Shea nuts play an important role in food security for rural folks within sub-Sahara Africa, serving as the main source of income for many people living in Northern Ghana. Unfortunately, the full economic potential of ...Shea nuts play an important role in food security for rural folks within sub-Sahara Africa, serving as the main source of income for many people living in Northern Ghana. Unfortunately, the full economic potential of the Sheanut tree has not been fully realized due to the difficulty involved in its domestication. This difficulty in vegetatively propagating sheanut trees has greatly hindered its cultivation and the realization of its true economic potential. Two experiments were conducted to investigate the effects of rooting media and varying indole 3-butyric acid (IBA) concentrations on adventitious root formation in cuttings taken from coppiced sheanut trees. Results indicated that 3000 ppm produced significantly (p 0.05) better rooting (57.5%) than 5000 ppm (30%), 7000 ppm (45.0%) and the control (7.5%). Although the levels of soluble sugars (SS) and total free phenols (TFP) in the cutting were significantly (p 0.05) higher at the end of the experiment (after IBA treatment) compared to the start (prior to IBA treatment), the SS and TFP trends observed did not clearly explain the rooting differences found between the IBA levels investigated. Callus formation was significantly (p 0.05) higher (35.0%) in the control (no IBA). Generally, callus formation decreased with increasing IBA concentration. In the rooting media experiment, rooting was significantly (p 0.05) higher in the rice husk medium (35.0%) compared to that in the palm fiber (18.3%), saw dust (14.1%) and top soil (16.7%) media.展开更多
AIM: To explore the mechanisms underlying the apoptosis of human pancreatic cancer BXPC-3 cells induced by indole-3-acetic acid (TAA) in combination with horseradish peroxidase (HRP).METHODS: BXPC-3 cells derived from...AIM: To explore the mechanisms underlying the apoptosis of human pancreatic cancer BXPC-3 cells induced by indole-3-acetic acid (TAA) in combination with horseradish peroxidase (HRP).METHODS: BXPC-3 cells derived from human pancreatic cancer were exposed to 40 or 80 μmol/L IAA and 1.2 μg/mL HRP at different times. Then, MTT assay was used to detect the cell proliferation. Flow cytometry was performed to analyze cell cycle. Terminal deoxynucleotidyl transferasemediated dUTP nick end labeling assay was used to detect apoptosis. 2,7-Dichlorofluorescin diacetate uptake was measured by confocal microscopy to determine free radicals. Level of malondialdehyde (MDA) and activity of superoxide dismutase (SOD) were measured by biochemical methods.RESULTS: IAA/HRP initiated growth inhibition of BXPC-3 cells in a dose- and time-dependent manner. Flow cytometry revealed that the cells treated for 48 h were arrested at G1/G0. After exposure to 80 μmol/L IAA plus 1.2 μg/mL HRP for 72 h, the apoptosis rate increased to 72.5‰,which was nine times that of control. Content of MDA and activity of SOD increased respectively after treatment compared to control. Meanwhile, IAA/HRP stimulated the formation of free radicals.CONCLUSION: The combination of IAA and HRP can inhibit the growth of human pancreatic cancer BXPC-3 cells in vitro by inducing apoptosis.展开更多
A series of ethyl 5-hydroxyindole-3-earboxylates 6a-10r was designed and synthesized. The structures of all the compounds were confirmed by IR, ^1H NMR, and MS and their anti-hepatitis B virus (HBV) activities were ...A series of ethyl 5-hydroxyindole-3-earboxylates 6a-10r was designed and synthesized. The structures of all the compounds were confirmed by IR, ^1H NMR, and MS and their anti-hepatitis B virus (HBV) activities were evaluated in 2.2.15 cells. Among them, compound 7g { ethyl 5-hydroxy-2- [ ( 3-methoxyphenylsulfinyl ) methyl ] -1-methyl-4- [ (4-methylpiperazin-1-yl) methyl ]-1H-indole-3-carboxylate} displays a significant anti-HBV activity, which is more potent than the positive control lamivudine.展开更多
