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1.
Chem Biodivers ; 21(2): e202301703, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38055204

RESUMO

Three undescribed limonoids (1-3), named aglaians G-I, and one new natural product azedaralide (4), together with nine known analogues (5-13) were isolated from the branches and leaves of Aglaia lawii by RP C18 column, silica gel column, Sephadex LH-20 column chromatography and preparative HPLC. The structures of the new compounds were elucidated by IR, HRESIMS, 1D, 2D NMR, electronic circular dichroism (ECD) calculations and X-ray crystallography diffraction analysis. The results of bioassay showed that the compound 12 exhibited potential inhibitory activity against six human tumor cell lines (MDA-MB-231, MCF-7, Ln-cap, A549, HeLa and HepG-2) with IC50 values as 8.0-18.6 µM.


Assuntos
Aglaia , Antineoplásicos , Limoninas , Humanos , Aglaia/química , Limoninas/farmacologia , Limoninas/química , Estrutura Molecular , Linhagem Celular Tumoral
2.
Chem Biodivers ; 21(3): e202400184, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38372676

RESUMO

The phytochemical study of Peucedanum praeruptorum led to the isolation of twenty-five coumarins (1-25). Of which, (±) praeruptol A (±1), one pair of previous undescribed seco-coumarin enantiomers were obtained. Their structures were established according to HR-ESI-MS, NMR, X-ray single crystal diffraction analysis, as well as ECD calculation. All compounds were tested for anti-inflammatory activity in the RAW264.7 macrophage model, and eight compounds (7-10, and 13-16) exhibited significant inhibitory effects with IC50 values ranging from 9.48 to 34.66 µM. Among them, compound 7 showed the strongest inhibitory effect, which significantly suppressed the production of IL-6, IL-1ß, and TNF-α, as well as iNOS and COX-2 in a concentration-dependent manner. Further investigated results showed that compound 7 exerted an anti-inflammatory effect via the NF-κB signaling pathway.


Assuntos
Cumarínicos , NF-kappa B , NF-kappa B/metabolismo , Cumarínicos/farmacologia , Cumarínicos/metabolismo , Anti-Inflamatórios/farmacologia , Extratos Vegetais/química , Transdução de Sinais , Lipopolissacarídeos/farmacologia
3.
Chem Biodivers ; 21(5): e202400030, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38511964

RESUMO

A traditional Chinese medicine ingredient, dendrobine, has been demonstrated to have anti-inflammatory properties. However, due to its poor anti-inflammatory properties, its clinical use is limited. Consequently, we have designed and synthesized 32 new amide/sulfonamide dendrobine derivatives and screened their anti-inflammatory activities in vitro. Experiments showed that nitric oxide (NO) generation in lipopolysaccharide (LPS)-induced RAW264.7 cells was strongly reduced by derivative 14, with an IC50 of 2.96 µM. Western blot research revealed that 14 decreased the concentration-dependent expression of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (INOS). Molecular docking was used to predict the binding of the inflammation-associated proteins COX-2 and INOS to compound 14.


Assuntos
Amidas , Ciclo-Oxigenase 2 , Lipopolissacarídeos , Simulação de Acoplamento Molecular , Óxido Nítrico Sintase Tipo II , Óxido Nítrico , Sulfonamidas , Animais , Camundongos , Células RAW 264.7 , Sulfonamidas/química , Sulfonamidas/farmacologia , Sulfonamidas/síntese química , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Óxido Nítrico Sintase Tipo II/metabolismo , Óxido Nítrico Sintase Tipo II/antagonistas & inibidores , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico/biossíntese , Óxido Nítrico/metabolismo , Ciclo-Oxigenase 2/metabolismo , Amidas/química , Amidas/farmacologia , Amidas/síntese química , Relação Estrutura-Atividade , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/síntese química , Estrutura Molecular , Relação Dose-Resposta a Droga , Anti-Inflamatórios não Esteroides/farmacologia , Anti-Inflamatórios não Esteroides/síntese química , Anti-Inflamatórios não Esteroides/química
4.
Zhongguo Zhong Yao Za Zhi ; 49(13): 3552-3565, 2024 Jul.
Artigo em Zh | MEDLINE | ID: mdl-39041127

