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1.
Molecules ; 27(14)2022 Jul 19.
Article in English | MEDLINE | ID: mdl-35889481

ABSTRACT

Oxytropis pseudoglandulosa plant is used in traditional Mongolian medicine. However, its chemical composition and biological properties are poorly explored. In this study, the total content of polyphenols and flavonoids as well as antioxidant activity were verified in plant extract. The total phenolic and flavonoid contents were determined by spectrometric (6.62 mg GAE/g and 10.32 mg QE/g) and chromatographic (17,598 mg/kg and 17,467 mg/kg) assays. The antioxidant potential was investigated by DPPH assay and yielded IC50 at 18.76 µg/mL. Twelve phenolic compounds were identified as components of O. pseudoglandulosa extract. Kaempferol-3-O-robinosyl-7-O-rhamnoside and kaempferol-3-(p-coumaroyl)-rutinosyl-7-rhamnoside made up 80% of determined components and were found to be the major polyphenolic compounds. The biological properties of O. pseudoglandulosa extracts were determined in vitro using human epithelial adenocarcinoma Caco-2 cell line. Low concentrations of extract (0-30 µg/mL) exhibited protective effects against cell damage caused by chemically induced oxidative stress. Elevated concentrations, on the other hand, resulted in apoptotic-type cell death induction. Metabolic failure, ROS elevation and membrane permeabilization observed in cells upon incubation with extract dosages above 50 µg/mL allowed us to conclude on O. pseudoglandulosa being predominantly a necrosis inducer.


Subject(s)
Oxytropis , Antioxidants/chemistry , Caco-2 Cells , Cell Death , Flavonoids/analysis , Flavonoids/pharmacology , Humans , Kaempferols , Oxytropis/chemistry , Phenols/analysis , Phenols/pharmacology , Plant Extracts/chemistry , Plant Extracts/pharmacology
2.
Molecules ; 27(5)2022 Mar 05.
Article in English | MEDLINE | ID: mdl-35268807

ABSTRACT

Oxytropis falcata Bunge is a plant used in traditional Tibetan medicine, with reported anti-inflammatory and antioxidants effects and alleviation of myocardial ischemia reperfusion injury (MIRI). However, the underlying mechanism against MIRI and the phytochemical composition of O. falcata are vague. One fraction named OFF1 with anti-MIRI activity was obtained from O. falcata, and the chemical constituents were identified by ultra-high-performance liquid chromatography coupled with tandem mass spectrometry (UHPLC-MS). The potential targets and signaling pathways involved in the action of O. falcata against MIRI were predicted by network pharmacology analysis, and its molecular mechanism on MIRI was determined by in vitro assays. The results revealed that flavonoids are the dominant constituents of OFF1. A total of 92 flavonoids reported in O. falcata targeted 213 potential MIRI-associated factors, including tumor necrosis factor (TNF), prostaglandin-endoperoxide synthase 2 (PTGS2), and the NF-κB signaling pathway. The in vitro assay on H9c2 cardiomyocytes subjected to hypoxia/reoxygenation injury confirmed that the flavonoids in OFF1 reduced myocardial marker levels, apoptotic rate, and the inflammatory response triggered by oxidative stress. Moreover, OFF1 attenuated MIRI by downregulating the ROS-mediated JNK/p38MAPK/NF-κB pathway. Collectively, these findings provide novel insights into the molecular mechanism of O. falcata in alleviating MIRI, being a potential therapeutic candidate.


Subject(s)
Myocardial Reperfusion Injury , Oxytropis , Flavonoids/pharmacology , Flavonoids/therapeutic use , Myocardial Reperfusion Injury/metabolism , NF-kappa B/metabolism , Oxytropis/chemistry , Signal Transduction
3.
Molecules ; 26(24)2021 Dec 14.
Article in English | MEDLINE | ID: mdl-34946654

