A Cytotoxic Natural Product from Patrinia villosa Juss

2019 ◽  
Vol 19 (11) ◽  
pp. 1399-1404 ◽  
Author(s):  
Yangcheng Liu ◽  
Wei Liu ◽  
Changlan Chen ◽  
Zheng Xiang ◽  
Hongwei Liu
Keyword(s):  
Cell Cycle ◽  
Cell Lines ◽  
Silica Gel ◽  
Column Chromatography ◽  
Bioactive Compound ◽  
Antitumor Agent ◽  
2D Nmr ◽  
Preparative Hplc ◽  
Dependent Manner ◽  
2D Nmr Spectra

Background and Purpose:: Patrinia villosa Juss is an important Chinese herbal medicine widely used for thousands of years, but few reports on the ingredients of the herb have been presented. In this study, we aim to isolate the bioactive compound from the plant. Material and Methods:: The air-dried leaves of P. villosa (15kg) were extracted three times with 70% EtOH under reflux. The condensed extract was suspended in H2O and partitioned with light petroleum, dichloromethane and n-BuOH. The dichloromethane portion was then subjected to normal-phase silica gel column chromatography, ODS silica gel column chromatography and semi-preparative HPLC to yield compound 1. Cytotoxicities of 1 were assayed on HepG2, A549 and A2780 cell lines. The mechanism of apoptosis and cell cycle on A549 was confirmed subsequently. Results: A new impecylone (Impecylone A) was isolated from the leaves of Patrinia villosa Juss, and its structures were established using 1D, 2D-NMR spectra and HR-ESI-MS. Impecylone A could selectivity inhibit HepG2 and A549 cell lines. The compound could induce apoptosis of A549 and arrest the cell cycle at G2/M phase in a dose-dependent manner. Conclusion: Impecylone A is a novel compound from Patrinia villosa Juss and could be a potential antitumor agent especially in the cell lines of A549.

scholarly journals Improved synthesis of SV2A targeting radiotracer [11C]UCB-J

2019 ◽  
Vol 4 (1) ◽  
Author(s):  
Johanna Rokka ◽  
Eva Schlein ◽  
Jonas Eriksson
Keyword(s):  
Methyl Iodide ◽  
Water Solution ◽  
Synthesis Method ◽  
Radiochemical Yield ◽  
Preparative Hplc ◽  
Step Method ◽  
Synaptic Density ◽  
Excellent Starting Point ◽  
Starting Point

Abstract Introduction [11C]UCB-J is a tracer developed for PET (positron emission tomography) that has high affinity towards synaptic vesicle glycoprotein 2A (SV2A), a protein believed to participate in the regulation of neurotransmitter release in neurons and endocrine cells. The localisation of SV2A in the synaptic terminals makes it a viable target for in vivo imaging of synaptic density in the brain. Several SV2A targeting compounds have been evaluated as PET tracers, including [11C]UCB-J, with the aim to facilitate studies of synaptic density in neurological diseases. The original two-step synthesis method failed in our hands to produce sufficient amounts of [11C]UCB-J, but served as an excellent starting point for further optimizations towards a high yielding and simplified one-step method. [11C]Methyl iodide was trapped in a clear THF-water solution containing the trifluoroborate substituted precursor, potassium carbonate and palladium complex. The resulting reaction mixture was heated at 70 °C for 4 min to produce [11C]UCB-J. Results After semi-preparative HPLC purification and reformulation in 10% ethanol/phosphate buffered saline, the product was obtained in 39 ± 5% radiochemical yield based on [11C]methyl iodide, corresponding to 1.8 ± 0.5 GBq at EOS. The radiochemical purity was > 99% and the molar activity was 390 ± 180 GBq/μmol at EOS. The product solution contained < 2 ppb palladium. Conclusions A robust and high yielding production method has been developed for [11C]UCB-J, suitable for both preclinical and clinical PET applications.

scholarly journals Chemical compositions, antimicrobial effects, and cytotoxicity of Asia minor wormwood (Artemisia splendens Willd.) growing in Iran

