Novel Juvenogens (Insect Hormonogenic Agents): Preparation and Biological Tests on Neobellieria bullata

Background: One of the four most incident species in mangrove is the Laguncularia racemosa, plant widely used in popular medicine against inflammation and fever. Objective: Here, L. racemosa was investigated in relation to their phytochemical profile, antioxidant activity, citotoxicity, antimicrobial and immunostimulatory effect. Method: Aqueous extract was obtained from leaves of plant, its phytochemical profile was investigated through UPLC method, the antioxidant assays performed were TAA, DPPH, ABTS, nitrite and lipid peroxidation assay. Antimicrobial assays were made using standard strains. For all biological tests were used mice splenocytes and from these cell cultures were measured cytotoxicity, proliferation index and cytokines production. Results: Laguncularia racemosa leaves showed the presence of ions, proteins, carbohydrates, vitamins and high concentration of phenolic compounds. Antioxidant activities were promoted by aqueous extract, especially in DPPH and NO assays. Extract in 6 µg/mL did not induce significant cell death, stimulated the cell proliferation and the IL-4 production. Moreover, decreases of proinflammatory cytokines IFN-γ, TNF-α and IL-6 were found. Conclusion: The presence of essential nutrients, significant antioxidant activity and immune stimulation confirm the use of this plant in folk medicine against inflammation.

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Analogues of the cholecystokinin octapeptide modified in the central part of the molecule

Collection of Czechoslovak Chemical Communications ◽

10.1135/cccc19911963 ◽

1991 ◽

Vol 56 (9) ◽

pp. 1963-1970 ◽

Cited By ~ 3

Author(s):

Jan Hlaváček ◽

Václav Čeřovský ◽

Jana Pírková ◽

Pavel Majer ◽

Lenka Maletínská ◽

...

Keyword(s):

Amino Acid ◽

Biological Activities ◽

Point Of View ◽

Biologically Active ◽

Side Chain ◽

Amino Acid Residues ◽

Cholecystokinin Octapeptide ◽

Biological Tests ◽

Biological Potency ◽

Biologically Active Conformation

In a series of analogues of the cholecystokinin octapeptide (CCK-8) the amino acid residues were gradually modified by substituting Gly by Pro in position 4, Trp by His in position 5, Met by Cle in position 6, or the Gly residue was inserted between Tyr and Met in positions 2 and 3 of the peptide chain, and in the case of the cholecystokinin heptapeptide (CCK-7) the Met residues were substituted by Nle or Aib. These peptides were investigated from the point of view of their biological potency in the peripheral and central region. From the results of the biological tests it follows that the modifications carried out in these analogues and in their Nα-Boc derivatives mean a suppression of the investigated biological activities by 2-3 orders of magnitude (at a maximum dose of the tested substance of 2 . 10-2 mg per animal).This means that a disturbance of the assumed biologically active conformation of CCK-8, connected with a considerable decrease of the biological potency of the molecule, takes place not only after introduction of the side chain into its centre (substitution of Gly4), but also after the modification of the side chains of the amino acids or by extension of the backbone in further positions around this central amino acid.

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Conditions for following the metabolism of oostatic peptides in Neobellieria bullata by mass spectrometry and radiolabelling

Collection Symposium Series ◽

10.1135/css200104093 ◽

2001 ◽

Author(s):

Richard Tykva ◽

Petr Šimek ◽

Blanka Bennettová ◽

Josef Holík ◽

Jan Hlaváček ◽

...

Keyword(s):

Mass Spectrometry ◽

Neobellieria Bullata

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Peptides with antimicrobial activity isolated from larvae of the flesh fly Neobellieria bullata

Collection Symposium Series ◽

10.1135/css200911084 ◽

2009 ◽

Author(s):

Tereza Neubauerová ◽

Martina Macková ◽

Tomáš Macek ◽

Miloslav Šanda ◽

Zdeněk Voburka

Keyword(s):

Antimicrobial Activity ◽

Flesh Fly ◽

Neobellieria Bullata

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Anti-Tumor and Anti-Inflammatory Activity In Vivo of Apodanthera congestiflora Cogn. (Cucurbitaceae)

Pharmaceutics ◽

10.3390/pharmaceutics13050743 ◽

2021 ◽

Vol 13 (5) ◽

pp. 743

Author(s):

Geovana F. G. Silvestre ◽

Renally P. Lucena ◽

Genil D. Oliveira ◽

Helimarcos N. Pereira ◽

Jhonatta A. B. Dias ◽

...

