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1.
Mol Biol Rep ; 51(1): 333, 2024 Feb 23.
Artigo em Inglês | MEDLINE | ID: mdl-38393425

RESUMO

BACKGROUND: Olfaction plays an important role in host-seeking by parasitoids, as they can sense chemical signals using sensitive chemosensory systems. Psyttalia incisi (Silvestri) (Hymenoptera: Braconidae) is the dominant parasitoid of Bactrocera dorsalis (Hendel) in fruit-producing regions of southern China. The olfactory behavior of P. incisi has been extensively studied; however, the chemosensory mechanisms of this species are not fully understood. RESULTS: Bioinformatics analysis of 64,515 unigenes from the antennal transcriptome of both male and female adults P. incisi identified 87 candidate chemosensory genes. These included 13 odorant-binding proteins (OBPs), seven gustatory receptors (GRs), 55 odorant receptors (ORs), 10 ionotropic receptors (IRs), and two sensory neuron membrane proteins (SNMPs). Phylogenetic trees were constructed to predict evolutionary relationships between these chemosensory genes in hymenopterans. Moreover, the tissue expression profiles of 13 OBPs were analyzed by quantitative real-time PCR, revealing high expression of seven OBPs (1, 3, 6, 7, 8, 12, and 13) in the antennae. CONCLUSION: This study represents the first identification of chemosensory genes and the determination of their expression patterns in different tissues of P. incisi. These results contribute to a better understanding of the function of the chemosensory system of this parasitoid species.


Assuntos
Himenópteros , Receptores Odorantes , Tephritidae , Animais , Himenópteros/genética , Filogenia , Perfilação da Expressão Gênica , Transcriptoma/genética , Receptores Odorantes/genética , Receptores Odorantes/metabolismo , Proteínas de Insetos/genética , Proteínas de Insetos/metabolismo
2.
Front Immunol ; 14: 1173487, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37342347

RESUMO

Triple-negative breast cancer (TNBC) is characterized by a high degree of malignancy, early metastasis, limited treatment, and poor prognosis. Immunotherapy, as a new and most promising treatment for cancer, has limited efficacy in TNBC because of the immunosuppressive tumor microenvironment (TME). Inducing pyroptosis and activating the cyclic guanosine monophosphate-adenosine monophosphate synthase/interferon gene stimulator (cGAS/STING) signaling pathway to upregulate innate immunity have become an emerging strategy for enhancing tumor immunotherapy. In this study, albumin nanospheres were constructed with photosensitizer-IR780 encapsulated in the core and cGAS-STING agonists/H2S producer-ZnS loaded on the shell (named IR780-ZnS@HSA). In vitro, IR780-ZnS@HSA produced photothermal therapy (PTT) and photodynamic therapy (PDT) effects. In addition, it stimulated immunogenic cell death (ICD) and activated pyroptosis in tumor cells via the caspase-3-GSDME signaling pathway. IR780-ZnS@HSA also activated the cGAS-STING signaling pathway. The two pathways synergistically boost immune response. In vivo, IR780-ZnS@HSA + laser significantly inhibited tumor growth in 4T1 tumor-bearing mice and triggered an immune response, improving the efficacy of the anti-APD-L1 antibody (aPD-L1). In conclusion, IR780-ZnS@HSA, as a novel inducer of pyroptosis, can significantly inhibit tumor growth and improve the efficacy of aPD-L1.