ABSTRACT

Oxytropis pseudoglandulosa is used in Mongolian traditional medicine due to its numerous reported health-promoting effects. To date, there are very few scientific reports that describe this species. In this article, its volatile oil composition, lipid extract composition, total phenolic and flavonoid content, antibacterial and allergenic properties are elucidated for the first time. Hexadecanoic acid, fokienol and tricosane were determined as the most notable components of the volatile oil, at 13.13, 11.46 and 5.55%, respectively. Methyl benzoate was shown to be the most abundant component of lipid extract at 40.69, followed by (E)-prop-2-enoic acid, 3-phenyl- and benzenepropanoic acid, at 18.55 and 9.97%. With a TPC of 6.620 mg GAE g-1 and TFC of 10.316 mg QE g-1, the plant extract of O. pseudoglandulosa indicated good antioxidant activity measured by IC50 at 18.761 µg mL-1. Of the 12 tested microorganisms, B. subtilis and S. cerevisiae were the shown to be most susceptible to the plant extract, with MIC at 2.081 and 0.260% (v/v), respectively. Bet v 1-a major birch pollen allergen found in plant-based foods-was determined to be at 192.02 ng g-1 with ELISA. Such a wide spectrum of biological activity indicated by O. pseudoglandulosa lends credence for its application in food industry. Its exerted antioxidant and antimicrobial effects could improve preservation of low-processed food dedicated for consumers afflicted with allergies. Hexadecanoic acid supplemented in foods with dietary plant extracts could add to the potential anti-inflammatory impact. The analysis of lipid makeup suggests O. pseudoglandulosa extract could also be considered as natural pesticide in organic farming.


Subject(s)
Anti-Infective Agents , Bacillus subtilis/growth & development , Oils, Volatile , Oxytropis/chemistry , Plants, Medicinal/chemistry , Saccharomyces cerevisiae/growth & development , Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Mongolia , Oils, Volatile/chemistry , Oils, Volatile/pharmacology
4.
J Nat Prod ; 81(2): 307-315, 2018 02 23.
Article in English | MEDLINE | ID: mdl-29400468

ABSTRACT

Ten isomeric cyclobutane- and cyclohexene-containing chalcone dimers, oxyfadichalcones A-G, were isolated from the aerial parts of Oxytropis chiliophylla. These included six new compounds and three pairs of enantiomers that are being reported from natural sources for the first time. The relative configurations were elucidated by spectroscopic data analysis, while the absolute configurations were determined by comparing the experimental and calculated electronic circular dichroism spectra. Quantitative LC-MS analysis of the main dimers from different parts of the plant revealed their characteristic accumulation in the viscous secretion and provided supporting evidence for the hypothesized photochemical biosynthesis. In addition, the cytotoxic activities of all isolates against the PC-3 human prostate cancer cell line are reported.


Subject(s)
Chalcones/chemistry , Cytotoxins/chemistry , Oxytropis/chemistry , Cell Line, Tumor , Chalcones/pharmacology , Cytotoxins/pharmacology , Humans , PC-3 Cells
5.
Molecules ; 23(10)2018 Sep 25.
Article in English | MEDLINE | ID: mdl-30257447

ABSTRACT

Eight azukisapogenol triterpene glycosides, including five new compounds, oxychiliotriterpenosides A⁻E (1⁻5), two new methyl glucuronide derivatives that proved to be artifacts, oxychiliotriterpenoside E-glucuronic acid methyl ester (6) and myrioside B-glucuronic acid methyl ester (7), and a known one, myrioside B (8), was isolated from the aerial part of Oxytropis chiliophylla Royle. Their structures were elucidated based on extensive spectroscopic analyses and chemical methods. Triterpene glycosides were first obtained from O. chiliophylla, and those containing a galactose unit (1, 2, 5 and 6) and diglucosidic or triglucosidic linkage at C-29 (1⁻4), were reported from Oxytropis species for the first time, which might be recognized as a chemotaxonomic feature of O. chiliophylla. All isolated compounds were evaluated for their anti-inflammatory activities against NO production using lipopolysaccharide (LPS)-induced RAW 264.7 cells, but no compounds showed potent inhibition on NO production.


