scholarly journals Liquid-Liquid Chromatography Separation of Guaiane-Type Sesquiterpene Lactones from Ferula penninervis Regel & Schmalh. and Evaluation of Their In Vitro Cytotoxic and Melanin Inhibitory Potential

2021 ◽  
Vol 22 (19) ◽  
pp. 10717
Author(s):  
Simon Vlad Luca ◽  
Katarzyna Gaweł-Bęben ◽  
Marcelina Strzępek-Gomółka ◽  
Ainur Jumabayeva ◽  
Zuriyadda Sakipova ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Liquid Chromatography ◽  
Sesquiterpene Lactones ◽  
Folk Medicine ◽  
Root Extract ◽  
Chromatography Method ◽  
Perennial Plant ◽  
B16f10 Cells ◽  
Inhibitory Potential

Ferula penninervis Regel & Schmalh. is a perennial plant used in Kazakh traditional folk medicine to treat epilepsy, neurosis, rheumatism, gastroduodenal ulcers, dyspepsia, wounds, abscesses or tumors. The aim of this work was to isolate series of sesquiterpene lactones from a crude methanolic root extract and investigate their in vitro cytotoxic potential against androgen-dependent prostate cancer LNCaP and epithelial prostate PNT2 cells, as well as to evaluate their melanin production inhibitory effects in murine melanoma B16F10 cells stimulated with α-melanocyte-stimulating hormone (αMSH). Two new (penninervin P and penninervin Q) and five known (olgin, laferin, olgoferin, oferin and daucoguainolactone F) guaiane-type sesquiterpene lactones were isolated with the use of a simple and fast liquid-liquid chromatography method. Olgin and laferin showed the most promising cytotoxic effects in LNCaP cells (IC50 of 31.03 and 23.26 μg/mL, respectively). Additionally, olgin, laferin, olgoferin, and oferin (10 μg/mL) potently impaired melanin release (40.67–65.48% of αMSH + cells) without influencing the viability of B16F10 cells. In summary, our findings might indicate that guaiane-type sesquiterpene lactones from F. penninervis could be regarded as promising candidates for further research in discovering new therapeutic agents with anti-prostate cancer and skin depigmentation properties.

Potential Anti-inflammatory Sesquiterpene Lactones from Eupatorium lindleyanum

Planta Medica ◽  
2017 ◽  
Vol 84 (02) ◽  
pp. 123-128 ◽  
Author(s):  
Fang Wang ◽  
Huanhuan Zhong ◽  
Shiqi Fang ◽  
Yunfeng Zheng ◽  
Cunyu Li ◽  
...  
Keyword(s):  
Sesquiterpene Lactones ◽  
Folk Medicine ◽  
2D Nmr ◽  
In Vitro Assays ◽  
Raw 264.7 Cells ◽  
Therapeutic Effects ◽  
In Vivo Experiments ◽  
Anti Inflammatory

Abstract Eupatorium lindleyanum has traditionally been used as folk medicine in Asian countries for its therapeutic effects on tracheitis and tonsillitis. Investigation of the anti-inflammatory active constituents from E. lindleyanum led to the isolation of two novel sesquiterpene lactones, named eupalinolide L (1) and eupalinolide M (2), and seven known sesquiterpene lactones (3–9). The structures and configurations of the new compounds were determined on the basis of spectroscopic analysis, especially 2D NMR techniques. In vivo experiments showed that the sesquiterpenes fraction significantly reduced mouse ear edema induced by xylene (18.6%, p < 0.05). In in vitro assays, compounds 1–9 showed excellent anti-inflammatory activities, as they lowered TNF-α and IL-6 levels in lipopolysaccharide-stimulated murine macrophage RAW 264.7 cells (p < 0.001). The above results suggest that the sesquiterpene lactones from E. lindleyanum can be developed as novel potential natural anti-inflammatory agents.

