Bioactive Products Research Articles

A rho-type GTPase activating protein affects the growth and development of Cordyceps cicadae.

Cordyceps cicadae is recognized for its medicinal properties, attributed to bioactive constituents like polysaccharides and adenosine, which have been shown to improve kidney and liver functions and possess anti-tumor properties. Rho GTPase activating proteins (Rho GAPs) serve as inhibitory regulators of Rho GTPases in eukaryotic cells by accelerating the GTP hydrolysis of Rho GTPases, leading to their inactivation. In this study, we explored the function of the CcRga8 gene in C. cicadae, which encodes a Rho-type GTPase activating protein. Our study found that the knockout of CcRga8 resulted in a decrease in polysaccharide levels and an increase in adenosine concentration. Furthermore, the mutants exhibited altered spore yield and morphology, fruiting body development, decreased infectivity, reduced resistance to hyperosmotic stress, oxidative conditions, and cell wall inhibitors. These findings suggest that CcRga8 plays a crucial role in the development, stress response, and bioactive compound production of C. cicadae.

Exploring the microbial community and biotechnological potential of the sponge Xestospongia sp. from an anchialine cave in the Yucatán Peninsula

Sponge-associated microorganisms are key influencers of nutrient biogeochemistry and important sources of bioactive natural products. This study provides the first insights into the taxonomic diversity of the microbial community associated with the sponge Xestospongia sp. from an anchialine cave in the coastal area of the underground river of the Yucatán Peninsula in Xcalak, Quintana Roo, Mexico, and the potential antimicrobial activity of its cultivable bacteria. High abundances of Sulfurospirillum and Desulfovibrio were detected with 16S rRNA amplicons, suggesting that the microbial community of Xestospongia sp. plays an important role in the geochemical sulfur cycle. Analysis with crude extracts of Nocardiopsis dasonvillei NCA-454 revealed antimicrobial activity against methicillin-sensitive Staphylococcus aureus ATCC 25913 (MSSA) and methicillin-​resistant ​S. aureus ATCC 43300 (MRSA). Studies of the microbiomes of sponges from the anchialine cave system in the Yucatán Peninsula can help elucidate the biogeochemical cycles of these poorly studied environments. Moreover, the microorganisms of these microbial communities represent an untapped source of secondary metabolites with biotechnological potential.

Cryptic enzymatic assembly of peptides armed with β-lactone warheads

Nature has evolved biosynthetic pathways to molecules possessing reactive warheads that inspired the development of many therapeutic agents, including penicillin antibiotics. Peptides armed with electrophilic warheads have proven to be particularly effective covalent inhibitors, providing essential antimicrobial, antiviral and anticancer agents. Here we provide a full characterization of the pathways that nature deploys to assemble peptides with β-lactone warheads, which are potent proteasome inhibitors with promising anticancer activity. Warhead assembly involves a three-step cryptic methylation sequence, which is likely required to reduce unfavorable electrostatic interactions during the sterically demanding β-lactonization. Amide-bond synthetase and adenosine triphosphate (ATP)-grasp enzymes couple amino acids to the β-lactone warhead, generating the bioactive peptide products. After reconstituting the entire pathway to β-lactone peptides in vitro, we go on to deliver a diverse range of analogs through enzymatic cascade reactions. Our approach is more efficient and cleaner than the synthetic methods currently used to produce clinically important warhead-containing peptides.

Green synthesized extracts/Au complex of Phyllospongia lamellosa: Unrevealing the anti-cancer and anti-bacterial potentialities, supported by metabolomics and molecular modeling

The anti-cancer and anti-bacterial potential of the Red Sea sponge Phyllospongia lamellosa in its bulk (crude extracts) and gold nanostructure (loaded on gold nanaoparticles) were investigated. Metabolomics analysis was conducted, and subsequently, molecular modeling studies were conducted to explore and anticipate the P. lamellosa secondary metabolites and their potential target for their various bioactivities. The chloroformic extract (CE) and ethyl acetate extract (EE) of the P. lamellosa predicted to include bioactive lipophilic and moderately polar metabolites, respectively, were used to synthesize gold nanoparticles (AuNPs). The prepared AuNPs were characterized through transmission electron microscopy (TEM), Fourier-transform infrared spectroscopy (FTIR), and UV–vis spectrophotometric analyses. The cytotoxic activities were tested against MCF-7, MDB-231, and MCF-10A. Moreover, the anti-bacterial, antifungal, and anti-biofilm activity were assessed. Definite classes of metabolites were identified in CE (terpenoids) and EE (brominated phenyl ethers and sulfated fatty amides). Molecular modeling involving docking and molecular dynamics identified Protein-tyrosine phosphatase 1B (PTP1B) as a potential target for the anti-cancer activities of terpenoids. Moreover, CE exhibited the most powerful activity against breast cancer cell lines, matching our molecular modeling study. On the other hand, only EE was demonstrated to possess powerful anti-bacterial and anti-biofilm activity against Escherichia coli. In conclusion, depending on their bioactive metabolites, P. lamellosa-derived extracts, after being loaded on AuNPs, could be considered anti-cancer, anti-bacterial, and anti-biofilm bioactive products. Future work should be completed to produce drug leads.