Keyword(s):

Inflammatory Activity ◽

Phytochemical Investigation ◽

Significant Toxicity ◽

Biological Tests ◽

Ehrlich's Carcinoma ◽

Anti Inflammatory ◽

Pharmacological Potential ◽

First Time ◽

Anti Tumor Activity

This work aimed to carry out a study of Apodanthera congestiflora by investigating its chemical composition and pharmacological potential. From the dichloromethane phase (Dic-Ac) of the A. congestiflora stems, three compounds were identified: cayaponoside C5b (Ac-1), cabenoside C (Ac-2) and fevicordin C2 glucoside (Ac-3), being last identified for the first time as a natural product. These compounds were obtained by chromatographic methods and their structures were elucidated by means of spectroscopic analysis of IR, MS and NMR. In the quantification of Dic-Ac, it was possible to observe the presence of 7% of cayaponoside C5b. Dic-Ac showed significant toxicity for in vivo tests, with macroscopic and biochemical changes. The anti-inflammatory activity of Dic-Ac was investigated using the paw edema model. A decrease in inflammatory signs was observed in the first 5 h and the most effective dose in reducing edema with was 7.5 mg kg−1 (66.6%). Anti-tumor activity of Dic-Ac was evaluated by Ehrlich’s carcinoma model, which showed inhibition rate of 78.46% at 15 mg kg−1 dosage. The phytochemical investigation, together with the biological tests carried out in this study, demonstrated that A. congestiflora is a promising species in the search for therapeutics, since it contains substances with high pharmacological potential in its composition.

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2-Cyclopropyl-6-phenyl-2,3-dihydrothieno[3,2-d][1,3,2]diazaborinin-4(1H)-one

Molbank ◽

10.3390/m1221 ◽

2021 ◽

Vol 2021 (2) ◽

pp. M1221

Author(s):

Romain Mustière ◽

Patrice Vanelle ◽

Nicolas Primas

Keyword(s):

Scaffold Hopping ◽

Simple Treatment ◽

Biological Tests

As part of our ongoing scaffold hopping work on antimalarial 2-aminothieno[3,2-d]pyrimidin-4-one scaffold, we explored the dihydrothieno[3,2-d][1,3,2]diazaborinin-4(1H)-one as a potential new antimalarial series. Using conditions found in the literature, we obtained 2-cyclopropyl-6-phenyl-2,3-dihydrothieno[3,2-d][1,3,2]diazaborinin-4(1H)-one with 93% yield through a simple treatment. It was then characterized by NMR (1H and 13C) and HRMS. Given the structure of this molecule, its aqueous stability was assessed to determine its suitability for biological tests. To our knowledge, this is the first dihydrothieno[3,2-d][1,3,2]diazaborinin-4(1H)-one described.

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EXPRESS: Routine use of natriuretic peptides: lessons from a Big Data analysis

Annals of Clinical Biochemistry International Journal of Laboratory Medicine ◽

10.1177/00045632211020779 ◽

2021 ◽

pp. 000456322110207

Author(s):

Francois-Xavier Goudot ◽

Sonia Msadek ◽

Tanissia Boukertouta ◽

Pierre-Olivier Schischmanoff ◽

Christophe Meune

Keyword(s):

Heart Failure ◽

Big Data ◽

Natriuretic Peptides ◽

Ventricular Dysfunction ◽

Big Data Analysis ◽

Left Ventricular ◽

Routine Practice ◽

Cardiac Diseases ◽

Biological Tests ◽

Risk Patients

Background: Natriuretic peptides (NPs) have broad indications during heart failure (HF) and the detection of left ventricular dysfunction in high-risk patients. They can also be used for the diagnosis/management of other cardiac diseases. However, very little is known regarding their use in routine practice. Methods: We examined all biological tests performed from February 2010 to August 2015 in two districts from the French Brittany, covering 13,653 km2 and including 22,265 physicians. We report the settings and conditions of N-terminal pro-B-type Natriuretic Peptide (NT-proBNP) measurements (the only locally NP available). Results: From a total of 3,606,432 tests requested in 557,650 adult (older than 20 years) patients, only 56,653 (1.6%) included at least one NT-proBNP measurement. NT-proBNP measurements gradually increased, from 9,188 in 2011 to 12,938 in 2014 (p<0.001). Most NT-proBNP tests were measured in urban laboratories (72.7%) and in private (62.9%) non-hospital/clinics laboratories, they were mostly ordered by general practitioners (66% compared with 11% by cardiologists). The number of NT-proBNP measurements increased with age up to 80-90 years, and 70.3% of tests were measured in â¥75y patients. Creatinine and electrolytes were not associated with NT-proBNP in 15.8% and 19.7% of tests, respectively. Conclusion: Among a very large cohort, we observed that NPs remain largely undermeasured. NT-proBNP is mostly measured in elderly patients, and its interpretation may be hazardous in up to 16% of all individuals because no measurement of creatinine was associated to NT-proBNP.

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