Subject(s)
Glycosides/chemistry , Oxytropis/chemistry , Plant Extracts/chemistry , Triterpenes/chemistry , Animals , Galactose/chemistry , Glycosides/isolation & purification , Glycosides/pharmacology , Lipopolysaccharides/chemistry , Mice , Molecular Structure , Nitric Oxide/chemistry , Plant Extracts/pharmacology , RAW 264.7 Cells , Sapogenins/chemistry , Sapogenins/pharmacology , Triterpenes/isolation & purification , Triterpenes/pharmacology
6.
J Sep Sci ; 40(18): 3593-3601, 2017 Sep.
Article in English | MEDLINE | ID: mdl-28719037

ABSTRACT

The separation of high-purity compounds from traditional Tibetan medicines plays an important role in investigating their bioactivity. Nevertheless, it is often quite difficult to isolate compounds with high purity because of the complexity of traditional Tibetan medicines. In this work, an offline two-dimensional reversed-phase preparative method was successfully developed for the separation of high-purity compounds from Oxytropis falcata. Based on the analysis results, an ODS C18 prep column was used for first-dimensional preparation, and 14.8 g of the crude sample was separated into five fractions with a recovery of 74.6%. Then, an XAqua C18 prep column was used to isolate high-purity compounds in the second-dimensional preparation because its separation selectivity is different with the ODS C18 stationary phase. As a result, eight compounds in the crude sample were isolated in more than 98% purity. This is the first report of trans-cinnamic acid (1) and trifolirhizin (2) from Oxytropis falcata. This method has the potential to be an efficient separation method of high-purity compounds from Oxytropis falcata and it shows great promise for the separation of high-purity compounds from complex samples.


Subject(s)
Chromatography, Reverse-Phase , Oxytropis/chemistry , Phytochemicals/isolation & purification
7.
Bioorg Med Chem Lett ; 26(5): 1495-7, 2016 Mar 01.
Article in English | MEDLINE | ID: mdl-26865176

ABSTRACT

Ten alkaloids (1-10), with sophoridine (1) as the most abundant component, were obtained from the whole plants of Oxytropis ochrocephala Bunge. Furthermore, eight new sophoridine derivatives (11-16, 20, 21), with modification on the C-14 position of 1 were synthesized. All compounds (1-16, 20, 21) were evaluated for antiproliferative activity against five human tumor cell lines. Among them, the newly synthesized derivative 20 exhibited the best inhibitory activity against the tested cell lines. Its activity was increased by more than fourfold as compared with parent compound 1.


Subject(s)
Alkaloids/chemistry , Alkaloids/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/pharmacology , Oxytropis/chemistry , Quinolizines/chemistry , Alkaloids/isolation & purification , Antineoplastic Agents, Phytogenic/isolation & purification , Cell Line, Tumor , Cell Proliferation/drug effects , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Humans , Molecular Structure , Structure-Activity Relationship , Matrines
8.
J Nat Prod ; 79(11): 2933-2940, 2016 11 23.
Article in English | MEDLINE | ID: mdl-27797518

ABSTRACT

Eleven 2,5-diphenyloxazole derivatives (1-11), together with six known isoflavonoid derivatives, were isolated from the roots of Oxytropis lanata. The 2,5-diphenyloxazole (1) obtained proved to be identical to a standard sample used as a scintillator and liquid laser dye. The other oxazole derivatives isolated were found to have one to four hydroxy and/or O-methyl groups in their phenyl rings. Seven of the oxazole derivatives obtained are new (3-9). The inhibitory activity of the isolated compounds was evaluated against Trypanosoma congolense, the causative agent of African trypanosomosis in animals. Oxazoles with di- and trihydroxy groups showed trypanocidal activity, and 2-(2',3'-dihydroxyphenyl)-5-(2″-hydroxyphenyl)oxazole (4) exhibited the most potent inhibitory activity (IC50 1.0 µM).


Subject(s)
Oxazoles/isolation & purification , Oxazoles/pharmacology , Oxytropis/chemistry , Plant Roots/chemistry , Trypanocidal Agents/isolation & purification , Trypanocidal Agents/pharmacology , Animals , Inhibitory Concentration 50 , Molecular Structure , Mongolia , Nuclear Magnetic Resonance, Biomolecular , Oxazoles/chemistry , Trypanocidal Agents/chemistry , Trypanosoma congolense/drug effects
9.
Zhongguo Zhong Yao Za Zhi ; 39(7): 1157-62, 2014 Apr.
Article in Zh | MEDLINE | ID: mdl-25011246

