[Anti-inflammatory activity of N-benzoyl-isatinic acids and N-p-chlorobenzoyl isatinic acids].
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Animals↗
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Isatin-enzyme interactions. VII. Mechanism of inhibition of rat kidney alkaline phosphatase.
Isatin has been found to inhibit rat kidney alkaline phosphatase (EC 3.1.3.1). The inhibition is dependent on isatin concentration and is of un-competitive type. The hydrolysis of disodium phenyl phosphate by the enzyme at different temperatures (17--37 degrees C) obeys the Arrhenius equation. Energy of activation in the absence and presence of isatin has been found to be 9.84 and 10.24 kCal/mol. The hyperbolic profile of isatin inhibition; the lowering of both Km and Vmax in the presence of isatin, and, small changes in enthalpy, free energy and entropy in the presence of isatin suggest a non-allosteric un-competitive inhibition of the enzyme.
Alkaline Phosphatase↗
Arenavirus inactivation on contact with N-substituted isatin beta-thiosemicarbazones and certain cations.
N-methyl and N-ethyl isatin beta-thiosemicarbazones inactivate cell-free Parana and Pichinde viruses as well as three strains of lymphocytic choriomeningitis virus. This antiviral activity is abolished in the presence of the chelating agent EDTA. The rate of virus inactivation by N-methyl isatin beta-thiosemicarbazone is greatly enhanced and controlled by the addition of cupric sulphate. Divalent cations of other first transition series metals are less effective. A difference exists in the copper requirement for fast inactivation of the prototype arenavirus (lymphocytic choriomeningitis) and the Tacaribe Complex of viruses (Parana and Pichinde). In the presence of 20 muM-N-methyl isatin beta-thiosemicarbazone, LCM and Pichinde viruses can be inactivated at about the same rate if 20 muM-CuSO4 is added to the former and 160 muM-CuSO4 is added to the latter. Using 20 muM-N-methyl isatin beta-semicarbazone and CuSO4 the inactivation of LCM is reduced, but not eliminated, in the presence of an equal amount of infectious Pichinde virus. Crude and highly purified Pichinde virus are inactivated at the same rate when exposed to identical concentrations of N-methyl isatin beta-thiosemicarbazone and cupric sulphate. There is little detectable change in the inactivation rates when Pichinde or LCM viruses are grown in a variety of different cell lines.
Cell Line↗
The influence of neuroprotector isatin on haloperidolinduced catalepsy and proteomic profile of mice brain.
Isatin (indol-2,3-dione) is an endogenous regulator found in humans and animals. It interacts with numerous target proteins and exhibits a wide range of biological activities, including neuroprotective action in animal models of Parkinson's disease (PD) induced by administration of neurotoxins MPTP (1-methyl-4-phenyl-1,2,3,6- tetrahydropyridine) or rotenone. An antipsychotic drug haloperidol, which impairs neurotransmitter balance in the nigrostriatal pathway, models dopamine deficiency and promotes the development of motor disorders characteristic of PD. In this work, the effect of two doses of isatin (10 mg/kg and 80 mg/kg) on the haloperidol catalepsy and on the proteomic profile of mice brain was investigated. The pretreatment of animals with isatin (1 h before haloperidol administration) reduced the occurrence of haloperidol catalepsy. The administration of haloperidol and also isatin with haloperidol influenced the relative content of a number of proteins associated with PD and other neurodegenerative diseases.
Animals↗
[Isatin-enzyme interactions. VI. Inhibition of rat kidney alkaline phosphatase].
Interaction of isatin with rat kidney alkaline phosphatase has been studied. Mode of attachment of isatin with the enzyme protein is most likely through amino group(s), which is also imperative for catalysis. Sulphydryl group(s) do not seem to be involved in enzyme action. Zinc is also needed for enzyme activity. Use of sulphydryl compounds suggests that isatin inhibition of the enzyme is through attachment at the metal site. However, this inhibition may not only be due to simple chelation of the metal by isatin.
Alkaline Phosphatase↗
Nature of inhibition of rat testicular alkaline phosphatase by isatin.
Isatin has been found to inhibit rat testicular alkaline phosphatase (EC 3.1.3.1). That the inhibition is non-competitive as well as non-allosteric is evident from a) the hyperbolic curve relating inhibition as a function of inhibitor concentration; b) the small change in enthalpy, free energy and entropy; c) the number of isatin molecules associating with 1 molecule of the enzyme (n=1.29); and, d) the decrease in the values of both Km and Vmax in the presence of isatin.
Alkaline Phosphatase↗
Inactivation of lambda phage infectivity and lambda deoxyribonucleic acid transfection by N-methyl-isatin beta-thiosemicarbazone-copper complexes.
The infectivity of intact lambda phage and transfection by lambda deoxyribonucleic acid were inactivated by exposure to the copper complexes of N-methyl-isatin beta-thiosemicarbazone, thiosemicarbazide, and semicarbazide, but not methyl-isatin. No inactivation was observed when these compounds were used in the absence of copper sulfate. This confirms our previous observation that the activity of N-methyl-isatin beta-thiosemicarbazone is mediated by its thiosemicarbazone moiety and that the presence of copper is required for action. This represents the first time, to our knowledge, that semicarbazide has been found to possess antiviral activity. It is clear that these compounds act directly on deoxyribonucleic acid; whether the compounds also act on proteins has not been determined.
Coliphages↗
Isatin inhibition of rat testicular alkaline phosphatase. A non-allosteric phenomenon.
