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1.
Br Poult Sci ; 58(5): 544-549, 2017 Oct.
Article in English | MEDLINE | ID: mdl-28817948

ABSTRACT

1. This experiment was conducted to evaluate the effects of dietary supplementation of resveratrol on laying performance, egg quality, egg yolk cholesterol and antioxidant enzyme activities of laying hens. 2. A total of 360 Beijing PINK-1 laying hens (60 weeks old) were randomly distributed among five dietary treatments, each of which included 6 replicates of 12 hens. Dietary treatments were basal diet supplemented with 0 (control), 0.5, 1.0, 2.0 and 4.0 g/kg diet resveratrol. The study lasted for 9 weeks including 1 week of adaptation and 8 weeks of the main experimental period. 3. The results indicated that dietary resveratrol significantly improved feed conversion ratios during 5-8 weeks and 1-8 weeks of the trial. Increasing dietary concentrations of the resveratrol linearly improved Haugh unit and albumen height of eggs. 4. The content of total cholesterol (TC), total triglyceride (TG), low density lipoprotein cholesterol (LDL-C), very low density lipoprotein cholesterol (VLDL-C) in serum and cholesterol in yolk was significantly decreased by dietary resveratrol, and there were significant linear correlations between these indexes and resveratrol supplemental levels. 5. Dietary resveratrol supplementation significantly improved serum Glutathione peroxidase (GSH-Px) enzyme activity and decreased serum malondialdehyde (MDA) content in groups with 2.0 and 4.0 g/kg resveratrol as compared to the control, respectively. However, supplementation of resveratrol did not affect the activity of serum superoxide dismutase (SOD). 6. It is concluded that resveratrol supplementation has a positive effect on performance, lipid-related traits and antioxidant activity of laying hens.


Subject(s)
Antioxidants/metabolism , Chickens/physiology , Cholesterol/metabolism , Egg Yolk/chemistry , Ovum/physiology , Stilbenes/metabolism , Animal Feed/analysis , Animals , Diet/veterinary , Dietary Supplements/analysis , Female , Resveratrol , Stilbenes/administration & dosage
2.
Biotech Histochem ; 91(5): 333-41, 2016 Jul.
Article in English | MEDLINE | ID: mdl-27058469

ABSTRACT

Aquaglycero-aquaporins (agAQPs) are the structural foundation of rapid water transport and they appear to participate in cancer proliferation and malignancy. AQP3 expression is increased and AQP9 expression is decreased in hepatocellular carcinoma (HCC) compared to normal liver, which suggests their possible use as targets for cancer treatment. AQP-based modifiers, such as Auphen and dibutyryladenosine 3', 5'-cyclic monophosphate (dbcAMP), might be used to treat several diseases and as chemical tools for assessing the functions of AQPs in biological systems. We investigated the effects of both Auphen on AQP3 and dbcAMP on AQP9 in SMMC-7721 cells. We used western blotting, real-time quantitative polymerase chain reaction (qPCR) and immunohistochemistry to evaluate changes in AQP3 and AQP9 expression in SMMC-7721 cells after culturing with Auphen and dbcAMP, respectively. We also determined the proliferation of SMMC-7721 cells. We found that compared to HL-7702 (L02) liver cells, Auphen increased AQP3 expression in tumor cells, whereas dbcAMP decreased expression of AQP9 in these cells. Also, high concentrations of Auphen and dbcAMP inhibited proliferation of SMMC-7721 cells in vitro. Auphen and dbcAMP may inhibit HCC development and could be considered targets for HCC diagnosis and therapy.


Subject(s)
Aquaporin 3/metabolism , Aquaporins/metabolism , Bucladesine/pharmacology , Carcinoma, Hepatocellular/metabolism , Liver Neoplasms/metabolism , Organogold Compounds/pharmacology , Carcinoma, Hepatocellular/pathology , Cell Line, Tumor , Humans , Liver Neoplasms/pathology , RNA, Messenger/metabolism
3.
Biotech Histochem ; 91(4): 269-76, 2016.
Article in English | MEDLINE | ID: mdl-26983346