BMC Chemistry ◽  
2021 ◽  
Vol 15 (1) ◽  
Author(s):  
Fariba Heshmati Afshar ◽  
Masumeh Zadehkamand ◽  
Zahra Rezaei ◽  
Abbas Delazar ◽  
Vahideh Tarhriz ◽  
...  
Keyword(s):  
Cell Line ◽  
Proliferative Activity ◽  
Methanolic Extract ◽  
Biologically Active ◽  
Flavonoid Glycosides ◽  
Control Group ◽  
Chemical Compositions ◽  
Preparative Hplc ◽  
Cytotoxicity Activity ◽  
Methanolic Extracts

Abstract Background Artemisia splendens from the Asteraceae family is a new source of biologically active compounds. The current study investigated to evaluate antimicrobial and cytotoxicity activity of methanolic extracts and their fractions obtained from aerial parts by agar disk diffusion and MTT methods, respectively. The active fractions were subjected to preparative HPLC for isolating the pure compounds, which were structurally elucidated, by 1H and 13C NMR. Results The results showed that the methanolic extract and its 60% SPE fraction have the anti-proliferative activity on A549 cell line in comparison with the control group. Meanwhile, the methanolic extract and its 40% SPE fraction can inhibit the growth of Gram-positive strains as anti-microbial activity. The 60% SPE fraction also illustrated anti-proliferative activity on the HT-29 cell line compared to the control group. Chromatographic separations via preparative HPLC yielded 5 flavonoids and three flavonoid glycosides. Conclusion Based on the results it can be concluded that A. splendens as a potential source of cytotoxic and antimicrobial compounds can be used in pharmaceutics.

HSCCC Separation of Three Main Compounds from the Crude Extract of Dracocephalum Tanguticum by Using Dimethyl Sulfoxide as Cosolvent

2020 ◽  
Author(s):  
Xue Yang ◽  
Yongling Liu ◽  
Tao Chen ◽  
Nana Wang ◽  
Hongmei Li ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Ethyl Acetate ◽  
Dimethyl Sulfoxide ◽  
Efficient Method ◽  
Crude Extract ◽  
High Speed ◽  
Glacial Acetic Acid ◽  
Butyl Alcohol ◽  
Preparative Hplc ◽  
Counter Current

Abstract Separation of natural compounds directly from the crude extract is a challenging work for traditional column chromatography. In the present study, an efficient method for separation of three main compounds from the crude extract of Dracocephalum tanguticum has been successfully established by high-speed counter-current chromatography (HSCCC). The crude extract was directly introduced into HSCCC by using dimethyl sulfoxide as cosolvent. Ethyl acetate/n-butyl alcohol/0.3% glacial acetic acid (4: 1: 5, v/v) system was used and three target compounds with purity higher than 80% were obtained. Preparative HPLC was used for further purification and three target compounds with purity higher than 98% were obtained. The compounds were identified as chlorogenic acid, pedaliin and pedaliin-6″-acetate.

Improved gram-quantity isolation of malto-oligosaccharides by preparative HPLC

1993 ◽  
Vol 242 ◽  
pp. 1-9 ◽  
Author(s):  
Arland T. Hotchkiss ◽  
Rebecca M. Haines ◽  
Kevin B. Hicks
Keyword(s):  
Preparative Hplc

Ultrafiltration-LC-MS combined with semi-preparative HPLC for the simultaneous screening and isolation of lactate dehydrogenase inhibitors fromBelamcanda chinensis

2016 ◽  
Vol 39 (23) ◽  
pp. 4533-4543 ◽  
Author(s):  
Senlin Li ◽  
Sainan Li ◽  
Ying Tang ◽  
Chunming Liu ◽  
Lina Chen ◽  
...  
Keyword(s):  
Lactate Dehydrogenase ◽  
Preparative Hplc

Antioxidant and anticancer activities of an Aporphine alkaloid isolated from Alphonsea sclerocarp

