The possible origin of recent human SARS coronavirus isolate from China.
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Animals↗
Biomedical subjects
S P Xu
Publications and source records attributed to S P Xu.
[Higher lint percent and drought tolerant cotton line selected by radiation breeding].
The Gossypium hirsutum cv. Liaomian No. 9 were mutagenized by 60Co gamma ray, from which the mutant line Zhonghuzhi PI 935 (be called "PI 935" for short) was bred by family selection method. The PI 935 not only has some good traits (growing period, drought tolerance, lint color and fiber quality) similar to the original cultivar, but also has higher lint outturn and lint yield than that of the Liaomian No. 9. The PI 935 has been identified and regional tested in nine places times for four years in the southern Xinjiang Weiwuer autonomous region. It was shown that the PI 935 had the higher lint outtrn for the average 47.3% was ten-point percentage more than that of the check cultivars (Junmian No. 1 or Xinluzhong No. 5), the similar lint yield by and large and the growing period by five days later than that of the checks. The PI 935 was collected in the National Bank of Crop Germplasm (unified No. ZM 114274 and named "Zhonghuzhi PI 935").
Cobalt Radioisotopes↗
[Synthesis and anticancer activity of 3-[(3'-methyl-4'-(substituted phenyl)-1',3'-butadienyl] indole derivatives].
AIM: To study the synthesis and anticancer activity of 3-[(3'-methyl-4'-(substituted phenyl)-1',3'-butadienyl] indole derivatives. METHODS: Electrophilic-substitution, aldol-condensation, selective-reduction, phase-transfer Wittig reaction and hydrolysis reaction were used in the synthesis of the title compounds. RESULTS: Eleven compounds of 3-[(3'-methyl-4'-(substituted phenyl)-1',3'-butadienyl] indole were synthesized. They are new compounds. Compound 8 showed different inhibitory effects on HL-60, HCT-8 and Bel7402 cell lines in vitro, and its inhibitory rate of antiinflammation was 100% at 10(-5) mol.L-1 concentration. CONCLUSION: Compound 8 showed high anticancer and antiinflammatory activities, and is worth further studying.
Anti-Inflammatory Agents, Non-Steroidal↗
[Synthesis and biological activity of 2-[(substituted phenyl)vinyl] indole derivatives].
AIM: To synthesize derivatives of 2-[substituted phenyl)vinyl] indole and find compounds with biological activities by screening in vitro. METHODS: Twenty-one compounds of 2-[(substituted phenyl) vinyl] indole were synthesized by reduction, oxidation and Witting reaction. MS, 1HNMR and elemental analysis were used to determine the structures of the new compounds. RESULTS: These compounds are new ones. CONCLUSION: Six compounds (3, 9, 11, 13, 18 and 20) showed effects on some different receptors, such as alpha 2, D2 and H1, and is worth further studying.
Animals↗
[Synthesis of substituted 4-styrylcoumarin and their antitumor activities].
AIM: A series of 4-styrylcoumarin derivatives had been designed and synthesized in order to find compounds of antitumor activities by screening. METHODS: Title compounds (1-20) were synthesized by Phase-Transfer Wittig-Horner reaction, and screened by several antitumor models in vitro. Their structures were determined by 1HNMR, MS and elemental analysis. RESULTS: Twenty compounds (1-20) are new compounds. Compound 18 had effects on KB cell lines in vitro. CONCLUSION: It was seen that compound 18 had certain antitumor activities, and it was worth further studying.
Antineoplastic Agents↗
[Interaction between protein and ciprofloxacin].
AIM: To study the interaction between ciprofloxacin and BSA in physiological condition by fluorescence spectroscopy. METHODS: The affection of drug to the protein conformation was investigated. The binding constant between drug and BSA from a double reciprocal Lineweaver-Burk plot was determined and the main sort of binding force was found according to the thermodynamic parameters. RESULTS: The binding constants between BSA and ciprofloxacin at 26 degrees C and 45 degrees C are about 10(4). At 26 degrees C, the thermodynamic parameters of reaction between BSA and ciprofloxacin are delta H = -49.13 kJ.mol-1, delta G = -26.45 kJ.mol-1, delta S = -75 kJ.mol-1. The maximum wavelength of the synchronous fluorescence spectra of BSA moved from 279 nm to 289 nm with the increasing of the amount of ciprofloxacin. CONCLUSION: There exists fluorescence energy transfer between BSA and ciprofloxacin. The main sort of binding force between BSA and ciprofloxacin is Van der Waals' interaction. Ciprofloxacin can be deposited and be transported by serum protein in vivo. Ciprofloxacin affects the protein conformation.
