Elemene Antitumor Drugs Development Based on "Molecular Compatibility Theory" and Clinical Application: A Retrospective and Prospective Outlook / 中国结合医学杂志

Elemene, derived from Curcuma wenyujin, one of the "8 famous genuine medicinal materials of Zhejiang province," exhibits remarkable antitumor activity. It has gained wide recognition in clinical practice for effectiveness on tumors. Dr. XIE Tian, introduced the innovative concept of "molecular compatibility theory" by combining Chinese medicine principles, specifically the "monarch, minister, assistant, and envoy" theory, with modern biomedical technology. This groundbreaking approach, along with a systematic analysis of Chinese medicine and modern biomedical knowledge, led to the development of elemene nanoliposome formulations. These novel formulations offer numerous advantages, including low toxicity, well-defined composition, synergistic effects on multiple targets, and excellent biocompatibility. Following the principles of the "molecular compatibility theory", further exploration of cancer treatment strategies and methods based on elemene was undertaken. This comprehensive review consolidates the current understanding of elemene's potential antitumor mechanisms, recent clinical investigations, advancements in drug delivery systems, and structural modifications. The ultimate goal of this review is to establish a solid theoretical foundation for researchers, empowering them to develop more effective antitumor drugs based on the principles of "molecular compatibility theory".

Migration of eleven DSD-FWAs from packaging paper to food / 预防医学

Objective@#To observe the migration of 4,4＇-diaminostilbene-2,2＇-disulfonc acid-based fluorescent whitening agents ( DSD-FWAs ) in food packaging paper, so as to provide evidence for quality and safety supervision for paper packaging materials.@*Methods@#Forty-one paper samples with DSD-FWAs positive were made into 6 cm2 pieces and were soaked in four food simulants ( distilled water, 3% acetic acid, 10% ethanol and 95% ethanol, 10 mL each ). The experiment was carried out at the specified soaking temperature and time. The migration amounts of eleven DSD-FWAs were detected by high performance liquid chromatography-fluorescence detection. @*Results@#C.I.220, C.I.24, C.I.210, C.I.85, C.I.113, C.I.264, C.I.353 and C.I.357 were found in all the four food simulants. At the same time and temperature, the migration amount was highest in 10% ethanol, followed by distilled water, 3% acetic acid and 95% ethanol. C.I.220 was dissolved in all four food simulants, in the range of 20-90 ℃, the migration amount increased with soaking temperature; at 20 ℃, 40 ℃ and 60 ℃, the migration amount increased first and then stabilized over time.@*Conclusion@#The higher the storage temperature and the longer the storage time of paper packaging, the easier the DSD-FWAs in packaging paper migrate to food.

Determination of perfluorocarboxylic acids in fish by ultra performance liquid chromatography tandem mass spectrometry / 预防医学

Objective@#To develop the ultra performance liquid chromatography tandem mass spectrometry ( UPLC-MS/MS ) for the determination of perfluorocarboxylic acids ( PFCAs ) in fish.@*Methods@#The fish samples were extracted with tert-butyl methyl ether and purified by WAX columns. The WAX cartridges were rinsed with methanol and 25 mmol/L ammonium acetate, and the target compound residues were eluted with 0.5% ammonia methanol and then redissolved with 50% methanol aqueous solution after nitrogen blowing to nearly dry. Nine kinds of PFCAs were simultaneously quantified by UPLC-MS/MS with 1 mmol/L ammonium acetate-methanol solution as the mobile phase.@*Results@#The extraction was separated well in UPLC BEH C18 column. There were good linear correlations of nine kinds of PFCAs in the range of 1.0-200.0 ng/mL, with the coefficients all more than 0.99. The limits of detection and quantification were 0.06-0.19 μg/kg and 0.19-0.62 μg/kg, respectively. The recovery rates were 70.08%-117.24% at different spiked levels ( 5.0, 25.0, 50.0 μg/kg ), and the relative standard deviations were 2.31%-19.68%. @*Conclusion@#Through optimizing the pretreatment conditions, the mobile phase of liquid chromatography and the detection conditions of mass spectrometry, the UPLC-MS/MS could meet the monitoring requirements of PFCAs in fish.

