Explore the vast range of titles available.

Anthraquinones (AQs) are found in a variety of consumer products, including foods, nutritional supplements, drugs, and traditional medicines, and have a wide range of pharmacological actions. Rubiadin, a 1,3-dihydroxy-2-methyl anthraquinone, primarily originates from Linn (Rubiaceae). It was first discovered in 1981 and has been reported for many biological activities. However, no review has been reported so far to create awareness about this molecule and its role in future drug discovery. Therefore, the present review aimed to provide comprehensive evidence of Rubiadin's phytochemistry, biosynthesis, physicochemical properties, biological properties and therapeutic potential. Relevant literature was gathered from numerous scientific databases including PubMed, ScienceDirect, Scopus and Google Scholar between 1981 and up-to-date. The distribution of Rubiadin in numerous medicinal plants, as well as its method of isolation, synthesis, characterisation, physiochemical properties and possible biosynthesis pathways, was extensively covered in this review. Following a rigorous screening and tabulating, a thorough description of Rubiadin's biological properties was gathered, which were based on scientific evidences. Rubiadin fits all five of Lipinski's rule for drug-likeness properties. Then, the in depth physiochemical characteristics of Rubiadin were investigated. The simple technique for Rubiadin's isolation from and the procedure of synthesis was described. Rubiadin is also biosynthesized via the polyketide and chorismate/o-succinylbenzoic acid pathways. Rubiadin is a powerful molecule with anticancer, antiosteoporotic, hepatoprotective, neuroprotective, anti-inflammatory, antidiabetic, antioxidant, antibacterial, antimalarial, antifungal, and antiviral properties. The mechanism of action for the majority of the pharmacological actions reported, however, is unknown. In addition to this review, an in silico molecular docking study was performed against proteins with PDB IDs: 3AOX, 6OLX, 6OSP, and 6SDC to support the anticancer properties of Rubiadin. The toxicity profile, pharmacokinetics and possible structural modifications were also described. Rubiadin was also proven to have the highest binding affinity to the targeted proteins in an in silico study; thus, we believe it may be a potential anticancer molecule. In order to present Rubiadin as a novel candidate for future therapeutic development, advanced studies on preclinical, clinical trials, bioavailability, permeability and administration of safe doses are necessary.

Two new anthraquinone derivatives, (±)-1'- -methyl-6-chloroaverantin ( and ) and 6-chloroaverythrin ( ), and one new diphenyl ether 1-(( )-but-2-en-2-yl)-3,8-dihydroxy-6-(( )-4-hydroxybut-2-en-2-yl)-4,9-dimethyl-11 -dibenzo[b,e][1,4]dioxepin-11-one ( ), along with six known compounds, were isolated from the fungus sp. SCSIO 41331 collected from the deep-sea sediment in the cold-seep area of the South China Sea. Elucidation of planar structures was achieved via 1D and 2D NMR and mass spectrometry, whereas stereochemistry was validated through optical rotation and NOE correlations, chiral phase HPLC analysis and NMR calculation. All compounds were assessed for antitumor activity, among which compound displayed moderate antiproliferative activity against HT29 cells and suppressed colony expansion.

Renal diseases including acute kidney injury (AKI) and chronic kidney disease (CKD) has become a significant public health concern due to its high morbidity and mortality. Baill (Polygonaceae) exhibits diuretic, renoprotective, lipid-lowering, anti-inflammatory, and antifibrotic properties. Accumulating evidence has highlighted the anthraquinones in as key components contributing to its renoprotective effects. The available information on was searched by several electronic database such as PubMed, Web of Science, Springer, ScienceDirect, etc. This review summarizes the anthraquinones and their renoprotective effects in , evaluating its clinical potential for managing renal disease including AKI and CKD. Studies demonstrate that contains bioactive components such as anthraquinones, stilbenes, phenylbutazones, and tannins. This review discusses the renoprotective effects of , including improvements in renal function, reduction of podocyte damage, and inhibition of renal fibrosis. These effects are mediated through the regulation of pro-inflammatory (IκB/NF-κB and Keap1/Nrf2), pro-fibrotic (TGF-β1/Smad and Wnt/β-catenin), AMP-activated protein kinase and phosphoinositide 3-kinase signaling pathways in AKI and CKD. Additional mechanisms include modulation of anti-ageing Klotho expression, autophagy, and apoptosis. These findings expand the understanding of the therapeutic effects on AKI and CKD of and provide valuable information on its clinical application in traditional Chinese medicine. This review presents a concept-driven therapeutic strategy for renal disease management.