RESUMO

Based on UHPLC-Q-Exactive Orbitrap HRMS coupled with the network pharmacology and molecular docking, the common material basis and molecular mechanisms of Bletillae Rhizoma for melasma, gastrointestinal hemorrhage, lung cancer and bronchoplumonary inflammation as "homotherapy for heteropathy" were explored. The fingerprint of 17 batches of Bletillae Rhizoma from different areas was established using HPLC, and the similarity analysis was carried out. The common chemical components of the 17 batches of Bletillae Rhizoma were identified using UHPLC-Q-Exactive Orbitrap HRMS. Depending on the bioavailability and drug-like properties of the common components, the active chemical components were screened, and then their protein targets were collected using the Traditional Chinese Medicine Database and Analysis Platform(TCMSP) and SwissTargetPrediction database. The protein targets related to diseases were retrieved from the databases DrugBank, TTD and GeneCards to produce a Venn diagram. The shared targets were obtained between drugs and diseases as "homotherapy for heteropathy" targets. The protein-protein interaction(PPI) was analyzed with the STRING database, and KEGG and GO analyses of the "homotherapy for heteropathy" targets were performed using the Bioconductor database. Cytoscape 3.7.2 software was employed to construct the "chemical components of Bletillae Rhizoma-homotherapy for heteropathy targets" network and PPI network, and topological analysis was conducted to screen out the key active chemical components and core targets. Finally, the affinity between the active components and core targets was evaluated using the molecular docking by AutoDock Vina 4.2.6, which verified the interaction between them. Thirteen common peaks were identified by fingerprint chromatography, and the similarity between different batches was 0.941-0.998. Fifty-three chemical components were identified by mass spectrometry in Bletillae Rhizoma, and 18 common chemical constituents were obtained in the 17 batches of Bletillae Rhizoma. Network pharmacologic screening showed that the pharmacodynamic substances of Bletillae Rhizoma for melasma, gastrointestinal hemo-rrhage, lung cancer and bronchoplumonary inflammation with "homotherapy for heteropathy" were 11 compounds, such as polysaccharides, biphenanthrenes, dihydrophenanthrenes and bibenzyls. There were 42 common targets identified for the treatment of different diseases. These targets were involved in biological processes such as cell response to chemical stress, reactive oxygen species and positive regulation of protein kinase B signal transduction. They were also involved in 121 signaling pathways, encompassing vital pathways such as PI3K-Akt, ErbB, Rap1, FoxO, MAPK and estrogen. Molecular docking results showed a strong affinity between the key active components and the core targets. This study provides a preliminary explanation of how Bletillae Rhizoma exerts its therapeutic effect on chloasma, gastrointestinal hemorrhage, lung cancer, and bronchopneumonic lesions as "homotherapy for heteropathy" through a combined action involving multiple components, targets, and pathways. These findings offer a certain theoretical basis for the further deve-lopment and application of Bletillae Rhizoma.


Assuntos
Medicamentos de Ervas Chinesas , Neoplasias Pulmonares , Simulação de Acoplamento Molecular , Farmacologia em Rede , Rizoma , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Humanos , Cromatografia Líquida de Alta Pressão , Rizoma/química , Neoplasias Pulmonares/tratamento farmacológico , Hemorragia Gastrointestinal/tratamento farmacológico , Melanose/tratamento farmacológico , Orchidaceae/química , Inflamação/tratamento farmacológico , Espectrometria de Massas
5.
Inorg Chem ; 62(49): 20467-20476, 2023 Dec 11.
Artigo em Inglês | MEDLINE | ID: mdl-38019638

RESUMO

Solid-state materials with efficient room-temperature phosphorescence (RTP) emission have been widely used in materials science, and organic RTP-emitting systems with heavy-metal doping in aqueous solutions have attracted much attention in recent years. A novel supramolecular interaction was induced by host-guest assembly using cucurbit[7]uril (Q[7]) as the host and brominated naphthalimide phosphor as the guest. This interaction was further enhanced through synergistic chelation stimulated by analytical silver ion complexation. This approach facilitated the system's structural rigidity, intersystem crossing, and oxygen shielding. We achieved deep red phosphorescence emission in aqueous solution and ambient conditions along with quantitative determination of silver ions. The new complex exhibited good reversible thermoresponsive behavior and was successfully applied for the first time to target phosphorescence imaging of silver ions in the mitochondria of A549 cancer cells. These results are beneficial for constructing novel RTP systems with stimulus-responsive luminescence in aqueous solution, contributing to future research in bioimaging, detection, optical sensors, and thermometry materials.

