scholarly journals High-Throughput Identification of Organic Compounds from Polygoni Multiflori Radix Praeparata (Zhiheshouwu) by UHPLC-Q-Exactive Orbitrap-MS

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3977
Author(s):  
Shaoyun Wang ◽  
Xiaozhu Sun ◽  
Shuo An ◽  
Fang Sang ◽  
Yunli Zhao ◽  
...  
Keyword(s):  
High Performance ◽  
Chemical Constituents ◽  
Water Extract ◽  
Ethanol Extract ◽  
In Vivo Studies ◽  
Polygonum Multiflorum ◽  
Q Exactive ◽  
Orbitrap Ms

Polygoni Multiflori Radix Praeparata (PMRP), as the processed product of tuberous roots of Polygonum multiflorum Thunb., is one of the most famous traditional Chinese medicines, with a long history. However, in recent years, liver adverse reactions linked to PMRP have been frequently reported. Our work attempted to investigate the chemical constituents of PMRP for clinical research and safe medication. In this study, an effective and rapid method was established to separate and characterize the constituents in PMRP by combining ultra-high performance liquid chromatography with hybrid quadrupole-orbitrap mass spectrometry (UHPLC-Q-Exactive Orbitrap-MS). Based on the accurate mass measurements for molecular and characteristic fragment ions, a total of 103 compounds, including 24 anthraquinones, 21 stilbenes, 15 phenolic acids, 14 flavones, and 29 other compounds were identified or tentatively characterized. Forty-eight compounds were tentatively characterized from PMRP for the first time, and their fragmentation behaviors were summarized. There were 101 components in PMRP ethanol extract (PMRPE) and 91 components in PMRP water extract (PMRPW). Simultaneously, the peak areas of several potential xenobiotic components were compared in the detection, which showed that PMRPE has a higher content of anthraquinones and stilbenes. The obtained results can be used in pharmacological and toxicological research and provided useful information for further in vitro and in vivo studies.

Antidiarrheal Activity of Ethanol Extract of Ophioglossum Vulgatum In Mice And Spasmolytic Effect on Smooth Muscle Contraction of Isolated Jejunum In Rabbits

2020 ◽  
Author(s):  
Jianwu Zhang ◽  
Lan Yang ◽  
Yingying Fang ◽  
Jing Li ◽  
Chunxia Gu ◽  
...  
Keyword(s):  
Smooth Muscle ◽  
High Performance ◽  
Chemical Constituents ◽  
Ethanol Extract ◽  
Gastrointestinal Diseases ◽  
Control Group ◽  
Response Curves ◽  
Antidiarrheal Activity

Abstract BackgroundOphioglossum vulgatum Linn. (Ophioglossaceae) (OV), which is traditionally used on wounds and burns, enjoys a reputation as the king of medicine in Taiwan. There are few studies on its role in gastrointestinal diseases. Our aim was to assess the antidiarrheal and spasmolytic effect of the ethanol whole plant extract of Ophioglossum vulgatum (EWOV).MethodsStudy was conducted from June 2018 to July 2019. The chemical constituents of EWOV were analyzed by high performance liquid chromatography (HPLC). In vivo, the antidiarrheal activity of EWOV (125, 250 and 500 mg/kg; orally) in castor oil-induced Kun Ming mice was evaluated. In vitro, the effect of EWOV (0.01-10 mg/mL) on the spontaneous contraction of isolated rabbit jejunum smooth muscle was studied. Verapamil was the positive control group in both vivo and vitro studies. The jejunum stripes were pre-contracted by ACh (10-5 M) and KCl (60 mM) which could induce the jejunum spasm. The possible spasmolytic effect was analyzed in the pretreatment of the jejunum preparations with EWOV (0.3, 1 mg/mL) or verapamil (0.03, 0.1 µM) in Ca2+-free and high-K+ (60 mM) solution containing EDTA.ResultsEWOV (250 and 500 mg/kg) exhibited antidiarrheal effect. EWOV (0.01-10 mg/mL) inhibited the spontaneous and ACh/KCl-induced contraction with an EC50 value of 1.46 (0.89-2.04), 1.06 (0.63-1.48) and 0.48 (0.29-0.67), and it shifted the concentration-response curves of CaCl2 to right with decreased in max, similar to verapamil. ConclusionsEWOV has significant antidiarrheal and spasmolytic effect, possibly by mediating calcium channel blocking activity, this provides the pharmacological basis for use in gastrointestinal disorders.

