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1.
Acta Pharmaceutica Sinica ; (12): 35-42, 2024.
Article in Chinese | WPRIM | ID: wpr-1005437

ABSTRACT

Sesquiterpenoids are widely found in nature, while nitrobenzoyl sesquiterpenoids are relatively rare. Twelve natural nitrobenzoyl sesquiterpenoids were all derived from marine Aspergillus fungi, which are typical natural products with marine characteristics. These natural products exhibit good antitumor, antiviral, and inhibition of osteoclast differentiation activity, especially in the treatment of osteoclast-related diseases, showing good medicinal development value. This article reviews the natural product sources, chemical structure, chemical synthesis, biosynthesis, bioactivity, and pharmacological mechanisms of nitrobenzoyl sesquiterpenoids and predicts and discusses their absorption, distribution, metabolism, excretion, toxicity (ADME/T), and drug-likeness, providing a comprehensive understanding of the natural products of nitrobenzoyl sesquiterpenoids from marine sources and their potential for pharmaceutical development.

2.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 149-154, 2019.
Article in English | WPRIM | ID: wpr-776898

ABSTRACT

Two new isomeric modified tripeptides, aspergillamides C and D (compounds 1 and 2), together with fifteen known compounds (compounds 3-17), were obtained from the marine sponge-derived fungus Aspergillus terreus SCSIO 41008. The structures of the new compounds, including absolute configurations, were determined by extensive analyses of spectroscopic data (NMR, MS, UV, and IR) and comparisons between the calculated and experimental electronic circular dichroism (ECD) spectra. Butyrolactone I (compound 11) exhibited strong inhibitory effects against Mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB) with the IC being 5.11 ± 0.53 μmol·L, and acted as a noncompetitive inhibitor based on kinetic analysis.


Subject(s)
Animals , 4-Butyrolactone , Chemistry , Pharmacology , Aspergillus , Chemistry , Chemistry Techniques, Analytical , Dipeptides , Chemistry , Pharmacology , Enzyme Inhibitors , Chemistry , Pharmacology , Indoles , Chemistry , Pharmacology , Molecular Structure , Mycobacterium tuberculosis , Peptides , Chemistry , Pharmacology , Polyketides , Chemistry , Pharmacology , Porifera , Microbiology , Protein Tyrosine Phosphatases , Chemistry
3.
Chinese Medical Journal ; (24): 81-86, 2012.
Article in English | WPRIM | ID: wpr-333537

ABSTRACT

<p><b>BACKGROUND</b>Although previous reports had reported the use of temporary internal distraction as an aid to correct severe scoliosis, two-stage surgery strategy (less invasive internal distraction followed by posterior correction and instrumentation) has never been reported in the treatment of patients with severe spinal deformity. This study aimed to report the results of the surgical treatment of severe scoliosis and kyphoscoliosis by two-stage and analyse the safety and efficacy of this surgical strategy in the treatment of severe spinal deformities.</p><p><b>METHODS</b>A total of 15 patients with severe scoliosis, kyphoscoliosis or kyphosis who underwent two-stage surgeries (less invasive internal distraction followed by posterior correction and instrumentation) were studied based on hospital records. Pretreatment radiographs and radiographs taken after first surgery (internal distraction by two small incisions), before second surgery (posterior correction, instrumentation and fusion), one week after second surgery and final follow-up were measured. Subjects were analyzed by age, gender, major coronal curve magnitude, flexibility of major curve, major sagittal curve magnitude before first surgery, after first surgery, before second surgery, after second surgery and at final follow-up. Complications related to two-stage surgeries were noted in each case.</p><p><b>RESULTS</b>The average major curve magnitude was 129.4° (range, 95° to 175°), reduced 58.9° or 45.4% after first stage surgery and reduced 30.6° or 24.6% after second stage surgery. The loss of correction during the interval between two surgeries was 7.1%. The total major coronal curve correction was 81.4° or 62.9%. At the final follow up, the average loss of correction of major coronal curve was 3.9° and the final average correction rate was 59.7%. The average major sagittal curve magnitude was 80.3° (range, 30° to 170°), and the total major sagittal curve correction was 48.2°. Loss of correction averaged 4.0° for major sagittal curve and the final correction averaged 42.2°. Clinical complications were noted in the peri-operative and long-term periods.</p><p><b>CONCLUSIONS</b>Two-stage surgery was a safe and effective surgical strategy in this difficult population. Using two-small-incision technique, the first stage surgery was less invasive. No permanent neurologic deficit was noted in this series.</p>