6.
Chem Biodivers ; 20(8): e202300691, 2023 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-37329501

RESUMO

Three new compounds, including two new sesquiterpenes (1-2), named Annuumine E-F, and one new natural product, 3-hydroxy-2,6-dimethylbenzenemethanol (3), together with seventeen known compounds (4-20) were isolated from the ethanol extract of the roots of Capsicum annuum L. Among them, five compounds (4, 5, 9, 10 and 20) were isolated from this plant for the first time. The structures of new compounds (1-3) were determined via detailed analysis of the IR, HR-ESI-MS and 1D and 2D NMR spectra. The anti-inflammatory activities of the isolated compounds were evaluated by their ability to reduce NO release by LPS-induced RAW 264.7 cells. Notably, compound 11 exhibited moderate anti-inflammatory activity (IC50 =21.11 µM). Moreover, the antibacterial activities of the isolated compounds were also evaluated.


Assuntos
Capsicum , Animais , Camundongos , Capsicum/química , Estrutura Molecular , Células RAW 264.7 , Anti-Inflamatórios/química , Antibacterianos/farmacologia
7.
Angew Chem Int Ed Engl ; 62(51): e202313687, 2023 Dec 18.
Artigo em Inglês | MEDLINE | ID: mdl-37950324

RESUMO

Herein, we report an unprecedented skeletal rearrangement reaction of tetrahydro-ß-carbolines enabled by copper-catalyzed single-electron oxidative oxygenation, in which H2 O and O2 act as oxygen sources to generate a unique 2-hydroxyl-3-peroxide indoline intermediate. The synthetic reactivity of 2-hydroxyl-3-peroxide indoline species was demonstrated by a unique multi-step bond cleavage and formation cascade. Using a readily available copper catalyst under open-air conditions, highly important yet synthetically difficult spiro[pyrrolidone-(3,1-benzoxazine)] products were obtained in a single operation. The synthetic utility of this methodology is demonstrated by the efficient synthesis of the natural products donaxanine and chimonamidine, as well as the 3-hydroxyl-pyrroloindoline scaffold, in just one or two steps.

8.
Molecules ; 27(13)2022 Jun 23.
Artigo em Inglês | MEDLINE | ID: mdl-35807286

RESUMO

As a typical dibenzylisoquinoline alkaloid, tetrandrine (TET) is clinically used for the treatment of silicosis, inflammatory pulmonary, and cardiovascular diseases in China. Recent investigations have demonstrated the outstanding anticancer activity of this structure, but its poor aqueous solubility severely restricts its further development. Herein, a series of its 14-N-amino acid-substituted derivatives with improved anticancer effects and aqueous solubility were designed and synthesized. Among them, compound 16 displayed the best antiproliferative activity against human colorectal cancer (HCT-15) cells, with an IC50 value of 0.57 µM. Compared with TET, 16 was markedly improved in terms of aqueous solubility (by 5-fold). Compound 16 significantly suppressed the colony formation, migration, and invasion of HCT-15 cells in a concentration-dependent manner, with it being more potent in this respect than TET. Additionally, compound 16 markedly impaired the morphology and motility of HCT-15 cells and induced the death of colorectal cancer cells in double-staining and flow cytometry assays. Western blot results revealed that 16 could induce the autophagy of HCT-15 cells by significantly decreasing the content of p62/SQSTM1 and enhancing the Beclin-1 level and the ratio of LC3-II to LC3-I. Further study showed that 16 effectively inhibited the proliferation, migration, and tube formation of umbilical vein endothelial cells, manifesting in a potent anti-angiogenesis effect. Overall, these results revealed the potential of 16 as a promising candidate for further preclinical studies.