A comprehensive exploration of the aminolysis mechanism for methyl indole-3-acetate with ammonia is carried out by employing the B3 LYP/6-311++G(d,p), M06-2 X/6-311++G(d,p) and MP2/6-311++G(d,p)//M06-2 X/6-311++G(d,p)...A comprehensive exploration of the aminolysis mechanism for methyl indole-3-acetate with ammonia is carried out by employing the B3 LYP/6-311++G(d,p), M06-2 X/6-311++G(d,p) and MP2/6-311++G(d,p)//M06-2 X/6-311++G(d,p) levels. Two alterative reaction channels of the concerted and addition/elimination stepwise processes including the uncatalyzed, base-catalyzed reactions are taken into consideration. Subsequently, the substituent effects and solvent effects in methanol are also evaluated at the M06-2 X/6-311++G(d,p) level. The calculated results indicate that the calculated values of M06-2 X level are quite close to those of MP2, the stepwise pathway has more advantages to the concerted one for all of the reaction processes and the catalyst facilitates the proton migration and decreases the energy barriers as well. It is shown that the most preferred mechanism is the based-catalyzed stepwise process, the substituent of NH2 group slightly accelerates all the aminolysis reaction processes, and the solvent effect does not remarkably change the mechanism of the reaction.展开更多
Objective:To study the derivatives of 1,2,4-triazino[5,6-b]indole-3-thione for antidepressant activity in olfactory bulbectomized(OBX)rats.Out of various derivatives tested for acute tail suspension test,the two deriv...Objective:To study the derivatives of 1,2,4-triazino[5,6-b]indole-3-thione for antidepressant activity in olfactory bulbectomized(OBX)rats.Out of various derivatives tested for acute tail suspension test,the two derivatives showiug prominent action were.selected for bilateral olfactory bulbeetomy rsodel of ehronic depression in rats.Methods:The sub aeute effects of 14-day oral pretreatment of two derivatives labeled as 3a(70 mg/kg)and 3r(70 mg/kg),imipramine(20 mg/kg),fluoxetiue(30 mg/kg)and moclobemide(15 mg/kg)were evaluated on bilateral bulbectomy induced rise in body weight,hyperphagia,hyperactivity,and on sexual dysfunction.The serum sodium concentration,body temperature,and heart rate were also recorded.Results:The derivatives3a and 3r showed reversal of drop in body weight,reversed OBX indueed hyperactivity,normalized body temperature,heart rate,and serum sodium concentration.In elevated maze test,moclobemide,3a,3r treatment significantly redueed time spent in open arm as compared to OBX rats.3a and 3r also irsproved sexual behavior parameters.Conclusions:The present study shows promising antidepressant action and provides a proof of concept for the chronic treatrsent of 3a,3r to treat depression.展开更多
Nitric oxide(NO)and hydrogen peroxide(H2O2)are essential signaling molecules with key roles in auxin induced adventitious root formation in many plants.However,whether they are the sole determinants for adventitio...Nitric oxide(NO)and hydrogen peroxide(H2O2)are essential signaling molecules with key roles in auxin induced adventitious root formation in many plants.However,whether they are the sole determinants for adventitious root formation is worth further study.In this study,endogenous NO and H2O2 were monitored in tea cutting with or without indole-3-butyric acid(IBA)treatment by using the fluorescent probes diaminofluorescein diacetate(DAF-2DA)and 2',7'-dichlorodihydrofluorescein diacetate(DCF-DA),respectively.The overproduction of NO and H2O2 was detected in the rooting parts of tea cuttings treated with or without IBA.But little NO and H2O2 was detected before the initiation phase of tea cuttings even with IBA treatment indicating that they might be not directly induced by IBA.Further carbon and nitrogen analysis found that the overproduction of NO and H2O2 were coincident with the consumption of soluble sugars and the assimilation of nitrogen.These results suggest that rooting phases should be taken into consideration with the hypothesis that auxin induces adventitious root formation via NO-and H2O2-dependent pathways and sink establishment might be a prerequisite for NO and H2O2 mediated adventitious root formation.展开更多
Effects of different Indole-3-Buteric Acid (IBA) concentrations (0, 1 000, 1 500 and 2 500 ppm) and curing types (soft wood, semi hard and hard wood) of plane tree were investigated with Randomized Complete Bloc...Effects of different Indole-3-Buteric Acid (IBA) concentrations (0, 1 000, 1 500 and 2 500 ppm) and curing types (soft wood, semi hard and hard wood) of plane tree were investigated with Randomized Complete Block Design (RCBD) at the Agricultural research station, Charsadda. The maximum survival percentage, plant height (cm), root length (era), numbers of roots and root weight per cutting were significantly higher in hard wood cuttings. IBA concentration had no speculative effect on plane tree cuttings. Thus, hard wood cutting was the best choice for plan tree propagation.展开更多