Anti-Infective Agents↗
[Plant regeneration from protoplast culture in flax (Linum usitatissimum)].
Shoot protoplasts of four fiber flax (Linum usitatissimum) varieties (7309, 948, Belinka and Viking) were isolated and cultured. The optimal condition for higher protoplast yield 1.8 x 10(6)/gFW and activity 85.5% (c.v. 948) were from 10 day old seedings. Culture in V-KM Agroase-island medium led to first divisions after 3 days (c. v. 948), and after twenty days with an efficiency of 36% of divided cells and 5.2% in plating efficiency. Plant regeneration was obtained in 7309 and Belinka on agar media B5-2, MS3 containing 0.6 mg/L 6-BA and 0.1 mg/L NAA. Roots and leaves regeneration were observed in Viking and 948 respectively.
Cell Division↗
[Inhibition of tumor invasion and metastasis by retinoid 4-APR].
The anti-invasive and anti-metastatic effects with new retinoid 4-acetamidophenyl retinoate (4-APR) were studied using in vitro and in vivo experiments. 4-APR, at the dose of 43.3 mg.kg-1.day-1 p.o., was shown to reduce the spontaneous lung metastatic foci of Lewis lung carcinoma. 4-APR was also found to inhibit the artificial lung metastasis of B16-F10 cells by 67.9% and 36.6% and suppress the reconstituted basement membrane invasion of B16-F10 cells by 54.2% and 41.9% at the concentrations of 10(-5) mol.L-1 and 10(-6) mol.L-1, respectively.
Animals↗
[Preparation of diclofenac sodium controlled release pellets and multiple-dose evaluation in healthy volunteers].
The yield of pellets obtained in preparing diclofenac sodium (DC-Na) controlled release pellets was affected by the lactose/starch ratio of the feed granules, viscosity of the binding solution and residence time in the rolling pot. The pellet shape was found to be correlated with surface tension of the binding solution. The concentration and composition of the coating solution and pellet size distribution were responsible for the agglutination in coating. The controlled release pellets (CRP) and commercial tablets (CT) of DC-Na were administrated orally to healthy volunteers by multiple-dose. The steady-state condition, based on trough plasma concentration on day 3-5, was achieved on day 3. A great difference in plasma drug concentration fluctuation index (FI) between CRP (0.476 +/- 0.0484) and CT (0.935 +/- 0.092) was observed (P < 0.05) during steady-state. The area under the plasma drug concentration-time curve for a 0-12 h interval (AUC) on day 5 of CRP (6.493 +/- 0.4169 micrograms.h.ml-1) and CT (7.551 +/- 0.4745 micrograms.h.ml-1) was shown to be not significantly different (P > 0.05). The relative bioavailability in the human was about 86%.
Adult↗
[Studies of chemopreventive agents against neoplasma: synthesis of 3-acetyl coumarin derivatives and relationship between antimutagenic activity and structure].
Twenty-five 3-acetylcoumarin derivatives were synthesized among which twenty-two were not reported before. Antimutagenic activity screen in vitro has shown that some of these compounds have various activities. The structure and activity relationship for 5-, 7-, 8-substituents has been studied. Pharmacological data showed that: the substituent on position 8 has important effect on its activity. When there is only a hydroxy group on position 7, its activity is the highest among those with other substituents, but when a methyl is on position 8, the order of the activity is reversed. Other trends have also been found which provided some clues for further structural modification.
Antimutagenic Agents↗
[Studies of antitumor and chemopreventive agents against neoplasm: synthesis of coumarin 3-glyoxal derivatives and relationship between structure and antimutagenic activity].
