scholarly journals Active constituents of Zanthoxylum nitidium from Yunnan Province against leukaemia cells in vitro

BMC Chemistry ◽  
2021 ◽  
Vol 15 (1) ◽  
Author(s):  
Ying Deng ◽  
Tongtong Ding ◽  
Lulu Deng ◽  
Xiaojiang Hao ◽  
Shuzhen Mu
Keyword(s):  
2D Nmr ◽  
Leukaemia Cell Line ◽  
Drug Candidates ◽  
Hel Cells ◽  
Inhibitory Activities ◽  
Induced Apoptosis ◽  
Aurantiamide Acetate ◽  
First Time ◽  
Potential Use

AbstractZanthoxylum nitidium (Roxb.) DC (Rutaceae) is well known for inhibiting the proliferation of human gastric, liver, kidney and lung cancer cells, though research on its potential use in treating leukaemia is relatively rare. Twenty-six compounds were isolated from the chloroform and petroleum ether extracts of the roots and leaves of Z. nitidium (Zanthoxylum nitidium). They were ( +)-9′-O-transferuloyl-5, 5′-dimethoxylaricriresinol (1), 8-(3′-oxobut-1′-en-1′-yl)-5, 7-dimethoxy-coumarin (2), 5, 7, 8-trimethoxy-coumarin (3), 5-(3′, 3′-dimethyl-2′-butenyloxy)-7, 8-dimethoxy-coumarin (4), 2-(5-methoxy-2-methyl-1H-indol-3-yl) methyl acetate (5), 2′-(5, 6-dihydrochleletrythrine-6-yl) ethyl acetate (6), 6-acetonyldi-hydrochelerythrine (7), 6β-hydroxymethyldihydronitidine (8), bocconoline (9), zanthoxyline (10), O-methylzanthoxyline (11), rhoifoline B (12), N-nornitidine (13), nitidine (14), chelerythrine (15), 4-hydroxyl-7,8-dimethoxy-furoquinoline (16), dictamnine (17), γ-fagarine (18), skimmianine (19), robustine (20), R-( +)-platydesmine (21), 4-methoxyl-1-methyl-2-quinoline (22), 4-methoxy-2-quinolone (23), liriodenine (24), aurantiamide acetate (25), 10-O-demethyl-12-O-methylarnottianamide (26). Four among them, compounds 4 – 6 and 16, were first confirmed in this study by UV, IR, 1D, 2D NMR and HR-ESI–MS spectra. Compounds 1 – 2 and 11 were isolated from Z. nitidium for the first time. Of the assayed compounds, 1, 2, 9, 10, 14, 15 and 24, exhibited good inhibitory activities in the leukaemia cell line HEL, whereas compound 14 (IC50: 3.59 µM) and compound 24 (IC50: 15.95 µM) exhibited potent inhibitory activities. So, to further investigate the possible mechanisms, cell cycle and apoptosis assays were performed, which indicated that compound 14 causes obvious S-phase arrest in HEL cells and induced apoptosis, whereas compound 24 only induced apoptosis. The present results suggested both compounds 14 and 24 are promising potential anti-leukaemia drug candidates.

scholarly journals Active constituents of Zanthoxylum nitidium from Yunnan Province against leukaemia cells in vitro

2020 ◽  
Author(s):  
Ying Deng ◽  
Tongtong Ding ◽  
Lulu Deng ◽  
Xiaojiang Hao ◽  
Shu Zhen Mu
Keyword(s):  
2D Nmr ◽  
Leukaemia Cell Line ◽  
Drug Candidates ◽  
Hel Cells ◽  
Inhibitory Activities ◽  
Induced Apoptosis ◽  
Aurantiamide Acetate ◽  
First Time ◽  
Potential Use