Assuntos
Nanopartículas , Fotoquimioterapia , Neoplasias de Mama Triplo Negativas , Humanos , Animais , Camundongos , Neoplasias de Mama Triplo Negativas/terapia , Piroptose , Albuminas , Microambiente Tumoral
3.
Front Oncol ; 13: 1095891, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36741011

RESUMO

Rationale: Breast leiomyoma is the rarest non-epithelial tumor of the breast. As a benign tumor, its main treatment is regular follow-up. Surgical treatment is often used in clinical practice when patients have symptoms or strongly require treatment. However, if the tumor is large or located around the nipple or areola, the cosmetic effect of surgery is not good, so it is urgent to find new treatment methods. We pioneered the use of microwave ablation in the treatment of giant breast leiomyoma and achieved good results. Patient concerns: A 37-year-old female was admitted to hospital because she found a breast mass of approximately 8 cm. She had no obvious clinical symptoms, but had great psychological pressure. Diagnosis: Pathological biopsy showed leiomyoma followingly the surgical operation of giant breast leiomyoma was planned. However, the breast mass was large, and the postoperative scar would affect the breast appearance. Interventions: The consent was obtained from the patient and her family. The Ultrasound-guided microwave ablation was successfully performed. Outcomes: The patient was followed up for 10 months, and the tumor volume ablation rate was 69.8%. The cosmetic effect of breast was excellent. Lessons: To our knowledge, this is the first case to using microwave ablation (MWA) for the treatment of breast leiomyoma. Ultrasound-guided MWA can be used for the treatment of breast leiomyoma, especially when the mass is large and requires traditional surgical resection. It can effectively improve the breast aesthetics and further improve the quality of life of patients. However, it is only a case report, and needs more research to verify MWA in breast leiomyoma.

4.
J Obstet Gynaecol Res ; 49(4): 1283-1290, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-36642419

RESUMO

AIMS: To compare the safety and therapeutic effect of ultrasound (US)-guided microwave ablation (MWA) and US-guided vacuum-assisted excision (VAE) for patients with B3 lesions of the breast. METHODS: Patients who underwent US-guided MWA or US-guided VAE at Sichuan Tumor Hospital from January 2016 to December 2021 were retrospectively analyzed. The technical success rate and residual rate of the two minimally invasive surgeries were recorded. During follow-up, differences in symptom relief, recurrence or progression, re-intervention, incidence of adverse events, or personal satisfaction were observed between the two groups. RESULTS: The follow-up time was comparable between the two groups. The technical success rate was similar between the two groups; no residue was found in the US-guided MWA group, and the residue rate in the US-guided VAE group was 3.4%. The symptoms of the two groups were improved after the operation. The incidence of postoperative adverse events in the US-guided MWA group was significantly lower than that in the US-guided VAE group. Additionally, the MWA group had a lower incidence of adverse events when the tumor diameter was >2.5 cm. Compared to the US-guided VAE group, the US-guided MWA group had a lower rate of tumor recurrence or progression, re-intervention rate, and higher personal satisfaction. CONCLUSIONS: The technical success rate of US-guided MWA for B3 lesions was comparable to that of US-guided VAE, but US-guided MWA had a lower incidence of adverse events and a higher degree of personal satisfaction compared with US-guided VAE.


Assuntos
Mama , Micro-Ondas , Humanos , Estudos Retrospectivos , Micro-Ondas/uso terapêutico , Mama/diagnóstico por imagem , Mama/cirurgia , Ultrassonografia , Ultrassonografia de Intervenção , Resultado do Tratamento
5.
Altern Ther Health Med ; 29(1): 238-244, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36150015