Assuntos
Antineoplásicos , Neoplasias Colorretais , Aminoácidos/farmacologia , Antineoplásicos/química , Apoptose , Benzilisoquinolinas , Linhagem Celular Tumoral , Proliferação de Células , Neoplasias Colorretais/tratamento farmacológico , Ensaios de Seleção de Medicamentos Antitumorais , Células Endoteliais , Humanos , Estrutura Molecular , Relação Estrutura-Atividade
9.
J Hepatol ; 75(4): 900-911, 2021 10.
Artigo em Inglês | MEDLINE | ID: mdl-34004215

RESUMO

BACKGROUND & AIMS: Contradictory roles of the androgen receptor (AR) in hepatocellular carcinoma (HCC) metastasis have been reported. We have shown that VETC (vessels encapsulating tumor clusters) mediates invasion-independent metastasis, whereas VETC- HCCs metastasize in an invasion-dependent manner. Herein, we aimed to reveal the roles of AR in HCC metastasis. METHODS: Mouse xenograft models, clinical samples, and cell models were used. RESULTS: AR expression was significantly lower in HCCs with a VETC pattern, portal vein tumor thrombus, endothelium-coated microemboli or high recurrence rates. Overexpressing AR in VETC+ hepatoma cells suppressed VETC formation and intrahepatic metastasis but promoted pulmonary metastasis of mouse xenografts. AR decreased the transcription of Angiopoietin-2 (Angpt2), a factor essential for VETC formation, by binding to the Angpt2 promoter. The roles of AR in inhibiting VETC formation and intrahepatic metastasis were attenuated by restoring Angpt2 expression, suggesting that AR may repress VETC-dependent intrahepatic metastasis by inhibiting Angpt2 expression and VETC formation. On the other hand, AR upregulated Rac1 expression, promoted lamellipodia formation and increased cell migration/invasion. A Rac1 inhibitor abrogated the AR-mediated promotion of migration/invasion and pulmonary metastasis of VETC+ hepatoma cells, but did not affect the AR-mediated inhibition of intrahepatic metastasis. Furthermore, an AR inhibitor decreased Rac1 expression and attenuated both intrahepatic and pulmonary metastasis of VETC- xenografts, an effect which was abrogated by restoring Rac1 expression. These data indicate that AR may facilitate the lung metastasis of VETC+ HCCs and both the liver/lung metastases of VETC- HCCs by upregulating Rac1 expression and then promoting migration/invasion. CONCLUSION: AR plays dual and opposing roles in VETC-dependent and invasion-dependent metastasis, which highlights the complex functions of AR and the importance of individualized cancer therapy. LAY SUMMARY: In this study, we uncovered the dual and opposing roles of the androgen receptor in VETC (vessels encapsulating tumor clusters)-dependent and invasion-dependent metastasis of hepatocellular carcinoma (HCC). We elucidated the underlying mechanisms of these processes, which provided novel insights into the complex regulatory network of the androgen receptor in HCC metastasis and may have important implications for precision medicine.


Assuntos
Neoplasias Hepáticas/etiologia , Metástase Neoplásica/imunologia , Receptores Androgênicos/análise , Animais , Estudos de Coortes , Modelos Animais de Doenças , Neoplasias Hepáticas/fisiopatologia , Camundongos , Metástase Neoplásica/prevenção & controle
10.
J Org Chem ; 86(23): 17164-17172, 2021 12 03.
Artigo em Inglês | MEDLINE | ID: mdl-34709032

RESUMO

The first transition metal catalytic one-step synthesis of the 3a, 3a'-bispyrrolidino [2,3-b] indoline scaffold via tandem cyclization/dimerization of tryptamines has been realized with the environmentally friendly O2/air as the sole oxidant. Different from the traditional direct oxidation of indole "N-H" group by excess amount of metal salts, a copper-catalyzed oxidative cyclization reaction is developed for the formation of the radical pyrrolidinoindoline intermediate in the current strategy. The robustness and practicality of this methodology is demonstrated by the step-economic, divergent total synthesis of natural products (±)-folicanthine and meso-folicanthine.