Determination of vanadium, chromium, nickel, selenium and arsenic in calcium based toothpastes by microwave digestion-ICP-MS/MS / 预防医学

Objective@#To establish analytical method for the determination of vanadium ( V ), chromium ( Cr ), nickel ( Ni ), selenium ( Se ) and arsenic ( As ) in calcium based toothpastes by microwave digestion-inductively coupled plasma tandem mass spectrometry ( ICP-MS/MS ).@*Methods@#The 21 calcium based toothpaste samples from supermarkets and shops in the urban areas of Hangzhou were digested by 6 mL HNO3 and 1 mL H2O2 in microwave digestion system. Then He-SQ mode and O2-MS/MS mode of ICP-MS/MS were respectively used for the determination of Ni and V, Cr, Se, As. Indium ( In ) was used as internal standard for calibration. @*Results@# Good linear relationships were obtained for these five elements from 1.0 to 32.0 μg/L, with the correlation coefficients ranged from 0.999 3 to 1.000 0. The detection limits of the method ranged from 0.000 25 to 0.006 08 mg/kg. The recovery rates of standard spiking were 80.7%-105.7% when set at 0.4, 0.8 and 1.6 mg/kg, the recovery of standard reference material was 102.2%, and the relative standard deviations were 2.6%-4.8%. The concentrations of V, Cr, Ni, Se and As in 21 calcium based toothpaste samples were 0.024-1.935 mg/kg, 0.085-5.759 mg/kg, 0.090-3.673 mg/kg, <0.002 72-0.016 mg/kg and <0.006 08-0.321 mg/kg.@*Conclusion@#Microwave digestion-ICP-MS/MS can effectively reduce the interferences of polyatomic ions and doubly charged ions from the matrix, which is suitable for the determination of V, Cr, Ni, Se and As in calcium based toothpaste.

Synthesis of 13-β-elemene ester derivatives and evaluation of their antioxidant activity in human umbilical vein endothelial cells / 中国天然药物

In the present study, a series of 13-β-elemene ester derivatives were designed and prepared, and their antioxidant activity was investigated in the H2O2-treated human umbilical vein endothelial cells (HUVECs). Among the test compounds, the dimer compounds 5v and 5w exhibited the most potent antioxidant activity with significant ROS suppression being observed. Both compounds markedly inhibited the H2O2-induced changes in various biochemical substances, such as superoxide dismutase (SOD), malonyldialdehyde (MDA), nitric oxide (NO), and lactic dehydrogenase (LDH), which were superior to that of the positive control vitamin E. Further more, they did not produce any obvious cytotoxicity, but increased the viability of HUVECs injured by H2O2 in a dose-dependent manner. Additionally, compound 5w, designed as a prodrug-like compound, showed improved stability relative to compound 4 in vitro.

Current natural products with antihypertensive activity / 中国天然药物

Natural products have been an important source of new drugs, which also played a dominant role in the discovery and research of new drugs for the treatment of hypertension. This review article reviews the recent progress in the research and development of natural lead compounds with antihypertensive activity, including alkaloids, diterpenes, coumarins, flavonoids, and peptides. We summarized their structures, sources, as well as the antihypertensive mechanisms. These information provides instructive reference for the following structural modifications and optimization.

Synthesis and β-adrenergic blocking activity of oxime ether hybrids derived from a natural isochroman-4-one / 中国天然药物

AIM@#In a search for new cardiovascular drug candidates, a series of novel oxime ethers derived from a natural isochroman-4-one were synthesized.@*METHOD@#Compounds 3 and 6, derived from the natural antihypertensive compound 7, 8-dihydroxy-3-methyl-isochroman-4-one (XJP), were designed and synthesized. Subsequently, a series of novel isochroman-4-one oxime ether hybrids were prepared by hybridizing various N-substituted isopropanolamine functionalities to isochroman-4-one oxime. Furthermore, β1-adrenergic blocking activities of the synthesized compounds were assayed using the isolated rat left atria.@*RESULTS@#Twenty target compounds were obtained, and the preliminary structure-activity relationships were deduced. The most promising compound Ic exhibited β1-adrenoceptor blocking activity (inhibition: 52.2%) at 10(-7) mol·L(-1), which was superior to that of propranolol (inhibition: 49.7%).@*CONCLUSION@#The results suggested that natural product XJP/isopropanolamine moiety hybrids may provide a promising approach for the discovery of novel cardiovascular drug candidates.