Phytochemistry and Pharmacology of the Genus Pedicularis Used in Traditional Chinese Medicine

2014 ◽  
Vol 42 (05) ◽  
pp. 1071-1098 ◽  
Author(s):  
Mao-Xing Li ◽  
Xi-Rui He ◽  
Rui Tao ◽  
Xinyuan Cao
Keyword(s):  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Chemical Constituents ◽  
Iridoid Glycosides ◽  
In Vivo Studies ◽  
Chemical Components ◽  
Wide Range ◽  
Phenylpropanoid Glycosides

In the present review, the literature data on the chemical constituents and biological investigations of the genus Pedicularis are summarized. Some species of Pedicularis have been widely applied in traditional Chinese medicine. A wide range of chemical components including iridoid glycosides, phenylpropanoid glycosides (PhGs), lignans glycosides, flavonoids, alkaloids and other compounds have been isolated and identified from the genus Pedicularis. In vitro and in vivo studies indicated some monomer compounds and extracts from the genus Pedicularis have been found to possess antitumor, hepatoprotective, anti-oxidative, antihaemolysis, antibacterial activity, fatigue relief of skeletal muscle, nootropic effect and other activities.

Effect of Gut Microbiota on the Metabolism of Chemical Constituents of Berberis kansuensis Extract Based on UHPLC-Orbitrap-MS Technique

Planta Medica ◽  
2021 ◽  
Author(s):  
Huan Du ◽  
Tong Xu ◽  
Huan Yi ◽  
Xinmei Xu ◽  
Chengcheng Zhao ◽  
...  
Keyword(s):  
Gut Microbiota ◽  
High Performance ◽  
Chemical Constituents ◽  
Chemical Components ◽  
Serum Samples ◽  
Chromatography Method ◽  
Metabolic Transformation ◽  
Orbitrap Ms

AbstractThe dried stem bark of Berberis kansuensis is a commonly used Tibetan herbal medicine for the treatment of diabetes. Its main chemical components are alkaloids, such as berberine, magnoflorine and jatrorrhizine. However, the role of gut microbiota in the in vivo metabolism of these chemical components has not been fully elucidated. In this study, an ultra-high performance liquid chromatography method coupled with Orbitrap mass spectrometry (UHPLC-Orbitrap-MS) technology was applied to detect and identify prototype components and metabolites in rat intestinal contents and serum samples after oral administration of a B. kansuensis extract. A total of 16 prototype components and 40 metabolites were identified. The primary metabolic pathways of the chemical components from B. kansuensis extract were demethylation, desaturation, deglycosylation, reduction, hydroxylation, and other conjugation reactions including sulfation, glucuronidation, glycosidation, and methylation. By comparing the differences of metabolites between diabetic and pseudo-germ-free diabetic rats, we found that the metabolic transformation of some chemical components in B. kansuensis extract such as bufotenin, ferulic acid 4-O-β-D-glucopyranoside, magnoflorine, and 8-oxyberberine, was affected by the gut microbiota. The results revealed that the gut microbiota can affect the metabolic transformation of chemical constituents in B. kansuensis extract. These findings can enhance our understanding of the active ingredients of B. kansuensis extract and the key role of the gut microbiota on them.

scholarly journals α-Glucosidase Inhibitory, Anti-Oxidant, and Anti-Hyperglycemic Effects of Euphorbia nivulia–Ham. in STZ-Induced Diabetic Rats