The present study, conducted during 2016 and 2017 seasons, aimed to investigate the effect of IBA on rooting of Piper betle L. stem cuttings (softwood and semi-hardwood). The experiment was undertaken in misting house...The present study, conducted during 2016 and 2017 seasons, aimed to investigate the effect of IBA on rooting of Piper betle L. stem cuttings (softwood and semi-hardwood). The experiment was undertaken in misting house field 2 UPM using the sand media to determine the adventitious roots initiation and development using the histological method. The cuttings were treated with different IBA concentrations (0, 500, 1000, 1500 and 2000 mg/L). The nodes explants were used in the development of a protocol for in vitro propagation of P. betle L., with different concentrations of Clorox with different times of immersion (20% Clorox 10 minutes, 30% Clorox 10 minutes, 20% Clorox 20 minutes, and 30% 20 minutes). In multiplication of the plantlets, Murashige and Skoog (MS) medium with different concentrations of BAP (0, 0.5, 1.0, 2.0 mg/L) were used to investigate the rooting of the explants. The results indicated that the types of the cuttings were different in the rooting capacity and the length of the roots. Moreover, it was found that in comparison with the control treatment, by a rise in the concentrations of the IBA, there was a significant upsurge in the rooting percentage, the root diameter, and the number of the roots. The results indicated that the types of cutting with 1000, 1500 and 2000 mg/L IBA perform better in the root percentage (100%) in the semi hardwood cuttings. The best results, however, were 2000 mg/L IBA in the semi hardwood cuttings, with the number of the roots to be 35.05, and the fresh weight of the roots to be 3.94 g, the dry weight of the roots to be 0.33 g, the length of the roots to be 391.88 cm, the roots diameter to be 1.21 mm, the surface area of the roots to be 121.83 cm2, and the root volume to be 2.99 cm3. Nonetheless, the optimal concentration of Clorox with the time immersion was 20% with the 20-minute immersion time, which produced a shoot induction percentage of 30% dead explants and a mean number of 70.00 shoots per explant and the optimal concentration of benzylaminopurine (BAP) at 1.0 mg/L. It is of note that a shoot induction percentage of 22.29% and a mean number of 4.1% number of auxiliary bud per treatment. P. betle shoots in MS medium without PGR MS (0.0) yielded a good rooting.展开更多
3-(1-Ethyl-1H-indole-3-carbonyl)aminopropionic acid has been synthesized by alkylation of 3-(1H-indole-3-carbonyl)aminopropionic acid methyl ester with bromoethane,follo-wed by saponifying and acidating,in 89.0% y...3-(1-Ethyl-1H-indole-3-carbonyl)aminopropionic acid has been synthesized by alkylation of 3-(1H-indole-3-carbonyl)aminopropionic acid methyl ester with bromoethane,follo-wed by saponifying and acidating,in 89.0% yield.Its crystal structure was gotten and determined by X-ray diffraction method.The crystal is of orthorhombic,space group P212121 with a = 8.9490(12),b = 11.1010(15),c = 13.0475(18) ,V = 1296.2(3) 3,Z = 4,Dc = 1.334 g/cm3,λ = 0.71073 ,μ(MoKα) = 0.095 mm-1,Mr = 260.29 and F(000) = 552.The structure was refined to R = 0.0306 and wR = 0.1445 for 2612 observed reflections with I 2σ(I).In the crystal structure,molecules are linked to each other through hydrogen bonds of N(2)-H(2)···O(1) and O(3)-H(3)···O(1),generating a three-dimensional network.展开更多
Methyl 3-(5-bromo-l-ethyl-lH-indole-3-carbonyl)aminopropionate has been synthesized by the acylation of 5-bromo-3-trichloroacetylindole with β-alanine methyl ester, followed by alkylation with ethyl iodide, in 82.6...Methyl 3-(5-bromo-l-ethyl-lH-indole-3-carbonyl)aminopropionate has been synthesized by the acylation of 5-bromo-3-trichloroacetylindole with β-alanine methyl ester, followed by alkylation with ethyl iodide, in 82.6% yield. Its crystal structure was gotten and determined by X-ray diffraction method. The crystal is of monoclinic, space group P2/c with a = 11.7927(8), b = 14.9342(8), c = 9.0060(5) A, β = 101.558(6)°, V = 1553.93(16) A3, Z = 4, Dc= 1.510 g/cm3, 2 = 0.71073 A,μ(MoKa) = 2.656 mm-1, Mr = 353.22 and F(000) = 720. The structure was refined to R = 0.0401 and wR = 0.0825 for 1704 observed reflections with I 〉 2σ(I). In the crystal structure, intermolecular N(2)-H(2)...O(1) hydrogen bond and weak intermolecular bonds (C(1)-H(1)...O(1) and C(10)-H(10B)-O(2)) are formed, and π-π stacking also exists.展开更多