Integrating Computational Methods into Antibacterial Drug Discovery and Development from Natural Products

Natural products have long been pivotal in sustaining civilizations due to their medicinal properties and have served as a rich source of bioactive compounds for drug discovery. With the rise of antibiotic-resistant bacteria, there is an urgent need for new antibacterial agents. Natural products, with their diverse chemical structures, provide a promising reservoir for identifying new lead compounds. Historically, the discovery of bioactive natural products often relied on serendipity, but modern advancements in computational approaches, particularly computer-aided drug design (CADD), have revolutionized this process. In the modern era, vast data from advanced technologies can provide valuable insights through computational methods. These approaches enable the structural analysis of molecules and the prediction of their biological activities, accelerating drug discovery. Advances in molecular sciences have identified more antibacterial targets, further facilitating this process. Integrating computational drug design with the study of natural products allows for the efficient identification and optimization of potential antibacterial agents. Moreover, many medicinal plants harbor mechanisms of action that remain unexplored by conventional methods. By employing computational techniques, researchers can uncover these mechanisms and develop novel antibacterial drugs. This combined approach not only enhances our understanding of natural products but also addresses the critical need for new treatments in the fight against bacterial infections.

Discovery of Loureirin analogues with colorectal cancer suppressive activity via regulating cell cycle and Fas death receptor

Chalcones and dihydrochalcones (DHCs) are important bioactive natural products (BNPs) isolated from traditional Chinese medicine. In this study, 13 chalcones were designed with the inspiration of Loureirin, a DHC extracted from Resina Draconis, and synthesized by classical Claisen-Schmidt reactions. Afterwards the reduction reactions were carried out to obtain the corresponding DHCs. Cytotoxicity assay indicated chalcones and DHCs possessed selective cytotoxicity against colorectal cancer (CRC) cells. The preliminary structure-activity relationships (SAR) of these compounds suggested the α, β-unsaturated ketone of the chalcones were crucial for the anticancer activity. Interestingly, compounds 3d and 4c exhibited selective anticancer activity against CRC cell line HCT116 with IC50s of 8.4 and 17.9 μM but not normal cell. Moreover, 4c could also inhibit the migration and invasion of CRC cells. Mechanism investigations showed 4c could induce cell cycle G2/M arrest by regulating cell cycle-associated proteins and could also up-regulate Fas cell surface death receptor. The virtual docking further pointed out that compounds 3d and 4c could nicely bind to the Fas/FADD death domain complex (ID: 3EZQ). Furthermore, silencing of Fas significantly enhanced the proliferation of CRC cells and attenuated the cytotoxicity induced by 4c. These results suggested 4c exerted its anticancer activity possibly regulating cell cycle and Fas death receptor. In summary, this study investigated the anticancer activity and mechanism of Loureirin analogues in CRC, suggesting these compounds may warrant further investigation as promising anticancer drug candidates for the treatment of CRC.

Exploring in vitro oryzalin-induced polyploidy in Astragalus membranaceus: implications for gene expression

This study investigates the effects of artificial in vitro polyploidisation of Astragalus membranaceus, focusing specifically on gene expression and metabolic pathway associated with the biosynthesis of calycosin and calycosin-7-O-β-D-glucoside. Using oryzalin as an antimitotic agent, we have systematically investigated different genotypic lines, under both in vitro and ex vitro conditions. Amid cases of reduced gene expression in certain lines, results showed a significant upregulation in specific lines, particularly in genotypes 16, 54, and 74. Genotype 54 showed an exceptional response, manifesting a statistically significant upregulation in all investigated genes studied under in vitro conditions (i.e. AmPAL, AmC4H and AmI3′H). Interestingly, even under ex vitro conditions after two years of greenhouse cultivation, certain lines showed significant variations in gene expression. The genotype 16, although no longer tetraploid, exhibited the highest expression levels among the examined genotypes, with statistically significant upregulation of both the AmPAL and AmC4H genes. In addition, the induced autotetraploid genotype 74 showed a significant upregulation of the AmI3′H gene and a concomitant downregulation of the AmC4H gene. These results highlight the complex regulatory mechanisms affected by the polyploidisation of A. membranaceus and provide promising avenues for manipulating gene expression to enhance the production of pharmacologically significant compounds.Key messageThis study investigates the effects of artificial polyploidisation on gene expression of Astragalus membranaceus, suggesting diverse regulatory influences for potential plant bioactive compound production.