ABSTRACT

Four different extracts of Oxytropis falcata, including the aerial aqueous extract, and the underground aqueous extract, the aerial lipophilic extract, and the underground lipophilic extract were prepared and then administrated orally to mice at the maximum dose (50 g x kg(-1) x d(-1) calculated by raw material) for fifteen days respectively. Compared with the control group, which was administrated of 1.0% tween-80, the treatment groups did not show significant differences in appearance and behavior. However, the organcoefficient, blood biochemical indicator and pathological section results showed that the lipophilic extracts of the aerial and underground parts of O. flacata showed mild injury to the liver of mice, while the aerial and underground aqueous extracts and the underground lipophilic extract showed mild toxicity to the kidney of male mice. Chemical analysis showed that the lipophilic extracts of the aerial and underground parts, especially aerial lipophilic extract, consisted of large amount of flavonoid aglycones with little amount of polysaccharides and proteins, while the aqueous extracts contained much polysaccharides and proteins with almost no flavonoid aglycones detected.


Subject(s)
Oxytropis/chemistry , Plant Extracts/chemistry , Plant Extracts/toxicity , Animals , Body Weight/drug effects , Female , Liver/drug effects , Liver/growth & development , Male , Medicine, Tibetan Traditional , Mice , Molecular Structure , Organ Size/drug effects , Oxytropis/adverse effects , Spectrometry, Mass, Electrospray Ionization
10.
J Nat Prod ; 76(10): 1984-8, 2013 Oct 25.
Article in English | MEDLINE | ID: mdl-24053110

ABSTRACT

Legumes belonging to the Astragalus, Oxytropis, and Swainsona genera have been noted by ranchers in the Americas, Asia, and Australia to cause a neurologic disease often referred to as locoism or peastruck. The toxin in these legumes is swainsonine, an α-mannosidase and mannosidase II inhibitor. Recent research has shown that in Astragalus and Oxytropis species swainsonine is produced by a fungal endophyte belonging to the Undifilum genus. Here Swainsona canescens is shown to harbor an endophyte that is closely related to Undifilum species previously cultured from locoweeds of North America and Asia. The endophyte produces swainsonine in vitro and was detected by PCR and culturing in S. canescens. The endophyte isolated from S. canescens was characterized as an Undifilum species using morphological and phylogenetic analyses.


Subject(s)
Alkaloids/isolation & purification , Fabaceae/chemistry , Swainsonine/pharmacology , Alkaloids/analysis , Alkaloids/chemistry , Alkaloids/pharmacology , Endophytes/chemistry , Fabaceae/genetics , Mannosidases/antagonists & inhibitors , Molecular Structure , Oxytropis/chemistry , Sequence Analysis, DNA , Swainsonine/analysis , Swainsonine/chemistry
11.
Phytochem Anal ; 24(2): 155-61, 2013 Feb.
Article in English | MEDLINE | ID: mdl-22961746

ABSTRACT

INTRODUCTION: Oxytropis racemosa Turcz is an important minority medicine that is used mainly to improve children's indigestion, especially in inner Mongolia and Tibet. Previous studies indicated that the characteristic constituents of this plant are acylated flavonoids. OBJECTIVE: Rapidly identify the characteristic chemical constituents of O. racemosa by high-performance liquid chromatography-diode array detection-electrospray ionisation/multi-stage mass spectrometry (HPLC-DAD-ESI/MS(n) ) and suggest a useful method to control the quality of this medicinal plant. METHODS: In the HPLC fingerprint, 32 flavonoids were tentatively identified by a detailed analysis of their mass spectra, UV spectra and retention times. Furthermore, 13 flavonoids were confirmed by comparison with previously isolated compounds obtained from O. racemosa. RESULTS: In total, 32 flavonoids, including 13 flavonoids with 3-hydroxy-3-methylglutaric acid (HMG) moieties and four flavonoids with 3-malonyl moieties, were identified in the extract of O. racemosa. Among the compounds identified, 10 were characterised as new compounds for their particular acylated sugar moieties. CONCLUSIONS: The method described is effective for obtaining a comprehensive phytochemical profile of plants containing unstable acylated flavonoids. The method is also useful for constructing the chromatographic fingerprint of the minority medicine -O. racemosa Turcz for quality control.


