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1.
Nat Prod Res ; : 1-13, 2023 Dec 25.
Article in English | MEDLINE | ID: mdl-38146230

ABSTRACT

A new benzophenanthridine alkaloid 6-butanoyldihydrochelerythrine (1) and five known alkaloids 6-acetonyldihydronitidine (2), 6-acetonyldihydrochelerythrine (3), isocorydine (4), (O)-methyltembamide (5), N-(4-methoxyphenethyl)benzamide (6) were isolated from the stem barks of Zanthoxylum rhetsa. These structures were elucidated by 1D, 2D NMR spectroscopy and by mass spectrometry. This is the first time that compounds 2-6 were identified from Zanthoxylum rhetsa and the first time that compounds 4 and 6 were identified from the genus Zanthoxylum. Bioactivity results of isolated compounds showed that 1, 2, 5 and 6 exhibited inhibitory activity against MCF7 and A549 cell lines, while 3 showed the inhibitory activity against A549 cell line; all isolated compounds 1-6 inhibited at least two strain microorganisms; compound 4 showed angiotensin II converting enzyme inhibitory activity in vitro with IC50 value of 65.58 µM and in silico with a docking score of -11.52 kcal/mol.

2.
Z Naturforsch C J Biosci ; 77(5-6): 207-218, 2022 May 25.
Article in English | MEDLINE | ID: mdl-34761648

ABSTRACT

Phytochemical investigation applying GC (gas chromatography)-MS (mass spectrometry)/GC-FID (flame ionization detection) on the hydro-distilled essential oils of the Vietnamese medicinal plant Uvaria boniana leaf and twig lead to the detection of 35 constituents (97.36%) in the leaf oil and 52 constituents (98.75%) in the twig oil. Monoterpenes, monoterpenoids, sesquiterpenes, and sesquiterpenoids were characteristic of U. boniana essential oils. The leaf oil was represented by major components (E)-caryophyllene (16.90%), bicyclogermacrene (15.95%), α-humulene (14.96%), and linalool (12.40%), whereas four compounds α-cadinol (16.16%), epi-α-muurolol (10.19%), α-pinene (11.01%), and ß-pinene (8.08%) were the main ones in the twig oil. As compared with the leaf oil, the twig oil was better in antimicrobial activity. With the same MIC value of 40 mg/mL, the twig oil successfully controlled the growth of Gram (+) bacterium Bacillus subtilis, Gram (-) bacterium Escherichia coli, fungus Aspergillus niger, and yeast Saccharomyces cerevisiae. In addition, both two oil samples have induced antiinflammatory activity with the IC50 values of 223.7-240.6 mg/mL in NO productive inhibition when BV2 cells had been stimulated by LPS. Docking simulations of four major compounds of U. boniana twig oil on eight relevant antibacterial targets revealed that epi-α-muurolol and α-cadinol are moderate inhibitors of E. coli DNA gyrase subunit B, penicillin binding protein 2X and penicillin binding protein 3 of Pseudomonas aeruginosa with similar free binding energies of -30.1, -29.3, and -29.3 kJ/mol, respectively. Furthermore, in silico ADMET studies indicated that all four docked compounds have acceptable oral absorption, low metabolism, and appropriated toxicological profile to be considered further as drug candidates.


Subject(s)
Oils, Volatile , Sesquiterpenes , Uvaria , Escherichia coli , Gas Chromatography-Mass Spectrometry , Oils, Volatile/chemistry , Plant Leaves/chemistry , Plant Oils/analysis , Sesquiterpenes/analysis , Sesquiterpenes/pharmacology
3.
J Nat Med ; 75(1): 186-193, 2021 Jan.
Article in English | MEDLINE | ID: mdl-32926336