Effect of Harvest Time on Growth and Bioactive Compounds in Salvia miltiorrhiza.

Danshen (Salvia miltiorrhiza) is a perennial medicinal plant belonging to the Lamiaceae family. It is adapted to a wide range of soil pH with the potential to serve as an alternative crop in the United States. To enhance its cultivation and economic viability, it is crucial to develop production practices that maximize bioactive compound yields for danshen. The objective of this study was to investigate the effects of different harvest times on plant growth and subsequent yields of bioactive components of danshen. Three harvest times were selected (60, 120, or 180 days after transplanting [DAT]). In general, plants harvested at 180 DAT had higher plant growth index (PGI), shoot number, shoot weight, root number, maximum root length, maximum root diameter, and root weight compared to plants harvested at 60 or 120 DAT. However, plants harvested at 60 or 120 DAT had higher SPAD (Soil Plant Analysis Development) values. Plants harvested at 120 or 180 DAT had a higher content of tanshinone I, tanshinone IIA, cryptotanshinone, and salvianolic acid B compared to those harvested at 60 DAT. This study provides insights for optimizing the time of harvest of danshen to maximize plant growth and bioactive compound production.

Enhanced Antioxidant, Anti-Aging, Anti-Tyrosinase, and Anti-Inflammatory Properties of Vanda coerulea Griff. Ex Lindl. Protocorm through Elicitations with Chitosan.

This study aimed to investigate the effects of elicitors on Vanda coerulea Griff. Ex Lindl. protocorms to enhance bioactive compound production and evaluate their biological activities relevant to cosmeceutical applications. The protocorms were developed from the callus treated with different elicitors, including 6-benzylaminopurine (BA), methyl jasmonate (MeJA), and chitosan. Both the adult plant and protocorms were extracted by maceration in 80% methanol and investigated for their chemical compositions using high-performance liquid chromatography. The extracts were evaluated for antioxidant, anti-collagenase, anti-elastase, and anti-tyrosinase activities. In addition, anti-inflammatory properties were assessed using a real-time polymerase chain reaction. The irritation potency was evaluated using the hen's egg test-chorioallantoic membrane test. The findings revealed that protocorms treated with BA and chitosan developed a greener color, while those treated with MeJA exhibited a distinct darker coloration. Elicitation with BA and chitosan resulted in protocorms with comparable or higher levels of syringic acid, rutin, and quercin compared with the adult plant, with rutin being the most prominent identified compound. Furthermore, rutin was reported as the compound responsible for all biological activities. The chitosan-treated protocorm extract exhibited potent inhibition against oxidation, collagenase, elastase, tyrosinase, and inflammatory cytokines, along with a nonirritating effect, making it a promising candidate for cosmeceutical applications.

A Glucose Oxidase-Curcumin Composite Nanoreactor for Multimodal Synergistic Cancer Therapy.

Glucose oxidase (GOx) selectively oxidizes β-d-glucose into gluconic acid and hydrogen peroxide; thus, it has emerged as a promising anticancer agent by tumor starvation and oxidative therapy. Here, we developed a nanoscale platform or "nanoreactor" that incorporates GOx and the bioactive natural product curcumin (CUR) to achieve a multimodal anticancer nanocomposite. The composite nanoreactor was formed by loading CUR in biodegradable polymeric nanoparticles (NPs) of poly(ethylene glycol)-b-poly(ε-caprolactone) (PEG-PCL). Prime-coating of the NPs with an iron(III)-tannic acid complex enabled facile immobilization of GOx on the NP surface. The NPs were monodisperse with a hydrodynamic diameter of 122 nm and a partially negative surface charge. The NPs were also associated with an excellent CUR loading efficiency and sustained release up to 96 h, which was accelerated by surface-immobilized GOx and followed supercase II transport. Viability assays were conducted on two model cancer cell lines, MCF-7 and MDA-MB-231 cells, as well as human dermal fibroblasts as a representative normal cell line. The assays revealed significantly improved potency of CUR in the composite nanoreactor, with up to 6000- and 1280-fold increase in MCF-7 and MDA-MB-231 cells, respectively, and lower toxicity toward normal cells. The NPs were also able to promote intracellular reactive oxygen species (ROS) generation and dissipation of the mitochondrial membrane potential, providing important clues on the mechanism of action of the nanoreactor. Further investigation of caspase-3 activity revealed that the nanoreactor had no effect or inhibited caspase-3 levels, signifying a caspase-independent mechanism of inducing apoptosis. Our findings present a promising nanocarrier platform that combines therapeutic agents with distinct mechanisms of action acting in synergy for more effective cancer therapy.