Subject(s)
Chromatography, High Pressure Liquid/methods , Flavonoids/analysis , Glucosides/analysis , Oxytropis/chemistry , Spectrometry, Mass, Electrospray Ionization/methods , China , Flavonoids/chemistry , Flavonoids/isolation & purification , Glucosides/chemistry , Glucosides/isolation & purification , Molecular Structure , Plants, Medicinal/chemistry , Reproducibility of Results , Spectrophotometry, Ultraviolet
12.
Pest Manag Sci ; 79(1): 55-67, 2023 Jan.
Article in English | MEDLINE | ID: mdl-36067067

ABSTRACT

BACKGROUND: Acyrthosiphon pisum Harris is the most destructive pest worldwide because of its ability to feed on plants directly and transmit plant viruses as a vector. This study aims to identify triterpenoid saponins from Oxytropis hirta Bunge as biopesticides to control aphids. RESULTS: Three new azukisapogenol triterpenoid saponins (1-3), a new pinoresinol lignan glycoside (8), and four known saponins (4-7) were identified from the root of O. hirta. Compounds 4-7 displayed significant aphicidal activities against A. pisum with oral toxicities (LC50  = 51.10-147.43 µg/mL, 72 h), deterrent effects (deterrence index = 1.00, 100-200 µg/mL, 24 h), and aphid reproduction inhibitory effects (inhibition rates = 75.91-86.73%, 400 µg/mL, 24 h), respectively. The carboxyl groups at C-3 GlcA and C-30 were functional groups for their aphicidal activities. The toxic symptoms caused by the optimal 5 involved insect body-color changes from light green to dark or gray-green, and then brown until death. The intestinal cavity, apical microvilli, nuclei, mitochondria, and electron dense granules in the midgut tissues of A. pisum were the target sites showing aphicidal activity. The suppression of pepsin and α-amylase, and the activation of lipase and trypsin could be the signs of organelle damage in the midgut tissues. CONCLUSION: Azukisapogenol triterpenoid saponins from O. hirta could be used as biopesticides to control aphids for their multiple efficacies, including oral toxicity, deterrent activity, and reproduction inhibitory activity. The toxic symptoms involved insect body-color changes. Midgut tissues and their related enzymes were the targets for saponins showing aphicidal activities. © 2022 Society of Chemical Industry.


Subject(s)
Aphids , Oxytropis , Saponins , Animals , Aphids/drug effects , Oxytropis/chemistry , Triterpenes/chemistry , Saponins/chemistry , Saponins/pharmacology , Insecticides/chemistry , Insecticides/pharmacology
13.
J Nat Prod ; 75(7): 1359-64, 2012 Jul 27.
Article in English | MEDLINE | ID: mdl-22775441

ABSTRACT

Five new 3-hydroxy-3-methylglutaryl (HMG) flavonol 3-O-glycosides, named oxytroflavosides A-E (1-5), and two new rhamnocitrin 3-O-glycosides, oxytroflavosides F and G (6 and 7) were isolated from the n-BuOH-soluble fraction of an EtOH extract of Oxytropis falcata together with seven known kaempferol glycosides (8-14), of which six were isolated from the genus Oxytropis for the first time. The structures of these compounds were elucidated by spectroscopic techniques and chemical methods. The absolute configuration of HMG in compounds 1-5 was determined to be S through spectroscopic analysis of the mevalonamide obtained by amidation and reduction of the HMG moiety. Compounds 1-10 were evaluated for anti-inflammatory activities using lipopolysaccharide-induced RAW 264.7 cells, but none of them showed inhibitory effects on NO production.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/isolation & purification , Drugs, Chinese Herbal/isolation & purification , Flavonols/isolation & purification , Glycosides/isolation & purification , Oxytropis/chemistry , Animals , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Drugs, Chinese Herbal/chemistry , Drugs, Chinese Herbal/pharmacology , Flavonols/chemistry , Flavonols/pharmacology , Glycosides/chemistry , Glycosides/pharmacology , Lipopolysaccharides/pharmacology , Mice , Molecular Structure , Nitric Oxide/biosynthesis
14.
J Ethnopharmacol ; 285: 114858, 2022 Mar 01.
Article in English | MEDLINE | ID: mdl-34826543

