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PubMed2003

[Principles of treatment and military medical examination of the patients with indolent Non-Hodgkin's lymphomas].

Non-Hodgkin's lymphomas (NHL) are the heterogeneous group of lymphoproliferative malignancies with distinct morphological, immuno-histochemical and genetic criteria of diagnosis, different character of clinical course, sensitivity to different treatment methods and disease prognosis. The WHO classification (1997) encompasses all the lymphoproliferative neoplasms. The NHL can be divided into 2 prognostic groups: the indolent lymphomas and the aggressive non-Hodgkin's lymphomas. The indolent NHL types have a relatively favorable clinical prognosis, with median survival as long as 10 years, but they usually are not curable in advanced clinical stages. Early-stage (I and II) indolent NHL can be effectively treated with radiation therapy alone. In advanced stages of indolent NHL the chemotherapy is conducted.

Aged↗
PubMed2004

New treatment approaches to indolent non-Hodgkin's lymphoma.

Disseminated indolent non-Hodgkin's lymphoma (NHL) is considered incurable with conventional chemotherapy regimens, and more than 50% of patients die within 5 years of their first relapse. Therefore, newer treatment approaches have been used to try to improve survival and ultimately provide a cure for patients with disseminated indolent NHL. The anti-CD20 monoclonal antibody rituximab has been extensively evaluated and is now an integral component of many treatment strategies. The activity of rituximab was first shown in the pivotal trial in patients with relapsed and refractory low-grade and follicular lymphoma. More recent studies have shown somewhat higher activity of rituximab when used first-line, with further improvements with maintenance therapy. Rituximab in combination with chemotherapy has been shown to achieve high response rates, and two prospective randomized studies from the German Low-grade Lymphoma Study Group have shown significantly higher response rates and longer survival for patients receiving rituximab concurrently with chemotherapy compared with those receiving chemotherapy alone. Further data from ongoing phase III studies are still needed to determine whether rituximab can help alter the natural history of indolent NHL, and longer follow-up of these patients will help determine the optimal role for rituximab in treatment of indolent NHL.

Antibodies, Monoclonal↗
PubMed1992

Mast-cell phenotype in indolent forms of mastocytosis. Ultrastructural features, fluorescence detection of avidin binding, and immunofluorescent determination of chymase, tryptase, and carboxypeptidase.

The factor(s) that causes excessive mast cell (MC) proliferation in indolent forms of mastocytosis is not known, nor is it known whether that proliferation is a regulated clonal expansion or merely a non-neoplastic hyperplasia. Human MCs display phenotypes that depend on the microenvironment. Thus, if the phenotype of MCs in mastocytosis lesions is determined to be abnormal for that tissue site (and therefore the MCs are refractory to microenvironmental signals) then a clonal process would be suggested. The authors determined the phenotypes of MCs from the lesional skin of 17 patients with indolent mastocytosis and the bone marrows of 9 patients. They compared them with the phenotypes of MCs from the lesional skin of 8 patients with various dermatitides, the skin of 2 patients with idiopathic anaphylaxis, and the breast skin of 15 control patients. MCs from all the skin specimens showed the characteristic skin MC phenotype, with predominantly scroll-poor granules by ultrastructure and containing tryptase and chymase by immunofluorescence detection (the MCTC immunophenotype). The skin MCs of each patient bound avidin and contained carboxypeptidase by immunofluorescence detection. MCs from the bone marrow of patients with indolent mastocytosis, the source of progenitors, also showed the scroll-poor and MCTC phenotypes. These findings do not support an unregulated clonal expansion in indolent forms of mastocytosis. They are consistent with a non-neoplastic hyperplasia or possibly a clonal process in which MCs remain responsive to microenvironmental regulation.

Avidin↗
PubMed2006

[Efficacy of rituximab-containing regimens on indolent B-cell lymphoma--a report of 34 cases].