The present study aimed to identify the composition of the aerial parts of Rubia cordifolia L. A chemical investigation on the EtOAc extracts from the aerial parts of Rubia cordifolia resulted in the isolation of four new anthraquinones, namely Cordifoquinone A–D (1–4), along with 16 known anthraquinones. Their structures were elucidated on the basis of NMR and HR-ESIMS data. All isolates were assessed for their inhibitory effects on NO production in LPS-stimulated RAW 264.7 macrophage cells. Compounds 1, 3 and 10 exhibited significant inhibitory activities with IC50 values of 14.05, 23.48 and 29.23 μmol·L−1, respectively. Their antibacterial activities of four bacteria, Escherichia coli (ATCC 25922), Staphylococcus aureus subsp. aureus (ATCC 29213), Salmonella enterica subsp. enterica (ATCC 14028) and Pseudomonas aeruginosa (ATCC 27853), were also evaluated. Our results indicated that the antibacterial activity of these compounds is inactive.

Marine alga-derived fungal strain КММ 4176 was identified as Aspergillus niveoglaucus based on ITS region BenA , CaM and RPB2 gene sequence analysis. The anthraquinone derivatives emodin anthrone ( 1 ) and 4-hydroxyemodin anthrone ( 2 ), chromone derivative aloesone ( 3 ), and indole diketopiperazine alkaloid neoechinulin B ( 4 ) were isolated from the ethyl acetate extract of this fungus. In addition, UPLC MS data analysis of the KMM 4176 extract showed the presence of 17 echinulin-family alkaloids, as well as their biogenetic precursor cyclo( l -alanyl- l -tryptophyl) and a number of polyketide compounds. Emodin anthrone and 4-hydroxyemodin anthrone were found as inhibitors of biofilm formation by Staphylococcus aureus with half-maximal inhibitory concentrations (IC 50 ) of 5.5 µM and 23.7 µM, respectively. Moreover, emodin anthrone ( 1 ) and 4-hydroxyemodin anthrone ( 2 ) inhibited staphylococcal sortase A activity with IC 50 of 9.2 µM and 37.6 µM, respectively. Aloesone ( 3 ) also inhibited S. aureus biofilm formation but was less active. The first data on neoechinulin B ( 4 ) antibiofilm activity and sortase A inhibition were obtained. The positive effects of the isolated compounds on the growth of HaCaT keratinocytes infected with S. aureus were also observed.

Two new chlorinated metabolites 4-chloro-1-hydroxy-3-methoxy-6-methyl-8-methoxycarbonyl-xanthen-9-one ( 1 ) and 2′-acetoxy-7-chlorocitreorosein ( 2 ), together with three known compounds ( 3 – 5 ), were obtained from the EtOAc extract of the endophytic fungus Penicillium citrinum HL-5126 isolated from the mangrove Bruguiera sexangula var. rhynchopetala collected in the South China Sea. Their structures were elucidated by the detailed analysis of comprehensive spectroscopic data. All compounds were evaluated for their antibacterial and topoisomerase I inhibitory activities. Compound 2 exhibited antibacterial activity against Vibrio parahaemolyticus with an MIC value of 10 μ m .

Rhubarb, traditionally used in China for neurological disorders, has recently attracted considerable scientific attention for its neuroprotective and cerebrovascular benefits. The main therapeutic components of rhubarb are anthraquinones, including emodin, aloe-emodin, chrysophanol, rhein, and physcion. Accumulating experimental evidence indicates that anthraquinones are of importance in neurodegenerative diseases (NDDs), such as Alzheimer's disease, Parkinson's disease, Huntington's disease, and multiple sclerosis. However, as a promising candidate for drug development, the mechanisms by which anthraquinones treat NDDs have not been systematically reviewed. Therefore, this article outlines the anti-neurodegenerative effects of anthraquinones, focusing on their molecular mechanisms. This article reviews recent research progress of anthraquinones in NDDs, focusing on their potential targets and pathways to provide new ideas for the intervention and treatment of NDDs. A comprehensive search of PubMed, Web of Science, and Google Scholar was conducted for articles on the intervention of anthraquinones in NDDs in the past 20 years. The collected information was then summarized and analyzed. Anthraquinones ameliorate NDDs through multiple mechanisms. They exhibit antioxidant and anti-inflammatory effects, protect mitochondria, and regulate microglial polarization. Furthermore, anthraquinones inhibit pyroptosis, apoptosis, tau phosphorylation, Aβ/α-synuclein aggregation, and acetylcholinesterase activity, while restoring metal homeostasis, activating estrogen receptors, modulating gut microbiota, increasing BDNF levels, and preserving blood-brain barrier permeability. More notably, these compounds play a neuroprotective role by mediating multiple signaling pathways and targets, including Nrf2, ERK1/2, PI3K/mTOR, ROS/TXNIP, SIRT1/PCG-1α, NLRP3, PI3K/Akt, MAPK, TLR4-NFκB, CaM/CaMKIV, and Ca /EGFR/PLCγ. The pleiotropic actions of anthraquinones highlight their potential as therapeutic candidates for NDDs, yet clinical validation remains essential. Future studies should emphasize rigorously designed clinical trials and optimized brain-targeted delivery platforms. This review consolidates current evidence to support their translational development.