The coupling reaction of 3-cyanoacetyl-2-methylindole 1a with the aromatic diazonium salts gave the corresponding arylhydrazones 2a-e. Compounds 2 were used for synthesis of 4-aminopyrazole-5-carbonitrile 4a-e and 5-a...The coupling reaction of 3-cyanoacetyl-2-methylindole 1a with the aromatic diazonium salts gave the corresponding arylhydrazones 2a-e. Compounds 2 were used for synthesis of 4-aminopyrazole-5-carbonitrile 4a-e and 5-amino-4-arylazo-3-pyrazoles 5a-e derivatives. Also, treatment of 3-cyanoacetyl-2-phenylindole 1b with phenyl isothiocyanate gave the corresponding thioacetanilide 7. The later compound 7 was utilized as the key intermediate for the synthesis of some new thiadiazole derivatives 9a-r. The structures of all new compounds were elucidated on the basis of elemental analysis and spectral data.展开更多
An efficient and facile method for the synthesis of 3-indolyl-substituted phthalides by Friedel-Crafts alkylation of indoles with 3-hydroxyisobenzofuran-1(3H)-one has been developed. Using only 2 mol-% TsOH·H2O a...An efficient and facile method for the synthesis of 3-indolyl-substituted phthalides by Friedel-Crafts alkylation of indoles with 3-hydroxyisobenzofuran-1(3H)-one has been developed. Using only 2 mol-% TsOH·H2O as the catalyst, various substituted indoles can react smoothly at room temperature to give the corresponding phthalides products in good to excellent yields (up to 96%).展开更多
The difference of sensitivity to indole- 3-acetic acid ( IAA ) combined with horseradish peroxidase (HRP) in K562 and BXPC- 3 cells was investigated. The cell proliferation was determined by MTF assay. The cell cy...The difference of sensitivity to indole- 3-acetic acid ( IAA ) combined with horseradish peroxidase (HRP) in K562 and BXPC- 3 cells was investigated. The cell proliferation was determined by MTF assay. The cell cycle and apoptosis of K562 and BXPC-3 cells were examined by a fluorescence flow cytometer (FCM) and terminal deoxynacleotidyl transferase-mediated dUTP nick-end labeling (TUNEL) respectively. The experimental results show that IAA and HRP could inhibit BXPC- 3 cell proliferation greatly compared with K562 cell during the first 48 h . The cell cycle was arrested predominantly at G2/ M phase in K562 and BXPC- 3 cells. The cell apoptosis of K562 and BXPC- 3 was induced by IAA/ HRP. There was a significant difference between the two cell lines since BXPC-3 cells were more sensitive than K562 cells by treatments with combination of IAA and HRP.展开更多
A new coordination polymer {[Cd(C_(21)H_(14)N_6)(C_8H_4O_4)]·H_2O}_n(1) was synthesized by an elaborate design via the reaction of 3-(2,6-di(pyrazin-2-yl)pyridin-4-yl)-1H-indole(bppi),1,4-benzene-...A new coordination polymer {[Cd(C_(21)H_(14)N_6)(C_8H_4O_4)]·H_2O}_n(1) was synthesized by an elaborate design via the reaction of 3-(2,6-di(pyrazin-2-yl)pyridin-4-yl)-1H-indole(bppi),1,4-benzene-dicarboxylic acid(H2bdc) and cadmium(Ⅱ) nitrate in CH_3OH/H_2O mixed solvents. Complex 1 crystallizes in orthorhombic,space group Ccca with a = 20.012(4),b = 31.881(6),c = 19.808(4) ?,V = 12638(4) ?~3,Z = 16,C_(29)H_(20)CdN_6O_5,M_r = 644.91,D_c = 1.356 g·cm^(-3),μ = 0.735 mm^(-1),F(000) = 5184,GOOF = 1.046,the final R = 0.0405 and wR = 0.1063 for 6870 observed reflections(I 〉 2σ(I)). The Cd(Ⅱ) centre is hepta-coordinated by three N and four O atoms from one bppi terminal ligand and two bdc2– ligands,respectively,displaying a capped trigonal prism geometry. Structure extension gives coordination polymeric chains,in which the bdc2– linkers connect Cd(Ⅱ) cations into a one-dimensional(1D) coordination polymer along the c axis,giving zigzag chains with the Cd···Cd separation of 11.178(1) ?. The adjacent bppi terminal ligands in the chains are anti-periplanar conformation. The three-dimensional(3D) structure is stabilized by π···π stacking and hydrogen-bonding interactions to form a supramolecular self-penetrating network with 1D channels. In 1,there are voids 2999.7 ?~3 with 23.7% of per unit cell volume. Thermal analysis indicates that the framework of 1 is stable until 651 K and the photoluminescence of 1 in the solid shows very weak fluorescence at 382 and 560 nm upon excitation at 310 nm.展开更多
Reaction of indole-3-carboxaldehydes 4 with hydrazine derivatives and different substituted acid hydrazides afforded the corresponding hydrazine derivatives 5a-c and acid hydrazide derivatives 7-11 respectively. Conde...Reaction of indole-3-carboxaldehydes 4 with hydrazine derivatives and different substituted acid hydrazides afforded the corresponding hydrazine derivatives 5a-c and acid hydrazide derivatives 7-11 respectively. Condensation of indole-3-carboxaldehydes 4 with phenacyl bromide and thiourea gives 1,3-thiazol-2-amine derivative 18. On the other hand, reaction 4 with 3-acetylchromene-2-one afforded chalcone derivative 19. Compound 4 undergoing Knoevenagel condensation with cyanoacetamide, ethyl cyanoacetate, benzimidazol-2-ylacetonitrile, rhodanine-3-acetic acid, 2,3-dihydropyrimidin-4-one derivative and 2,4-dihydropyrazol-3-one afforded the compounds 20a,b, 22, 23, 27 and 28 respectively. The structure of the newly synthesized compounds has been confirmed by elemental analysis and spectra data. The antimicrobial activities of the some newly synthesized compounds were measured and showed that most of them have high展开更多