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Idiopathic pulmonary fibrosis (IPF) is an interstitial lung disease with unknown etiology. Oxytropis falcata Bunge (O. falcata) is a 1-35 cm high perennial clustered herb, also known as edaxia, has viscosity and a special smell, and is mainly distributed in the western areas of China. The root of O. falcata has a diameter of 6 mm, is straight and deep, dark red and its stems are shortened, woody and multibranched. O. falcata has heat-clearing, detoxification, analgesic, anti-inflammatory, antibacterial, hemostatic and antitumor activities. Furthermore, O. falcata has excellent anti-inflammatory and analgesic effects, and it is one of the three major anti-inflammatory drugs in Tibetan medicine, known as "the king of herbs". Total flavonoids of Oxytropis falcata Bunge (FOFB) were previously extracted, and their pharmacological activities are consistent with those of the whole herb. In this study, FOFB was extracted from O. falcata by ethanol extraction, and the mechanism of FOFB on IPF was verified by in vivo and in vitro experiments. AIM OF THE STUDY: In this study, we aimed to observe the effects of FOFB on idiopathic pulmonary fibrosis. MATERIALS AND METHODS: In in vivo experiments, an IPF rat model was established by bleomycin induction. The rats were treated with FOFB (100, 200, 400 mg kg-1·d-1) for 4 weeks. Masson staining and the expression of TGF-ß, p-Smad2, p-Smad3 and Smad7 in the lung tissue of rats were detected. In in vitro experiments, we perfused normal rats with FOFB (100, 200, 400 mg kg-1·d-1) and obtained the corresponding drug-containing serum. The HFL-1 cell model induced by TGF-ß1 was used to detect the corresponding indices through intervention with drug-containing serum. The best intervention time for drug-containing serum was detected by the CCK-8 method. Changes in apoptosis, cytoskeleton and rough endoplasmic reticulum structure were detected. Finally, the expression of TGF-ß, p-Smad2, p-Smad3 and Smad7 in cells was examined. RESULTS: In vivo, Masson staining indicated that the degree of pulmonary fibrosis increased significantly, the expression of TGF-ß, p-smad2 and p-Smad3 increased significantly, and the expression of Smad7 decreased in the model group. We found that the degree of pulmonary fibrosis gradually decreased and that the inhibition of the TGF-ß/Smad signaling pathway became more obvious with increasing FOFB dose. FOFB (400 mg kg-1·d-1) significantly improved the degree of pulmonary fibrosis in rats. In in vitro experiments, the CCK-8 results showed that 120 h was the best intervention time for drug-containing serum. In the model group, there was no obvious apoptosis or changes in microfilaments and microtubules, the number of rough endoplasmic reticulum increased, and the expression of TGF-ß, p-Smad2 and p-Smad3 increased significantly, while the expression of Smad7 decreased significantly. We found that with the increase in drug-containing serum concentration, the apoptosis, cytoskeleton and degree of destruction of the rough endoplasmic reticulum in the HFL-1 cell model also increased, and the inhibition of the TGF-ß/Smad signaling pathway became more pronounced; the effect of the drug-containing serum administered with FOFB (400 mg kg-1·d-1) was the most significant. CONCLUSIONS: The results suggest that FOFB can improve the occurrence and development of IPF. The effect of FOFB on IPF may be mediated by inhibition of the TGF-ß1/Smad signaling pathway.


Subject(s)
Flavonoids/therapeutic use , Oxytropis/chemistry , Phytotherapy , Pulmonary Fibrosis/drug therapy , Smad Proteins/metabolism , Transforming Growth Factor beta1/metabolism , Animals , Antibiotics, Antineoplastic/toxicity , Bleomycin/toxicity , Cell Line , Female , Gene Expression Regulation/drug effects , Humans , Male , Plant Extracts/chemistry , Random Allocation , Rats , Rats, Sprague-Dawley , Signal Transduction , Smad Proteins/genetics , Specific Pathogen-Free Organisms , Transforming Growth Factor beta1/genetics
15.
J Ethnopharmacol ; 290: 115066, 2022 May 23.
Article in English | MEDLINE | ID: mdl-35122975