RESUMO

Context: Pituitary adenoma is a clinical syndrome in which excessive production of pituitary corticotropin (ACTH). For ACTH tumor cells, researchers know little about the influence of the cell-cycle process on ACTH production and cell proliferation. Some research has shown that imatinib can induce apoptosis of tumor cells. Objective: The study intended to explore the effects and molecular mechanisms of imatinib combined with everolimus on AtT-20 cells in AtT-20 mouse pituitary tumors. Design: The research team performed a laboratory study using murine corticotropin tumor AtT-20 cells. Setting: The study took place at the Department of Neurosurgery at Renmin Hospital of the Hubei University of Medicine in Shiyan, Hubei, China. Intervention: The research team cultured the cells in AtT-20-cell-specific medium containing 100 µg/mL of streptomycin, 100 U/mL of penicillin, and 10% fetal bovine serum at 37°C and 5% CO2. The team divided the cells into a control group, a normal culture without the drug, and an intervention group, incubated for 24 hours with 1 µM of imatinib and 3 µM of everolimus when the cells grew to 40% confluence. Outcome Measures: The research team: (1) determined the effects of the combined drugs on cell viability using a methyl thiazolyl tetrazolium (MTT) assay; (2) detected the cell's mitochondrial membrane potential and LDH leakage using "sytox blue, 5',6,6'-tetrachloro-1,1',3,3'-tetraethylbenzimidazolylcarbocyanine iodide," CBIC2(3) or JC-1, and lactate dehydrogenase (LDH) assay kits, respectively; (3) detected AtT-20 cell apoptosis using a "terminal deoxynucleotidyl transferase (TdT)-mediated deoxyuridine triphosphate (dUTP) nick-end labeling" (TUNEL) kit; (4) analyzed the expression of protein kinase B (p-Akt), cAMP-response element binding protein (p-CREB), p27, p53, and cyclin E using a Western blot test; (5) detected the mRNA expression of opioid melanin procorticotropin (POMC)), caspase-3, and pituitary tumor transforming gene 1 (PTTG1) using reverse transcription-polymerase chain reaction (RT-PCR); (6) measure the concentration of adreno-cortico-tropic-hormone (ACTH) in the supernatant using an enzyme-linked immunoassay (ELISA) kit; and (7) assessed the cell cycle distribution using flow cytometry. Results: No differences existed in cell viability between the groups at the baseline (0 h) of the culture period (P > .05). Compared to the control group, the intervention group's: (1) cell viability was significantly lower at 4, 8, and 12 hours and postintervention at 16 hours (P < .001); (2) LDH concentration was significantly higher (P < .001); (3) mitochondrial membrane potential was significantly lower (P < .001); (4) apoptosis rate of TUNEL was significantly higher (P < .001 ); (5) expression of p-Akt, p-CREB phosphorylation, and cyclin E was significantly lower (P < .001), (6) expression of p27 and p53 protein was significantly higher (P < .001); (7) mRNA expression of POMC and PTTG1 were significantly lower (P < .001); (8) mRNA expression of caspase-3 was significantly higher (P < .001); (9) concentration of ACTH was lower (P < .001); and (10) percentage of cells in the G0/G1 phase was significantly higher, while the percentage of cells in the S phase was significantly lower (P < .05). Conclusions: Imatinib combined with everolimus can affect the AtT-20 cell cycle through the signaling pathway of the phosphatidylin-ositol-3-kinase (PI3K)/Akt/ protein kinase A (PKA) system and can inhibit cell proliferation and induce cell apoptosis. Therefore, Imatinib and everolimus may be an effective combination of candidates for drugs for mouse pituitary tumor.


Assuntos
Neoplasias Hipofisárias , Camundongos , Animais , Proteínas Proto-Oncogênicas c-akt/metabolismo , Proteínas Proto-Oncogênicas c-akt/farmacologia , Everolimo/farmacologia , Mesilato de Imatinib/farmacologia , Proteína Supressora de Tumor p53/metabolismo , Proteína Supressora de Tumor p53/farmacologia , Caspase 3/metabolismo , Caspase 3/farmacologia , Ciclina E/metabolismo , Ciclina E/farmacologia , Pró-Opiomelanocortina/genética , Pró-Opiomelanocortina/metabolismo , Linhagem Celular Tumoral , Hormônio Adrenocorticotrópico/metabolismo , Apoptose , RNA Mensageiro/farmacologia , Proliferação de Células
6.
Front Oncol ; 12: 895678, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36081558