BACKGROUND & OBJECTIVE: The efficacy of rituximab given alone or in combination with chemotherapy on naive or relapsed indolent lymphoma is good. This study was to investigate the efficacy and safety of rituximab-containing regimens for patients with indolent B-cell lymphoma in China. METHODS: From Mar. 1999 to Jan. 2005, 34 patients with indolent B-cell lymphoma received rituximab-containing regimens with a median of 5 cycles (ranged from 3 to 8 cycles). Of the 34 patients, 2 received rituximab alone, and 32 received rituximab-based regimens, which including CHOP (16 cases), FMD (5 cases), CHOPE (4 cases), EPOCH (2 cases), DICE (2 cases), DAHP (2 cases), and FN (1 case). RESULTS: Of the 34 patients, 30 were evaluable for objective response. The overall response (OR) rate was 93.3%, and the complete response (CR) rate was 60.0%; the OR rate and CR rate of 22 evaluable naive patients were 95.4% and 66.7%, those of 18 evaluable follicular lymphoma patients were 88.9% and 66.7%. With a median follow-up of 17 months (4-68 months), the 1-year progression-freely survival rate was 85.3%. Myelosuppression was the major adverse event: 19 patients suffered from leukopenia with 4 cases of grade III-IV event, 5 suffered from thrombocytopenia with 4 cases of grade III-IV event, and 2 suffered from febrile neutropenia. Other adverse events included grade I-II nausea/vomiting, mild alopecia, and transient liver function abnormality. The infusional reaction of rituximab consisted of grade I-II rigor/febrile, skin rash, mild hypotension, and asymptomatic ventricular premature beat. CONCLUSION: Rituximab-containing chemotherapeutic regimens are effective for indolent B-cell lymphoma with mild toxicity.

Adult↗
PubMed1976

Isolation and characterization of indole-3-acetaldehyde reductases from Cucumis sativus.

In a continuing study of the biosynthetic pathway and regulatory mechanisms governing indole-3-acetic acid (auxin) formation, we report the isolation and initial characterization of three distinct indole-3-acetaldehyde reductases from cucumber seedlings. These enzymes catalyze the reduction of indole-3-acetaldehyde to indole-3-ethanol with the concomitant oxidation of NAD(P)H to NAD(P)+. Two of the reductases are specific for NADPH as second substrate, while the third is specific for NADH. The enzymes show a strong specificity for indoleacetaldehyde, with apparent Km values of 73mum, 130mum, and 400mum being calculated for the two NADPH-specific reductases and the NADH-specific reductase, respectively. Under no conditions of substrate concentration, incubation time, or assay method could the reverse reaction be observed. Chromatography on a calibrated Sephadex gel column led to estimated molecualr weights of 52,000 and 17,000 for the NADPH-specific reductases, while a value of 33,000 was obtained for the NADH-specific reductase. Both NADPH-specific reductases showed a pH optimum of 5.2 with a secondary optimum at 7.0, and both enzymes were activated by increasing ionic strength. The NADH-specific reductase showed a pH optimum of 7.0 with a secondary optimum at 6.1 and was slightly inhibited by increasing ionic strength.

Aldehyde Oxidoreductases↗
PubMed1983

Effects of enzyme/substrate ratio and of cofactors on the oxidation products of indole-3-acetic acid catalyzed by peroxidase.

During the oxidation of indole-3-acetic acid catalyzed by peroxidase, the relative amounts of the products closely depends on the enzyme/substrate ratio. In the absence of cofactors, high enzyme/substrate ratio induces a rise in the level of indole-3-aldehyde and indole-3-methanol, and a drop in that of oxindoles. 2,4-dichlorophenol, although a very efficient cofactor, promotes inhibition of the oxidation after a few minutes, presumably through the formation of a phenol-derivative inhibitor. 2-4-dichlorophenol also inhibits the production of oxindoles at all stages. Both inhibitory effects are abolished by a low concentration of enzyme. Mn2+, itself a weak inhibitor, synergizes the catalytic effect of 2,4-dichlorophenol, perhaps by preventing the formation of the inhibitor. The results are discussed against more widely accepted mechanisms of indole-3-acetic acid oxidation.

Chlorophenols↗
PubMed1980

Localized and indolent myeloma.

