• Natural Product Sciences
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• v.23 no.4
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• pp.247-252
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• 2017

The methylglyoxal (MGO) trapping constituents from onion (Allium cepa L.) peels were investigated using pre-column incubation of MGO and crude extract followed by HPLC analysis. The peak areas of MGO trapping compounds decreased, and their chemical structures were identified by HPLC-ESI/MS. Among major constituents in outer scale of onion, 2-(3,4-dihydroxybenzoyl)-2,4,6-trihydroxy-3(2H)-benzofuranone (2) was more effective MGO scavenger than quercetin (6) and its 4'-glucoside, spiraeoside (3). After 1 h incubation, compound 2 trapped over 90% MGO at a concentration of 0.5 mM under physiological conditions, but compounds 3 and 6 scavenged 45%, 16% MGO, respectively. HPLC-ESI/MS showed that compound 2 trapped two molecules of MGO to form a di-MGO adduct and compounds 3 and 6 captured one molecule of MGO to form mono-MGO adducts, and the positions 6 and 8 of the A ring of flavonoids were major active sites for trapping MGO.

• Archives of Pharmacal Research
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• v.29 no.11
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• pp.1006-1017
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• 2006

A series of 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-one, 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-thione and 2, 2'-dithiobis 3-(substituted-benylidene)-1, 3-dihydro-indole derivatives was investigated as inhibitor of $p60^{c-Src}$tyrosine kinase by performing receptor docking studies and inhibitory activity toward tyrosine phosphorylation. Some compounds were shown to be docked at the site, where the selective inhibitor PP1 [1-tert-Butyl-3-p-tolyl-1H-pyrazolo[3,4-d]pyrimidine-4-yl-amine] was embedded at the enzyme active site. Evaluation of all compounds for the interactions with the parameters of lowest binding energy levels, capability of hydrogen bond formations and superimposibility on enzyme active site by docking studies, it can be assumed that 3-(substituted-benzylidene)-1, 3-dihydro-indolin-2-one and thione derivatives have better interaction with enzyme active site then 2, 2'-dithiobis 3-(substituted-benzylidene)-1, 3-dihydro indole derivatives. The test results for the inhibitory activity against tyrosine kinase by Elisa method revealed that 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-thione derivatives have more activity then 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-one derivatives.

• The Korea Journal of Herbology
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• v.22 no.2
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• pp.97-102
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• 2007

Objectives : This study presents a high performance liquid chromatography - electrospray ionization-mass spectrometer (HPLC-MS/MS) methods for the quantitative and qualitative analysis of various active components in Samul-tang, which is composed of four crude herbs. Methods : HPLC-ESI-MS/MS for the determinations of paeoniflorin and 5-HMF (5-hydroxymethyl 2-furaldehyde) in the Samul-tang, the separation method was performed on an COSMOS1L 5C18-AR-Il (2.0 X 150 mm I.D.) column by gradient elution with 0.1% acetic acid and 5% CH3CN in water (A)-0.1% acetic acid and 5% H20 in CH3CN (B) as the mobile phase at a flow-rate of 300 ${\mu}L/min$ with detection at quadrupole mass spectrometer. The all marker substances were always detected as the base peaks in the positive ion mode. Results : The paeoniflorin of Paeoniae Radix in Samul-tang showed a strong base peak [M+H2O]+ in the positive detection mode to give the following as; paeoniflorin (498.109 [M+H2O]+, 479.8 [M]+, 301 [M-glucose]+, 179.3 [glucose]+). Based on the HPLC retnetion time and MS of standard compounds confirmed the identity of active compounds in Rehmanniae Radix Preparata as follows; 5-HMF (127.0[M+H]+, 109.3 [M-OH]+) in the positive ion mode. Conclusion : According to the above results, HPLC-ESI-MS method permits assignment of tentative structures such as paeoniflorin and 5-HMF in the Samul-tang.

• YAKHAK HOEJI
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• v.58 no.5
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• pp.314-321
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• 2014

Cibotii Rhizoma, the dried rhizome of Cibotium barometz J. Smith (C. barometz), has long been used to treat bone or nervous system disorders. In this regard, we isolated three main phenolic compounds, onitin-4-O-${\beta}$-D-glucopyranoside (1), irisdichototins E & F epimeric mixture (2), and protocatechuic acid (3) from C. barometz methanol extract. In addition, we screened their antioxidative activities by DPPH, ABTS radical, and superoxide scavenging assays. Among these three compounds, irisdichototins E & F and protocatechuic acid showed strong antioxidant activities. Also, the antioxidant activities of the C. barometz extracts were proportional to the contents of irisdichototins E & F and protocatechuic acid, thus these two phenolic compounds could be main active compounds of C. barometz. In addition, onitin-4-O-${\beta}$-D-glucopyranoside is considered as a marker compound of C. barometz because this compound is specifically contained in C. barometz which belongs to Pteridophyta order. A rapid analysis method for the simultaneous determination of phenolic compounds was also developed by UPLC (Ultra Performance Liquid Chromatography). Using the developed method, the two active compounds (irisdichototins E & F and protocatechuic acid) and a marker compound (onitin-4-O-${\beta}$-D-glucopyranoside) were successfully quantified in 14 commercial samples that were collected from different regions.