RESUMO

Hepatocellular carcinoma (HCC) is one of the most common malignant tumors. Hepatectomy, liver transplantation, and ablation are the three radical treatments for early-stage hepatocellular carcinoma (ESHCC), but not all patients are fit for or can tolerate surgery; moreover, liver donors are limited. Therefore, ablation plays an important role in the treatment of ESHCC. However, some studies have shown that ablation has a higher local recurrence (LR) rate than hepatectomy and liver transplantation. The specific mechanism is unknown. The latest perspectives on the mechanism of recurrence after ablation of HCC were described and summarized. In this review, we discussed the possible mechanisms of recurrence after ablation of HCC, including epithelial-mesenchymal transition (EMT), activating autophagy, changes in non-coding RNA, and changes in the tumor microenvironment. A systematic and comprehensive understanding of the mechanism will contribute to the research and development of related treatment, combined with ablation to improve the therapeutic effect in patients with ESHCC.

7.
Front Oncol ; 12: 950228, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36110931

RESUMO

Background: Tongue cancer is a common malignant tumor of the head and neck. Its treatment methods include surgery, radiotherapy, and chemotherapy. However, these treatments have serious side effects and poor cosmetic effect, so it is urgent to find new treatment methods. We pioneered the use of microwave ablation (MWA) in the treatment of early tongue cancer and achieved good results. Case Presentation: A 67-year-old woman (Han nationality) was admitted to the hospital because of progressive aggravation of tongue pain. She had a history of tongue pain of more than 1 year. Pathological biopsy showed squamous cell carcinoma; following this, radical operation of the tongue cancer was planned. The preoperative examination showed thyroid occupation in the upper mediastinum region compressing the airway; hence, the risk of general anesthesia was high. Consent was obtained from the patient and her family. Ultrasound-guided MWA was successfully performed under the lingual nerve block. The patient was followed for 1 year. She recovered well with no dysphagia and unclear articulation symptoms, and the cosmetic effect was excellent. Conclusion: To our knowledge, this is the first case of using MWA for the treatment of early-stage tongue cancer (ESTC). Ultrasound-guided MWA may be used for ESTC that can completely ablate the tumor and retain the function of the tongue, further improving the quality of life of the patient. However, it is only a case report and needs more research to verify the use of MWA in ESTC.

9.
Front Surg ; 9: 837008, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35425803

RESUMO

Objective: The study aimed to explore the efficacy and safety of modified transfrontal puncture drainage in patients with hypertensive basal ganglia hemorrhage. Methods: The study enrolled 102 patients with hypertensive basal ganglia hemorrhage who received treatment at our hospital between April 2020 and June 2020. They were divided into a control group (51 cases, burr hole evacuation of intracranial hematoma) and a study group (51 cases, modified transfrontal puncture drainage) using the random number table method. The operative time, hematoma evacuation rate, time to recovery of consciousness, postoperative Glasgow coma scales (GOS), and the length of hospital stay were compared between the two groups. The postoperative recovery of neurological function in the two groups was observed, and activities of daily living at 3 months postoperatively in the two groups were statistically analyzed. The postoperative complications and recurrent bleeding, as well as prognosis in the two groups, were recorded. Results: The operative time, hematoma evacuation rate, time to recovery of consciousness, postoperative GOS scores, time to extubation, and the length of hospital stay of the two groups were compared postoperatively, and the difference was statistically significant (p < 0.05). The preoperative neurological function of the two groups was compared, and the difference was statistically insignificant (P > 0.05). The postoperative neurological function of the study group was lower than that of the control group, and the difference was statistically significant (P < 0.05). The postoperative incidence of stress ulcer, renal failure, and recurrent bleeding in the two groups was compared, and the difference was statistically insignificant (p > 0.05). The rate of pulmonary infections and gastrointestinal bleeding in the study group was lower than that of the control group, and the difference was statistically significant (P < 0.05). The mortality rate of the study group was 1.96% (1/51) and that of the control group was 3.92% (2/51), and the difference was statistically insignificant (p > 0.05). The activities of daily living in the two groups were compared and the difference was statistically insignificant (p > 0.05). Conclusion: Modified transfrontal puncture drainage can effectively treat hypertensive basal ganglia hemorrhage patients and has relatively good safety.