Abstract Zanthoxylum nitidium (Roxb.) DC (Rutaceae) is well known for inhibiting the proliferation of human gastric, liver, kidney and lung cancer cells, though research on its potential use in treating leukaemia is relatively rare. Twenty-six compounds were isolated from the chloroform and petroleum ether extracts of the roots and leaves of Z. nitidium. They were (+)-9′-O-transferuloyl-5, 5′-dimethoxylaricriresinol (1), 8-(3′-oxobut-1′-en-1′-yl)-5, 7-dimethoxy-coumarin (2), 5, 7, 8-trimethoxy-coumarin (3), 5-(3′, 3′-dimethyl-2′-butenyloxy)-7, 8-dimethoxy-coumarin (4), 2-(5-methoxy-2-methyl-1H-indol-3-yl) methyl acetate (5), 2′-(5, 6-dihydrochleletrythrine-6-yl) ethyl acetate (6), 6-acetonyldi-hydrochelerythrine (7), 6β-hydroxymethyldihydronitidine (8), bocconoline (9), zanthoxyline (10), O-methylzanthoxyline (11), rhoifoline B (12), N-nornitidine (13), nitidine (14), chelerythrine (15), 4-hydroxyl-7,8-dimethoxy-furoquinoline (16), dictamnine (17), γ-fagarine (18), skimmianine (19), robustine (20), R-(+)-platydesmine (21), 4-methoxyl-1-methyl-2-quinoline (22), 4-methoxy-2-quinolone (23), liriodenine (24), aurantiamide acetate (25), 10-O-demethyl-12-O-methylarnottianamide (26). Four among them, compounds 4-6 and 16, were first confirmed in this study by UV, IR, 1D, 2D NMR and HR-ESI-MS spectra. Compounds 1-2 and 11 were isolated from Z. nitidium for the first time. Of the assayed compounds, 1, 2, 9, 10, 14, 15 and 24, exhibited good inhibitory activities in the leukaemia cell line HEL, whereas compound 14 (IC50: 3.59 µM) and compound 24 (IC50: 15.95 µM) exhibited potent inhibitory activities. So, to further investigate the possible mechanisms, cell cycle and apoptosis assays were performed, which indicated that compound 14 causes obvious S-phase arrest in HEL cells and induced apoptosis, whereas compound 24 only induced apoptosis. The present results suggested both compounds 14 and 24 are promising potential anti-leukaemia drug candidates.

scholarly journals Active constituents of Zanthoxylum nitidum from Yunnan Province against leukemia cells in vitro

2021 ◽  
Author(s):  
Ying Deng ◽  
Tongtong Ding ◽  
Lulu Deng ◽  
Xiaojiang Hao ◽  
Shu Zhen Mu
Keyword(s):  
2D Nmr ◽  
Leukaemia Cell Line ◽  
Drug Candidates ◽  
Hel Cells ◽  
Inhibitory Activities ◽  
Induced Apoptosis ◽  
Aurantiamide Acetate ◽  
First Time ◽  
Potential Use