ABSTRACT

Although aquaporins (AQPs) play important roles in transcellular water movement, their precise quantification and localization remains controversial. We investigated expression levels and localizations of AQP3 and AQP8 and their possible functions in the rat digestive system using real-time polymerase chain reactions, western blot analysis and immunohistochemistry. We investigated the expression levels and localizations of AQP3 and AQP8 in esophagus, forestomach, glandular stomach, duodenum, jejunum, ileum, proximal and distal colon, and liver. AQP3 was expressed in the basolateral membranes of stratified epithelia (esophagus and forestomach) and simple columnar epithelia (glandular stomach, ileum, and proximal and distal colon). Expression was particularly abundant in the esophagus, and proximal and distal colon. AQP8 was found in the subapical compartment of columnar epithelial cells of the jejunum, ileum, proximal colon and liver; the most intense staining occurred in the jejunum. Our results suggest that AQP3 and AQP8 play significant roles in intestinal function and/or fluid homeostasis and may be an important subject for future investigation of disorders that involve disruption of intestinal fluid homeostasis, such as inflammatory bowel disease and irritable bowel syndrome.


Subject(s)
Aquaporin 3/genetics , Aquaporin 3/metabolism , Aquaporins/genetics , Aquaporins/metabolism , Digestive System/metabolism , Gene Expression Regulation , Animals , Aquaporin 3/chemistry , Aquaporins/chemistry , Blotting, Western , Immunohistochemistry , Male , Protein Transport , Rats , Rats, Sprague-Dawley , Real-Time Polymerase Chain Reaction
4.
Clin Genet ; 74(6): 513-21, 2008 Dec.
Article in English | MEDLINE | ID: mdl-18554280

ABSTRACT

The symptomatic treatment of dopa-responsive dystonia (DRD) emphasizes the importance of molecular analyses of the GCH-1, TH and parkin genes. However, these analyses have not been extensively studied in Chinese DRD patients. Ten DRD families from the Han ethnic group including 14 patients and 28 clinically unaffected relatives were screened for GCH-1, TH and parkin mutations by direct sequencing, semiquantitative polymerase chain reaction (PCR), polymerase chain reaction-restriction fragment length polymorphism analysis and allele-specific PCR. Variations were verified in 200 unrelated control subjects. We have identified six novel mutations and three known mutations. The novel mutations are Leu91Val, Pro95Leu, Val204Gly and 628delC in GCH-1 gene; Gly216Ser in TH gene; and Cys253Phe in parkin gene. After molecular analyses of seven families with identified GCH-1 mutations, nine asymptomatic cases were found among 23 relatives, which confirmed the low penetrance of DRD. Unlike previous publications, male patients with GCH-1 mutations have early onset ages, while some female patients have very late onset ages in this medium-size series. Our data show that it is difficult to establish an evident genotype-phenotype correlation for DRD. However, it is necessary to know the genetic defects of DRD patients in clinics, which will help elucidate the mode of inheritance, facilitate causal therapy with levodopa and evaluate the prognosis.


Subject(s)
Asian People/genetics , Dystonia/genetics , GTP Cyclohydrolase/genetics , Tyrosine 3-Monooxygenase/genetics , Ubiquitin-Protein Ligases/genetics , Adolescent , Adult , Aged , Benserazide/pharmacology , Child , Child, Preschool , Dopamine Agents/pharmacology , Drug Combinations , Dystonia/drug therapy , Female , Genetic Variation/genetics , Humans , Levodopa/pharmacology , Male , Middle Aged , Mutation , Pedigree , Young Adult
5.
Space Med Med Eng (Beijing) ; 13(1): 38-41, 2000 Feb.
Article in Chinese | MEDLINE | ID: mdl-12214608

ABSTRACT

OBJECTIVE: To study the hemodynamic changes of pulmonary circulation during simulated weightlessness. METHOD: 12 subjects were studied using echocardiography and electrocardiography during head-down tilt (HDT) of -30 degrees lasting for 45 min. RESULT: Right ventricular ejection time increased significantly (P<0.05); peak velocity of pulmonary arterial blood flow decreased significantly (P<0.05); acceleration time of pulmonary arterial blood flow did not change significantly; significant decrease of right ventricular output occurred at the 10th minute and the 30th minute (P<0.05); pre-ejection period significantly decreased at the 30th minute and recovery. Heart rate, mean velocity of pulmonary arterial blood flow, and acceleration of pulmonary arterial blood flow did not change significantly; left ventricular cardiac output, stroke volume and blood pressure remained constant throughout the experiment. CONCLUSION: Changes of the parameters of pulmonary circulation suggested that pulmonary resistance increased, and the increase of pulmonary resistance maybe be the direct cause of the increase of pulmonary arterial pressure.