13.
J Neuropathol Exp Neurol ; 81(2): 127-134, 2022 01 29.
Artigo em Inglês | MEDLINE | ID: mdl-35015875

RESUMO

Autism is a common neurodevelopmental disorder that severely affects patients' quality of life. We aimed to investigate whether acupuncture at Zusanli (ST36) could alleviate the behavior disorder of autistic rats by inhibiting thioredoxin-interacting protein (TXNIP)-mediated activation of NLRP3. An autism model was induced by intraperitoneal injection of pregnant rats with valproic acid (VPA). The pups' behaviors were analyzed using hot plate, open field, Morris water maze, and 3-chamber social interaction tests. Nissl staining was used to visualize neurons in prefrontal cortex. Levels of TXNIP, NLRP3, interleukin (IL)-1ß, and caspase were determined by Western blot or quantitative real-time PCR. After ST36 acupuncture, pain sensitivity, autonomous activity, sociability index, sociability preference index, and learning and memory were improved in the autism model rats. Levels of TXNIP, NLRP3, IL-1ß, and caspase 1 were decreased after acupuncture. Interference with TXNIP alleviated the behavior disorders and inhibited NLRP3, caspase 1, and IL-1ß levels. In summary, ST36 acupuncture reduced TXNIP expression, inhibited the activation of the NLRP3 inflammasome, and alleviated the behavior disorder related to the prefrontal cortex of the autistic rats. These results point to a potential mechanism for acupuncture-induced improvement of autistic behavioral disorders.


Assuntos
Terapia por Acupuntura/métodos , Transtorno Autístico/metabolismo , Proteínas de Ciclo Celular/metabolismo , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Córtex Pré-Frontal/metabolismo , Pontos de Acupuntura , Animais , Comportamento Animal/fisiologia , Modelos Animais de Doenças , Ratos , Ratos Sprague-Dawley
14.
Mitochondrial DNA B Resour ; 7(1): 66-67, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-34993312

RESUMO

Fopius arisanus (Sonan, 1932), an important egg parasitoid of several notorious tephritid pests, plays a key role in biological control programs. In the present study, the whole mitochondrial genome of F. arisanus was sequenced and characterized. The mitogenome of F. arisanus is 16,425 bp in length with 14.94% GC content, and contains 13 protein-coding genes (PCGs), 22 transfer RNA genes (tRNAs), and two ribosomal RNA genes (rRNAs). The phylogenetic trees demonstrated that F. arisanus is sister group to Psyttalia concolor, P. humilis, P. lounsburyi and Diachasmimorpha longicaudata.

16.
J Econ Entomol ; 114(2): 560-570, 2021 04 13.
Artigo em Inglês | MEDLINE | ID: mdl-33459786

RESUMO

One environmentally friendly method used to manage Bactrocera dorsalis (Hendel), a key agricultural pest of substantial economic importance, is the sterile insect technique (SIT). Nevertheless, several deficiencies related to this strategy impair the success of the SIT, including the inferior performance of released sterile males compared with wild males, which could be partly solved by the utilization of gut symbionts as probiotic dietary components. In this study, a culture-dependent method was used to isolate and characterize gut-associated bacterial species in adult B. dorsalis genetic sexing strain (GSS) males. In addition, three bacterial isolates from the Enterobacteriaceae family, namely, Enterobacter sp., Morganella morganii, and Moellerella wisconsensis, were used as supplements in larval and adult diets to assess their effects on the life-history traits of irradiated males. Consistent with many previous studies, Enterobacter spp. was shown to be beneficial, with some quality control indices, such as adult size, pupal weight, survival rate under stress and nutritionally rich conditions, and mating competitiveness, being significantly increased, while slight nonsignificant increases in emergence rate and flight ability were observed. Conversely, the M. morganii and M. wisconsensis strains both had negative effects on irradiated male fitness and mating competitiveness. Our results, in combination with those of earlier studies, can contribute to improving the effectiveness of SIT application by enhancing the different aspects of augmentative rearing and biological traits of pests under laboratory rearing conditions.


