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Marine bioactive compounds: stereospecific anti-inflammatory activity of natural and synthetic cordiachromene A.

A new synthesis is proposed for cordiachromene A (CCA), a bioactive component of the ascidian Aplidium antillense Gravier, using a method producing a racemic mixture. The anti-inflammatory activities of a natural extract and a chemically synthetic form of CCA were assessed in vivo by carrageenan-induced rat-paw edema. The activity of synthetic CCA was confirmed by a test on kaolin-induced granuloma in the rat. Strong activities were measured for both CCA, but comparison of results of the first test suggests that only the natural optically active isomer has an anti-inflammatory effect. CCA is similar to indomethacin in its effect on carrageenan-induced rat-paw edema and ten times as active as phenylbutazone.

Animals↗

Binding of the bioactive compound 5,7,4'-trihydroxy-6,3',5'-trimethoxyflavone to human serum albumin.

5,7,4'-trihydroxy-6,3',5'-trimethoxyflavone is one of the bioactive components isolated from Artemisia plants possessing antitumor therapeutic activities. In this paper, its binding properties and binding sites located on human serum albumin (HSA) have been studied using UV absorption spectroscopy, fluorescence spectroscopy and Fourier transform infrared (FT-IR) spectra. The results of fluorescence titration revealed that 5,7,4'-trihydroxy-6,3',5'-trimethoxyflavone could strongly quench the intrinsic fluorescence of HSA by static quenching and there was only one class of binding sites on HSA for this drug. The binding constants at four different temperatures (289, 298, 310, and 318 K) were 1.93, 1.56, 1.22, and 0.93x10(5) L mol-1, respectively. The FT-IR spectra evidence showed that the protein secondary structure changed with reduction of alpha-helices about 27.6% at the drug to protein molar ratio of 3. The thermodynamic functions standard enthalpy change (DeltaH0) and standard entropy change (DeltaS0) for the reaction were calculated to be -18.70 kJ mol-1 and 36.62 J mol-1 K-1 according to the van't Hoff equation. These results and the molecular modeling study suggested that hydrophobic interaction was the predominant intermolecular force stabilizing the complex, and 5,7,4'-trihydroxy-6,3',5'-trimethoxyflavone could bind to the site I of HSA (the Warfarin Binding site).

Binding Sites↗

The himanimides, new bioactive compounds from Serpula himantoides (Fr.) Karst.

In a screening of basidiomycete cultures from Chile for the production of antibiotics we identified a Serpula himantoides strain as a producer of metabolites inhibiting the growth of bacteria and fungi. Bioactivity guided purification resulted in the isolation of four new antibiotics. Their structures were elucidated by spectroscopic methods. All four compounds are succinimide and maleimide derivatives, of which two are N-hydroxylated.

Animals↗

From bioactive compounds to volatile profiles: a multidimensional characterization of Indonesian stingless bee honeys.

BACKGROUND: Stingless bee honeys are drawing increasing attention as ingredients for functional foods and health-oriented products because of their distinctive sensory characteristics and bioactive potential. In this study, honeys collected from nine stingless bee species reared in West Sumatra, Indonesia, were comprehensively characterized using physicochemical indices, antioxidant assays [DPPH (i.e. 2,2-diphenyl-1-picrylhydrazyl) and ferric reducing antioxidant power], microbiological screening, volatile profiling [gas chromatography-mass spectrometry (GC-MS)] and Fourier transform infrared (FTIR) fingerprinting. RESULTS: Marked between-sample variability was observed across key quality attributes, including pH (2.80-3.68), Brix (49.83-61.25), viscosity (23.36-175.22 cP) and color parameters. FTIR spectra were consistent with carbohydrate-rich matrices and exhibited carbonyl-related bands. GC-MS profiling identified linalool oxide isomers and junenol among the predominant volatiles. To the best of our knowledge, junenol has not previously been reported in stingless bee honey and may represent a potential regional chemical marker for Indonesian stingless bee honeys. Lactic acid bacteria were detected in selected samples, whereas yeast and mold were not detected. Antioxidant activities were comparatively low, which may reflect local environmental and ecosystem-related factors. CONCLUSION: The results provide a multi-parameter baseline for stingless bee honeys produced within a shared ecosystem in West Sumatra and demonstrate the value of integrating conventional chemical indices with FTIR and volatile fingerprints for quality assessment. This combined approach may also support future authentication and origin-tracing frameworks for Indonesian stingless bee honeys. © 2026 Society of Chemical Industry.

Animals↗

[New bioactive compounds of the adrenal medullary layer].

The review of new data of the studies of the cerebral layers of eight cardioactive peptide and clieopeptide combinations. Research of the physical-chemical and biochemical properties confirm nonidentity of these combinations to the known bioactive peptides of adrenals. The proteins connecting the factors under exploration have also been discovered, suggesting existence of cardioactive protein-peptide complexes in this region. Based on comparison of the studied chemical and biological properties of these combinations with the combinations of hypothalamic cardioactive neurohormones, in particular, with the neurohormone "C", a conclusion was made that combinations of the two regions are structurally and functionally related. The obtained data can be used in practical medicine for prophylactics and treatment of several cardiovascular diseases.

Adrenal Medulla↗

Enzymes in the synthesis of bioactive compounds: the prodigious decades.