Assuntos
Cobre , Triptaminas , Catálise , Ciclização , Dimerização , Indóis , Oxidantes
11.
Bioorg Chem ; 101: 104025, 2020 08.
Artigo em Inglês | MEDLINE | ID: mdl-32599368

RESUMO

Metastatic progression of cancer is a complex and clinically daunting process, with migration, invasion and angiogenesis being the key features. Tetrandrine (TET) is a typical dibenzylisoquinoline alkaloid with promising anti-tumor activity. In our previous work, a number of TET derivatives were designed and synthesized with obvious anti-proliferation activities against cancer cells, however, the anti-metastatic effects of these compounds were not evaluated. In the current investigation, five TET derivatives (8, 18, 32, 71, and 72) with pronounced anti-proliferative activities (IC50 values of 1.00, 1.91, 3.43, 3.78, and 1.93 µM, respectively) against human umbilical vein endothelial cells (HUVECs) were screened out. Scratch assays showed that these compounds significantly suppressed the migration of HUVECs and induced their apoptosis. Among them, derivatives 8 and 72 obviously inhibited the proliferation, colony formation and invasion of HCT-15 cells. Tube formation assays revealed that 4 µM of 8 or 72 remarkably inhibited the tube forming capacity of HUVECs. Moreover, 8 and 72 surpressed the formation of filopodia in HUVECs and severely impaired their motility. Both compounds effectively inhibited the angiogenesis in the zebrafish model with low toxicities in vivo. These results indicated that TET derivatives 8 and 72 are promising anti-metastatic inhibitors.


Assuntos
Inibidores da Angiogênese/uso terapêutico , Antineoplásicos Fitogênicos/uso terapêutico , Benzilisoquinolinas/uso terapêutico , Células Endoteliais da Veia Umbilical Humana/efeitos dos fármacos , Neoplasias/tratamento farmacológico , Inibidores da Angiogênese/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Benzilisoquinolinas/farmacologia , Linhagem Celular Tumoral , Movimento Celular , Humanos , Invasividade Neoplásica , Neoplasias/genética
12.
Molecules ; 25(7)2020 Apr 09.
Artigo em Inglês | MEDLINE | ID: mdl-32283819

RESUMO

Tetrandrine, a dibenzyltetrahydroisoquinoline alkaloid isolated from the root of the traditional Chinese medicinal plant Stephania tetrandra S. Moore, a member of the Menispermaceae, showed anti-cancer activity by inhibiting cell proliferation, preventing cell cycle progress and induction of cell death and autophagy. In this study, twelve tetrandrine-l-amino acid derivatives and twelve tetrandrine-14-l-amino acid-urea derivatives were designed and synthesized, using C14-aminotetrandrine as raw material. Then the preliminary in vitro anti-cancer activities of these derivatives against human breast cancer cell line MDA-MB-231, human leukemia cell lines HEL and K562 were evaluated. The in vitro cytotoxicity results showed that these derivatives exhibited potent inhibitory effects on cancer cell growth, and the primary structure-activity relationships were evaluated. Notably, compound 3f exhibited satisfactory anticancer activity against all three cancer cell lines, especially the HEL cell line, with the IC50 value of 0.23 µM. Further research showed that 3f could induce G1/S cycle arrest and apoptosis in a dose- and time- dependent manner on the leukemia cell line HEL. The results suggested that 3f may be used as a potential anti-cancer agent for human leukemia.


Assuntos
Aminoácidos/química , Antineoplásicos/química , Antineoplásicos/farmacologia , Benzilisoquinolinas/química , Técnicas de Química Sintética , Desenho de Fármacos , Ureia/química , Antineoplásicos/síntese química , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Relação Estrutura-Atividade
13.
Molecules ; 24(15)2019 Jul 26.
Artigo em Inglês | MEDLINE | ID: mdl-31357486

