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1.
Bioorg Chem ; 148: 107434, 2024 Jul.
Article in English | MEDLINE | ID: mdl-38744168

ABSTRACT

Azaphilones represent a particular group of fascinating pigments from fungal source, with easier industrialization and lower cost than the traditional plant-derived pigments, and they also display a wide range of pharmacological activities. Herein, 28 azaphilone analogs, including 12 new ones, were obtained from the fermentation culture of a marine fungus Penicillium sclerotium UJNMF 0503. Their structures were elucidated by MS, NMR and ECD analyses, together with NMR and ECD calculations and biogenetic considerations. Among them, compounds 1 and 2 feature an unusual natural benzo[d][1,3]dioxepine ring embedded with an orthoformate unit, while 3 and 4 represent the first azaphilone examples incorporating a novel rearranged 5/6 bicyclic core and a tetrahydropyran ring on the side chain, respectively. Our bioassays revealed that half of the isolates exhibited neuroprotective potential against H2O2-induced injury on RSC96 cells, while compound 13 displayed the best rescuing capacity toward the cell viability by blocking cellular apoptosis, which was likely achieved by upregulating the PI3K/Akt signaling pathway.


Subject(s)
Apoptosis , Benzopyrans , Dose-Response Relationship, Drug , Hydrogen Peroxide , Neuroprotective Agents , Penicillium , Phosphatidylinositol 3-Kinases , Pigments, Biological , Proto-Oncogene Proteins c-akt , Apoptosis/drug effects , Penicillium/chemistry , Neuroprotective Agents/pharmacology , Neuroprotective Agents/chemistry , Neuroprotective Agents/isolation & purification , Proto-Oncogene Proteins c-akt/metabolism , Proto-Oncogene Proteins c-akt/antagonists & inhibitors , Phosphatidylinositol 3-Kinases/metabolism , Pigments, Biological/pharmacology , Pigments, Biological/chemistry , Pigments, Biological/isolation & purification , Hydrogen Peroxide/pharmacology , Hydrogen Peroxide/antagonists & inhibitors , Molecular Structure , Benzopyrans/pharmacology , Benzopyrans/chemistry , Benzopyrans/isolation & purification , Structure-Activity Relationship , Animals , Cell Survival/drug effects , Rats , Signal Transduction/drug effects
2.
Chin Med Sci J ; 22(4): 224-7, 2007 Dec.
Article in English | MEDLINE | ID: mdl-18254186

ABSTRACT

OBJECTIVE: To evaluate the efficacy and safety of long-term treatment with arotinolol in patients with idiopathic dilated cardiomyopathy (IDCM). METHODS: Sixty-three patients with IDCM were evaluated at baseline and after 12-month therapy with arotinolol. The conventional therapy for congestive heart failure was continued throughout the study with arotinolol as the only beta-blocker. Left ventricular function was assessed with the New York Heart Association functional class and two-dimensional echocardiography. RESULTS: After 12-month arotinolol treatment, there was a significant improvement in left ventricular systolic function. Left ventricular end-systolic dimension significantly decreased from 59.52 +/- 8.83 mm to 50.89 +/- 8.17 mm (P < 0.001). Left ventricular ejection fraction significantly increased from 27.39% +/- 7.94% to 41.13% +/- 9.45% ( P < 0.001). Left ventricular mass index decreased from 150.47 +/- 42.42 g/m2 to 141.58 +/- 34.36 g/m2 (P < 0.01). No adverse events leading to premature discontinuation of study drug occurred. CONCLUSION: In this preliminary study, 12-month arotinolol treatment has a favorable effect on left ventricular function in patients with IDCM, and it is safe and well tolerated.


Subject(s)
Adrenergic beta-Antagonists/pharmacology , Cardiomyopathy, Dilated/drug therapy , Propanolamines/pharmacology , Ventricular Function, Left/drug effects , Adrenergic beta-Antagonists/adverse effects , Adrenergic beta-Antagonists/therapeutic use , Adult , Cardiomyopathy, Dilated/physiopathology , Echocardiography , Female , Humans , Male , Middle Aged , Propanolamines/adverse effects , Propanolamines/therapeutic use
3.
Chin Med J (Engl) ; 119(12): 998-1002, 2006 Jun 20.
Article in English | MEDLINE | ID: mdl-16805983

ABSTRACT

BACKGROUND: Pulmonary thromboembolism (PTE) has become a common disease that severely endangers people's health. This study analysed the changes in proportion and mortality of PTE in hospitalized patients to provide data for prevention and management of the disease. METHODS: The data of 763 hospitalized patients with PTE from 1974 to 2005 in Fuwai Hospital were analysed. RESULTS: During the 1970s, 0.27% of patients in a cardiovascular hospital had PTE (< 5 cases per year); while so far this century the proportion is 0.94% (48 to 113 per year). The mortality of hospitalized PTE patients fell from 20.00% in the 1970s to 4.10% this century. Prior to 1990, the mortality of hospitalized PTE patients was 12.50%, and in the years after 1990 only 3.40%. The difference was statistically significant (P < 0.005). People with this disease were mostly between the ages of 30 and 69 years. Men were most susceptible between the ages of 30 and 69 years, while women between the ages of 40 and 69 years. Men contracted PTE 10 years earlier than women. The mortality of male PTE patients was 4.70%, not significantly different from female patients, 5.06% (0.50 < P < 0.75). There were not any significant differences between the mortality of patients in the different age groups overall (< or = 39, 40 - 49, 50 - 59, and > or = 60 years, P > 0.1). More people contracted the disease in winter than in other seasons (P < 0.05). There was no obvious difference between the mortality in different seasons overall (0.75 < P < 0.90). CONCLUSION: PTE is an increasingly significant disease and deserves adequate attention.


