transportador de Glucose Tipo 4/genética , Transportador de Glucose Tipo 4/metabolismo , Hipoglicemiantes/farmacologia , Proteínas Substratos do Receptor de Insulina/genética , Proteínas Substratos do Receptor de Insulina/metabolismo , Resistência à Insulina , Camundongos , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Rosiglitazona , Tiazolidinedionas/farmacologia , Compostos de Vanádio/farmacologia
7.
Arch Pharm (Weinheim) ; 341(2): 132-6, 2008 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-18186542

RESUMO

A series of novel platinum(II) complexes involving a physiologically active carrier histamine as the carrier, cis-[Pt(histamine)X2] (X2=2Cl-, oxalate, malonate, 1,1-cyclobutanedicarboxylate (CBDCA), 3-hydroxy-1,1-cyclobutanedicarboxylate (HO-CBDCA)), have been synthesized and characterized by elemental analysis and spectroscopic data along with X-ray crystal structure for a representative complex cis-[Pt(histamine)Cl2]. The cytotoxicity of the complexes has also been assessed in the human cancer cell lines A549/ATCC, HT-29, and LNcap. One complex, cis-[Pt(histamine)Cl2], is more active than carboplatin against both the sensitive and resistant cells.


Assuntos
Antineoplásicos/farmacologia , Quelantes/química , Histamina/análogos & derivados , Histamina/química , Compostos Organoplatínicos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Linhagem Celular Tumoral , Cristalografia por Raios X , Resistencia a Medicamentos Antineoplásicos , Histamina/síntese química , Histamina/farmacologia , Humanos , Espectroscopia de Ressonância Magnética , Compostos Organoplatínicos/síntese química , Compostos Organoplatínicos/química , Relação Estrutura-Atividade
8.
Eur J Med Chem ; 43(7): 1438-43, 2008 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-17959272

RESUMO

Novel lipophilic platinum(II) complexes (LSPt-1-3), containing 3,5-diisopropylsalicylate (DIPS) as a leaving group and 2NH(3) or 1R,2R-diaminocyclohexane or (4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane as the carrier, have been synthesized, characterized and evaluated in vitro and in vivo. The octanol/water distribution coefficient of the complexes has also been measured. The results showed that the complexes achieved a typical square planar and the octanol/water distribution coefficient logP was 4.27, 4.37 and 4.31. The complexes were tested by SRB method to be more cytotoxic than Carboplatin, Oxaliplatin and Eptaplatin against 3AO, A549, NCI-H460 and SGC-7901 human cancer cell lines. Among complexes, LSPt-2 was much more effective than Carboplatin and Oxaliplatin in treating the NCI-H460 non-small-cell lung tumor-bearing mice. Its optimal activity was 38.8% (T/C) at a dose of 30 mg/kg following i.p. administration. LD(50) for the complex was found to be 230.9 mg/kg. LSPt-2 exhibited great anticancer activity, good lipophilic ability and low toxicity and therefore, it is a promising candidate for effective and stable pharmaceutical liposomal platinum anticancer drug.


Assuntos
Compostos de Platina/síntese química , Compostos de Platina/farmacologia , Salicilatos/química , Animais , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Dose Letal Mediana , Espectroscopia de Ressonância Magnética , Camundongos , Compostos de Platina/química , Espectrometria de Massas de Bombardeamento Rápido de Átomos , Espectrofotometria Ultravioleta
9.
Arch Pharm (Weinheim) ; 340(11): 599-602, 2007 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-17924364

RESUMO

Four diam(m)ineplatinum(II) complexes containing beta-phenylisosuccinate as the leaving groups were prepared, characterized, and evaluated for their cytotoxicity against A549/ATCC human lung cancer cell line and SGC-7901 human gastric cancer cell line. One of the complexes, (trans-1R,2R-diaminocyclohexane)-beta-phenylisosuccinatoplatinum(II) 4, was much more active than cisplatin and carboplatin.


Assuntos
Antineoplásicos , Cisplatino/análogos & derivados , Compostos Organoplatínicos , Succinatos/química , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Desenho de Fármacos , Humanos , Isomerismo , Ligantes , Estrutura Molecular , Compostos Organoplatínicos/síntese química , Compostos Organoplatínicos/química , Compostos Organoplatínicos/farmacocinética
10.
Bioorg Med Chem Lett ; 17(8): 2146-9, 2007 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-17306532

RESUMO

Novel lipophilic (diamine)platinum(II) complexes of salicylate derivatives as the leaving groups were synthesized and characterized by elemental analysis, FAB(+)-MS, FT-IR, and (1)H NMR spectroscopy. Most of the resulting platinum complexes had high solubility in organic solvents such as ethanol, acetone, and ether, and had right partition coefficient suited to be encapsulated in liposomes. The pertinent complexes were evaluated for their in vitro cytotoxicity against A549 human lung carcinoma and SGC-7901 human gastric carcinoma cell lines. They showed better cytotoxic activity than carboplatin and oxaliplatin.


Assuntos
Antineoplásicos/síntese química , Diaminas/síntese química , Platina/farmacologia , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Diaminas/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Lipossomos , Neoplasias Pulmonares/tratamento farmacológico , Platina/química , Salicilatos , Solubilidade , Solventes , Análise Espectral , Neoplasias Gástricas/tratamento farmacológico
11.
Se Pu ; 20(4): 345-7, 2002 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-12541919

RESUMO

Cis-dichloroamine (4-amino-2, 2, 6, 6-tetramethylpiperidine-1-oxyl) platinum (II) (abbreviated to HJ5) is a novel platinum anticancer compound which has prospects for research and application. In order to establish a conventional analytical method, an HPLC has been studied. Under the conditions of acetonitrile-water (10:90, volume ratio) as mobile phase, detection wavelength of 210 nm, a Phenomenex column C18(150 mm x 3.9 mm i.d., 10 microns). The linear equation, recovery and accuracy of the method were determined with external standard method. The HPLC has satisfactory resolution between the peaks of HJ5 and impurities. The peak areas of HJ5 were linear to its amounts detected and the detection limit was 0.07 microgram. The hydration of HJ5 can be inhibited effectively by NaCl solution. In a 9 g/L NaCl solution, the stability can be kept for more than 2 hours which is enough for analysis.


Assuntos
Antineoplásicos/análise , Cromatografia Líquida de Alta Pressão , Óxidos N-Cíclicos/análise , Compostos Organoplatínicos/análise , Antineoplásicos/química , Cromatografia Líquida de Alta Pressão/métodos , Cisplatino/análise , Cisplatino/química , Óxidos N-Cíclicos/química , Compostos Organoplatínicos/química
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