Qualitative and Quantitative Analysis of Resveratrol and Oxyresveratrol by Liquid Chromatography

2020 ◽  
Vol 7 (1) ◽  
pp. 24-31
Author(s):  
Rajeshree Khambadkar ◽  
Selvan Ravindran ◽  
Digamber Singh Chahar ◽  
Srushti Utekar ◽  
Amlesh Tambe
Keyword(s):  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
High Performance ◽  
Pharmacokinetic Profile ◽  
Quantitative Information ◽  
In Vivo Studies ◽  
Chromatography Method ◽  
Qualitative And Quantitative

Introduction: Resveratrol and its monooxygenated metabolite oxyresveratrol were the subject matter of intense research due to their medicinal value. Absorption, distribution, metabolism and excretion are important to understand the bioavailability and pharmacokinetic profile of resveratrol and oxyresveratrol. Quantification of resveratrol and oxyresveratrol is essential for both in vitro and in vivo studies. Methods: During in vitro drug metabolism studies, both qualitative and quantitative information are essential to understand the metabolic profile of resveratrol and oxyresveratrol. In the present study, a simple and stable method is outlined using high performance liquid chromatography to quantify both resveratrol and oxyresveratrol. This method is suitable to understand the metabolic stability, plasma stability, pharmacokinetics and toxicokinetics of resveratrol and oxyresveratrol. Results: Generally, in vitro incubation studies are performed at high concentrations and in vivo studies are carried out at both high and low concentrations, therefore high performance liquid chromatography method is demonstrated as a suitable technique to quantify resveratrol and oxyresveratrol. Conclusion: Retention time of resveratrol and oxyresveratrol from liquid chromatography qualitatively confirm its identity.

DEVELOPMENT OF HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY METHOD FOR THE SIMULTANEOUS ANALYSIS OF AMLODIPINE AND VALSARTAN IN COMBINED DOSAGE FORM AND IN VITRO DISSOLUTION STUDIED

2018 ◽  
Vol 11 (5) ◽  
pp. 200
Author(s):  
Olga Yuryeva ◽  
Yuliya Kondratova ◽  
Liliya Logoyda
Keyword(s):  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
High Performance ◽  
Drug Product ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Combination Drug ◽  
Chromatography Method ◽  
Liquid Chromatography Method

 Objective: A simple, rapid, and reproducible high-performance liquid chromatography method was developed for the simultaneous determination of amlodipine and valsartan in their combined dosage forms and for drug dissolution studies.Methods: A C18 column (Zorbax Eclipse ХDB-C18, 5 μm, 2.1 mm × 150 mm) and a mobile phase of water:acetonitrile:trifluoroacetic acid (55:45:0.1 v/v/v) mixture were used for separation and quantification. Analyses were run at a flow rate of 0.4 mL/min and at ambient temperature. The injection volume was 5 μL and the ultraviolet detector was set at 265 nm. The method was validated as per ICH guidelines.Results: Under these conditions, amlodipine and valsartan were eluted at 1.64 min and 4.08 min, respectively. Total run time was shorter than 7 min. The results were 99.6 ± 0.6 and 98.5 ± 0.8 for amlodipine and valsartan, respectively. Valsartan was released within 15 min (98.32%) and amlodipine was also released within 30 min (96.16%) both at a pH of 6.8.Conclusion: The developed method was applied successfully for quality control assay of amlodipine and valsartan in their combination drug product and in vitro dissolution studies.

scholarly journals Scopoletin: Antiamyloidogenic, Anticholinesterase, and Neuroprotective Potential of a Natural Compound Present in Argyreia speciosa Roots by In Vitro and In Silico Study

2020 ◽  
Vol 15 ◽  
pp. 263310552093769 ◽  
Author(s):  
Priya Kashyap ◽  
Heera Ram ◽  
Sunil Dutt Shukla ◽  
Suresh Kumar
Keyword(s):  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
Enzyme Inhibition ◽  
In Silico ◽  
High Performance ◽  
Amyloid Β ◽  
Root Extract ◽  
Aβ Peptides ◽  
Disease Modifying