Assuntos
Controle Biológico de Vetores , Tephritidae , Animais , Bactérias , Dieta , Enterobacteriaceae , Masculino , Reprodução , Comportamento Sexual Animal
17.
Behav Brain Res ; 403: 113094, 2021 04 09.
Artigo em Inglês | MEDLINE | ID: mdl-33359845

RESUMO

Autism spectrum disorder (ASD) is an immensely challenging developmental disorder characterized primarily by two core behavioral symptoms of social communication deficits and restricted/repetitive behaviors. Investigating the etiological process and identifying an appropriate therapeutic target remain as formidable challenges to overcome ASD due to numerous risk factors and complex symptoms associated with the disorder. Among the various mechanisms that contribute to ASD, the maintenance of excitation and inhibition balance emerged as a key factor to regulate proper functioning of neuronal circuitry. In this study, we employed prenatally exposed to valproic acid (VPA) to establish a validated ASD mouse model and found impaired inhibitory gamma-aminobutyric acid (GABAergic) neurotransmission through a presynaptic mechanism in these model mice, which was accompanied with decreased GABA release and GABA-A and GABA-B receptor subunits expression. And acute administration of individual GABA-A or GABA-B receptor agonists partially reversed autistic-like behaviors in the model mice. Furthermore, acute administration of the combined GABA-A and GABA-B receptor agonists palliated sociability deficits, anxiety and repetitive behaviors in the animal model of autistic-like behaviors, demonstrating the therapeutic potential of above cocktail in the treatment of ASD.


Assuntos
Transtorno do Espectro Autista/tratamento farmacológico , Comportamento Animal/efeitos dos fármacos , Agonistas de Receptores de GABA-A/farmacologia , Agonistas dos Receptores de GABA-B/farmacologia , Córtex Pré-Frontal/efeitos dos fármacos , Efeitos Tardios da Exposição Pré-Natal/tratamento farmacológico , Potenciais Sinápticos/efeitos dos fármacos , Transmissão Sináptica/efeitos dos fármacos , Ácido gama-Aminobutírico/efeitos dos fármacos , Animais , Anticonvulsivantes/farmacologia , Transtorno do Espectro Autista/induzido quimicamente , Transtorno do Espectro Autista/fisiopatologia , Modelos Animais de Doenças , Quimioterapia Combinada , Feminino , Agonistas de Receptores de GABA-A/administração & dosagem , Agonistas dos Receptores de GABA-B/administração & dosagem , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Gravidez , Efeitos Tardios da Exposição Pré-Natal/induzido quimicamente , Efeitos Tardios da Exposição Pré-Natal/fisiopatologia , Ácido Valproico/farmacologia
18.
Insects ; 11(11)2020 Nov 22.
Artigo em Inglês | MEDLINE | ID: mdl-33266412

RESUMO

Cold storage and heat exposure are crucial components of tephritid fruit fly mass-rearing programs, as they influence the development and fitness traits of produced flies. This work investigated the effects of cold storage on the pupal developmental parameters and quality of Bactrocera dorsalis (Hendel) genetic sexing strain (GSS) adults. Furthermore, the impact of short-term thermal exposure on the fecundity of B. dorsalis (GSS) that also underwent pupal cold storage was examined. Our results show that pupal development time, emergence rate, partial emergence rate, flight ability and fecundity were significantly affected by low temperature and pupal age and their interaction. Pupal cold storage did not pose negative impacts on the mating competition and response to methyl eugenol (ME) in the males. In addition, compared with the adults that were subjected to the same pupal storage protocol (five-day-old pupae stored at 13 °C), adult exposure to 41 °C for 1 h showed significant reparative effects on fecundity. In summary, the cold storage procedure of B. dorsalis (GSS) pupae has the potential to improve the flexibility and efficiency of mass-rearing schedules. Furthermore, short-term thermal exposure showed reparative effects on the fecundity costs induced by pupal cold storage in B. dorsalis (GSS).