A novel series of ethyl 5-hydroxy-4-substituted aminomethyl-2-sulfinylmethyl-lH-indole-3-carboxylates 8a--8j and 11e--11f was synthesized and evaluated in HepG2.2.15 cells for their anti-hepatitits B virus(HBV) acti...A novel series of ethyl 5-hydroxy-4-substituted aminomethyl-2-sulfinylmethyl-lH-indole-3-carboxylates 8a--8j and 11e--11f was synthesized and evaluated in HepG2.2.15 cells for their anti-hepatitits B virus(HBV) activity and cytotoxicity. Among them, six compounds showed more potent inhibitory activity than lamivudine. Compound 8e exhibited the most significant anti-HBV activity with an IC50 value of 1.62 μmol/L, which was 33-times more potent than the reference drug lamivudine(IC50=54.78μmol/L).展开更多
文摘Shea nuts play an important role in food security for rural folks within sub-Sahara Africa, serving as the main source of income for many people living in Northern Ghana. Unfortunately, the full economic potential of the Sheanut tree has not been fully realized due to the difficulty involved in its domestication. This difficulty in vegetatively propagating sheanut trees has greatly hindered its cultivation and the realization of its true economic potential. Two experiments were conducted to investigate the effects of rooting media and varying indole 3-butyric acid (IBA) concentrations on adventitious root formation in cuttings taken from coppiced sheanut trees. Results indicated that 3000 ppm produced significantly (p 0.05) better rooting (57.5%) than 5000 ppm (30%), 7000 ppm (45.0%) and the control (7.5%). Although the levels of soluble sugars (SS) and total free phenols (TFP) in the cutting were significantly (p 0.05) higher at the end of the experiment (after IBA treatment) compared to the start (prior to IBA treatment), the SS and TFP trends observed did not clearly explain the rooting differences found between the IBA levels investigated. Callus formation was significantly (p 0.05) higher (35.0%) in the control (no IBA). Generally, callus formation decreased with increasing IBA concentration. In the rooting media experiment, rooting was significantly (p 0.05) higher in the rice husk medium (35.0%) compared to that in the palm fiber (18.3%), saw dust (14.1%) and top soil (16.7%) media.
基金Supported by the Natural Science Foundation of Shaanxi Province, No. 2003C215
文摘AIM: To explore the mechanisms underlying the apoptosis of human pancreatic cancer BXPC-3 cells induced by indole-3-acetic acid (TAA) in combination with horseradish peroxidase (HRP).METHODS: BXPC-3 cells derived from human pancreatic cancer were exposed to 40 or 80 μmol/L IAA and 1.2 μg/mL HRP at different times. Then, MTT assay was used to detect the cell proliferation. Flow cytometry was performed to analyze cell cycle. Terminal deoxynucleotidyl transferasemediated dUTP nick end labeling assay was used to detect apoptosis. 2,7-Dichlorofluorescin diacetate uptake was measured by confocal microscopy to determine free radicals. Level of malondialdehyde (MDA) and activity of superoxide dismutase (SOD) were measured by biochemical methods.RESULTS: IAA/HRP initiated growth inhibition of BXPC-3 cells in a dose- and time-dependent manner. Flow cytometry revealed that the cells treated for 48 h were arrested at G1/G0. After exposure to 80 μmol/L IAA plus 1.2 μg/mL HRP for 72 h, the apoptosis rate increased to 72.5‰,which was nine times that of control. Content of MDA and activity of SOD increased respectively after treatment compared to control. Meanwhile, IAA/HRP stimulated the formation of free radicals.CONCLUSION: The combination of IAA and HRP can inhibit the growth of human pancreatic cancer BXPC-3 cells in vitro by inducing apoptosis.
基金Supported by the National Natural Science Foundation of China(No.20042047).
文摘A series of ethyl 5-hydroxyindole-3-earboxylates 6a-10r was designed and synthesized. The structures of all the compounds were confirmed by IR, ^1H NMR, and MS and their anti-hepatitis B virus (HBV) activities were evaluated in 2.2.15 cells. Among them, compound 7g { ethyl 5-hydroxy-2- [ ( 3-methoxyphenylsulfinyl ) methyl ] -1-methyl-4- [ (4-methylpiperazin-1-yl) methyl ]-1H-indole-3-carboxylate} displays a significant anti-HBV activity, which is more potent than the positive control lamivudine.