Background Malaria remains a major global parasitic disease, increasingly complicated by resistance to frontline antimalarial drugs such as chloroquine and artemisinin. This challenge underscores the urgent need for novel antimalarial agents with alternative mechanisms of action. Endophytic fungi constitute a promising yet underexplored source of structurally diverse bioactive metabolites. This study investigated the antimalarial potential of ( +)-2,2′-epicytoskyrin A (Epi-A), a bisanthraquinone isolated from Diaporthe sp. GNBP-10, an endophyte of Uncaria gambir (Hunter) Roxb., was utilized in both in vitro and in vivo models. Methods In vitro antimalarial activity was assessed against chloroquine-sensitive Plasmodium falciparum 3D7 using microscopic examination of Giemsa-stained thin blood smears. At the same time, cytotoxicity was evaluated in MCF-7 cells by measuring absorbance at 450 nm and calculating CC₅₀ values using GraphPad Prism. In vivo efficacy was evaluated in Plasmodium berghei– infected Swiss Webster mice. Animals were assigned to five groups: oral Epi-A (12.5, 25, and 50 mg/kg BW), artemisinin (20 mg/kg BW), and an untreated infected group. Treatment was administered for four consecutive days after the mean parasitaemia reached 10%. Histopathological analysis of the liver, spleen, kidney, and intestine was performed on day 8 pi using one mouse per group, while the remaining mice were monitored until day 15 pi for parasitaemia, survival, clinical manifestations, and body weight changes. Results Epi-A demonstrated potent in vitro activity, with an IC₅₀ of 0.24 µM, a CC₅₀ of 4.4 µM, and a selectivity index of 18.33. In vivo, on day 8 pi, histopathology revealed haemozoin deposition with mild tissue alterations in the liver, spleen, kidney, and intestine. Parasitaemia did not differ among Epi-A–treated groups but was significantly lower than in the negative control. Epi-A achieved > 50% inhibition (63.6%, 77.4%, and 50% at 12.5, 25, and 50 mg/kg BW, respectively), classifying it as a very good antimalarial activity. No post-treatment weight loss was observed, and only mild clinical signs were noted, compared with the severe manifestations observed in the negative control. Conclusions Epi-A demonstrates potent in vitro and very good in vivo antimalarial activity, with low toxicity and potential organ-protective effects, supporting its promise as a candidate for further mechanistic studies.

Antimicrobial resistance is a critical global health issue, with rising resistance among bacteria and fungi. Marine organisms have emerged as promising, but underexplored, sources of new antimicrobial agents. Among them, marine polychaetes, such as Halla parthenopeia, which possess chemical defenses, could attract significant research interest. This study explores the antimicrobial properties of hallachrome, a unique anthraquinone found in the purple mucus of H. parthenopeia, against Gram-negative bacteria (Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 9027), Gram-positive bacteria (Enterococcus faecalis ATCC 29212, Staphylococcus aureus ATCC 6538, Staphylococcus epidermidis ATCC 12228), and the most common human fungal pathogen Candida albicans ATCC 10231. Antibacterial susceptibility testing revealed that Gram-negative bacteria were not inhibited by hallachrome at concentrations ≤2 mM. However, Gram-positive bacteria showed significant growth inhibition at 0.12–0.25 mM, while C. albicans was inhibited at 0.06 mM. Time-kill studies demonstrated dose-dependent growth inhibition of susceptible strains by hallachrome, which exerted its effect by altering the membrane permeability of C. albicans, E. faecalis, and S. epidermidis after 6 h and S. aureus after 24 h. Additionally, hallachrome significantly reduced biofilm formation and mature biofilm in S. aureus, E. faecalis, and C. albicans. Additionally, it inhibited hyphal growth in C. albicans. These findings highlight hallachrome’s potential as a novel antimicrobial agent, deserving further exploration for clinical experimentation.

Antimicrobial resistance (AMR) has emerged as a global health crisis, with methicillin-resistant Staphylococcus aureus (MRSA) representing one of the most clinically significant multidrug-resistant pathogens. In this study, three structurally unique anthracycline derivatives—keto-ester (1), 4-deoxy-ε-pyrromycinone (2), and misamycin (3)—were first isolated and characterized from the fermentation broth of the marine-derived Streptomyces tauricus NBUD24. These compounds exhibited notable antibacterial efficacy against MRSA, with minimum inhibitory concentrations (MICs) ranging from 16 to 32 µg/mL. Cytotoxicity assays confirmed their safety profile at therapeutic concentrations. The biofilm formation assay demonstrated that 4-deoxy-ε-pyrromycinone inhibited biofilm formation of MRSA ATCC43300, with an inhibition rate of 64.4%. Investigations of antibacterial mechanisms revealed that these compounds exert antibacterial effects primarily through disruption of bacterial cell wall integrity and destruction of DNA structure. These findings underscore the potential of marine-derived microbial metabolites as promising scaffolds for developing next-generation antimicrobial candidates to combat drug-resistant infections.