Subject(s)
Head-Down Tilt , Hemodynamics/physiology , Pulmonary Circulation/physiology , Weightlessness Simulation , Adult , Blood Flow Velocity , Blood Pressure/physiology , Heart Rate/physiology , Humans , Pulmonary Artery/physiology , Stroke Volume/physiology , Vascular Resistance/physiology , Ventricular Function, Right/physiology
6.
Space Med Med Eng (Beijing) ; 13(3): 187-90, 2000 Jun.
Article in Chinese | MEDLINE | ID: mdl-11543480

ABSTRACT

OBJECTIVE: To investigate the effects of short-term simulated weightlessness on lung function in healthy males. METHOD: -30 degrees head down tilt for 45 min was used to simulate short-period weightlessness. Lung function of 12 healthy males, aged 18-21, were studied with plethysmography during seating, supine and head down tilt positions. At the same time, blood flow in pulmonary artery and function of right ventricle were measured with Doppler Echo-Cardiography. Comparative analysis was done. RESULT: As body position changed from seating or supine into head down tilt, FVC, FEV1, FEV1%, MVV, VA and IVC decreased. The change of MVV was the most prominent (P < 0.000). As the position changed, pulmonary diffusion increased dramatically (DL(CO) P<0.001, K(CO) P<0.000). CONCLUSION: HDT may lead to a decrease of pulmonary ventilation and lung capacity. The increased pulmonary diffusion might be related to uniform distribution of pulmonary blood flow and increased effective pulmonary vascular bed.


Subject(s)
Head-Down Tilt , Lung/physiology , Pulmonary Artery/physiology , Pulmonary Circulation/physiology , Weightlessness Simulation , Adolescent , Adult , Bed Rest , Echocardiography, Doppler , Humans , Lung Volume Measurements , Male , Posture/physiology , Pulmonary Diffusing Capacity , Supine Position
7.
Space Med Med Eng (Beijing) ; 12(2): 101-5, 1999 Apr.
Article in Chinese | MEDLINE | ID: mdl-12430534

ABSTRACT

Objective. To find a real-time, quick and audio-visual method to evaluate the subject's physiological function condition and possible development. Method. Star figure technique was adopted to analyse multiple physiological indices during lower body negative pressure test (LBNP). Based on the character and stability of the stars figure, the steadiness of the subjects physiological function can be judged. Result. Physiological function can be accurately assessed only when the model of stress response of an individual is formed. Conclusion. The changes of star figure can indicate the possible development of the physiological function stage.


Subject(s)
Lower Body Negative Pressure , Monitoring, Physiologic , Stress, Physiological/physiopathology , Adaptation, Physiological , Blood Pressure/physiology , Data Interpretation, Statistical , Heart Rate/physiology , Humans
8.
Bioorg Med Chem ; 5(3): 501-6, 1997 Mar.
Article in English | MEDLINE | ID: mdl-9113328

ABSTRACT

Trilobalicin (1), a new nonadjacent bis-THF ring annonaceous acetogenin, 2,4-cis- (2) and 2,4-trans-trilobacinone (3), the ketolactones of trilobacin, an adjacent bis-THF ring acetogenin, were isolated from the stem bark of Asimina triloba (L.) Dunal (Annonaceae). Their structures were established based on chemical and spectral evidence. The relative stereochemistry of 1 was determined as trans/threo/threo/trans/erythro from C-10 to C-22 by comparisons of NMR data with those of model compounds. Compound 1 is the first example of a nonadjacent bis-THF acetogenin being isolated from the title species and represents a new type of these compounds. Bioactivities of these new structures against brine shrimp larvae and six human solid tumor cell lines were determined, and cytotoxic selectivities were shown for the lung (A-549) and breast (MCF-7) cell lines with up to a million times the potency of adriamycin.