Dose-Response ◽  
2020 ◽  
Vol 18 (3) ◽  
pp. 155932582093942
Author(s):  
Muhammad Younus ◽  
Muhammad Mohtasheem ul Hasan ◽  
Khalil Ahmad ◽  
Ali Sharif ◽  
Hafiz Muhammad Asif ◽  
...  
Keyword(s):  
High Performance ◽  
Wistar Rat ◽  
Inhibitory Effect ◽  
Diabetic Rats ◽  
In Vivo Studies ◽  
Control Group ◽  
Control Drug ◽  
Antidiabetic Effects

In this study, we aimed to investigate the antidiabetic effects of Euphorbia nivulia (En), native to Cholistan Desert area of Bahawalpur, Pakistan. First, we performed high-performance liquid chromatography analysis and found that this plant contains ferulic acid, gallic acid, quercetin, benzoic acid, polyphenols, and flavonoids. Then, we performed in vitro and in vivo studies to assess its effects on diabetic Wistar rat model. The experiments were performed and compared with control drug glibenclamide. The 70% hydroalcoholic extract of En exhibited 97.8% in vitro α-glucosidase inhibitory effect at a dose of 1.0 mg/mL. We orally administered the extract of En and control drug to the streptozotocin (STZ)-induced diabetic rats and analyzed its antidiabetic effects. We found that the extract of En with a dose of 500 mg/kg/body weight exhibited significant effect to reduce blood glucose in STZ-induced rats as compared with the control group ( P < .001). Our histological data also showed that the extract significantly improved the histopathology of pancreas. Collectively, both in vitro and in vivo studies revealed that En possesses α-glucosidase inhibitory, antioxidant, and anti-hyperglycemic effect in STZ-induced diabetic rats.

scholarly journals Identifying of Anti-Thrombin Active Components From Curcumae Rhizoma by Affinity-Ultrafiltration Coupled With UPLC-Q-Exactive Orbitrap/MS

2021 ◽  
Vol 12 ◽  
Author(s):  
Zhenwei Lan ◽  
Ying Zhang ◽  
Yue Sun ◽  
Lvhong Wang ◽  
Yuting Huang ◽  
...  
Keyword(s):  
Quality Control ◽  
Molecular Docking ◽  
Targeted Therapy ◽  
Screening Method ◽  
Active Ingredients ◽  
Active Compounds ◽  
Q Exactive ◽  
Orbitrap Ms

Recent studies concerning products that originate from natural plants have sought to clarify active ingredients, which both explains the mechanisms of the function and aids in quality control during production. As a traditional functional plant, Curcumae Rhizoma (CR) has been proven to be effective in promoting blood circulation and removing blood stasis. However, the components that play a role in its huge compound library are still unclear. The present study aimed to develop a high-throughput screening method to identify thrombin inhibitors in CR and validate them by in vitro and in vivo experiments. The effect of CR on thrombin in HUVECs cells was determined by ELISA, then an affinity-ultrafiltration-UPLC-Q-Exactive Orbitrap/MS approach was applied. Agatroban and adenosine were used as positive and negative drugs respectively to verify the reliability of the established method. The in vitro activity of the compounds was determined by specific substrate S-2238. The in vivo effect of the active ingredients was determined using zebrafish. Molecular docking was used to understand the internal interactions between compounds and enzymes. ELISA results showed that CR had an inhibitory effect on thrombin. The screening method established in this paper is reliable, by which a total of 15 active compounds were successfully identified. This study is the first to report that C7, 8, and 11 have in vitro thrombin-inhibitory activity and significantly inhibit thrombosis in zebrafish models at a safe dose. Molecular docking studies were employed to analyze the possible active binding sites, with the results suggesting that compound 16 is likely a better thrombin inhibitor compared with the other compounds. Based on the affinity-ultrafiltration-UPLC-Q-Exactive Orbitrap/MS approach, a precisely targeted therapy method using bio-active compounds from CR might be successfully established, which also provides a valuable reference for targeted therapy, mechanism exploration, and the quality control of traditional herbal medicine.

scholarly journals Comparative Studies on the Anticoagulant Profile of Branded Enoxaparin and a New Biosimilar Version