Isatin has been found to inhibit rat testicular alkaline phosphatase (EC 3.1.3.1) uncompetitively. The hyperbolic curve relating inhibition as a function of substrate concentration; the persistence of inhibition after the tertiary structure of the enzyme has been altered by heat denaturation, exposure to urea or papain digestion; the small changes in entropy, free energy and enthalpy in the presence of isatin, and the number of isatin molecules (n = 1.29) combining with one molecule of enzyme indicate the non-allosteric nature of inhibition.
Alkaline Phosphatase↗
Effect of isatin (2,3-dioxoindoline) on audiogenic seizures in rats and its relationship to electrographic and behavioural phenomena.
In doses of 160 and 80 mg/kg, isatin (2,3-dioxoindoline) significantly reduced the total incidence of audiogenic epileptic seizures in rats highly sensitive to an acoustic epileptogenic stimulus. The number of severest forms of seizure (running, clonic convulsions) was higher than in the control tests, however. The acoustic epileptogenic stimuls was applied one hour after the i.p. injection of isatin. At that time some postural reflexes were still inhibited after 160 mg isatin/kg, while after smaller doses they were already normal again. One hour after administering isatin there were marked changes in the electroencephalogram, the chief ones being an increase in rhythmic episodic activity against a desynchronization background and a decrease in slow wave sleep activity.
Acoustic Stimulation↗
Isatin enzyme interactions. V. Activation of rat liver acid phosphatase.
Influence of Isatin on rat tissue acid phosphatase has been studied. It has an organ-specific effect, the liver enzyme is activated, the brain enzyme is inhibited while those of kidney and intestine are not affected. Isatin activation of the liver enzyme is of mixed type and pH dependent. Rat liver enzyme appears to require intact amino and sulfhydryl groups for activity. Isatin seems to combine with the enzyme through the sulfhydryl group of the latter.
Acid Phosphatase↗
Some histochemical and electrophysiological effects of isatin.
Qualitative and semiquantitative histochemical investigations of acetylcholinesterase after a single or repeated administration of isatin, 160 mg/kg ip once or daily for 8 consecutive days have revealed a significant decrease of the histochemical reaction for acetylcholinesterase in chronically treated rats. The cholinergic effect of isatin was tested in the electrophysiological experiment after a single dose of 160 mg/kg isatin and was partially antagonized by atropine.
Acetylcholinesterase↗
[Biologically active N-Mannich bases of isatin-3-(phenyl)-imines (author's transl)].
By the condensation of isatin and 5-nitroisatin with substituted aromatic amines, isatin- and 5-nitroisatin-3-(phenyl)-imines (azomethines) are formed which are converted into N-Mannich-bases by aminomethylation and may be formulated as azomethines with E configuration. A biotest of Lepidium sativum L. was used to prove mitodepressive properties. Some compounds showed a significant growth-inhibiting activity. It was found that a change in activity is produced by condensation on the carbon atom in position 3 and by aminomethylation on the nitrogen atom in the isatin nucleus.
Imines↗
Antibacterial and antifungal activities of isatin N-Mannich bases.
The antimicrobial and antifungal activities of 29 congeneric isatin N-Mannich bases were investigated by testing against standard test microorganisms and 21 pathogenic Gram-negative microorganisms. Considerable growth inhibition of Gram-negative bacteria and yeasts and slight inhibition of Gram-positive bacteria resulted when they were treated with the various N-Mannich bases of isatin and 5-nitroisatin, respectively.
Anti-Bacterial Agents↗
Effect of administration of isatin on alkaline phosphatase of various organs of rat.
In vivo administration of isatin (200 mg/kg) significantly lowered the activity of rat kidney alkaline phosphatase after 5 hr but enhanced the activity of rat duodenal and jejunal enzyme after 2 and 5 hr (P less than 0.01). The increased activity of the duodenal and jejunal alkaline phosphatase might be due to the induction of the enzyme by isatin.
Alkaline Phosphatase↗
Antiviral, antibacterial, and antifungal activities of isatin N-Mannich bases.
Preliminary antiviral, antibacterial, and antifungal screening results of a series of isatin N-Mannich bases are provided.
Amines↗
Isatin-3-anils as excystment and cysticidal agents against Schizopyrenus russelli.
A series of isatin-3-anils (with or without a N-piperidino/morpholinomethyl substituent) have been screened for their cysticidal activity against Schizopyrenus russelli. Their ability to cause excystment has also been studied.
Amebiasis↗
Isatin-beta-thiosemicarbazone causes premature cessation of vaccinia virus-induced late post-replicative polypeptide synthesis.
The effects of isatin-beta-thiosemicarbazone on vaccinia virus-induced polypeptide synthesis has been examined by polyacrylamide gel electrophoresis and autoradiography. The synthesis of pre-replicative and early post-replicative polypeptides proceeded normally in the presence of the drug; the onset of late post-replicative polypeptide synthesis occurred with normal timing under these conditions but the rate of synthesis of all virus polypeptides then declined rapidly.
Cell Line↗
Formation of vaccinia virus DNA-protein complex in the presence of isatin beta thiosemicarbazone (IBT).
The association of newly synthesized vaccinia virus DNA with proteins in infected HeLa cells was followed. A shift from a high density to a low density complex occurred between 3 and 6 h after infection. This process was not affected by isatin beta thiosemicarbazone (IBT), an inhibitor of pox virus growth. At 22 h after infection in the absence of IBT, mature virions of high density were observed; however, in the presence of the drug, high density DNA-protein complexes, which lack the two main virus core polypeptides, were formed.
DNA, Viral↗