Subject(s)
4-Butyrolactone/analogs & derivatives , Antineoplastic Agents, Phytogenic/pharmacology , Furans/chemistry , Furans/pharmacology , Trees/chemistry , 4-Butyrolactone/chemistry , 4-Butyrolactone/pharmacology , Animals , Antineoplastic Agents, Phytogenic/chemistry , Artemia , Drug Screening Assays, Antitumor , Humans , Magnetic Resonance Spectroscopy , Models, Chemical , Tumor Cells, Cultured
9.
J Nat Prod ; 60(1): 38-40, 1997 Jan.
Article in English | MEDLINE | ID: mdl-9014350

ABSTRACT

Two new sesquiterpenes, 10 alpha-hydroxyamorphan-4-en-3-one (1) and 4 alpha-methylcadinane-4 alpha-methyl-1 alpha,2 alpha,10 alpha-triol (2), together with four known compounds, sesquiterpenes 10 alpha-hydroxycadinan-4-en-3-one (3) and alpha-cadinol (4), diterpene ferruginol and lignan helioxanthin, were isolated from the whole plant of Taiwania cryptomerioides under bioassay-guided fractionations. The structures of 1 and 2 were elucidated mainly by the NMR spectroscopic analyses. Bioactivities of the isolated compounds against brine shrimp, yellow fever mosquito larvae, and human tumor cells are reported; compound 4 was the most bioactive, showing selectivity for the human colon tumor cell line (HT-29).


Subject(s)
Antineoplastic Agents, Phytogenic/isolation & purification , Insecticides/isolation & purification , Plants, Medicinal/chemistry , Aedes , Animals , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/pharmacology , Artemia , Drug Screening Assays, Antitumor , HT29 Cells , Humans , Insecticides/chemistry , Insecticides/pharmacology , Magnetic Resonance Spectroscopy , Molecular Conformation , Plant Extracts/pharmacology , Tumor Cells, Cultured
10.
J Nat Prod ; 59(11): 1029-34, 1996 Nov.
Article in English | MEDLINE | ID: mdl-8946743

ABSTRACT

Three new adjacent bis-tetrahydrofuran ring Annonaceous acetogenins with four hydroxy groups, bullatetrocin (1), 10-hydroxyasimicin (2), and 10-hydroxytrilobacin (3), were isolated by activity-directed fractionation from the stem bark of Asimina triloba. Their structures were established on the basis of chemical and spectral evidence. The absolute stereochemistry at the C-10 hydroxy position was determined by converting 2 and 3 to their ketolactone isomers, 2,4-cis/trans 10-hydroxyasimicinones and 2,4-cis/trans 10-hydroxytrilobacinones, respectively. The bioactivities of the new compounds against brine shrimp larvae and six human solid-tumor cell lines are reported, and structure-activity relationships between trihydroxylated and tetrahydroxylated acetogenins are discussed. In addition to 1-3, gigantetrocin A, 2,4-cis/trans-gigantetrocin A-ones, annonacin, and annonacin A were also isolated for the first time from this species.


Subject(s)
Furans/isolation & purification , Plant Epidermis/chemistry , Plants, Medicinal/chemistry , Animals , Artemia , Drug Screening Assays, Antitumor , Furans/pharmacology , Humans , Magnetic Resonance Spectroscopy , Mass Spectrometry , Spectrometry, Mass, Fast Atom Bombardment , Structure-Activity Relationship , Tumor Cells, Cultured
11.
Nat Toxins ; 4(3): 128-34, 1996.
Article in English | MEDLINE | ID: mdl-8743934

ABSTRACT

Two novel bioactive ketolactone Annonaceous acetogenins, (2,4-cis)-asimicinone (1) and (2,4-trans)-asimicinone (2), have been isolated from Asimina triloba (Annonaceae) by bioactivity directed fractionation. The separation of these two epimeric compounds was achieved by HPLC methods using a Si gel normal phase column eluted with acetone in hexane gradients. The assignments of cis or trans stereochemistry of the ketolactone moieties were made on the bases of 1H-1H COSY and NOESY experiments. 1 and 2 showed selective cytotoxicities against A-549 (human lung cancer) and MCF-7 (human breast cancer) cell lines with ED50 values as low as < 10(-7) micrograms/ml with 2 being the more active isomer.