2020 ◽  
Vol 26 ◽  
pp. 107602962096082
Author(s):  
Dalia Qneibi ◽  
Eduardo Ramacciotti ◽  
Ariane Scarlatelli Macedo ◽  
Roberto Augusto Caffaro ◽  
Leandro Barile Agati ◽  
...  
Keyword(s):  
Molecular Weight ◽  
High Performance ◽  
Thrombin Generation ◽  
Area Under The Curve ◽  
Factor Xa ◽  
In Vivo Studies ◽  
In Vitro Tests ◽  
Thrombin Time

Low molecular weight heparins (LMWH) represent depolymerized heparin prepared by various methods that exhibit differential, biochemical and pharmacological profiles. Enoxaparin is prepared by benzylation followed by alkaline depolymerization of porcine heparin. Upon the expiration of its patent, several biosimilar versions of enoxaparin have become available. Heparinox (Sodic enoxaparine; Cristália Produtos Químicos Farmacêuticos LTDA, Sao Paulo, Brazil) is a new biosimilar form of enoxaparin. We assessed the molecular weight and the biochemical profile of Heparinox and compared its properties to the original branded enoxaparin (Lovenox; Sanofi, Paris, France). Clotting profiles compared included activated clotting time, activated partial thromboplastin time (aPTT), and thrombin time (TT). Anti-protease assays included anti-factor Xa and anti-factor IIa activities. Thrombin generation was measured using a calibrated automated thrombogram and thrombokinetic profile included peak thrombin, lag time and area under the curve. USP potency was determined using commercially available assay kits. Molecular weight profiling was determined using high performance liquid chromatography. We determined that Heparinox and Lovenox were comparable in their molecular weight profile. Th anticoagulant profile of the branded and biosimilar version were also similar in the clot based aPTT and TT. Similarly, the anti-Xa and anti-IIa activities were comparable in the products. No differences were noted in the thrombin generation inhibitory profile of the branded and biosimilar versions of enoxaparin. Our studies suggest that Heparinox is bioequivalent to the original branded enoxaparin based upon in vitro tests however will require further in vivo studies in animal models and humans to determine their clinical bioequivalence.

scholarly journals Chemical Constituents and Antidepressant-Like Effects in Ovariectomized Mice of the Ethanol Extract of Alternanthera philoxeroides

Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2202 ◽  
Author(s):  
Charinya Khamphukdee ◽  
Orawan Monthakantirat ◽  
Yaowared Chulikhit ◽  
Suradet Buttachon ◽  
Michael Lee ◽  
...  
Keyword(s):  
Crude Extract ◽  
Estrogenic Activity ◽  
Chemical Constituents ◽  
Corticosterone Level ◽  
Ethanol Extract ◽  
Alternanthera Philoxeroides ◽  
Ovariectomized Mice ◽  
Propenoic Acid

The previously unreported flavone glycoside, demethyltorosaflavone B (2) and the E-propenoic acid substituted flavone, torosaflavone E (3a), were isolated together with nine previously reported metabolites, including indole-3-carbaldehyde, oleanonic acid, vanillic acid, p-hydroxybenzoic acid, altheranthin (1a), alternanthin B (1b), demethyltorosaflavone D (3b), luteolin 8-C-E-propenoic acid (4) and chrysoeriol 7-O-rhamnoside (5), from the ethanol extract of the aerial part of Althernanthera philoxeroides. The crude ethanol extract was evaluated for its in vitro estrogenic activity in MCF-7 breast cancer cell line. The crude ethanol extract was also investigated in vivo for its antidepressant-like effects on ovariectomized mice using tail suspension and forced swimming tests, while its effect on the locomotor activity was evaluated by a Y-maze test. The effect of the crude extract on the serum corticosterone level, size and volume of uterus of the ovariectomized mice were also investigated. The expression of the mouse cyclic adenosine monophosphate (cAMP) response element-binding protein (CREB), brain-derived neurotrophic factor (BDNF) and β-actin mRNAs in hippocampus and frontal cortex was also evaluated, using semiquantitative reverse transcription-polymerase chain reaction. The crude extract and the isolated compounds 1a, 1b, 3a, 3b and 5, were evaluated for their inhibitory effects on monoamine oxidases (MAOs)-A and -B.