2018 ◽  
Vol 7 (1) ◽  
pp. 51-55
Author(s):  
Suman Joshi DSD ◽  
◽  
Chander Amgoth ◽  
Surya Narayana S ◽  
Padmavathi CH ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Medicinal Plant ◽  
Chronic Myeloid Leukaemia ◽  
Mtt Assay ◽  
Preparative Hplc ◽  
Spectroscopic Techniques ◽  
Anticancer Activities ◽  
Frap Assay ◽  
Aporphine Alkaloid ◽  
Dose Dependent

Herein, we report on the anticancer and antioxidant activity of an Aporphine alkaloid isolated from medicinal plant Alphonsea sclerocarpa. Conventional column chromatography and preparative HPLC methods were used to isolate and purify the alkaloid. Based on NMR, FTIR and MS/MS spectroscopic techniques the compound was identified as Crebanine. This is the first report on the presence of Crebanine from the leaves of Alphonsea sclerocarpa. Antioxidant activity was evaluated using DPPH and FRAP assay. The antioxidant activity was dose-dependent and activity increased with the increase in the concentration. The cytotoxicity assay was carried out using MTT assay. The results showed remarkable cytotoxic activity against K562 (CML-chronic myeloid Leukaemia blood cancer) cells with a % inhibition of 37.545 at 500µm concentration after an incubation of 24h

scholarly journals Application of HPCCC Combined with Polymeric Resins and HPLC for the Separation of Cyclic Lipopeptides Muscotoxins A–C and Their Antimicrobial Activity

Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2653 ◽  
Author(s):  
José Cheel ◽  
Jan Hájek ◽  
Marek Kuzma ◽  
Kumar Saurav ◽  
Iva Smýkalová ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Inhibitory Concentration ◽  
Pathogenic Fungus ◽  
High Yield ◽  
Preparative Hplc ◽  
Efficient Tool ◽  
Cyclic Lipopeptides ◽  
Potential Applications ◽  
Polymeric Resins ◽  
Weak Antibacterial Activity

Muscotoxins are cyanobacterial cyclic lipopeptides with potential applications in biomedicine and biotechnology. In this study, Desmonostoc muscorum CCALA125 strain extracts were enriched by polymeric resin treatment, and subjected to HPCCC affording three cyclic lipopeptides (1–3), which were further repurified by semi-preparative HPLC, affording 1, 2, and 3, with a purity of 86%, 92%, and 90%, respectively. The chemical identities of 2–3 were determined as muscotoxins A and B, respectively, by comparison with previously reported ESI-HRMS/MS data, whereas 1 was determined as a novel muscotoxin variant (muscotoxin C) using NMR and ESI-HRMS/MS data. Owing to the high yield (50 mg), compound 2 was broadly screened for its antimicrobial potential exhibiting a strong antifungal activity against Alternaria alternata, Monographella cucumerina, and Aspergillus fumigatus, with minimum inhibitory concentration (MIC) values of 0.58, 2.34, and 2.34 µg/mL; respectively, and weak antibacterial activity against Bacillus subtilis with a MIC value of 37.5 µg/mL. Compounds 1 and 3 were tested only against the plant pathogenic fungus Sclerotinia sclerotiorum due to their low yield, displaying a moderate antifungal activity. The developed chromatographic method proved to be an efficient tool for obtaining muscotoxins with potent antifungal properties.

Long-acting androgens: Analytical and preparative HPLC of testosterone esters

1987 ◽  
Vol 10 (4) ◽  
pp. 186-190 ◽  
Author(s):  
S. A. Matlin ◽  
L. Chan ◽  
M. A. Prazeres ◽  
S. Mehani ◽  
Q. B. Cass
Keyword(s):  
Preparative Hplc ◽  
Long Acting

Preparative HPLC Optimization

2005 ◽  
pp. 1347-1354
Author(s):  
Michael Breslav ◽  
Vera Leshchinskaya
Keyword(s):  
Preparative Hplc
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