Criteria were defined for recognizing 29 patients with a localized plasmacytoma of bone and 20 patients with an indolent variety of multiple myeloma in order to justify long-term follow-up without chemotherapy. All patients with indolent myeloma were asymptomatic from their low tumor mass disease, had a hemoglobin greater than 10 g/dl, and showed no more than 3 lytic bone lesions. The presence of more than 200 mg/day of Bence Jones protein was usually followed by disease progression within 2 yr. Serial assessments of myeloma protein level provided a useful index of changing tumor load and the need for chemotherapy. In patients with localized disease, radiotherapy usually reduced myeloma proteins markedly with subsequent disease control for many years, even though small serum peaks persisted. Chemotherapy for multiple myeloma was not required for a median of 8 yr in patients presenting with localized disease and of 3 yr in those with indolent myeloma. The additional survival from the start of drug treatment was similar to that of comparable patients treated promptly for overt multiple myeloma. The delay of chemotherapy until evidence of tumor progression did not affect the long-term outcome of patients with localized or indolent myeloma.

Diagnosis, Differential↗
PubMed1993

Stimulation of brain steroidogenesis by 2-aryl-indole-3-acetamide derivatives acting at the mitochondrial diazepam-binding inhibitor receptor complex.

The 2-aryl-indole-3-acetamide derivatives, 2-hexyl-indole-3-acetamide (FGIN-1-27) and 2-hexyl-indole-3-acetamide-N-benzene-tricarboxylic acid (FGIN-1-44) displaced [3H]1-(2-chlorophenyl)-N-methyl-N-(1- methylpropyl)-3-isoquinoline-carboxamide([3H]PK 11195) and [3H]4-chlorodiazepam ([3H]4'CD) from binding sites located on the rat brain mitochondrial DBI receptor complex (MDRC) with Ki values in the nanomolar range. Both 2-aryl-indole-3-acetamide derivatives acted as agonists at the MDRC and thereby stimulated the rate of pregnenolone synthesis in isolated rat brain mitochondria; this effect was inhibited by PK 11195, an MDRC ligand that does not possess steroidogenic activity. FGIN-1-27 and FGIN-1-44 failed to bind to other transmitter receptors, including gamma-aminobutyric-A receptors. When administered orally to rats, both FGIN-1-27 and FGIN-1-44 reduced fear of novelty in the elevated plus maze test. This action was prevented by PK 11195, but not by flumazenil. FGIN-1-44, which was rapidly converted to FGIN-1-27 in the rat brain, was 3 to 4 times more potent than FGIN-1-27 in reducing fear of novelty because of its greater bioavailability. FGIN-1-27 increased the brain pregnenolone content in adrenalectomized-castrated rats pretreated with trilostane (in order to prevent metabolism of pregnenolone to progesterone). This increase was blocked by pretreatment with PK 11195. Although FGIN-1-27 and FGIN-1-44 increased the corticosterone concentration in adrenal glands and plasma of hypophysectomized rats in a PK 11195-sensitive manner, both drugs failed to increase adrenal steroidogenesis in sham-operated rats.(ABSTRACT TRUNCATED AT 250 WORDS)

Adrenal Glands↗
PubMed1996

Synthesis of indole-N-propionitrile, N-propionic acid and N-propionamide derivatives of potential biological activity.

Cyanoethylation of a selected group from indole derivatives 1a-i using acrylonitrile in pyridine and potassium hydroxide afforded the corresponding indole-1-propionitrile 2a-h derivatives which readily hydrolysed in basic medium to the corresponding indole-1-propionic acid derivatives 4a-c. A several attempts to cyclize the above products-to the corresponding dihydropyrroloquinolin-4-one derivatives. The indole-1-propionamide derivatives reacted with diethyl carbonate and ethyl acetate under Claisen condensation also, with diazonium salts and nitric acid.

Amides↗
PubMed2006

New procedure to mask the 2,3-pi bond of the indole nucleus and its application to the preparation of potent opioid receptor agonists with a Corynanthe skeleton.

Treatment of indole alkaloids with hypervalent iodine in the presence of ethylene glycol provides 2,3-ethylene glycol bridged adducts that could be converted into the original indoles under mild reductive conditions. This procedure, which involves masking of the reactivity of the indole nucleus at the beta-position, was utilized for the modification of the benzene ring of the indoline derivative and was applied to the preparation of potent opioid receptor agonists with the Corynanthe skeleton. [reaction: see text]

Alkaloids↗
PubMed2000

An herbivore elicitor activates the gene for indole emission in maize.