RESUMO

Seventeen new flavone derivatives substituted at the 4'-OH position were designed, synthesized and evaluated for their anticancer and antibacterial activities. Among them, compounds 3, 4, 6f, 6e, 6b, 6c and 6k demonstrated the most potent antiproliferative activities against a human erythroleukemia cell line (HEL) and a prostate cancer cell line (PC3). The results also showed that the IC50 value of compounds 3, 4, 6f, 6e, 6b, 6c and 6k were close to that of the anticancer drug cisplatin (DDP) and lower than that of apigenin. All of the derivatives did not present antibacterial activities. The structure-activity relationships evaluation showed that the configuration of methyl amino acid might affect their biological activities.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Flavonas/química , Flavonas/farmacologia , Antineoplásicos/síntese química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Técnicas de Química Sintética , Relação Dose-Resposta a Droga , Flavonas/síntese química , Humanos , Estrutura Molecular , Relação Estrutura-Atividade
14.
Molecules ; 24(9)2019 May 06.
Artigo em Inglês | MEDLINE | ID: mdl-31064088

RESUMO

Flavonoids are well-characterized polyphenolic compounds with pharmacological and therapeutic activities. However, most flavonoids have not been developed into clinical drugs, due to poor bioavailability. Herein, we report a strategy to increase the drugability of flavonoids by constructing C(sp2)-O bonds and stereo- as well as regioselective alkenylation of hydroxyl groups of flavonoids with ethyl-2,3-butadienoate allenes. Twenty-three modified flavonoid derivatives were designed, synthesized, and evaluated for their anti-cancer activities. The results showed that compounds 4b, 4c, 4e, 5e, and 6b exhibited better in vitro inhibitory activity against several cancer cell lines than their precursors. Preliminary structure-activity relationship studies indicated that, in most of the cancer cell lines evaluated, the substitution on position 7 was essential for increasing cytotoxicity. The results of this study might facilitate the preparation or late-stage modification of complex flavonoids as anti-cancer drug candidates.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/uso terapêutico , Éteres/química , Flavonoides/síntese química , Flavonoides/uso terapêutico , Alcadienos/química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Desenho de Fármacos , Humanos , Estrutura Molecular , Estereoisomerismo , Relação Estrutura-Atividade
15.
Molecules ; 24(22)2019 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-31731682

RESUMO

Twenty-seven L-shaped ortho-quinone analogs were designed and synthesized using a one pot double-radical synthetic strategy followed by removing methyl at C-3 of the furan ring and introducing a diverse side chain at C-2 of the furan ring. The synthetic derivatives were investigated for their cytotoxicity activities against human leukemia cells K562, prostate cancer cells PC3, and melanoma cells WM9. Compounds TB1, TB3, TB4, TB6, TC1, TC3, TC5, TC9, TC11, TC12, TC14, TC15, TC16, and TC17 exhibited a better broad-spectrum cytotoxicity on three cancer cells. TB7 and TC7 selectively displayed potent inhibitory activities on leukemia cells K562 and prostate cancer cells PC3, respectively. Further studies indicated that TB3, TC1, TC3, TC7, and TC17 could significantly induce the apoptosis of PC3 cells. TC1 and TC17 significantly induced apoptosis of K562 cells. TC1, TC11, and TC14 induced significant apoptosis of WM9 cells. The structure-activity relationships evaluation showed that removing methyl at C-3 of the furan ring and introducing diverse side chains at C-2 of the furan ring is an effective strategy for improving the anticancer activity of L-shaped ortho-quinone analogs.


Assuntos
Antineoplásicos , Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Citotoxinas , Neoplasias , Quinonas , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Citotoxinas/síntese química , Citotoxinas/química , Citotoxinas/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Células K562 , Neoplasias/tratamento farmacológico , Neoplasias/metabolismo , Neoplasias/patologia , Células PC-3 , Quinonas/síntese química , Quinonas/química , Quinonas/farmacologia , Relação Estrutura-Atividade
16.
Zhongguo Yi Xue Ke Xue Yuan Xue Bao ; 41(4): 572-574, 2019 Aug 30.
Artigo em Zh | MEDLINE | ID: mdl-31484624

RESUMO

Bronchogenic cysts are rare congenital cysts caused by anomalism of foregut in the embryonic stage.They locate most frequently in the mediastinum and are rarely seen in stomach.Here we report a case of gastric bronchogenic cysts that was diagnosed and treated in Peking Union Medical College Hospital from April 2 to 9,2018.