Subject(s)
Furans/isolation & purification , Lactones/chemistry , Toxins, Biological/isolation & purification , Acetylation , Animals , Artemia/drug effects , Chromatography, High Pressure Liquid , Chromatography, Thin Layer , Furans/chemistry , Furans/toxicity , Humans , Lactones/toxicity , Lethal Dose 50 , Magnetic Resonance Spectroscopy , Molecular Weight , Plant Stems/metabolism , Spectrometry, Mass, Fast Atom Bombardment , Spectrophotometry, Ultraviolet , Spectroscopy, Fourier Transform Infrared , Stereoisomerism , Structure-Activity Relationship , Toxins, Biological/chemistry , Toxins, Biological/toxicity
12.
Bioorg Med Chem ; 4(1): 25-32, 1996 Jan.
Article in English | MEDLINE | ID: mdl-8689234

ABSTRACT

A novel acetogenin, asiminocin (1), was isolated by activity-directed fractionation from the stem bark of the paw paw tree, Asimina triloba. By spectral and chemical methods, 1 was identified as (30S)-hydroxy-4-deoxyasimicin. The absolute configuration of 1, along with those of previously reported acetogenins asimin, asiminacin, bullatin, (30S)-bullanin, and (30R) bullanin, was determined by Mosher ester methodology. Compound 1 was highly inhibitory to three human solid tumor cell lines with over a billion times the potency of adriamycin.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Furans/chemistry , Furans/pharmacology , Lactones/chemistry , Lactones/pharmacology , Tetrahydrofolates/chemistry , Trees/chemistry , Animals , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/isolation & purification , Artemia/drug effects , Circular Dichroism , Drug Screening Assays, Antitumor , Furans/isolation & purification , Humans , Lethal Dose 50 , Magnetic Resonance Spectroscopy , Models, Molecular , Molecular Structure , Stereoisomerism , Structure-Activity Relationship , Tumor Cells, Cultured
13.
J Nat Prod ; 58(9): 1398-406, 1995 Sep.
Article in English | MEDLINE | ID: mdl-7494147

ABSTRACT

Longicin [1] and (2,4-cis and trans)-goniothalamicinone [2], two new monotetrahydrofuran Annonaceous acetogenins, have been isolated from the leaves and twigs of Asimina longifolia (the long leaf paw paw) by the use of the brine shrimp lethality test for bioactivity-directed fractionation. The structures were elucidated based on spectroscopic and chemical methods. Compound 1 was converted to its ketolactone isomer, (2,4-cis and trans)-longicinone [3], to aid the stereochemical elucidation of 1. Compounds 1-3 showed selective and potent cytotoxicities to certain human tumor cell lines, with the potency of 1 against pancreatic carcinoma (PaCa-2) over one million times that of adriamycin. Nine known cytotoxic acetogenins, annonacin, xylomaticin, isoannonacin, gigantetrocins A and B, muricatetrocins A and B, gigantetrocin-A-one and goniothalamicin, were also isolated for the first time from this species.


Subject(s)
4-Butyrolactone/analogs & derivatives , Antineoplastic Agents, Phytogenic/isolation & purification , Plants, Medicinal/chemistry , Trees/chemistry , 4-Butyrolactone/chemistry , 4-Butyrolactone/isolation & purification , 4-Butyrolactone/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/pharmacology , Humans , Magnetic Resonance Spectroscopy , Molecular Structure , Tumor Cells, Cultured
14.
J Nat Prod ; 58(9): 1430-7, 1995 Sep.
Article in English | MEDLINE | ID: mdl-7494150

ABSTRACT

In a continuation of our research on bioactive components from the leaves of Annona muricata, three novel monotetrahydrofuran Annonaceous acetogenins, namely, annomutacin [1], (2,4-trans)-10R-annonacin-A-one [2], and (2,4-cis)-10R- annonacin-A-one [3], have been identified. Their structures were deduced by ms, nmr, ir, and uv spectral and chemical methods, and the absolute configurations were determined by Mosher ester methodology. A known bioactive amide, N-p-coumaroyl tyramine, was also found. Compound 1 and the mixture of compounds 2 and 3 showed selective cytotoxicities against the human A-549 lung tumor cell line.


Subject(s)
4-Butyrolactone/analogs & derivatives , Antineoplastic Agents, Phytogenic/isolation & purification , Plants, Medicinal/chemistry , 4-Butyrolactone/chemistry , 4-Butyrolactone/isolation & purification , 4-Butyrolactone/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/pharmacology , Humans , Magnetic Resonance Spectroscopy , Molecular Structure , Stereoisomerism , Tumor Cells, Cultured
15.
J Nat Prod ; 58(6): 830-6, 1995 Jun.
Article in English | MEDLINE | ID: mdl-7673926

ABSTRACT

The leaves of Annona muricata have yielded eight monotetrahydrofuran Annonaceous acetogenins. Two of them, annomuricins A [1] and B [2], whose chemical structures were deduced by ms, nmr, ir, and uv spectral and chemical methods, are novel and unusual. Compounds 1 and 2 each possess five hydroxyl groups; two hydroxyl groups are vicinal, with the vicinal group of 1 threo and that of 2 erythro. The absolute configurations of 1 and 2 were determined by Mosher ester methodology. Six monotetrahydrofuran acetogenins, previously described in the seeds, were found in the leaves; these are gigantetrocin A, annonacin-10-one, muricatetrocins A and B, annonacin, and goniothalamicin.