Maize and a variety of other plant species release volatile compounds in response to herbivore attack that serve as chemical cues to signal natural enemies of the feeding herbivore. N-(17-hydroxylinolenoyl)-l-glutamine is an elicitor component that has been isolated and chemically characterized from the regurgitant of the herbivore-pest beet armyworm. This fatty acid derivative, referred to as volicitin, triggers the synthesis and release of volatile components, including terpenoids and indole in maize. Here we report on a previously unidentified enzyme, indole-3-glycerol phosphate lyase (IGL), that catalyzes the formation of free indole and is selectively activated by volicitin. IGL's enzymatic properties are similar to BX1, a maize enzyme that serves as the entry point to the secondary defense metabolites DIBOA and DIMBOA. Gene-sequence analysis indicates that Igl and Bx1 are evolutionarily related to the tryptophan synthase alpha subunit.

Animals↗
PubMed1994

[Antimycobacterial indole derivatives].

1,3-Dinitro-2-(indol-3'-yl)-propanes 3 are synthesized by Michael reaction of nitromethane with the indolylnitroethenes 2. Reaction of the aldehydes 4 and 10 with the benzylamines 12 as well as the reaction of the indolylalkylamines 6a and 9a with the benzaldehydes 11 lead to Schiff bases which are reduced to N-benzyl-(indol-3-ylmethyl)-amines 13 and N-benzyl-(indol-3-ylethyl)-amines 14, respectively; tert amines 16 are synthesized via the formamides 15, amines 18 are prepared according to Mannich. Inhibitory effects on Mycobacterium tuberculosis H 37 Ra are investigated, a structure-activity relationship is discussed.

Anti-Bacterial Agents↗
PubMed2003

Dopamine receptor ligands. Part VII [1]: novel 3-substituted 5-phenyl-1, 2, 3, 4, 5, 6-hexahydro-azepino-[4, 5-b]indoles as ligands for the dopamine receptors.

A number of 5-phenyl-1, 2, 3, 4, 5, 6-hexahydro-azepino-[4, 5-b]indoles 3 were synthesized with different substituents at the azepine-N position (methyl-, allyl-, 2-phenyl-ethyl-, cyclopropylmethyl- and unsubstituted). Furthermore, the indole-N-methylated compound was generated and by using norephedrines and norpseudoephedrines as a chiral pool, 4-methyl-5-phenyl-1, 2, 3, 4, 5, 6-hexahydro-azepino-[4, 5-b]indoles were prepared which contained racemisation at the reacting C-atom. These compounds, as well as the ring-open amino-alcohols, were screened for their affinity to the hD(1)-, hD(5)-, hD(2L)-, and hD(4)-receptors (ç please check sentence). They had micromolar affinities for the receptors and showed the highest affinity to the D(1)-subtype family. The cyclic compounds possessed the highest affinity, with the cyclopropylmethyl-(3c) and methyl-substituents (3 e) being the most active of the tested compounds. Based on an intracellular cAMP-assay, the unsubstituted compound (at the azepine-N position) turned out to be an agonist for the D(1)-and D(5)-subtype family, whereas the substituted compounds showed (partial) agonistic, or even inverse agonistic activity.

Animals↗
PubMed2005

Syntheses of novel indole lipoic acid derivatives and their antioxidant effects on lipid peroxidation.

The aim of the study was to examine antioxidant properties of conjugates based on indole and lipoic acid moieties. The design and syntheses of novel indole alpha-lipoic acid derivatives were performed. The antioxidant properties of target compounds were investigated using rat liver microsomal, NADPH-dependent lipid peroxidation inhibition. Some of the target compounds, especially those containing amide linker at position 5 of indole ring, proved to be highly effective in inhibiting lipid peroxidation as compared to alpha-lipoic acid.

Animals↗
PubMed2004

Expression of a feedback-resistant anthranilate synthase in Catharanthus roseus hairy roots provides evidence for tight regulation of terpenoid indole alkaloid levels.