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Oxytropis falcata Bunge is a legume distributed in Northwest China, which is mainly used to treat knife wounds and inflammation. Quercetin is a bioactive flavonoid in O. falcata and becomes a promising healing compound for its angiogenic and anti-inflammatory activities. However, the healing mechanism of quercetin in cutaneous wound remains elusive. AIM OF THE STUDY: The purpose of this study was to evaluate the healing effect of quercetin on cutaneous wound models in vivo and in vitro, and to reveal the Wnt/ß-catenin pathway and Telomerase reverse transcriptase (TERT) involved mechanisms. MATERIALS AND METHODS: The effects of quercetin on the proliferation and migration of 4 kinds of skin cells were determined by CCK-8 and scratch assay. The wound-healing capacity of quercetin was evaluated in cutaneous wound model of C57BL/6 mice and the wound healing degree was observed by histological staining. The expressions of inflammatory factors, growth factors and the related proteins were detected via Western blot and RT-qPCR analyses. The molecular docking was adopted to evaluate the binding ability of quercetin and TERT. RESULTS: Quercetin could promote both proliferation and migration of fibroblasts, and enhance cutaneous wound healing capacity in mice. Compared to the control group, the wound healing rates in low (1.5 mg/mL), medium (3.0 mg/mL) and high dose (6.0 mg/mL) quercetin groups reached 94.67%, 97.31% and 98.42%, respectively. Moreover, the dermal structure in quercetin treated mice restored normal and the content of collagen fiber became abundant after administration. The levels of inflammatory factors, including tumor necrosis factor-α, interleukin-1ß and interleukin-6 were significantly reduced after quercetin administration. Among which, the level of IL-1ß in cutaneous wound was 0.007 times higher than that of the control group when treated with quercetin of high dose (6.0 mg/mL). The improved level of GSH in quercetin treated cutaneous wounds also indicated its higher antioxidant ability. In addition, dose-dependent positive associations were found in the expression levels of vascular endothelial growth factor, fibroblast growth factor and alpha smooth muscle actin in quercetin treated cutaneous wounds. The significantly upregulated protein levels of Wnt and ß-catenin further indicated the important role of quercetin in promoting wound healing in mice. According to molecular docking analysis, the formed hydrogen bonds between quercetin and Ala195, Gln308, Asn369 and Lys372 residues of TERT also indicated the indispensable role of TERT in improving wound healing capacity. CONCLUSION: Quercetin effectively promoted cutaneous wound healing by enhancing the proliferation and migration of fibroblasts, as well as inhibiting inflammation and increasing the expression of growth factors in mice via Wnt/ß-catenin signaling pathway and TERT. It provides a basis for a more thorough understanding of mechanism of action of O. falcata Bunge in the treatment of knife wounds and burns.


Subject(s)
Oxytropis/chemistry , Quercetin/pharmacology , Telomerase/drug effects , Wnt Signaling Pathway/drug effects , Wound Healing/drug effects , Animals , Cell Movement/drug effects , Cell Proliferation/drug effects , China , Dose-Response Relationship, Drug , Fibroblast Growth Factors/drug effects , Humans , Inflammation Mediators , Interleukin-1beta/drug effects , Interleukin-6/metabolism , Male , Mice , Mice, Inbred C57BL , Molecular Docking Simulation , Skin/drug effects , Tumor Necrosis Factor-alpha/drug effects , Vascular Endothelial Growth Factor A/drug effects
16.
Phytochem Anal ; 22(2): 124-7, 2011.
Article in English | MEDLINE | ID: mdl-20799276

ABSTRACT

INTRODUCTION: Swainsonine, a polyhydroxy indolizidine alkaloid and known glycosidase inhibitor, is found in a number of different plants that cause a lysosomal storage disease known as locoism in the western USA. Most recently swainsonine has been analysed by LC-MS/MS after sample extraction and preparation from ion-exchange resins. OBJECTIVE: To compare previously published sample preparation procedures with several new alternative procedures to provide methods using either commercially available solid-phase extraction equipment or procedures which significantly reduce sample preparation time. METHODOLOGY: A previously reported and validated sample preparation method using ion-exchange resin was compared with methods using a commercially available solid-phase extraction cartridge, a solvent partitioning procedure or a single solvent extraction procedure using one of two solvents. Twenty different plant samples of varying swainsonine concentrations were prepared in triplicate and analysed by LC-MS/MS. The measured concentration of swainsonine was then statistically compared between methods. RESULTS: There were no statistically significant differences found between four of the five different sample preparation methods tested. CONCLUSION: A commercially available SPE cartridge can be used to replace the previously used ion-exchange resin for swainsonine analysis. For very rapid analyses the SPE procedure can be eliminated and a simple, single solvent extraction step used for sample preparation.