基金supported by the Special Funds of the National Natural Science Foundation of China(No.11347161)
文摘A comprehensive exploration of the aminolysis mechanism for methyl indole-3-acetate with ammonia is carried out by employing the B3 LYP/6-311++G(d,p), M06-2 X/6-311++G(d,p) and MP2/6-311++G(d,p)//M06-2 X/6-311++G(d,p) levels. Two alterative reaction channels of the concerted and addition/elimination stepwise processes including the uncatalyzed, base-catalyzed reactions are taken into consideration. Subsequently, the substituent effects and solvent effects in methanol are also evaluated at the M06-2 X/6-311++G(d,p) level. The calculated results indicate that the calculated values of M06-2 X level are quite close to those of MP2, the stepwise pathway has more advantages to the concerted one for all of the reaction processes and the catalyst facilitates the proton migration and decreases the energy barriers as well. It is shown that the most preferred mechanism is the based-catalyzed stepwise process, the substituent of NH2 group slightly accelerates all the aminolysis reaction processes, and the solvent effect does not remarkably change the mechanism of the reaction.
文摘Objective:To study the derivatives of 1,2,4-triazino[5,6-b]indole-3-thione for antidepressant activity in olfactory bulbectomized(OBX)rats.Out of various derivatives tested for acute tail suspension test,the two derivatives showiug prominent action were.selected for bilateral olfactory bulbeetomy rsodel of ehronic depression in rats.Methods:The sub aeute effects of 14-day oral pretreatment of two derivatives labeled as 3a(70 mg/kg)and 3r(70 mg/kg),imipramine(20 mg/kg),fluoxetiue(30 mg/kg)and moclobemide(15 mg/kg)were evaluated on bilateral bulbectomy induced rise in body weight,hyperphagia,hyperactivity,and on sexual dysfunction.The serum sodium concentration,body temperature,and heart rate were also recorded.Results:The derivatives3a and 3r showed reversal of drop in body weight,reversed OBX indueed hyperactivity,normalized body temperature,heart rate,and serum sodium concentration.In elevated maze test,moclobemide,3a,3r treatment significantly redueed time spent in open arm as compared to OBX rats.3a and 3r also irsproved sexual behavior parameters.Conclusions:The present study shows promising antidepressant action and provides a proof of concept for the chronic treatrsent of 3a,3r to treat depression.
基金indebted to the earmarked fund for China Agriculture Research System (CARS-19)the Innovation Project for Agricultural Sciences and Technology from the Chinese Academy of Agricultural Sciences (CAAS-ASTIP2017-TRICAAS) for their financial supports
文摘Nitric oxide(NO)and hydrogen peroxide(H2O2)are essential signaling molecules with key roles in auxin induced adventitious root formation in many plants.However,whether they are the sole determinants for adventitious root formation is worth further study.In this study,endogenous NO and H2O2 were monitored in tea cutting with or without indole-3-butyric acid(IBA)treatment by using the fluorescent probes diaminofluorescein diacetate(DAF-2DA)and 2',7'-dichlorodihydrofluorescein diacetate(DCF-DA),respectively.The overproduction of NO and H2O2 was detected in the rooting parts of tea cuttings treated with or without IBA.But little NO and H2O2 was detected before the initiation phase of tea cuttings even with IBA treatment indicating that they might be not directly induced by IBA.Further carbon and nitrogen analysis found that the overproduction of NO and H2O2 were coincident with the consumption of soluble sugars and the assimilation of nitrogen.These results suggest that rooting phases should be taken into consideration with the hypothesis that auxin induces adventitious root formation via NO-and H2O2-dependent pathways and sink establishment might be a prerequisite for NO and H2O2 mediated adventitious root formation.
文摘Effects of different Indole-3-Buteric Acid (IBA) concentrations (0, 1 000, 1 500 and 2 500 ppm) and curing types (soft wood, semi hard and hard wood) of plane tree were investigated with Randomized Complete Block Design (RCBD) at the Agricultural research station, Charsadda. The maximum survival percentage, plant height (cm), root length (era), numbers of roots and root weight per cutting were significantly higher in hard wood cuttings. IBA concentration had no speculative effect on plane tree cuttings. Thus, hard wood cutting was the best choice for plan tree propagation.
