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1.
Eur J Med Chem ; 257: 115492, 2023 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-37210838

RESUMO

Multiple myeloma (MM) is a hematologic neoplasm of plasma cells that is currently deemed incurable. Despite the introduction of novel immunomodulators and proteasome inhibitors, MM remains a challenging disease with high rates of relapse and refractoriness. The management of refractory and relapsed MM patients remains a formidable task, primarily due to the emergence of multiple drug resistance. Consequently, there is an urgent need for novel therapeutic agents to address this clinical challenge. In recent years, a significant amount of research has been dedicated to the discovery of novel therapeutic agents for the treatment of MM. The clinical utilization of proteasome inhibitor carfilzomib and immunomodulator pomalidomide has been successively introduced. As basic research continues to advance, novel therapeutic agents, including panobinostat, a histone deacetylase inhibitor, and selinexor, a nuclear export inhibitor, have progressed to the clinical trial and application phase. This review aims to furnish a comprehensive survey of the clinical applications and synthetic pathways of select drugs, with the intention of imparting valuable insights for future drug research and development geared towards MM.


Assuntos
Mieloma Múltiplo , Humanos , Mieloma Múltiplo/tratamento farmacológico , Recidiva Local de Neoplasia/tratamento farmacológico , Panobinostat/uso terapêutico , Inibidores de Histona Desacetilases/uso terapêutico , Inibidores de Proteassoma , Fatores Imunológicos/farmacologia , Fatores Imunológicos/uso terapêutico , Protocolos de Quimioterapia Combinada Antineoplásica/uso terapêutico
2.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-773175

RESUMO

The specifications of Chinese herbal medicines naturally form and exist in the circulation and use of Chinese herbal medicines.Buyers and sellers negotiate price by quality. With the increasing demand for public health care,the cultivation,processing methods and circulation of Chinese herbal medicines have changed. Under the mode of pursuing output and short-term benefits,the traditional grade evaluation method has been difficult to apply to the current quality status of the pieces. Bran stir-baked Aurantii Fructus is a genuine medicinal material in Jiangxi province. It is widely used,but the quality level of bran stir-baked Aurantii Fructus on the market is not uniform. Quality constant method was used in this paper for grading the Chinese herbal slices of bran stir-baked Aurantii Fructus. Sixteen batches of different quality samples were collected and tested,and finally,eleven qualified batches of them were chosen as researcher objects. The results showed that the relative quality constant ranged from 2. 52 to 5. 60. The relative quality constant was ≥4. 48 for first grade bran stir-baked Aurantii Fructus,2. 80-4. 48 for the second grade pieces,and <2. 80 for the third grade pieces. The grades evaluation method for bran stir-baked Aurantii Fructus established in this paper included both appearance and index composition. The results were objective,accurate,quantitative,applicable,and the method was simple to operate and easy to popularize. This study showed that the quality constant method could be applied to the grade evaluation of bran stir-baked Aurantii Fructus,providing a reference for the grade evaluation of fruit-type decoction pieces.


Assuntos
Citrus , Química , Medicamentos de Ervas Chinesas , Padrões de Referência , Frutas , Química , Controle de Qualidade
3.
Knee ; 24(6): 1289-1298, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28970120

RESUMO

BACKGROUND: The iliotibial band (ITB) trifurcates into the anterior, central and posterior branches at the knee level, and sometimes the branches must be selectively released to correct the valgus knee deformity during total knee arthroplasty. However, the anatomical morphology of the trifurcate ITBs has not been investigated. METHODS: Fifty-two knees from 26 embalmed cadavers were dissected to observe and record the relationship of the three branches given off from the ITB trifurcation. Fourteen parameters with regard to the length, width, thickness, and trifurcate angle of each branch were measured. These parameters were compared between sex and sides (left or right). Meanwhile, the correlations between parameters and subject age, weight and height were assessed. RESULTS: The longest, widest and thickest branches of the ITB were the posterior band (59.82±5.14mm), anterior band (39.56±4.17mm) and central band (2.61±0.36mm), respectively. The length and thickness of ITB were significantly larger in males than in females (P<0.05). No significant differences were found between sides (P>0.05). The ITB thickness showed a negative correlation with subject age, while the length and width of the ITB were positively correlated with subject height and weight, respectively. CONCLUSIONS: This study provided an anatomical reference of trifurcate ITBs to help the release of ITB in valgus knees. The anatomical variations regarding the subject's sex, age, height and weight should be considered in the selective release of ITB.


Assuntos
Fáscia/anatomia & histologia , Geno Valgo/cirurgia , Articulação do Joelho/cirurgia , Adulto , Fatores Etários , Idoso , Estatura , Peso Corporal , Cadáver , Fasciotomia , Feminino , Humanos , Masculino , Pessoa de Meia-Idade
4.
Artigo em Inglês | WPRIM (Pacífico Ocidental) | ID: wpr-812291

RESUMO

AIM@#This study was designed to evaluate the anti-cancer actions of tanshinone I and tanshinone IIA, and six derivatives of tanshinone IIA on normal and cancerous colon cells. Structure activity relationship (SAR) analysis was conducted to delineate the significance of the structural modifications of tanshinones for improved anti-cancer action.@*METHOD@#Tanshinone derivatives were designed and synthesized according to the literature. The cytotoxicity of different compounds on colon cancer cells was determined by the MTT assay. Apoptotic activity of the tanshinones was measured by flow cytometry (FCM).@*RESULTS@#Tanshinone I and tanshinone IIA both exhibited significant cytotoxicity on colon cancer cells. They are more effective in p53(+/+) colon cancer cell line. It was also noted that the anti-cancer activity of tanshinone I was more potent and selective. Two of the derivatives of tanshinone IIA (N1 and N2) also exhibited cytotoxicity on colon cancer cells.@*CONCLUSION@#The anti-colon cancer activity of tanshinone I was more potent and selective than tanshinone IIA, and is p53 dependent. The derivatives obtained by structural modifications of tanshinone IIA exhibited lower cytotoxicity on both normal and colon cancer cells. From steric and electronic characteristics point of view, it was concluded that structural modifications of ring A and furan or dihydrofuran ring D on the basic structure of tanshinones influences the activity. An increase of the delocalization of the A and B rings could enhance the cytotoxicity of such compounds, while a non-planar and small sized D ring region would provide improved anti-cancer activity.


Assuntos
Humanos , Abietanos , Química , Farmacologia , Usos Terapêuticos , Antineoplásicos Fitogênicos , Química , Farmacologia , Usos Terapêuticos , Linhagem Celular , Colo , Neoplasias do Colo , Tratamento Farmacológico , Medicamentos de Ervas Chinesas , Química , Farmacologia , Usos Terapêuticos , Células HCT116 , Células HT29 , Fitoterapia , Salvia miltiorrhiza , Química , Relação Estrutura-Atividade
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