Subject(s)
Pulmonary Embolism/epidemiology , Adult , Age Factors , Aged , Female , Hospitalization , Humans , Male , Middle Aged , Pulmonary Embolism/mortality , Seasons , Time Factors
4.
Zhonghua Jie He He Hu Xi Za Zhi ; 29(3): 161-3, 2006 Mar.
Article in Chinese | MEDLINE | ID: mdl-16677477

ABSTRACT

OBJECTIVE: To describe the clinical features of paradoxical embolism and therefore to improve its diagnosis. METHODS: Case analysis and literature review. RESULTS: Eight cases of pulmonary embolism complicated with paradoxical embolism were diagnosed, of whom there were six men and two women (mean age, 47.6 years). Patent foramen ovale with right to left shunt was identified in only 3 cases. Cerebral embolism occurred in three patients, kidney artery embolism in 2 patients, left atrial thrombus in 1 patient, lower limb artery and aortic embolism in 1 patients respectively. The diagnosis of paradoxical embolism can only be confirmed when a venous thrombus was detected lodged at arterial-venous communication; otherwise, paradoxical embolism was considered a clinical diagnosis. Of the 8 cases, 7 were clinically diagnosed, while 1 was confirmed. CONCLUSIONS: Paradoxical embolism is not uncommon. The diagnosis should be considered when venous thromboembolism is complicated with systematic embolism or unknown cause of systematic embolism.


Subject(s)
Embolism, Paradoxical/diagnosis , Pulmonary Embolism/diagnosis , Adult , Embolism, Paradoxical/etiology , Female , Humans , Male , Middle Aged , Pulmonary Embolism/complications
5.
Zhonghua Yi Xue Za Zhi ; 85(23): 1605-7, 2005 Jun 22.
Article in Chinese | MEDLINE | ID: mdl-16185526

ABSTRACT

OBJECTIVE: To investigate the vicissitudes of the proportion and the mortality of patients with pulmonary thromboembolism (PTE). METHODS: To analyze respectively the data of 442 patients with PTE admitted to the Fuwai Hospital during the period 1974-2002 were analyzed retrospectively. RESULTS: The numbers of PTE in-patients every year during the 1970s and 48-79 cases in the early 2000s. The hospitalization constituent ratio of PTE was 0.1152% in 1970s and was 0.5866% in early 2000s. The age of onset ranged from 30 to 60. The tide age was from 30 to 60 in the male patients and from 40 to 60 in the female patients. The in-hospital mortality of PTE patients was descending from 20.0% in 1970s to 5.8% in early 2000s. The in-hospital mortality was 12.5% before 1990 and was 4.5% after 1990 (P = 0. 005). The in-hospital mortality rates of the male and female patients were 4.6% and 8.6% respectively (P = 0.09). The in-hospital mortality rates of the patients younger than 70 and elder than 70 were 5.5% and 19.0% respectively (P < 0.05). CONCLUSION: PTE The mortality of PTE, which attacks males more frequently than females, and the proportions of the number of PTE in-patients to the number of the whole in-patients increased and the in-hospital mortality increased during the past 3 decades.


Subject(s)
Hospital Mortality , Pulmonary Embolism/mortality , Adult , Age Factors , China/epidemiology , Female , Hospitalization , Humans , Incidence , Male , Middle Aged , Pulmonary Embolism/epidemiology , Retrospective Studies , Sex Factors
6.
Zhonghua Jie He He Hu Xi Za Zhi ; 27(11): 737-9, 2004 Nov.
Article in Chinese | MEDLINE | ID: mdl-15634383

ABSTRACT

OBJECTIVE: To improve the differential diagnosis of pulmonary artery sarcoma from pulmonary embolism. METHOD: Case analysis and literature review. RESULTS: Pulmonary artery sarcoma had similar clinical features as pulmonary thromboembolism. When the radiological features such as unilateral hilar enlargement and massive lumps in main trunk of pulmonary artery were observed and clinical deterioration occurred after thrombolytic and anticoagulant therapy, pulmonary artery sarcoma should be considered seriously in patients with suspected pulmonary thromboembolism. CONCLUSION: Pulmonary artery Sarcoma can be easily misdiagnosed as pulmonary thromboembolism.


Subject(s)
Diagnostic Errors , Pulmonary Artery/pathology , Pulmonary Embolism/diagnosis , Sarcoma/diagnosis , Vascular Neoplasms/diagnosis , Adult , Diagnosis, Differential , Female , Humans , Male , Middle Aged , Pulmonary Artery/diagnostic imaging , Tomography, X-Ray Computed/methods
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