Assuntos
Cisto Broncogênico/diagnóstico , Estômago/patologia , Humanos
17.
Dis Colon Rectum ; 61(8): 903-910, 2018 08.
Artigo em Inglês | MEDLINE | ID: mdl-29944579

RESUMO

BACKGROUND: Patients with locally advanced rectal cancer could be managed by a watch-and-wait approach if they achieve clinical complete response after preoperative chemoradiotherapy. Mucosal integrity, endorectal ultrasound, and rectal MRI are used to evaluate clinical complete response; however, the accuracy remains questionable. Clinical practice based on those assessment methods needs more data and discussion. OBJECTIVE: The aim of this prospective study was to evaluate the accuracy of mucosal integrity, endorectal ultrasound, and rectal MRI to predict clinical complete response after chemoradiotherapy. DESIGN: Endorectal ultrasound and rectal MRI were undertaken 6 to 7 weeks after preoperative chemoradiation therapy. Patients then received radical surgery based on the principles of total mesorectal excision. Preoperative tumor staging achieved by endorectal ultrasound and rectal MRI was compared with postoperative staging by pathologic examination. Sensitivity, specificity, and accuracy of each evaluation method were calculated. SETTINGS: The study was conducted at a single tertiary care center. PATIENTS: Patients diagnosed with mid-low rectal cancer by biopsy between May 2014 and December 2016 were enrolled in this study. RESULTS: A total of 124 patients were enrolled in this study, and postoperative pathology revealed that 20 patients (16.13%) achieved complete response (ypT0N0). The sensitivity of mucosal integrity, endorectal ultrasound, and MRI to predict clinical complete response was 25%. The specificity of mucosal integrity, endorectal ultrasound, and MRI was 94.23%, 93.90%, and 93.27%. The combination of each 2 or all 3 methods did not improve accuracy. Regression analysis showed that none of these methods could predict postoperative ypT0. LIMITATIONS: The sample size is small, and we did not focus on the follow-up data and cannot compare prognosis data with previous research studies. CONCLUSIONS: Both single-method and combined mucosal integrity, endorectal ultrasound, and rectal MRI have poor correlation with postoperative pathologic examination. A watch-and-wait approach based on these methods might not be a proper strategy compared with radical surgery after neoadjuvant therapy. See Video Abstract at http://links.lww.com/DCR/A693.


Assuntos
Adenocarcinoma , Quimiorradioterapia , Endossonografia/métodos , Imageamento por Ressonância Magnética/métodos , Neoplasias Retais/diagnóstico por imagem , Adenocarcinoma/diagnóstico , Adenocarcinoma/patologia , Adenocarcinoma/terapia , Idoso , Quimiorradioterapia/métodos , Quimiorradioterapia/estatística & dados numéricos , China , Feminino , Humanos , Mucosa Intestinal/diagnóstico por imagem , Mucosa Intestinal/patologia , Masculino , Pessoa de Meia-Idade , Terapia Neoadjuvante/métodos , Estadiamento de Neoplasias , Valor Preditivo dos Testes , Cuidados Pré-Operatórios/métodos , Prognóstico , Neoplasias Retais/diagnóstico , Neoplasias Retais/patologia , Neoplasias Retais/terapia , Reto/diagnóstico por imagem , Reto/patologia , Resultado do Tratamento
18.
Chem Biodivers ; 14(12)2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28963759

RESUMO

Two new flavones, 6,7-methylenedioxy-4-hydroxypeltogynan-7'-one (1), cochliophilin B (2), as well as two known ones, cochliophilin A (3) and 6-methoxy-7-hydroxy flavone (4), were isolated from the ethanol extract of the root of Phytolacca acinosa Roxb. Compound 1 is a flavanol framework with one δ-lactone unit, which is rather rare in nature. The structures of the new compounds were determined on the basis of extensive spectroscopic (IR, MS, 1D- and 2D-NMR) analyses, the absolute configuration of 1 was established by comparing experimental and calculated electronic circular dichroism spectra. The structures of known compounds were fixed by comparison with literatures data. Compounds 2 and 4 showed modest inhibitory activities against BEL-7402 cell line, with IC50 values of 28.22 and 39.16 µmol/L, respectively.