Subject(s)
Adolescent , Child , Female , Humans , Male , Kyphosis , Diagnostic Imaging , General Surgery , Radiography , Scoliosis , Diagnostic Imaging , General Surgery , Treatment Outcome
4.
Chinese Journal of Hepatology ; (12): 612-615, 2008.
Article in Chinese | WPRIM | ID: wpr-279727

ABSTRACT

<p><b>OBJECTIVE</b>To evaluate the effect and the possible mechanism of HCCR siRNA on cell proliferation and apoptosis of hepatocarcinoma cells.</p><p><b>METHODS</b>pRIV2-siHCCR plasmids, which express small interfering RNA of HCCR were constructed and transfected into HepG2 cells. The mRNA and protein expressions of HCCR were detected by real time PCR and Western blot. The proteins p15, p16, p27, p53, and PTEN were detected by Western blot. The cell proliferation and apoptosis were observed by MTT and FACS.</p><p><b>RESULTS</b>The plasmid pRIV2-siHCCR was constructed successfully. Real time PCR and Western blot analysis showed that the HCCR siRNA effectively inhibited HCCR expression in HepG2 cells after pRIV2-siHCCR transfection. MTT method confirmed that HepG2 cell proliferation was suspended, while the cell apoptosis was increased much more than that in the control group. After the transfection with the plasmid of pRIV2-siHCCR into HepG2 cells, the expression of p53 protein was decreased, and P15 increased; and levels of PTEN, p16, and p27 were evidently not changed.</p><p><b>CONCLUSION</b>After being transfected with HCCR siRNA expression plasmid, the cell proliferation of HepG2 was arrested, while the apoptosis of HepG2 cells increased. Our results demonstrate the potential role of p53 and p15 in HCCR signaling.</p>


Subject(s)
Female , Humans , Carcinoma, Hepatocellular , Metabolism , Pathology , Cell Proliferation , Gene Expression Regulation, Neoplastic , Hep G2 Cells , Liver Neoplasms , Metabolism , Pathology , Plasmids , Proto-Oncogene Proteins , Genetics , RNA, Small Interfering , Genetics , Transfection , Tumor Suppressor Protein p53 , Metabolism , Uterine Cervical Neoplasms , Genetics
5.
Chinese Journal of Surgery ; (12): 1289-1292, 2004.
Article in Chinese | WPRIM | ID: wpr-345089

ABSTRACT

<p><b>OBJECTIVES</b>To discuss and evaluate the selection of surgical procedure for the treatment of idiopathic scoliosis according to the location and degree of the deformity.</p><p><b>METHODS</b>175 patients with idiopathic scoliosis underwent surgical treatment with correction and fusion. The patients were divided into four groups according to the location and degree of the deformity and four different procedures were used for each group. For each group, the blood loss, surgery time, correction rate, loss of correction at final follow up and complications were compared and analyzed.</p><p><b>RESULTS</b>All patients underwent surgery safely and no neurological complication occurred. The correction rate was 81% for Group I, 86% for Group II, 68% for Group III and 72% for Group IV. All patients were followed up at least 2 years and the average time was 38 months (24 approximately 52).</p><p><b>CONCLUSION</b>Proper selection of surgical procedure according to the location and degree of the scoliotic deformity, satisfactory results can be achieved in the treatment of idiopathic scoliosis.</p>


Subject(s)
Adolescent , Adult , Child , Female , Humans , Male , Follow-Up Studies , Scoliosis , General Surgery , Spinal Fusion , Methods , Treatment Outcome
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