ABSTRACT

As part of an ongoing search for new protein tyrosine phosphatase 1B inhibitors and glucose uptake stimulators from nature, a new coumarin, selaginolide A (1) and four known isoflavones (2‒5) were isolated from the ethanol extract of a Vietnamese medicinal plant Selaginella rolandi-principis. The chemical structures of the isolates were elucidated by extensive analysis of spectroscopic and physicochemical data. Compounds 3‒5 have been identified from Selaginella genus for the first time. The antidiabetic properties of the isolates (1‒5) were investigated using in vitro assay on 2-NBDG uptake in 3T3-L1 adipocytes and against PTP1B and α-glucosidase enzyme activities as well. Compounds 1 exhibited the most potency with inhibitory IC50 values of 7.40 ± 0.28 and 7.52 ± 0.37 µM against PTP1B and α-glucosidase, respectively. Compounds 3 and 5 possessed potential inhibitions on PTP1B enzyme with IC50 values of 23.02 ± 1.29 and 11.08 ± 0.92 µM and moderate inhibitions on α-glucosidase with IC50 values of 36.47 ± 1.87 and 55.73 ± 2.58 µM, respectively. Compounds 2 and 4 showed weak PTP1B inhibitory activity (IC50 > 30 µM) but displayed remarkable α-glucosidase inhibition with IC50 values of 3.39 ± 0.87 and 9.72 ± 0.62 µM, respectively. Furthermore, ursolic acid as a positive control (IC50 3.42 ± 0.26 µM) and compounds 1 and 5 acted as mixed-competitive inhibitors against PTP1B enzyme with Ki values of 6.46, 10.28, and 15.01 µM, respectively. In addition, compounds 1 and 5 also showed potent stimulatory effects on 2-NBDG uptake at a concentration of 10 µM. The obtained result might suggest the potential of new coumarin (1) as a new type of natural PTP1B and α-glucosidase inhibitor for further research and development of antidiabetic and obese agents.Graphic abstract.


Subject(s)
Diabetes Mellitus/drug therapy , Enzyme Inhibitors/chemistry , Glucose/chemistry , Glycoside Hydrolase Inhibitors/chemistry , Plants, Medicinal/chemistry , Protein Tyrosine Phosphatase, Non-Receptor Type 1/antagonists & inhibitors , Selaginellaceae/chemistry , Adult , Aged , Animals , Humans , Mice , Middle Aged , Molecular Structure , Young Adult
4.
Microbiol Res ; 159(1): 19-28, 2004.
Article in English | MEDLINE | ID: mdl-15160603

ABSTRACT

DNA transfer between pro- and eukaryotes occurs either during natural horizontal gene transfer or as a result of the employment of gene technology. We analysed the capacity of DNA sequences from a eukaryotic donor organism (Saccharomyces cerevisiae) to serve as promoter region in a prokaryotic recipient (Escherichia coli) by creating fusions between promoterless luxAB genes from Vibrio harveyi and random DNA sequences from S. cerevisiae and measuring the luminescence of transformed E. coli. Fifty-four out of 100 randomly analysed S. cerevisiae DNA sequences caused considerable gene expression in E. coli. Determination of transcription start sites within six selected yeast sequences in E. coli confirmed the existence of bacterial -10 and -35 consensus sequences at appropriate distances upstream from transcription initiation sites. Our results demonstrate that the probability of transcription of transferred eukaryotic DNA in bacteria is extremely high and does not require the insertion of the transferred DNA behind a promoter of the recipient genome.


Subject(s)
DNA, Fungal/genetics , Escherichia coli/genetics , Gene Expression , Promoter Regions, Genetic , Transcription, Genetic , Artificial Gene Fusion , Bacterial Proteins/genetics , Bacterial Proteins/physiology , Base Sequence , DNA, Fungal/isolation & purification , Genes, Bacterial , Genes, Reporter , Luciferases/genetics , Luciferases/metabolism , Luminescent Measurements , Molecular Sequence Data , Saccharomyces cerevisiae/genetics , Transcription Initiation Site , Transformation, Bacterial
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