A treasure trove of 1034 actinomycete genomes.

Filamentous Actinobacteria, recently renamed Actinomycetia, are the most prolific source of microbial bioactive natural products. Studies on biosynthetic gene clusters benefit from or require chromosome-level assemblies. Here, we provide DNA sequences from >1000 isolates: 881 complete genomes and 153 near-complete genomes, representing 28 genera and 389 species, including 244 likely novel species. All genomes are from filamentous isolates of the class Actinomycetia from the NBC culture collection. The largest genus is Streptomyces with 886 genomes including 742 complete assemblies. We use this data to show that analysis of complete genomes can bring biological understanding not previously derived from more fragmented sequences or less systematic datasets. We document the central and structured location of core genes and distal location of specialized metabolite biosynthetic gene clusters and duplicate core genes on the linear Streptomyces chromosome, and analyze the content and length of the terminal inverted repeats which are characteristic for Streptomyces. We then analyze the diversity of trans-AT polyketide synthase biosynthetic gene clusters, which encodes the machinery of a biotechnologically highly interesting compound class. These insights have both ecological and biotechnological implications in understanding the importance of high quality genomic resources and the complex role synteny plays in Actinomycetia biology.

Chemoenzymatic Synthesis of 2‐Aryl Thiazolines from 4‐Hydroxybenzaldehydes Using Vanillyl Alcohol Oxidases

AbstractNitrogen heterocycles are commonly found in bioactive natural products and drugs. However, the biocatalytic tools for nitrogen heterocycle synthesis are limited. Herein, we report the discovery of vanillyl alcohol oxidases (VAOs) as efficient biocatalysts for the one‐pot synthesis of 2‐aryl thiazolines from various 4‐hydroxybenzaldehydes and aminothiols. The wild‐type biocatalyst features a broad scope of 4‐hydroxybenzaldehydes. Though the scope of aminothiols is limited, it could be improved via semi‐rational protein engineering, generating a variant to produce previously inaccessible cysteine‐derived bioactive 2‐aryl thiazolines using the wild‐type VAO. Benefiting from the derivatizable functional groups in the enzymatic products, we further chemically modified these products to expand the chemical space, offering a new chemoenzymatic strategy for the green and efficient synthesis of structurally diverse 2‐aryl‐thiazoline derivatives to prompt their use in drug discovery and catalysis.

Chemoenzymatic Synthesis of 2-Aryl Thiazolines from 4-Hydroxybenzaldehydes Using Vanillyl Alcohol Oxidases.

Nitrogen heterocycles are commonly found in bioactive natural products and drugs. However, the biocatalytic tools for nitrogen heterocycle synthesis are limited. Herein, we report the discovery of vanillyl alcohol oxidases (VAOs) as efficient biocatalysts for the one-pot synthesis of 2-aryl thiazolines from various 4-hydroxybenzaldehydes and aminothiols. The wild-type biocatalyst features a broad scope of 4-hydroxybenzaldehydes. Though the scope of aminothiols is limited, it could be improved via semi-rational protein engineering, generating a variant to produce previously inaccessible cysteine-derived bioactive 2-aryl thiazolines using the wild-type VAO. Benefiting from the derivatizable functional groups in the enzymatic products, we further chemically modified these products to expand the chemical space, offering a new chemoenzymatic strategy for the green and efficient synthesis of structurally diverse 2-aryl-thiazoline derivatives to prompt their use in drug discovery and catalysis.