• YAKHAK HOEJI
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• v.14 no.1_2
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• pp.1-14
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• 1970

Seventeen N,N/sup I/-disubstituted thiourea derivatives were synthesized by the Hugershof reaction and reported. Antitumor activities of the synthesized compounds against ascitic Ehrlich Carcinoma and ascitic sarcoma 180 were reported. It was found that 1,1/sup I/-(p-Phenylene)-3,3/sup I/-bis (2-carboxyphenyl)-2,2/sup I/-dithiourea was considerably active against ascitic Ehrlich Carcinoma and Sarcoma 180 respectively. 1-(2-Carboxyphenyl)-3-(p-ethoxyphenyl)-2 thiourea was active against ascitic Sarcoma 180. 1-Salicyloyl-3-(p-ethoxyphenyl)-2-thiourea and 1,1/sup I/-(p-Phenylene)-3,3/sup I/-bis(2-hydroxyethyl)-2,2/sup I/-dithiourea were active against ascitic Ehrlich Carcinoma. Antitubercular activities of the synthesized compounds against Mycobacterium tuberculosis H/sub 37/ R/sub v/ were also reported. It was found that 1-Isonicotinyl-4-cyclohexyl-3-thiosemicarbazide was considerably active at 100 .mu.g/ml. 1,1/sup I/-(p-Phenylene)-3,3/sup I/-bis(2-hydroxyethyl)-2,2/sup I/-dithiourea and 1-Salicyloyl-3-(p-ethoxyphenyl)-2-thiourea were active at 1000 .mu.g/ml respectively. Antibacterial activities of nine compounds of the synthesized compounds against S. aureus and E. Coli were reported. It was found that 1,1-(p-Phenylene)-4,4/sup I/-bis(isonicotinyl)-2,2/sup I/-dithiosemicarbazide and 1-Isonicotinyl-4-cyclohexyl-3-thiosemicarbazide were considerably active against S. aureus and E. Coli respectively. 1-(6-Methyl-2-benzothiazolyl)-3-(1-naphthyl)-2-thiourea was active against S. aureus. 1,1/sup I/-(p-Phenylene)-3,3/sup I/-bis (2-hydroxyethyl)-2,2/sup I/-dithiourea was active against E. Coli.

• Microbiology and Biotechnology Letters
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• v.51 no.4
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• pp.333-352
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• 2023

Transaminase represents the most important biocatalysts used for the synthesis of chiral amines due to their stereoselectivity. They allow asymmetric synthesis with high yields and enantioselectivity from their corresponding ketones. Due to their environmentally friendly access for the preparation of chiral amines, they have attracted growing attention in recent times. Thus, the production of chiral compounds by transaminase catalysed reactions is considered as an important application in synthetic organic chemistry. Therefore, transaminase is considered to be an important enzyme in the pharmaceutical and chemical industries. ω-Transaminase holds great potential because of its wide substrate specificity thus making it a suitable enzyme to be used at an industrial scale. This review highlights the reaction mechanism, classification, substrate specificity, and biochemical properties. The review also showcases the application of ω-transaminase in organic chemistry with a focus on the production of active pharmaceutical ingredients (APIs).

• CELLMED
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• v.2 no.3
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• pp.22.1-22.9
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• 2012

The aim of this study is to collate all available data on experiments reporting the antiproliferative, cytotoxic effects of plants and natural products in Morocco in the last two decades. A bibliographic investigation was carried out by analyzing recognized books and peer-reviewed papers, consulting worldwide accepted scientific databases (Scirus, Embase, HighWire, MEDLINE/PubMed, LILACS, Ovid, ScienceDirect, SciELO, Google Scholar). We used medical subject heading terms and the words 'anticancer', 'antiproliferative', 'antineoplastic', 'antitumoral', 'cytotoxic', 'Morocco', to identify relevant articles. Moroccan plants with attributed anti-cancer properties studied as plant extracts that have been evaluated for cytotoxic effects, antitumoral effects, plants with active compounds tested on cancer cell lines, and plants with active compounds that have been assayed on animal models were chosen for this research. In the present study, interest is focused on experimental research conducted on medicinal plants, particularly those which show antiproliferative or cytotoxic activities alongside bioactive components. A total of 20 plant species belonging to 12 families have been identified as active or promising sources of phytochemicals with antiproliferative properties. The plant families, which cover all the species studied in this field, are Lamiaceae (7 species) and Asteraceae (4 species); the most studied species being Argania spinosa (Sapotaceae) and Arisarum vulgare (Araceae), Thymus Genus (Labiateae) and Peganum harmala (Zygophyllaceae). Based on the search results, it is recommended to increase the number of experimental studies and to begin conducting clinical trials with Moroccan plants and their active compounds selected by in vitro and in vivo activities.

• Archives of Pharmacal Research
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• v.13 no.4
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• pp.314-318
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• 1990

2-Bromo (2'-benzofury)gloxal-2-aryhydrazones I reacted with nucleophiles displacing the bromide. Treatment of I with active methylene compounds yield the pyrazole derivatives VIII-XI. Compounds XII-XIV reacted with hydrazine to give pyrazolo (3, 4-dipyridazine derivative XIV-XIV. The structures of the products were assigned and confirmed on the basis of their elemental analysis and spectral data.

• YAKHAK HOEJI
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• v.45 no.1
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• pp.16-22
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• 2001

Novel yakuchinone derivatives have been designed, synthesized and evaluated their inhibitory activity of NO production in lipopolysaccharide (LPS)-activated macrophages. From this study, some enone compounds have been found to be highly active in the assay. In view of the importance of NO in septic shock and inflammation, these compounds may be useful candidates for the development of new drug to treat endotoxemia and inflammation accompanying overproduction of NO.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.176.1-176.1
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• 2003

Bradykinin is an autocoid related to acute and chronic pain and inflammation. The non-peptide bradykinin antagonists are of interest as novel anti-inflammatory therapeutics. To understand the structural basis for the bradykinin antagonistic activity and to guide the design of more potent compounds we analysed the three dimensional pharmacophore model. Seven active compounds very recently reported such as FR 167344, FR 173657, LF 160687, and bradyzide were used as our pharmacophore model analysis. (omitted)