Different plant species produce a variety of terpenoid indole alkaloids, which are of interest as plant defensive secondary metabolites and as valuable pharmaceuticals. Although significant progress has been made, the mechanisms regulating the levels of this important class of compounds require continued elucidation. Previous precursor feeding studies have indicated that alkaloid accumulation can be improved during the exponential growth phase of hairy root cultures through enhanced tryptophan availability. To test this relationship, transgenic hairy root cultures of Catharanthus roseus were established with a glucocorticoid-inducible promoter controlling the expression of an Arabidopsis feedback-resistant anthranilate synthase alpha subunit. Enzyme assays demonstrated that the Arabidopsis alpha subunit is compatible with the native beta subunit and that anthranilate synthase activity is more resistant to tryptophan inhibition in induced than in uninduced extracts. The metabolic effects of expressing the feedback-resistant anthranilate synthase alpha subunit were also dramatic. Over a 6-day induction period during the late exponential growth phase, tryptophan and tryptamine specific yields increased from almost undetectable levels to 2.5 mg/g dry weight and from 25 microg/g to 267 microg/g dry weight, respectively. The greater than 300-fold increase in tryptophan levels observed in these studies under certain induction conditions compares favorably with the fold increases obtained in previous constitutive expression studies. Despite the large increases in tryptophan and tryptamine, the levels of most terpenoid indole alkaloids were not significantly altered, with the exception of lochnericine, which increased 81% after a 3-day induction period. These results suggest that terpenoid indole alkaloid levels are tightly controlled.

Anthranilate Synthase↗
PubMed2004

2-(2,3-Dihydro-1H-indol-3-yl)ethanol: synthesis, separation of enantiomers, and assignment of absolute stereochemistry by X-ray structure analysis.

The first direct resolution of racemic 2-(2,3-dihydro-lH-indol-3-yl)ethanol-prepared by catalytic hydrogenation of 2-(lH-indol-3-yl)ethanol-has been accomplished by chiral simulated moving bed (SMB) chromatography. The single enantiomers were isolated as their dihydrogen phosphate salts. Single-crystal X-ray analyses were successful, revealing that the (+)-enantiomer of 2-(2,3-dihydro-lH-indol-3-yl)ethanol has the (S) configuration. Chirality 16:126-130, 2004.

Chromatography, High Pressure Liquid↗
PubMed1991

The protein encoded by the rolB plant oncogene hydrolyses indole glucosides.

The rolB gene of Agrobacterium rhizogenes, whose expression stimulates the formation of roots by transformed plant tissues and other growth alterations in transgenic plants, codes for a beta-glucosidase able to hydrolyse indole-beta-glucosides. Indeed, we show that extracts of bacteria and/or plant tissue expressing the rolB protein hydrolyse indoxyl-beta-glucoside (plant indican). Because of the structural similarity between indoxyl-beta-glucoside and indole-3-acetyl-beta-glucoside (IAA-beta-glucoside), we propose that the physiological and developmental alterations in transgenic plants expressing the rolB gene could be the result of an increased intracellular auxin activity caused by the release of active auxins from inactive beta-glucosides. Thus two of the oncogenes carried by the T-DNA of the plant pathogen Agrobacterium rhizogenes (rolB and rolC) perturb plant growth and development by coding for beta-glucosidases with distinct specificities. Whereas the rolC beta-glucosidase releases cytokinins from their glucoside conjugates, the rolB encoded protein hydrolyses indole-beta-glucosides. The combined action of these two genes therefore is expected to modulate the intracellular concentration of two of the main growth factors active in plants.

Base Sequence↗
PubMed2007

Indole, a core nucleus for potent inhibitors of tubulin polymerization.

Microtubules are the basic components of cell structure, which take part in a wide number of pivotal cellular functions. Drugs that are able to modulate the microtubule assembly either by inhibition of tubulin polymerization or by blocking microtubule disassembly are of great interest in anti-cancer therapy. Several tubulin polymerization inhibitors characterized by the presence of an indole nucleus have been obtained from natural sources or have been prepared by semi-synthesis. In the last decade an ever increasing number of synthetic indoles have been reported. We have reviewed anti-tubulin agents obtained by synthesis having an indole as core nucleus. The synthesis, the biological activity, and the structure - activity relationship aspects of 3-formyl-2-phenylindoles, heterocombretastatins, diarylindoles, 2-aroylindoles, D-24851, 2-aryl-3-aroylindoles, 3-aroyl- and 1-aroylindoles, and arylthioindoles are discussed.

Antimitotic Agents↗