Subject(s)
4-Butyrolactone/analogs & derivatives , Antineoplastic Agents, Phytogenic/isolation & purification , Furans/isolation & purification , Plants, Medicinal/chemistry , 4-Butyrolactone/analysis , 4-Butyrolactone/isolation & purification , Antineoplastic Agents, Phytogenic/analysis , Drug Screening Assays, Antitumor , Furans/analysis , Humans , Indonesia , Magnetic Resonance Spectroscopy , Mass Spectrometry , Molecular Conformation , Spectrophotometry, Infrared , Spectrophotometry, Ultraviolet , Tumor Cells, Cultured
16.
J Nat Prod ; 58(6): 902-8, 1995 Jun.
Article in English | MEDLINE | ID: mdl-7673935

ABSTRACT

The leaves of Annona muricata have yielded the novel monotetrahydrofuran Annonaceous acetogenins, muricatocins A [1] and B [2]. Each compound possesses five hydroxyl groups, with two hydroxyl groups at the C-10 and C-12 positions. The absolute configurations of 1 and 2 (except for positions C-10 and C-12) were determined by Mosher ester methodology. The C-10, C-12 acetonides (1c, 2c) suggested relative stereochemistry and significantly enhanced cytotoxicity against the A-549 human lung tumor cell line. Three known monotetrahydrofuran acetogenins, annonacin A, (2,4-trans)-isoannonacin, and (2,4-cis)-isoannonacin, were also found.


Subject(s)
4-Butyrolactone/analogs & derivatives , Antineoplastic Agents, Phytogenic/isolation & purification , Furans/isolation & purification , Plant Leaves/chemistry , Plants, Medicinal/chemistry , 4-Butyrolactone/chemistry , 4-Butyrolactone/isolation & purification , 4-Butyrolactone/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/pharmacology , Drug Screening Assays, Antitumor , Furans/chemistry , Furans/pharmacology , Humans , Magnetic Resonance Spectroscopy , Mass Spectrometry , Molecular Conformation , Tumor Cells, Cultured
17.
J Nat Prod ; 58(6): 909-15, 1995 Jun.
Article in English | MEDLINE | ID: mdl-7673936

ABSTRACT

The leaves of Annona muricata have yielded two additional monotetrahydrofuran Annonaceous acetogenins, annomuricin C [1] and muricatocin C [2]. Compounds 1 and 2 each possess five hydroxyl groups; two hydroxyl groups are at the C-10/C-11 and C-10/C-12 positions in 1 and 2, respectively. The absolute configurations of 1 and 2, except for positions C-10 and C-11 or C-12, were determined by Mosher ester methodology. The C-10/C-11 and C-10/C-12 acetonides (1c, 2c) suggested relative stereochemistry and significantly enhanced the cytotoxicities against the A-549 human lung and the MCF-7 human beast solid tumor cell lines. One known monotetrahydrofuran acetogenin, gigantetronenin, not described previously from this plant, was also found.


Subject(s)
4-Butyrolactone/analogs & derivatives , Antineoplastic Agents, Phytogenic/isolation & purification , Furans/isolation & purification , Plants, Medicinal/chemistry , 4-Butyrolactone/analysis , 4-Butyrolactone/isolation & purification , 4-Butyrolactone/pharmacology , Antineoplastic Agents, Phytogenic/analysis , Antineoplastic Agents, Phytogenic/pharmacology , Drug Screening Assays, Antitumor , Furans/analysis , Furans/pharmacology , Humans , Indonesia , Magnetic Resonance Spectroscopy , Mass Spectrometry , Molecular Conformation , Spectrophotometry, Infrared , Spectrophotometry, Ultraviolet , Tumor Cells, Cultured
18.
J Nat Prod ; 58(4): 532-9, 1995 Apr.
Article in English | MEDLINE | ID: mdl-7623031