Construction of Acyclic Quaternary Carbon Stereocenters via Enantioselective Nickel Catalysis†

Comprehensive SummaryThe construction of acyclic quaternary carbon stereocenters, which are ubiquitous in many bioactive compounds, pharmaceuticals and natural products, has been a long persuit in synthetic organic chemistry. Among numerous methods, enantioselective nickel‐catalysis has attracted incremental attention in recent years. This review summarizes the recent development in the asymmetric strategies, research progress, mechanistic investigations for the generation of acyclic quaternary carbon stereocenters via enantioselective nickel catalysis. Key ScientistsIn 2006, the Zhou group and RajanBabu group realized the nickel‐catalyzed enantioselective hydrovinylation of α‐substituted styrenes and ethylene to construct acyclic quaternary carbon stereocenters (QCSs) by using spiro‐ and binaphthyl phosphoramidite ligands, respectively. In 2016, Watson developed a nickel‐catalyzed Suzuki‐Miyaura arylation to generate acyclic QCSs via chirality transfer reaction. In 2017, the Feng and the Fu group developed nickel‐catalyzed enantioselective conjugated/Michael additions to build acyclic QCSs, respectively. In 2020, the Fang group made the first success in the construction of QCSs by nickel‐catalyzed hydrocyanation of alkenes and allenes. In 2021, Gregory C. Fu and co‐workers disclosed a nickel‐catalyzed enantioselective α‐functionalization of carbonyl compounds that could form acyclic QCSs. At the same time, the Shi group constructed chiral acyclic QCSs via nickel‐catalyzed functionalization of alkenes. In 2023, Kleij and co‐workers applied a new strategy for Ni‐catalyzed regio‐ and enantioselective homoallylic coupling to construct acyclic QCSs. In the same year, Tao and co‐workers demonstrated a novel strategy that is dinickel‐catalyzed enantioselective α‐alkylation of carbonyl compounds with alkyl iodides.

Heterologous Expression and Characterization of a pH-Stable Chitinase from Micromonospora aurantiaca with a Potential Application in Chitin Degradation.

To promote the bioconversion of marine chitin waste into value-added products, we expressed a novel pH-stable Micromonospora aurantiaca-derived chitinase, MaChi1, in Escherichia coli and subsequently purified, characterized, and evaluated it for its chitin-converting capacity. Our results indicated that MaChi1 is of the glycoside hydrolase (GH) family 18 with a molecular weight of approximately 57 kDa, consisting of a GH18 catalytic domain and a cellulose-binding domain. We recorded its optimal activity at pH 5.0 and 55 °C. It exhibited excellent stability in a wide pH range of 3.0-10.0. Mg2+ (5 mM), and dithiothreitol (10 mM) significantly promoted MaChi1 activity. MaChi1 exhibited broad substrate specificity and hydrolyzed chitin, chitosan, cellulose, soluble starch, and N-acetyl chitooligosaccharides with polymerization degrees ranging from three to six. Moreover, MaChi1 exhibited an endo-type cleavage pattern, and it could efficiently convert colloidal chitin into N-acetyl-D-glucosamine (GlcNAc) and (GlcNAc)2 with yields of 227.2 and 505.9 mg/g chitin, respectively. Its high chitin-degrading capacity and exceptional pH tolerance makes it a promising tool with potential applications in chitin waste treatment and bioactive oligosaccharide production.

Phytochemical profile, antioxidant, antidiabetic, and antimicrobial activities of Parkia timoriana bark extracts

Abstract. Sariwati A, Suryanti V, Sari F, Kamei I, Trisnawati EW. 2024. Phytochemical profile, antioxidant, antidiabetic, and antimicrobial activities of Parkia timoriana bark extracts. Biodiversitas 25: 2427-2433. Plants have various bioactive compounds that have pharmacological activity. Kedawung (Parkia timoriana (DC) Merr) is an indigenous plant in Indonesia that contains bioactive compounds. The leaves, bark, seeds, and roots of P. timoriana are commonly used in traditional medicine. The purpose of this study was to determine the chemical composition of P. timoriana bark extract and to assess its antioxidant, antidiabetic, and antibacterial activity. The bark of P. timoriana was extracted with various solvents that differ in polarity, such as water, methanol, ethyl acetate, and hexane. All extracts were investigated for antioxidant activities by 2,2-diphenyl-1-picrylhydrazyl) (DPPH) free-radical and 2,2’-azinobis (3-ethylbenz-thiazoline-6-sulfonic-acid) (ABTS) scavenging ability. The in-vitro antidiabetic activity was carried out by ?-amylase and ?-glucosidase inhibition. Antibacterial and antifungal activities were determined by the agar disc diffusion method. Parkia timoriana bark extracts contained alkaloids, flavonoids, steroids, tannins, terpenoids, saponins, reducing sugars, and cardiac glycosides. The ethyl acetate extract possessed the highest total phenolics, alkaloids, flavonoids, saponins, tannic acid, and terpenoids. Secondary metabolites in all extracts contributed to free radical scavenging, antidiabetic, antibacterial, and antifungal properties. The P. timoriana bark contains natural chemical compounds that might be useful as therapeutic agents for producing bioactive products and pharmaceuticals in the future.