Chemical Constituents of Pedicularis densispica Franch

2011 ◽  
Vol 66 (6) ◽  
pp. 641-646 ◽  
Author(s):  
Hong Biao Chu ◽  
Guang Zhi Zeng ◽  
Mei Ju Zhu ◽  
Wen Jun He ◽  
Yu Mei Zhang ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Chemical Constituents ◽  
Iridoid Glycosides ◽  
Sinapic Acid ◽  
Acid Methyl Ester ◽  
Ethanol Extract ◽  
Spectroscopic Studies ◽  
Pai 1

An ethanol extract of the dried aerial of Pedicularis densispica Franch (Scrophulariaceae) afforded a new lignan, densispicoside (1), and two new iridoids, densispicnin C and D (14, 15), together with four lignans, (+)-isolarisiresinol 3a-O-β -D-glucopyranoside (2), (-)-pinoresinol-β - D-glucopyranoside (3), syringaresinol mono-β -D-glucopyranoside (4), longifloroside B (5), eight phenylpropanoids, 4-O-β -D-glucopyranosyl-sinapic acid methyl ester (6), 3-(4-hydroxy-3-methoxyphenyl)- 1,2,3-propantriol (7), citrusin C (8), robustaside B (9), verbascoside (10), martynoside (11), 2ʺ-O-acetylverbascoside (12), cis-martynoside (13), and two iridoid glycosides, shanzhiside methyl ester (16), and 8-epiloganin (17). Their structures were established on the basis of chemical and spectroscopic studies. Bioactivity results indicate that P. densispica shows activity on PAI-1 antithrombus assay in vitro and antifatigue activities in vivo.

scholarly journals IN VITRO AND IN VIVO STUDIES OF ANTIHYPERURICEMIC AND ANTIOXIDANT ACTIVITY FROM BULBS OF BAWANG TIWAI (ELEUTHERINE PALMIFOLIA (L.) MERR.) FROM INDONESIA

2019 ◽  
Vol 12 (1) ◽  
pp. 497
Author(s):  
Dian Ratih Laksmitawati ◽  
Rininta Firdaus ◽  
Mediana Astika Zein
Keyword(s):  
Antioxidant Activity ◽  
Body Weight ◽  
Uric Acid ◽  
Ethanol Extract ◽  
Positive Control ◽  
In Vivo Studies ◽  
Inhibit Lipid Peroxidation ◽  
Plasma Malondialdehyde

Objectives: This study would like to investigate the in vitro antioxidant activity through 2,2-diphenyl-1-picrylhydrazyl assay and in vitro xanthine oxidase activity of the bulbs. This study performs in vivo assays to study the antihyperuricemic activity and antioxidant in the hyperuricemic rat through plasma malondialdehyde measurement. Method: The study was conducted by testing the fresh bulbs of bawang tiwai (Eleutherine palmifolia (L.) Merr. with chemical solvent of ethanol 70% to extract the bulbs. Allopurinol and Vitamin C were used as positive control for the antihyperuricemic assay and antioxidant assay, respectively. Other chemical substances were also used in this study. This study used chicken extract (Brands) 20 ml/kg/body weight to induce the level of uric acid in the blood serum, and potassium oxonate (Sigma 156124) to inhibit the uricase in rats. Results: The results show that the levels of uric acid were measured using spectrophotometer with dichloro-hydroxybenzen sulfonate (Biolabo) a as reagent. The ethanol extract of bawang tiwai (EBT) (E. palmifolia (L.) Merr) was potential to reduce uric acid level at 140, 280, and 560 mg/kg body weight, but possibly without inhibition against xanthine oxydase activity. Conclusion: All doses of EBT could inhibit lipid peroxidation in hyperuricemic condition caused by high purine diet in 14 days.

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