It has been shown that alpha-glyoxal and its derivatives possess antivirus and antitumor activities. Eighteen new coumarin 3-glyoxal derivatives were synthesized in our laboratory. The fragmentation pattern of MS and the characteristic signals of 1HNMR of these compounds have also been studied. In pharmacological test in vitro most of these analogues showed antimutagenic activities, among them, compound 9 exhibited very strong antimutagenic activity and eight compounds showed strong effects. The struture-activity relationship and the possible active substructure responsible for the activity of these compounds were discussed. As expected, coumarin 3-glyoxals showed higher antimutagenic activities than their 3-acetyl coumarin counterparts. We also found that alkylation or esterification of 7-hydroxy were favorable to their activities.
Antimutagenic Agents↗
[Studies on compounds of cancer chemoprevention: synthesis of some amides].
In search for cancer chemoprevention agents, seven new amide compounds have been synthesized. The structures have been determined based on spectral and chemical data. N-4-(ethoxycarbophenyl)-alpha-naphthamide and N-4-(ethoxycarbophenyl)-beta-naphthamide were shown to be 81% and 79% effective, respectively, for inducing different in HL-60 human promyelocytic leukemia cells at the concentration of 10(-5) mol/L in NBT tests.
Amides↗
Synthesis and antimalarial activity of 2-aziridinyl- and 2,3-bis(aziridinyl)-1,4-naphthoquinonyl sulfonate and acylate derivatives.
A series of 2-aziridinyl- and 2,3-bis(aziridinyl)-1,4-naphthoquinonyl sulfonate and acylate derivatives has been synthesized and evaluated for antimalarial activity in vitro against the human malaria parasite, Plasmodium falciparum (Vietnam Smith strain, chloroquine-resistant at the R3 level). The most active compounds, 2-aziridinyl-1,4-naphthoquinon-5-yl p-ethylbenzenesulfonate (13), 2-aziridinyl-1,4-naphthoquinon-5-yl p-tert-butylbenzenesulfonate (48), and 2-aziridinyl-5-hydroxy-1,4-naphthoquinone (5) produced 50% inhibition of the growth of P. falciparum at 9.6 x 10(-8), 2.4 x 10(-8), and 8.8 x 10(-8) M, respectively.
Animals↗
Synthesis of 2,3-diaziridinyl-1,4-naphthoquinone sulfonate derivatives as potential antineoplastic agents.
A new class of 2,3-diaziridinyl-1,4-naphthoquinone sulfonates (27 compounds) has been synthesized and evaluated as potential antineoplastic agents. The most active compounds, benzenesulfonate 4, p-toluenesulfonate 5, p-methoxybenzenesulfonate 7,8-quinolinesulfonate 17, and 2-thiophenesulfonate 20, in the aromatic sulfonate series, at their optimum daily dosage level of 25 mg/kg X 6, produced 100%, 90%, 75%, 80%, and 100% 50-day survivors, respectively, of L1210 tumor-bearing mice. At a lower optimum daily dosage level of 20 mg/kg X 6, treatments with p-fluorobenzenesulfonate 11 and p-nitrobenzenesulfonate 15 resulted in 100% and 80% 50-day survivors. In the aliphatic sulfonate series, methanesulfonate 21 produced 80% 50-day survivors at a 10 mg/kg daily dosage level X 6. Benzenesulfonate 4, p-fluorobenzenesulfonate 11, 8-quinolinesulfonate 17, and 2-thiophenesulfonate 20 derivatives were also tested in mice bearing the B16 melanoma; these agents gave T/C X 100 values of 180, 182, 219, and 161, respectively, in this neoplastic cell system. Structure-activity relationships of compounds of this class are discussed.
Animals↗
Inhibitory effect of retinoids on Epstein-Barr virus induction in Raji cells.
Induction of Epstein-Barr virus (EBV) early antigen after treatment with various combinations of croton oil and n-butyrate was markedly inhibited by retinoids 7901, 7902, Ro 10-9359 and Ro 11-1430. Possible administration of retinoids to virus capsid antigen IgA antibody-positive individuals in high-risk areas for nasopharyngeal carcinoma to prevent EBV activation and development of this cancer is discussed.
Butyrates↗
[Studies on compounds of tumor prevention--synthesis of derivatives of retinoic acid].
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Animals↗
[The isolation of antitumor active principle of Crotalaria sessiliflora and synthesis of its derivatives (author's transl)].
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Alkaloids↗