Analysis of protamine content in patients with asthenozoospermia / 中华男科学杂志

<p><b>OBJECTIVE</b>To study the significance of the change of protamine content in the management of male infertility.</p><p><b>METHODS</b>Sperm nuclear proteins extracted from 199 infertile patients were analyzed by polyacrylamide gel-electrophoresis and scanning microdensitometry.</p><p><b>RESULTS</b>Forty-two (21%) cases of the total number had normal sperm nuclear proteins and 157 (79%) had aberrant ones, which mainly presented the interruption of HPRR and abnormality of P2 protamine. Thirty patients were selected at random from 157 abnormal cases for clinical treatment. After the treatment, the sperm nuclear proteins were extracted and analyzed and the results demonstrated that 11 cases (36.6%) improved markedly, 5 (16.6%) restored to normal and the other 16 (46.6%) remained unchanged.</p><p><b>CONCLUSION</b>There is a reduced level or selective absence or even complete selective absence of protamines in infertile patients. Protamines may act as a parameter for evaluating the treatment effect of infertile males and protamine content can be influenced by a certain or several factors.</p>

Expression of human phosphodiesterase 3A gene using baculovirus expression system in insect cell / 药学学报

<p><b>AIM</b>To investigate the expression of recombinant human phosphodiesterase 3A (HPDE3A) using baculovirus expression system in Tn cell line.</p><p><b>METHODS</b>The HPDE3A cDNA was recombined with baculovirus, and then the recombinant was transfected into Tn cell line. The expression of HPDE3A in Tn cell line was detected and identified by the RT-PCR, SDS-PAGE and Western blotting.</p><p><b>RESULTS</b>The recombinant HPDE3A protein was stably expressed in Tn cell line and detected by the distinct morphological changes of Tn cell, RT-PCR, SDS-PAGE and Western blotting using polyclonal antibody. The M(w) of the recombinant protein was about 120 kD.</p><p><b>CONCLUSION</b>Recombinant HPDE3A can be expressed in Tn cell line using the baculovirus expression system, and thus provided the basic material for studying its bioactivity and application in screening for HPDE3A inhibitor.</p>

Expression of rat protamine gene in MEL cells / 中国医学科学院学报

<p><b>OBJECTIVE</b>To investigate the expression of rat protamine (RP) gene in MEL cells and the effect on cell growth.</p><p><b>METHODS</b>Eukaryotic expression plasmid pCR-3.1-RP was constructed and transfected into MEL cells. The changes of cell growth rate, mitotic index and colony-forming rate in semi-solid medium were investigated.</p><p><b>RESULTS</b>Transfected MEL cells showed lower growth rate, mitotic index and colony-forming rate. Volumes of cells were reduced and reduction of RNA transcription was observed.</p><p><b>CONCLUSION</b>These results suggest that expression of RP in MEL cell may inhibit the cell growth and proliferation.</p>

Preparation and application of monoclonal antibodies to recombinant human IFN alpha / 中华实验和临床病毒学杂志

<p><b>OBJECTIVE</b>To prepare and apply monoclonal antibodies (McAb) against recombinant human interferon alpha (rHu IFN-alpha).</p><p><b>METHODS</b>Five cell lines (2E9, 4G1, 2A7, 2C9, 4G10) secreting McAbs against rHu IFN-alpha were established by hybridoma technique.</p><p><b>RESULTS</b>All the cell lines secreted monoclonal antibodies stably. Functions of secreting antibodies of the five cell lines lasted for 6 months in BALB/c mice and 8 months in cell culture. The specificity of antibody was constant. The Ig subclasses of the McAbs were IgG1. Anti-IFN McAb affinity purification column was prepared by coupling the anti IFN-alpha McAb to Sepharose 4B. The combining rate reached was higher than 95%.</p><p><b>CONCLUSIONS</b>The highest purification efficiency was obtained by using 4G10 column.</p>