Abstract Zanthoxylum nitidium (Roxb.) DC (Rutaceae) is well known for inhibiting the proliferation of human gastric, liver, kidney and lung cancer cells, though research on its potential use in treating leukaemia is relatively rare. Twenty-six compounds were isolated from the chloroform and petroleum ether extracts of the roots and leaves of Z. nitidium (Zanthoxylum nitidium). They were (+)-9′-O-transferuloyl-5, 5′-dimethoxylaricriresinol (1), 8-(3′-oxobut-1′-en-1′-yl)-5, 7-dimethoxy-coumarin (2), 5, 7, 8-trimethoxy-coumarin (3), 5-(3′, 3′-dimethyl-2′-butenyloxy)-7, 8-dimethoxy-coumarin (4), 2-(5-methoxy-2-methyl-1H-indol-3-yl) methyl acetate (5), 2′-(5, 6-dihydrochleletrythrine-6-yl) ethyl acetate (6), 6-acetonyldi-hydrochelerythrine (7), 6β-hydroxymethyldihydronitidine (8), bocconoline (9), zanthoxyline (10), O-methylzanthoxyline (11), rhoifoline B (12), N-nornitidine (13), nitidine (14), chelerythrine (15), 4-hydroxyl-7,8-dimethoxy-furoquinoline (16), dictamnine (17), γ-fagarine (18), skimmianine (19), robustine (20), R-(+)-platydesmine (21), 4-methoxyl-1-methyl-2-quinoline (22), 4-methoxy-2-quinolone (23), liriodenine (24), aurantiamide acetate (25), 10-O-demethyl-12-O-methylarnottianamide (26). Four among them, compounds 4-6 and 16, were first confirmed in this study by UV, IR, 1D, 2D NMR and HR-ESI-MS spectra. Compounds 1-2 and 11 were isolated from Z. nitidium for the first time. Of the assayed compounds, 1, 2, 9, 10, 14, 15 and 24, exhibited good inhibitory activities in the leukaemia cell line HEL, whereas compound 14 (IC50: 3.59 µM) and compound 24 (IC50: 15.95 µM) exhibited potent inhibitory activities. So, to further investigate the possible mechanisms, cell cycle and apoptosis assays were performed, which indicated that compound 14 causes obvious S-phase arrest in HEL cells and induced apoptosis, whereas compound 24 only induced apoptosis. The present results suggested both compounds 14 and 24 are promising potential anti-leukaemia drug candidates.

scholarly journals Active constituents of Zanthoxylum nitidum from Yunnan Province against leukemia

2020 ◽  
Author(s):  
Ying Deng ◽  
Tongtong Ding ◽  
Lulu Deng ◽  
Xiaojiang Hao ◽  
Shu Zhen Mu
Keyword(s):  
2D Nmr ◽  
Leukaemia Cell Line ◽  
Drug Candidates ◽  
Hel Cells ◽  
Zanthoxylum Nitidum ◽  
Inhibitory Activities ◽  
Induced Apoptosis ◽  
Aurantiamide Acetate ◽  
First Time ◽  
Potential Use

Abstract Zanthoxylum nitidium (Roxb.) DC (Rutaceae) is well known for inhibiting the proliferation of human gastric, liver, kidney and lung cancer cells, though research on its potential use in treating leukaemia is relatively rare. Twenty-six compounds were isolated from the chloroform and petroleum ether extracts of the roots and leaves of Z. nitidium. They were (+)-9′-O-transferuloyl-5, 5′-dimethoxylaricriresinol (1), 8-(3′-oxobut-1′-en-1′-yl)-5, 7-trimethoxy-coumarin (2), 5, 7, 8-trimethoxy-coumarin (3), 5-(3′, 3′-dimethyl-2′-butenyloxy)-7, 8-dimethoxy-coumarin (4), 2-(5-methoxy-2-methyl-1H-indol-3-yl) methyl acetate (5), 2′-(5,6-dihydrochleletrythrine-6-yl) ethyl acetate (6), 6-acetonyldi-hydrochelerythrine (7), 6β-hydroxymethyldihydronitidine (8), bocconoline (9), zanthoxyline (10), O-methylzanthoxyline (11), rhoifoline B (12), N-nornitidine (13), nitidine (14), chelerythrine (15), 4-hydroxyl-7,8-dimethoxy-furoquinoline (16), dictamnine (17), γ-fagarine (18), skimmianine (19), robustine (20), R-(+)-platydesmine (21), 4-O-methyl-1-methyl-quinoline-2-one (22), 4-methoxy-2-quinolone (23), liriodenine (24), aurantiamide acetate (25), 10-O-demethyl-12-O-methylarnottianamide (26). Four among them, compounds 4-6 and 16, were first confirmed in this study by UV, IR, 1D, 2D NMR and HR-ESI-MS spectra. Compounds 1-2 and 11 were isolated from Z. nitidium for the first time. Of the assayed compounds, 1, 2, 9, 10, 14, 15 and 24, exhibited good inhibitory activities in the leukaemia cell line HEL, whereas compound 14 (IC50: 3.59 µM) and compound 24 (IC50: 15.95 µM) exhibited potent inhibitory activities. So, to further investigate the possible mechanisms, cell cycle and apoptosis assays were performed, which indicated that compound 14 causes obvious S-phase arrest in HEL cells and induced apoptosis, whereas compound 24 only induced apoptosis. The present results suggested both compounds 14 and 24 are promising potential anti-leukaemia drug candidates.