The growing demand for enantiomerically pure pharmaceuticals has impelled research on enzymes as catalysts for asymmetric synthetic transformations. However, the use of enzymes for this purpose was rather limited until the discovery that enzymes can work in organic solvents. Since the advent of the PCR the number of available enzymes has been growing rapidly and the tailor-made biocatalysts are becoming a reality. Thus, it has been possible the use of enzymes for the synthesis of new innovative medicines such as carbohydrates and their incorporation to modern methods for drug development, such as combinatorial chemistry. Finally, the genomic research is allowing the manipulation of whole genomes opening the door to the combinatorial biosynthesis of compounds. In this review, our intention is to highlight the main landmarks that have led to transfer the chemical efficiency shown by the enzymes in the cell to the synthesis of bioactive molecules in the lab during the last 20 years.

Animals↗

Marine-derived Bioactive Compounds: A Promising Frontier against Multidrug-resistant Microbial Infections.

The global escalation of Multidrug-Resistant (MDR) bacterial infections poses a serious and growing threat to public health, contributing to increased morbidity, mortality, and substantial economic burden worldwide. The widespread and often indiscriminate use of antibiotics in clinical and agricultural settings has accelerated the emergence of resistance, significantly diminishing the efficacy of conventional antimicrobial therapies. This pressing challenge necessitates the exploration of alternative sources for novel antibiotics. Marine ecosystems-renowned for their immense biodiversity and ecological complexity-have gained attention as a rich and largely untapped reservoir of bioactive natural products with potent antimicrobial activity. Marine organisms, such as sponges, tunicates, algae, and bacteria and fungi derived from marine sources, produce structurally diverse and pharmacologically active metabolites, including peptides, polyketides, alkaloids, terpenoids, sterols, lactones, and halogenated compounds. Many of these marine-derived molecules possess unique chemical scaffolds and novel mechanisms of action, offering the potential to circumvent existing resistance pathways. Some compounds have shown promising activity against MDR pathogens, including Staphylococcus aureus, Pseudomonas aeruginosa, and Acinetobacter baumannii. However, challenges such as low natural abundance, difficulty in cultivation, and structural complexity have limited their clinical translation. Recent advancements in marine biotechnology, genomics, metagenomics, and synthetic biology have opened new avenues for the discovery, biosynthesis, and structural optimization of these compounds. These innovative approaches not only facilitate sustainable production but also enhance the pharmacological properties.

Humans↗

Structural studies on bioactive compounds. 40.(1) Synthesis and biological properties of fluoro-, methoxyl-, and amino-substituted 3-phenyl-4H-1-benzopyran-4-ones and a comparison of their antitumor activities with the activities of related 2-phenylbenzothiazoles.

A new series of fluoro-, methoxyl-, and amino-substituted isoflavones have been synthesized as potential antitumor agents based on structural similarities to known flavones and isoflavones (quercetin and genistein respectively) and antitumor 2-phenylbenzothiazoles. Target compounds were synthesized using palladium-catalyzed coupling methodologies to construct the central aryl carbon-carbon single bond. The new isoflavone derivatives were tested for in vitro activity in human breast (MDA-MB-468 and MCF-7) and colon (HT29 and HCT-116) cancer cell lines. Low micromolar GI50 values were obtained in a number of cases, with the MDA-MB-468 cell line being the most sensitive overall. Notably, significant potentiation of growth inhibitory activity (GI50<1 microM for 12d, 12f, 12h, 12k, 12l, 12o but not the methylene-bridged derivative 12i) was observed when MDA-MB-468 cells were co-incubated with TBDD, a powerful inducer of cytochrome P450 (CYP)-1A1 activity, suggesting that isoflavone derivatives can act as substrates for CYP1A1 bioactivation.

Antineoplastic Agents↗

Use of liquid chromatography for the determination of interactions between bioactive compounds.

Molecular interactions can be easily determined both by thin-layer and high performance liquid chromatography. The theory and practice of the determination of molecular interactions and the various methods for the calculation of complex stability are presented. Examples of the application of liquid chromatographic methods for the measurements of molecular interactions are also discussed.

Chemical Phenomena↗

On-line identification of the bioactive compounds from Blumea gariepina by HPLC-UV-MS and HPLC-UV-NMR, combined with HPLC-micro-fractionation.

The dichloromethane extract of the aerial parts of Blumea gariepina (Asteraceae) was shown to be active against the phytopathogenic fungus Cladosporium cucumerinum and to inhibit acetylcholinesterase. In order rapidly to identify the active principles, the crude extract was analysed by on-flow HPLC-1H-NMR. HPLC-micro-fractionation was performed and all peaks collected were submitted to assays against C. cucumerinum and acetylcholinesterase. By this means, the biological activities could be efficiently associated with selected HPLC peaks. Complementary on-line structural data for all peaks of interest in the crude extract were obtained from HPLC-MS and from HPLC-UV with post-column addition of UV shift reagents. This chemical screening strategy with integrated bioassays permitted the on-line identification of a number of constituents and gave useful information for an efficient isolation procedure.

Antifungal Agents↗

Selected bioactive compounds from Japanese anaspideans and nudibranchs.

Marine opisthobranchs are mollusks scarcely protected by a shell which can be either reduced or completely absent. It is generally accepted that they possess chemical defenses (allelochemicals) against predators. These protective molecules can derive from dietary habits (algae, sponges, tunicates, soft corals, etc.) and can be used either in their intact form or as derived metabolites. Added to this, other compounds are biogenetically obtained. These defensive compounds are very often concentrated in the external parts of the animal and are also released into the mucous secretion to deter predators. The chemical defenses of sea hares (order Anaspidea) and sea slugs (order Nudibranchia) are well studied. This review highlights the allelochemicals reported from Japanese anaspideans and nudibranchs, with particular attention to the finding of our group.

Animals↗