Albafuran C

Prenylated phenolics from Morus alba against MRSA infections as a strategy for wound healing.[Pubmed:36532741]

Front Pharmacol. 2022 Nov 30;13:1068371.

Antimicrobial resistance is a public health threat and the increasing number of multidrug-resistant bacteria is a major concern worldwide. Common antibiotics are becoming ineffective for skin infections and wounds, making the search for new therapeutic options increasingly urgent. The present study aimed to investigate the antibacterial potential of prenylated phenolics in wound healing. Phenolic compounds isolated from the root bark of Morus alba L. were investigated for their antistaphylococcal potential both alone and in combination with commonly used antibiotics. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) were determined by microdilution and agar method. Synergy was investigated using the checkerboard titration technique. Membrane-disrupting activity and efflux pump inhibition were evaluated to describe the potentiating effect. Prenylated phenolics inhibited bacterial growth of methicillin-resistant Staphylococcus aureus (MRSA) at lower concentrations (MIC 2-8 mug/ml) than commonly used antibiotics. The combination of active phenolics with kanamycin, oxacillin, and ciprofloxacin resulted in a decrease in the MIC of the antimicrobial agent. Kuwanon C, E, T, morusin, and Albafuran C showed synergy (FICi 0.375-0.5) with oxacillin and/or kanamycin. Prenylated phenolics disrupted membrane permeability statistically significantly (from 28 +/- 16.48% up to 73 +/- 2.83%), and membrane disruption contributes to the complex antibacterial activity against MRSA. In addition, kuwanon C could be considered an efflux pump inhibitor. Despite the antibacterial effect on MRSA and the multiple biological activities, the prenylated phenolics at microbially significant concentrations have a minor effect on human keratinocyte (HaCaT) viability. In conclusion, prenylated phenolics in combination with commonly used antibiotics are promising candidates for the treatment of MRSA infections and wound healing, although further studies are needed.

Antiproliferative activity of stilbene derivatives and other constituents from the stem bark of Morus nigra L.[Pubmed:30822142]

Nat Prod Res. 2020 Dec;34(24):3506-3513.

The antiproliferative activities of 2',3,4',5,5'-pentahydroxy-cis-stilbene 1, resveratrol 2, oxyresveratrol 3, norartocarpetin 4, kuwanon C 5, morusin 6, cudraflavone A7, kuwanon G 8, Albafuran C 9, mulberrofuran G 10, 3-acetyl-O-alpha-amyrin 11, 3-acetyl-O-beta-amyrin 12, ursolic acid-3-O-acetate 13 and uvaol 14, previously identified from the barks of Morus nigra L., were investigated against HepG2 and MCF-7 cell lines. In addition, a series of methylated stilbenes 15-19 were prepared using compounds 1-3 and their antiproliferative effects were similarly investigated. The structure of a new 2',3,4'-trimethoxy-5-hydroxy-trans-stilbene 19 was elucidated using spectroscopic techniques. It showed remarkable activity against MCF-7 cells with IC(50) 12.5 muM. However, kuwanon C (5) showed the highest antiproliferative activity with IC(50) 3.92 and 9.54 muM against MCF-7 and HepG2, respectively.

Fluorescence resonance energy transfer assay for high-throughput screening of ADAMTS1 inhibitors.[Pubmed:22186957]

Molecules. 2011 Dec 20;16(12):10709-21.

A disintegrin and metalloprotease with thrombospondin type I motifs-1 (ADAMTS1) plays a crucial role in inflammatory joint diseases and its inhibitors are potential candidates for anti-arthritis drugs. For the purposes of drug discovery, we reported the development and validation of fluorescence resonance energy transfer (FRET) assay for high-throughput screening (HTS) of the ADAMTS1 inhibitors. A FRET substrate was designed for a quantitative assay of ADAMTS1 activity and enzyme kinetics studies. The assay was developed into a 50-microL, 384-well assay format for high throughput screening of ADAMTS1 inhibitors with an overall Z' factor of 0.89. ADAMTS1 inhibitors were screened against a diverse library of 40,960 total compounds with the established HTS system. Four structurally related hits, naturally occurring compounds, kuwanon P, kuwanon X, Albafuran C and mulberrofuran J, extracted from the Chinese herb Morus alba L., were identified for further investigation. The results suggest that this FRET assay is an excellent tool, not only for measurement of ADAMTS1 activity but also for discovery of novel ADAMTS1 inhibitors with HTS.

Three new compounds from Morus nigra L.[Pubmed:20552479]

J Asian Nat Prod Res. 2010 Jun;12(6):431-7.

A new 2-arylbenzofuran derivative, mornigrol D (1), along with two new flavones, mornigrol G (2) and mornigrol H (3), and six known compounds, norartocarpetin (4), dihydrokaempferol (5), albanin A (6), albanin E (7), moracin M (8), and Albafuran C (9), were isolated from the barks of Morus nigra. Their structures were elucidated by spectroscopic analysis. Compounds 1 and 9 showed antioxidative activities in vitro with inhibition ratios of 98 and 99% at the concentration of 10(-4) mol/l, and of 74 and 75% at the concentration of 10(-5) mol/l. In addition, compounds 1 and 4 showed potent anti-inflammatory activities (inhibition of release of beta-glucuronidase from rat polymorphonuclear leucocytes induced by platelet activating factor) with inhibitory ratios of 65.9% (P < 0.01) and 67.7% (P < 0.01) at a concentration of 10(-5) mol/l.

Bioactive diels-alder type adducts from the stem bark of Morus macroura.[Pubmed:15368673]

Planta Med. 2004 Aug;70(8):758-63.

Five new compounds, named guangsangons A (1), B (5), C (6), D (7), and E (8), along with four known compounds, Albafuran C (2), kuwanon X (3), kuwanon P (4), and kuwanon Y (9) were isolated from Morus macroura Miq.. Their structures were determined by means of spectroscopic analyses and chemical methods. These compounds were regarded biogenetically as Diels-Al-der type adducts, and 1H-NMR variable temperature experience suggested that they all existed as an equilibrium mixture of conformational isomers in solution. Compounds 1-3 and 5-9 showed good anti-oxidation activity, with the inhibitory rate of malondialdehyde being from 90.1% to 102.7% at a concentration of 10(-4) mol/L and from 70.9% to 88.1% at a concentration of 10(-5) mol/L. Compounds 1, 5, and 7 showed anti-inflammation activity, with the inhibitory rates of release of lysosome enzyme from polymorphonuclear leukocytes of rats being 19.0% (P > 0.05), 57.3% (P < 0.001) and 24.3% (P < 0.05) at concentrations of 10(-5) mol/L, respectively.

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