scholarly journals Active constituents of Zanthoxylum nitidum from Yunnan Province against leukemia

2020 ◽  
Author(s):  
Ying Deng ◽  
Tongtong Ding ◽  
Lulu Deng ◽  
Xiaojiang Hao ◽  
Shu Zhen Mu
Keyword(s):  
Yunnan Province ◽  
2D Nmr ◽  
Leukaemia Cell Line ◽  
Drug Candidates ◽  
Hel Cells ◽  
Zanthoxylum Nitidum ◽  
Inhibitory Activities ◽  
Induced Apoptosis ◽  
First Time ◽  
Potential Use

Abstract Zanthoxylum nitidium (Roxb.) DC (Rutaceae) is well known for inhibiting the proliferation of human gastric, liver, kidney and lung cancer cells, though research on its potential use in treating leukaemia is relatively rare. Twenty-six compounds were isolated from the chloroform and petroleum ether extracts of the roots and leaves of Z. nitidium . Four among them, compounds 4-6 and 16 , were first confirmed in this study by UV, IR, 1D, 2D NMR and HR-ESI-MS spectra. Compounds 1-2 and 11 were isolated from Z. nitidium for the first time. Of the assayed compounds, 1 , 2 , 9 , 10 , 14 , 15 and 24, exhibited good inhibitory activities in the leukaemia cell line HEL, whereas compound 14 (IC 50 : 3.59 µM) and compound 24 (IC 50 : 15.95 µM) exhibited potent inhibitory activities. So, to further investigate the possible mechanisms, cell cycle and apoptosis assays were performed, which indicated that compound 14 causes obvious S-phase arrest in HEL cells and induced apoptosis, whereas compound 24 only induced apoptosis. The present results suggested both compounds 14 and 24 are promising potential anti-leukaemia drug candidates.

scholarly journals Active constituents of Zanthoxylum nitidum from Yunnan Province against leukemia

2020 ◽  
Author(s):  
Ying Deng ◽  
Tongtong Ding ◽  
Lulu Deng ◽  
Xiaojiang Hao ◽  
Shu Zhen Mu
Keyword(s):  
Cell Apoptosis ◽  
Yunnan Province ◽  
2D Nmr ◽  
Phase Arrest ◽  
Hel Cells ◽  
Ic50 Values ◽  
Uv Visible ◽  
Zanthoxylum Nitidum ◽  
First Time ◽  
Potential Use

Abstract Zanthoxylum nitidium (Roxb.) DC (Rutaceae) is well known for inhibiting the proliferation of human gastric, liver, kidney and lung cancer cells, whereas research on its potential use in treating leukaemia is relatively rare. 26 compounds were isolated from the chloroform and petroleum ether extracts of the roots and leaves of Z. nitidium. The structures of four compounds (4-6 and 16) were confirmed and attributed firstly by UV-visible spectroscopy, 1D and 2D NMR and HR-ESI-MS. Compounds 1-2 and11 were isolated from Z. nitidium for the first time. Of the assayed compounds, compounds 14 and24 showed inhibitory activities against leukaemia HEL cells with IC50 values of 3.59 and 15.95 µM. In addition, to further investigate the possible mechanism, the cell cycle and apoptosis assays were investigated, which indicated that compound14 caused obvious S phase arrest in HEL cells and induced cell apoptosis, but compound 24 induced only cell apoptosis of HEL cells. These results suggested that compounds 14 and 24 were the potential candidates for anti-leukaemia drug for the first time.