文摘The present study, conducted during 2016 and 2017 seasons, aimed to investigate the effect of IBA on rooting of Piper betle L. stem cuttings (softwood and semi-hardwood). The experiment was undertaken in misting house field 2 UPM using the sand media to determine the adventitious roots initiation and development using the histological method. The cuttings were treated with different IBA concentrations (0, 500, 1000, 1500 and 2000 mg/L). The nodes explants were used in the development of a protocol for in vitro propagation of P. betle L., with different concentrations of Clorox with different times of immersion (20% Clorox 10 minutes, 30% Clorox 10 minutes, 20% Clorox 20 minutes, and 30% 20 minutes). In multiplication of the plantlets, Murashige and Skoog (MS) medium with different concentrations of BAP (0, 0.5, 1.0, 2.0 mg/L) were used to investigate the rooting of the explants. The results indicated that the types of the cuttings were different in the rooting capacity and the length of the roots. Moreover, it was found that in comparison with the control treatment, by a rise in the concentrations of the IBA, there was a significant upsurge in the rooting percentage, the root diameter, and the number of the roots. The results indicated that the types of cutting with 1000, 1500 and 2000 mg/L IBA perform better in the root percentage (100%) in the semi hardwood cuttings. The best results, however, were 2000 mg/L IBA in the semi hardwood cuttings, with the number of the roots to be 35.05, and the fresh weight of the roots to be 3.94 g, the dry weight of the roots to be 0.33 g, the length of the roots to be 391.88 cm, the roots diameter to be 1.21 mm, the surface area of the roots to be 121.83 cm2, and the root volume to be 2.99 cm3. Nonetheless, the optimal concentration of Clorox with the time immersion was 20% with the 20-minute immersion time, which produced a shoot induction percentage of 30% dead explants and a mean number of 70.00 shoots per explant and the optimal concentration of benzylaminopurine (BAP) at 1.0 mg/L. It is of note that a shoot induction percentage of 22.29% and a mean number of 4.1% number of auxiliary bud per treatment. P. betle shoots in MS medium without PGR MS (0.0) yielded a good rooting.
基金supported by the Natural Science Foundation of Guangdong Province (No.06300581)
文摘3-(1-Ethyl-1H-indole-3-carbonyl)aminopropionic acid has been synthesized by alkylation of 3-(1H-indole-3-carbonyl)aminopropionic acid methyl ester with bromoethane,follo-wed by saponifying and acidating,in 89.0% yield.Its crystal structure was gotten and determined by X-ray diffraction method.The crystal is of orthorhombic,space group P212121 with a = 8.9490(12),b = 11.1010(15),c = 13.0475(18) ,V = 1296.2(3) 3,Z = 4,Dc = 1.334 g/cm3,λ = 0.71073 ,μ(MoKα) = 0.095 mm-1,Mr = 260.29 and F(000) = 552.The structure was refined to R = 0.0306 and wR = 0.1445 for 2612 observed reflections with I 2σ(I).In the crystal structure,molecules are linked to each other through hydrogen bonds of N(2)-H(2)···O(1) and O(3)-H(3)···O(1),generating a three-dimensional network.
基金supported by the Natural Science Foundation of Guangdong Province (No.06300581)
文摘Methyl 3-(5-bromo-l-ethyl-lH-indole-3-carbonyl)aminopropionate has been synthesized by the acylation of 5-bromo-3-trichloroacetylindole with β-alanine methyl ester, followed by alkylation with ethyl iodide, in 82.6% yield. Its crystal structure was gotten and determined by X-ray diffraction method. The crystal is of monoclinic, space group P2/c with a = 11.7927(8), b = 14.9342(8), c = 9.0060(5) A, β = 101.558(6)°, V = 1553.93(16) A3, Z = 4, Dc= 1.510 g/cm3, 2 = 0.71073 A,μ(MoKa) = 2.656 mm-1, Mr = 353.22 and F(000) = 720. The structure was refined to R = 0.0401 and wR = 0.0825 for 1704 observed reflections with I 〉 2σ(I). In the crystal structure, intermolecular N(2)-H(2)...O(1) hydrogen bond and weak intermolecular bonds (C(1)-H(1)...O(1) and C(10)-H(10B)-O(2)) are formed, and π-π stacking also exists.
文摘The coupling reaction of 3-cyanoacetyl-2-methylindole 1a with the aromatic diazonium salts gave the corresponding arylhydrazones 2a-e. Compounds 2 were used for synthesis of 4-aminopyrazole-5-carbonitrile 4a-e and 5-amino-4-arylazo-3-pyrazoles 5a-e derivatives. Also, treatment of 3-cyanoacetyl-2-phenylindole 1b with phenyl isothiocyanate gave the corresponding thioacetanilide 7. The later compound 7 was utilized as the key intermediate for the synthesis of some new thiadiazole derivatives 9a-r. The structures of all new compounds were elucidated on the basis of elemental analysis and spectral data.
文摘An efficient and facile method for the synthesis of 3-indolyl-substituted phthalides by Friedel-Crafts alkylation of indoles with 3-hydroxyisobenzofuran-1(3H)-one has been developed. Using only 2 mol-% TsOH·H2O as the catalyst, various substituted indoles can react smoothly at room temperature to give the corresponding phthalides products in good to excellent yields (up to 96%).