ABSTRACT

Asimicin and a new cytotoxic Annonaceous acetogenin, venezenin [1], were isolated from the bark of Xylopia aromatica by bioactivity-directed fractionation using lethality to brine shrimp. Compound 1 represents an unusual type of C37 Annonaceous acetogenin, lacking either tetrahydrofuran (THF) or epoxide rings and possessing a double bond located two methylenes away from a vicinal diol in the hydrocarbon chain. The structure of 1 was elucidated by 1H- and 13C-nmr, COSY, single-relayed COSY, and by HMBC techniques, and derivatization. Annomontacin 10-one [6] and 18/21-cis-annomontacin-10-one [7], two semi-synthetic mono-THF acetogenins were prepared from 1. These acetogenins showed cytotoxicity, comparable or superior to adriamycin, against three human solid tumor cell lines. Reduction of the 10-keto of 1 to the racemic OH-10 derivative enhanced the bioactivity, as did the conversion of 1 to 6 and 7. Venezenin [1], like other Annonaceous acetogenins, showed inhibition of oxygen uptake by rat liver mitochondria and demonstrated that the THF ring may not be essential to this mode of action.


Subject(s)
Antineoplastic Agents, Phytogenic/isolation & purification , Furans/isolation & purification , Plants, Medicinal/chemistry , Animals , Antineoplastic Agents, Phytogenic/pharmacology , Artemia , Doxorubicin/pharmacology , Drug Screening Assays, Antitumor , Furans/pharmacology , Gas Chromatography-Mass Spectrometry , Humans , In Vitro Techniques , Magnetic Resonance Spectroscopy , Mitochondria, Liver/drug effects , Mitochondria, Liver/metabolism , Oxygen Consumption/drug effects , Rats , Venezuela
19.
Zhonghua Wai Ke Za Zhi ; 32(10): 619-20, 1994 Oct.
Article in Chinese | MEDLINE | ID: mdl-7750423

ABSTRACT

5 cases of complete bladder exstrophy were treated by one stage reconstruction with abdominal wall skin flap and rectus abdominis muscle flap. Closure of the abdominal wall and bladder defect were achieved satisfactorily in all the patients. 4 patients have been followed up for 1.5-10.5 years. 3 patients whose bladder neck had been augmented by rectus abdominis muscle flap were continent but 1 patient whose bladder neck had not been, had giggle incontinence. The renal functions were all normal in these patients.


Subject(s)
Bladder Exstrophy/surgery , Epispadias/surgery , Rectus Abdominis/transplantation , Surgical Flaps/methods , Adult , Bladder Exstrophy/complications , Child , Child, Preschool , Epispadias/complications , Follow-Up Studies , Humans , Male
20.
J Med Chem ; 37(13): 1971-6, 1994 Jun 24.
Article in English | MEDLINE | ID: mdl-8027979

ABSTRACT

Activity-directed fractionation of the stem bark extracts of the North American paw paw tree, Asimina triloba (Annonaceae), has yielded three further acetogenins: asimin (2), asiminacin (3), and asiminecin (4). 2-4 are structural isomers of asimicin (1), which is a potent inhibitor of mitochondrial NADH:ubiquinone oxidoreductase, and thus exhibits potent antitumor and pesticidal effects. 2-4 have the same carbon skeleton and configurations as those of 1, but they have the third hydroxyl group located at C-10, C-28, and C-29, respectively, rather than at C-4. The determinations of the hydroxyl group locations were largely based on mass spectral analyses of TMSi and TMSi-d9 derivatives. 2-4 all showed highly potent cytotoxicities (ED50 values as low as < 10(-12) micrograms/mL) with notable selectivities for the HT-29 human colon cancer cell line. The presence of a third hydroxyl at C-4, C-10, C-28, or C-29, as in 1-4, greatly enhances the bioactivity of 4-deoxyasimicin (5).


Subject(s)
Antineoplastic Agents, Phytogenic/chemistry , Furans/chemistry , Furans/pharmacology , Lactones/pharmacology , Neoplasms/drug therapy , Antineoplastic Agents, Phytogenic/pharmacology , Cell Death/drug effects , Drug Screening Assays, Antitumor , Furans/isolation & purification , Humans , Lactones/chemistry , Lactones/isolation & purification , Magnetic Resonance Spectroscopy , Mass Spectrometry , Neoplasms/pathology , Stereoisomerism , Structure-Activity Relationship , Tumor Cells, Cultured
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