scholarly journals Two New 11(15→1)Abeotaxanes with a 2,20-Epoxy Ring from the Needles of Taxus canadensis

2009 ◽  
Vol 64 (1-2) ◽  
pp. 43-48 ◽  
Author(s):  
Man-Li Zhang ◽  
Jing Zhang ◽  
Mei Dong ◽  
Shu-Hua Feng ◽  
Chang-Hong Huo ◽  
...  
Keyword(s):  
High Resolution ◽  
2D Nmr ◽  
Epoxy Ring ◽  
Taxus Canadensis ◽  
Growth Inhibitory ◽  
Weak Growth ◽  
Inhibitory Activities ◽  
First Time

1Two 11(15→1)abeotaxanes having a tetrahydrofuran ring along the carbon atoms C-2, C-3, C-4, C-20 were identified for the first time from the needles of the Canadian yew, Taxus canadensis. The compounds could be identified as 4α,10β,13α-triacetoxy-15-benzoyloxy-2α,20β- epoxy-11(15→1)abeotax-11-ene-5α,7β,9α-triol () and 4α,7β,9α,10β,15-pentaacetoxy-2α,20β- epoxy-11(15→1)abeotax-11-ene-5α,13α-diol (2) on the basis of 1D-, 2D-NMR evidence and high-resolution FABMS analysis. Compound 1 showed weak growth inhibitory activities against T-98 and MM1-CB cells in vitro.

scholarly journals Active constituents of Zanthoxylum nitidum from Yunnan Province against leukemia

2020 ◽  
Author(s):  
Ying Deng ◽  
Tongtong Ding ◽  
Lulu Deng ◽  
Xiaojiang Hao ◽  
Shu Zhen Mu
Keyword(s):  
Cell Apoptosis ◽  
Yunnan Province ◽  
2D Nmr ◽  
S Phase ◽  
Phase Arrest ◽  
Hel Cells ◽  
Uv Visible ◽  
Zanthoxylum Nitidum ◽  
First Time ◽  
Potential Use

Abstract Zanthoxylum nitidium (Roxb.) DC (Rutaceae) is well known for inhibiting the proliferation of human gastric, liver, kidney and lung cancer cells, whereas research on its potential use in treatments of leukaemia targeting Fli-1 gene is relatively rare. 26 compounds were isolated from the chloroform and petroleum ether extracts of the roots and leaves of Z. nitidium . The structures of four compounds ( 4-6 and 16 ) were confirmed and attributed for the first time by UV-visible spectroscopy, 1D and 2D NMR and HR-ESI-MS. Compounds 1-2 and 11 were isolated from Z. nitidium for the first time. Of the assayed compounds, compounds 14 and 24 showed inhibitory activities against leukaemia HEL cells with IC 50 values of 3.59 and 15.95 µM. In addition, to further investigate the possible mechanism, the cell cycle and apoptosis assays were investigated for the first time, which indicated that compound 14 caused obvious S phase arrest in HEL cells and induced cell apoptosis, but compound 24 induced only cell apoptosis of HEL cells. These results suggested that compounds 14 and 24 were the potential candidates for anti-leukaemia drug for the first time.

Rhipicephalus turanicus, a new vector of Hepatozoon canis

Parasitology ◽  
2016 ◽  
Vol 144 (6) ◽  
pp. 730-737 ◽  
Author(s):  
ALESSIO GIANNELLI ◽  
RICCARDO PAOLO LIA ◽  
GIADA ANNOSCIA ◽  
CANIO BUONAVOGLIA ◽  
ELEONORA LORUSSO ◽  
...  
Keyword(s):  
Southern Italy ◽  
Rhipicephalus Sanguineus ◽  
Hepatozoon Canis ◽  
Time Data ◽  
Tick Vector ◽  
First Time ◽  
Potential Use ◽  
Potential Tool