19.
Insects ; 11(2)2020 Feb 04.
Artigo em Inglês | MEDLINE | ID: mdl-32033080

RESUMO

This study aims to evaluate several life-history traits of a T. drosophilae population from southern China and its parasitic preference of three Drosophila species. For mated T. drosophilae females, the mean oviposition and parasitization period were 27.20 and 37.80 d, respectively. The daily mean parasitization rate was 59.24% per female and the lifetime number of emerged progeny was 134.30 per female. Trichopria drosophilae females survived 37.90 and 71.61 d under host-provided and host-deprived conditions, respectively. To assess the potential for unmated reproduction in T. drosophilae, the mean oviposition and parasitization period of unmated females was 22.90 and 47.70 d, respectively. They had a daily mean parasitization rate of 64.68%, produced a total of 114.80 offspring over their lifetime, and survived 52 d. Moreover, T. drosophilae showed a preference towards D. suzukii based on the total number of emerged offspring under a choice test. Our findings indicate that T. drosophilae from southern China appears to be suitable for the control of D. suzukii in invaded areas, due to its reproductive potential.

20.
Cancer Biother Radiopharm ; 34(9): 597-603, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31644317

RESUMO

Purpose: The purpose of this study was to evaluate melanoma-targeting property of 90Y-DOTA-GGNle-CycMSHhex to facilitate its potential therapeutic application. Materials and Methods: DOTA-GGNle-CycMSHhex was synthesized and readily labeled with 90Y in 0.25 M NH4Ac-buffered solution to generate 90Y-DOTA-GGNle-CycMSHhex. The specific receptor binding, internalization, and efflux of 90Y-DOTA-GGNle-CycMSHhex were determined on B16/F10 murine melanoma cells. The biodistribution property of 90Y-DOTA-GGNle-CycMSHhex was examined on B16/F10 melanoma-bearing C57 mice. Results: 90Y-DOTA-GGNle-CycMSHhex displayed receptor-specific binding, rapid internalization, and prolonged efflux on B16/F10 melanoma cells. 90Y-DOTA-GGNle-CycMSHhex exhibited high uptake and prolonged retention in melanoma, and fast urinary clearance on B16/F10 melanoma-bearing C57 mice. The B16/F10 tumor uptake was 20.73% ± 7.99%, 19.93% ± 5.73%, 14.8% ± 4.61%, and 6.69% ± 1.85% ID/g at 0.5, 2, 4, and 24 h postinjection, respectively. Conclusions: 90Y-DOTA-GGNle-CycMSHhex displayed melanocortin-1 receptor (MC1R) targeting and specificity on B16/F10 melanoma cells and tumors. The favorable melanoma-targeting property and fast urinary clearance of 90Y-DOTA-GGNle-CycMSHhex warranted its evaluation for melanoma therapy in future studies.


Assuntos
Lactamas/farmacocinética , Melanoma Experimental/metabolismo , Compostos Radiofarmacêuticos/farmacocinética , Radioisótopos de Ítrio/farmacocinética , alfa-MSH/farmacocinética , Animais , Linhagem Celular Tumoral , Compostos Heterocíclicos com 1 Anel/química , Compostos Heterocíclicos com 1 Anel/farmacocinética , Lactamas/química , Melanoma Experimental/diagnóstico por imagem , Melanoma Experimental/patologia , Camundongos , Camundongos Endogâmicos C57BL , Estrutura Molecular , Compostos Radiofarmacêuticos/síntese química , Compostos Radiofarmacêuticos/química , Distribuição Tecidual , Tomografia Computadorizada de Emissão de Fóton Único , Ensaios Antitumorais Modelo de Xenoenxerto , Radioisótopos de Ítrio/química , alfa-MSH/química
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