Alzheimer’s disease (AD) is characterized by depositions of amyloid β (Aβ) peptides aggregates resulting in plaques formation in the central nervous system (CNS). This study evaluates the disease-modifying potential of scopoletin against multiple factors associated with AD such as cholinesterase enzymes, Aβ peptides, and neuroprotective properties against Aβ- and H2O2-induced cytotoxicity under in vitro conditions. Scopoletin was identified and quantified using UPLC-QTOF (ultra-high performance liquid chromatography-quadrupole time-of-flight) and high-performance liquid chromatography (HPLC), respectively. The antiamyloidogenic potential was evaluated by thioflavin T and congo red binding assay. Inhibition of key enzymes, that is, acetylcholinesterase and butyrylcholinesterase, was investigated by Ellman’s assay. UPLC-QTOF analysis showed that most abundant phytoconstituent present in Argyreia speciosa hydroalcoholic root extract was scopoletin followed by festuclavine and ergometrine. Scopoletin was further quantified using novel reverse phase (RP)-HPLC method developed in this study. The neuroprotective potential of scopoletin was found to be 69% against Aβ42-induced neurotoxicity and 73% against H2O2-induced cytotoxicity in PC12 cell culture at 40 μM final concentration. At the same concentration, scopoletin inhibited Aβ42 fibril formation up to 57%. The IC50 concentration for AChE and BuChE enzyme inhibition by scopoletin was 5.34 and 9.11 μM, respectively. The antiaggregation and enzyme inhibition results were complemented with strong molecular interactions of scopoletin with target proteins validated by in silico molecular docking analysis. Based on this study, it can be concluded that scopoletin can be used as a lead for amelioration of symptoms and disease-modifying effects in AD.

scholarly journals In vitro Elucidation of Antiproliferative and Apoptotic Effects of Thymol against Prostate Cancer LNCaP Cells

2021 ◽  
Vol 12 (1) ◽  
pp. 1279-1289
Keyword(s):  
Prostate Cancer ◽  
Anticancer Agents ◽  
Lncap Cells ◽  
Dapi Staining ◽  
Antitumor Effects ◽  
Inhibitory Potential ◽  
Dependent Growth ◽  
Nuclear Alterations ◽  
Apoptotic Effects

Recent research suggested the role of plant-derived bioactive compounds as potent anticancer agents. Thymol, a monoterpene phenol, possesses numerous pharmacological properties such as antioxidant, anti-inflammatory, and antitumor effects. However, the inhibitory potential of thymol on prostate cancer cells still elusive. Therefore, the purpose of this study is to explore the antiproliferative and apoptotic effects of thymol against prostate cancer LNCaP cells. Our results indicated dose-dependent growth inhibitory effects of thymol on prostate cancer LNCaP cells. Morphological analysis and DAPI staining revealed that thymol induces marked morphological and nuclear alterations in LNCaP cells. Moreover, thymol could induce significant apoptosis in LNCaP cells through caspase-3 activation and modulation of mRNA expression of apoptotic-related genes. Overall, these findings showed that thymol could offer a novel therapeutic approach against prostate cancer.

Latanoprost Quantification in Ocular Implants and Tissues: HPLC-Fluorescence vs HPLC-UV

2020 ◽  
Vol 59 (1) ◽  
pp. 64-70
Author(s):  
Karim Soliman ◽  
Feras Jirjees ◽  
Rahul Sonawane ◽  
Ravi Sheshala ◽  
Yujing Wang ◽  
...  
Keyword(s):  
Liquid Chromatography ◽  
Reversed Phase ◽  
Eye Drops ◽  
Uv Detector ◽  
Fluorescence Detector ◽  
Fluorescence Excitation ◽  
Chromatography Method ◽  
Uv Detectors ◽  
Ocular Implants

Abstract Anti-glaucoma latanoprost-loaded ocular implants provide prolonged delivery and enhanced bioavailability relative to the conventional eye drops. This study aims at the development and validation of a reversed-phase high-performance liquid chromatography method for quantitative analysis of nanogram levels of latanoprost in the eye, and for the first time, compares the use of fluorescence vs ultraviolet (UV) detectors in latanoprost quantification. The mobile phase was composed of acetonitrile:0.1% v/v formic acid (60:40, v/v) with a flow rate of 1 mL/min and separation was done using a C18 column at temperature 40°C. The fluorescence excitation and emission wavelengths were set at 265 and 285 nm, respectively, while the UV absorption was measured at 200 nm. The latanoprost concentration-peak area relationship maintained its linearity (R2 = 0.9999) over concentration ranges of 0.063–10 μg/mL and 0.212–10 μg/mL for the fluorescence and UV detectors, respectively. The UV detector showed better precision, while the fluorescence detector exhibited higher robustness and greater sensitivity, with a detection limit of 0.021 μg/mL. The fluorescence detector was selected for quantification of latanoprost released from ocular implants in vitro and in porcine ocular tissues. The developed method is a robust, rapid and cost-effective alternative to liquid chromatography–mass spectrometry for routine analysis of latanoprost released from ocular implants.

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