SUMMARYThe distribution of Hepatozoon canis mainly encompasses areas where its main tick vector, Rhipicephalus sanguineus sensu lato, is present. However, the detection of this pathogen in dogs, foxes and golden jackals well outside the areas inhabited by this tick species reinforced the hypothesis that additional ixodids are involved in the life cycle and transmission of this protozoon. The present study provides, for the first time, data supporting the sporogonic development of H. canis in specimens of Rhipicephalus turanicus collected from a naturally infected fox from southern Italy. The epidemiological role of R. turanicus as a vector of H. canis is discussed, along with information on the potential use of cell cultures for the experimental infection with H. canis sporozoites. The in vitro infection of canine leucocytes by sporozoites from ticks is proposed as a potential tool for future in-depth studies on the biology of H. canis.

scholarly journals Identification of a Proanthocyanidin from Litchi Chinensis Sonn. Root with Anti-Tyrosinase and Antioxidant Activity

Biomolecules ◽  
2020 ◽  
Vol 10 (9) ◽  
pp. 1347
Author(s):  
Matthew Saive ◽  
Manon Genva ◽  
Thibaut Istasse ◽  
Michel Frederich ◽  
Chloé Maes ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Biological Activities ◽  
Chemical Characterization ◽  
2D Nmr ◽  
Ethnobotanical Study ◽  
Traditional Use ◽  
Litchi Chinensis ◽  
Isolated Compound ◽  
First Time

This work follows an ethnobotanical study that took place in the island of Mayotte (France), which pointed out the potential properties of Litchi chinensis Sonn. roots when used to enhance skin health and appearance. Through in vitro testing of a crude methanolic extract, high anti-tyrosinase (skin whitening effect) and antioxidant activities (skin soothing effect) could be measured. HPLC successive bio-guided fractionation steps allowed the purification of one of the compounds responsible for the biological activities. The isolated compound was characterized by UV, IR, MS and 2D-NMR, revealing, for the first time in Litchi chinensis Sonn. roots, an A-type proanthocyanidin and thus revealing a consensus among the traditional use shown by the ethnobotanical study, in vitro biological activities and chemical characterization.

Drug Discovery by Drug Repurposing: Combating COVID-19 in the 21st Century

2020 ◽  
Vol 20 ◽  
Author(s):  
Nitesh Sanghai ◽  
Kashfia Shafiq ◽  
Geoffrey K. Tranmer
Keyword(s):  
Drug Discovery ◽  
Drug Repurposing ◽  
Compassionate Use ◽  
Drug Candidates ◽  
Working Day ◽  
Novel Coronavirus ◽  
Approved Drugs ◽  
Day By Day ◽  
Potential Use

: Due to the rapidly developing nature of the current COVID-19 outbreak and its almost immediate humanitarian and economic toll, coronavirus drug discovery efforts have largely focused on generating potential COVID-19 drug candidates as quickly as possible. Globally, scientists are working day and night to find the best possible solution to treat the deadly virus. During the first few months of 2020, the SARS-CoV-2 outbreak quickly developed into a pandemic, with a mortality rate that was increasing at an exponential rate day by day. As a result, scientists have turned to a drug repurposing approach, to rediscover the potential use and benefits of existing approved drugs. Currently, there is no single drug approved by the U.S. Food and Drug Administration (FDA), for the treatment of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2, previously known as 2019-nCoV) that causes COVID-19. Based on only in-vitro studies, several active drugs are already in the clinical pipeline, made possible by following the compassionate use of medicine protocols. This method of repurposing and the use of existing molecules like Remdesivir (GS-5734), Chloroquine, Hydroxychloroquine, etc. has proven to be a landmark in the field of drug rediscovery. In this review article we will discuss the repurposing of medicines for treating the deadly novel coronavirus (SARS-CoV-2).

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