Assuntos
Flavonas/química , Phytolacca/química , Células A549 , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Flavonas/isolamento & purificação , Flavonas/toxicidade , Humanos , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Conformação Molecular , Mycobacterium tuberculosis/efeitos dos fármacos , Phytolacca/metabolismo , Raízes de Plantas/química , Raízes de Plantas/metabolismo , Espectrofotometria Infravermelho
19.
Electromagn Biol Med ; 35(1): 1-7, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-25188418

RESUMO

Insects show a variety of responses to electric fields and most of them are associated with immediate effects. To investigate the long-term effects of static electric field on the wheat aphid Sitbion avenae, the insert was exposed to 4 min of a static electric field at intensities of 0, 2, 4, or 6 kV/cm. Development effects over 30 consecutive generations of the insect were studied. The results showed that the electric field could exert adverse effects on the developmental duration and total longevity of S. avenae nymphs regardless of exposure intensities or generations. The effects appeared to be more intense and fluctuated at higher electric field intensities and more insect generations. The most favorable exposure for development was 6 kV/cm for 4 min while the most detrimental electric fields were 2 kV/cm for 4 min and 4 kV/cm for 4 min. Among the treatments, the first instar duration was significantly prolonged while the adult longevities were significantly shortened in the sixth generation. The intrinsic rate of increase and net reproductive rate in the sixth generation were also the lowest among the 30 consecutive generations studied. Based on the results, the adverse effects of electric fields on insects may be used in the bio-control of pest insects in terms of pest management.


Assuntos
Afídeos/crescimento & desenvolvimento , Eletricidade , Controle de Insetos , Triticum , Análise de Variância , Animais , Afídeos/fisiologia , Longevidade , Ninfa/crescimento & desenvolvimento , Ninfa/fisiologia , Reprodução , Eletricidade Estática , Fatores de Tempo
20.
Zhongguo Yi Xue Ke Xue Yuan Xue Bao ; 38(3): 312-7, 2016 06 10.
Artigo em Inglês | MEDLINE | ID: mdl-27469917

RESUMO

Objective To compare the sensitivity of multislice spiral CT dual phase and somatosatatin receptor scintigraphy (SRS) in the diagnosis of pancreas nuroendocrine tumors (pNET). Methods Totally 28 patients with pathologically confirmed pNET recieved both CT dual phase contrast and SRS and the results were compared. Results Of these 28 pNET patients,26 (92.8%) were accurately diagnosed by CT dual-phase scan and 20 (71.4%) by SRS (P=0.031).In the functioning pNET cases,the diagnosis sensitivity of CT dual phase scan and SRS was 94.1% (16/17)and 58.8% (10/17)(P=0.218). In the non-functioning pNET cases,the sensitivity was 90.9% (10/11) and 90.9% (10/11) (P=0.740).Diagnostic sensitivity of CT dual phase scan and SRS for pNET without metastasis was 90.4% (19/21) and 57.1% (12/21) (P=0.125).The sensitivity for pNET with metastasis was 100%(7/7)and 100% (7/7). Corresponding to the pathological grading,the diagnostic sensitivity of CT dual phase scanning and SRS was 84.6% (11/13) and 53.8% (7/13) for G1,100% (12/12) and 83.3% (10/12) for G2,and 100% (3/3) and 100% (3/3) for G3. The diagnostic sensitivity of CT dual phase scan and SRS for pNET with diameter less than or equal to 2.0 cm was 94.7% (18/19) and 52.6% (10/19) (P=0.008). For pNET with diameter more than 2.0 cm,the sensitivity was 92.8% (13/14) and 100% (14/14). Conclusions Compared with SRS,dual phase CT scan is more sensitive in diagnosing pNET,especially for those in lower pathological stages. For lesions sized less than or equal to 2.0 cm,SRS should be combined with other imaging examinations to minimize false negative results.


Assuntos
Tumores Neuroendócrinos/diagnóstico por imagem , Neoplasias Pancreáticas/diagnóstico por imagem , Cintilografia , Tomografia Computadorizada Espiral , Humanos , Sensibilidade e Especificidade
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