基金Funded by the National Natural Science Foundation of China(No.30170011) ,the Construction Fund for"211"Project of theMinistry of Education of China and the Natural Science Foundationof Hubei Province (No.2006ABA197)
文摘The difference of sensitivity to indole- 3-acetic acid ( IAA ) combined with horseradish peroxidase (HRP) in K562 and BXPC- 3 cells was investigated. The cell proliferation was determined by MTF assay. The cell cycle and apoptosis of K562 and BXPC-3 cells were examined by a fluorescence flow cytometer (FCM) and terminal deoxynacleotidyl transferase-mediated dUTP nick-end labeling (TUNEL) respectively. The experimental results show that IAA and HRP could inhibit BXPC- 3 cell proliferation greatly compared with K562 cell during the first 48 h . The cell cycle was arrested predominantly at G2/ M phase in K562 and BXPC- 3 cells. The cell apoptosis of K562 and BXPC- 3 was induced by IAA/ HRP. There was a significant difference between the two cell lines since BXPC-3 cells were more sensitive than K562 cells by treatments with combination of IAA and HRP.
基金supported by the National Natural Science Foundation of China(Nos.21571118&21271121)
文摘A new coordination polymer {[Cd(C_(21)H_(14)N_6)(C_8H_4O_4)]·H_2O}_n(1) was synthesized by an elaborate design via the reaction of 3-(2,6-di(pyrazin-2-yl)pyridin-4-yl)-1H-indole(bppi),1,4-benzene-dicarboxylic acid(H2bdc) and cadmium(Ⅱ) nitrate in CH_3OH/H_2O mixed solvents. Complex 1 crystallizes in orthorhombic,space group Ccca with a = 20.012(4),b = 31.881(6),c = 19.808(4) ?,V = 12638(4) ?~3,Z = 16,C_(29)H_(20)CdN_6O_5,M_r = 644.91,D_c = 1.356 g·cm^(-3),μ = 0.735 mm^(-1),F(000) = 5184,GOOF = 1.046,the final R = 0.0405 and wR = 0.1063 for 6870 observed reflections(I 〉 2σ(I)). The Cd(Ⅱ) centre is hepta-coordinated by three N and four O atoms from one bppi terminal ligand and two bdc2– ligands,respectively,displaying a capped trigonal prism geometry. Structure extension gives coordination polymeric chains,in which the bdc2– linkers connect Cd(Ⅱ) cations into a one-dimensional(1D) coordination polymer along the c axis,giving zigzag chains with the Cd···Cd separation of 11.178(1) ?. The adjacent bppi terminal ligands in the chains are anti-periplanar conformation. The three-dimensional(3D) structure is stabilized by π···π stacking and hydrogen-bonding interactions to form a supramolecular self-penetrating network with 1D channels. In 1,there are voids 2999.7 ?~3 with 23.7% of per unit cell volume. Thermal analysis indicates that the framework of 1 is stable until 651 K and the photoluminescence of 1 in the solid shows very weak fluorescence at 382 and 560 nm upon excitation at 310 nm.
文摘Reaction of indole-3-carboxaldehydes 4 with hydrazine derivatives and different substituted acid hydrazides afforded the corresponding hydrazine derivatives 5a-c and acid hydrazide derivatives 7-11 respectively. Condensation of indole-3-carboxaldehydes 4 with phenacyl bromide and thiourea gives 1,3-thiazol-2-amine derivative 18. On the other hand, reaction 4 with 3-acetylchromene-2-one afforded chalcone derivative 19. Compound 4 undergoing Knoevenagel condensation with cyanoacetamide, ethyl cyanoacetate, benzimidazol-2-ylacetonitrile, rhodanine-3-acetic acid, 2,3-dihydropyrimidin-4-one derivative and 2,4-dihydropyrazol-3-one afforded the compounds 20a,b, 22, 23, 27 and 28 respectively. The structure of the newly synthesized compounds has been confirmed by elemental analysis and spectra data. The antimicrobial activities of the some newly synthesized compounds were measured and showed that most of them have high
基金Supported by the National Natural Science Foundation of China(No.30672519)
文摘A novel series of ethyl 5-hydroxy-4-substituted aminomethyl-2-sulfinylmethyl-lH-indole-3-carboxylates 8a--8j and 11e--11f was synthesized and evaluated in HepG2.2.15 cells for their anti-hepatitits B virus(HBV) activity and cytotoxicity. Among them, six compounds showed more potent inhibitory activity than lamivudine. Compound 8e exhibited the most significant anti-HBV activity with an IC50 value of 1.62 μmol/L, which was 33-times more potent than the reference drug lamivudine(IC50=54.78μmol/L).