Oxidative Coupling of Hydroquinone Derivatives with Olefins to Dihydrobenzofurans.

Dihydrobenzofuran is an important skeleton for bioactive compounds and natural products. Hydroquinones can be easily modified into substituted hydroquinones, which effectively undergo oxidation to produce the corresponding benzoquinone derivatives. Benzoquinones are reactive electrophiles that are frequently utilized in coupling with olefins to dihydrobenzofurans. Herein, we report the one-pot oxidative coupling of hydroquinones bearing an electron-withdrawing group at the C2 position with olefins to dihydrobenzofurans in the presence of the Lewis acidic FeCl3 and 2,3-dichloro-5,6-dicyano-p-benzoquinone (DDQ) oxidant. Furthermore, this method was applied to the oxidative coupling of N-electron-withdrawing group-substituted 4-aminophenol.

A Genomics-Based Discovery of Secondary Metabolite Biosynthetic Gene Clusters in the Potential Novel Strain Streptomyces sp. 21So2-11 Isolated from Antarctic Soil.

Streptomyces species are attractive sources of secondary metabolites that serve as major sources of antibiotics and other drugs. In this study, genome mining was used to determine the biosynthetic potential of Streptomyces sp. 21So2-11 isolated from Antarctic soil. 16S rRNA gene sequencing revealed that this strain is most closely related to Streptomyces drozdowiczii NBRC 101007T, with a similarity of 98.02%. Genome comparisons based on average nucleotide identity (ANI) and digital DNA-DNA hybridization (dDDH) showed that strain 21So2-11 represents a novel species of the genus Streptomyces. In addition to a large number of genes related to environmental adaptation and ecological function, a total of 28 putative biosynthetic gene clusters (BGCs) responsible for the biosynthesis of known and/or novel secondary metabolites, including terpenes, lantipeptides, polyketides, nonribosomal peptides, RiPPs and siderophores, were detected in the genome of strain 21So2-11. In addition, a total of 1456 BGCs were predicted to contribute to the biosynthesis of more than 300 secondary metabolites based on the genomes of 47 Streptomyces strains originating from polar regions. The results indicate the potential of Streptomyces sp. 21So2-11 for bioactive secondary metabolite production and are helpful for understanding bacterial adaptability and ecological function in cold terrestrial environments.

Marine algae-derived characterized bioactive compounds as therapy for cancer: A review on their classification, mechanism of action, and future perspectives.

In 2022, there were around 20 million new cases and over 9.7 million cancer-related deaths worldwide. An increasing number of metabolites with anticancer activity in algae had been isolated and identified, which were promising candidates for cancer therapy. Red algae are well-known for the production of brominated metabolites, including terpenoids and phenols, which have the capacity to induce cell toxicity. Some non-toxic biological macromolecules, including polysaccharides, are distinct secondary metabolites found in many algae, particularly green algae. They possess anticancer activities by inhibiting tumor angiogenesis, stimulating the immune response, and inducing apoptosis. However, the structure-activity relationship between these components and antitumor activity, as well as certain taxa within the algae, remains relatively unstudied. This work is based on the reports published from 2003 to 2024 in PubMed and ISI Web of Science databases. A comprehensive review of the characterized algal anticancer active compounds, together with their structure and mechanism of action was performed. Also, their structure-activity relationship was preliminarily summarized to better assess their potential properties as a natural, safe bioactive product to be used as an alternative for the treatment of cancers, leading to new opportunities for drug discovery.

Application of Cyclic Diaryliodonium Salts in the Synthesis of Axially Chiral Natural Product Analogues.

The application of cyclic diaryliodonium salts in the synthesis of bioactive natural product analogues was demonstrated. Axially chiral biaryls were obtained via the enantioselective ring opening of cyclic diaryliodonium salts. Regioselective borylation was key in accessing both enantiomers of a biphenol key intermediate in eight steps overall. 8,8″-Amino biflavones were synthesized, their bioactivity profiled, and the eutomer identified. The structure-activity relationship was probed.