Subject(s)
Astragalus Plant/chemistry , Enzyme Inhibitors/isolation & purification , Oxytropis/chemistry , Plant Extracts/isolation & purification , Swainsonine/isolation & purification , Chromatography, High Pressure Liquid , Enzyme Inhibitors/analysis , Enzyme Inhibitors/chemistry , Glycoside Hydrolases/antagonists & inhibitors , Plant Extracts/analysis , Solid Phase Extraction , Swainsonine/analysis , Swainsonine/chemistry , Tandem Mass Spectrometry , United States
17.
Zhongguo Zhong Yao Za Zhi ; 36(9): 1227-30, 2011 May.
Article in Zh | MEDLINE | ID: mdl-21842655

ABSTRACT

OBJECTIVE: To investigate the influences of extracts of Oxytropis falcata on proliferation of SMMC-7721 cells and expression of MMP-2 (matrix metalloproteinase-2). METHOD: SMMC-7721 cells were treated for 24 h with five fractions obtained from 0. falcata in different concentrations. Inhibition on proliferation of the SMMC-7721 cells was assessed by MT method. Secretion of MMP-2 was measured by ELISA in the supernatant of SMMC-7721 cells treated with fractions of essential oil and total flavonoids for 24 h. Transcription of mRNA of MMP-2 was detected by Real-time PCR. RESULT: In MT assay, essential oil and total flavonoids showed potential antiproliferative activity on SMMC-7721 in a concentration dependent manner. Data of ELISA showed that fraction of essential oil suppressed secretion of MMP-2 significantly. Results of Real-time PCR indicated that both essential oil and total flavonoids restrained expression of mRNA of MMP-2. CONCLUSION: It suggested that essential oil and total flavonoids of O. falcata inhibit proliferation of SMMC-7721 cells through down-regulating secretion and expression of MMP-2 in cells. However, further experiments are necessary to carry out to investigate the potential mechanism.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Carcinoma, Hepatocellular/metabolism , Drugs, Chinese Herbal/pharmacology , Matrix Metalloproteinase 2/metabolism , Oxytropis/chemistry , Cell Line, Tumor , Cell Proliferation/drug effects , Enzyme-Linked Immunosorbent Assay , Humans , Polymerase Chain Reaction
18.
Zhongguo Zhong Yao Za Zhi ; 36(10): 1362-5, 2011 May.
Article in Zh | MEDLINE | ID: mdl-21837984

ABSTRACT

OBJECTIVE: To examine apoptosis of SMMC-7721 hepatocarcinoma cells induced by total flavonoids of Oxytropis falcata (TFOF) and its preliminary mechanism. METHOD: SMMC-7721 cells were treated for 24 h with TFOF in different concentrations. Inhibition on proliferation of SMMC-7721 cells was assessed by MTT assay. The morphology of treated SMMC-7721 cells was observed by optical microscope. Effect of TFOF on the nuclear morphology of cells was analyzed using Hoechst 33258 staining by fluorescence microscope. Annexin V-FITC/PI staining and flow cytometric measurement were used for investigating the effect of TFOF on induction of apoptosis in SMMC-7721 cells and cell cycle analysis. RESULT: The results of MTT assay showed that TFOF could induce cytotoxicity in SMMC-7721 cells in a dose-dependent manner. Hoechst 33258 staining analysis indicated that TFOF caused typical characteristics of apoptotic programmed cell death, such as cell shrinkage, apoptotic body formation etc. Flow cytometric analysis demonstrated that TFOF caused a dose-dependent apoptosis of SMMC-7721 cells and arrested cell cycle in G1 phase. CONCLUSION: It suggested that TFOF inhibit proliferation of SMMC-7721 cells by inducing apoptosis of the cells and arresting cell cycle in G1 phase.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Apoptosis/drug effects , Carcinoma, Hepatocellular/physiopathology , Drugs, Chinese Herbal/pharmacology , Liver Neoplasms/physiopathology , Oxytropis/chemistry , Carcinoma, Hepatocellular/drug therapy , Cell Cycle/drug effects , Cell Line, Tumor , Humans , Liver Neoplasms/drug therapy
19.
Zhong Yao Cai ; 34(9): 1396-8, 2011 Sep.
Article in Zh | MEDLINE | ID: mdl-22260009

ABSTRACT

OBJECTIVE: To study the pharmacokinetics of Oxytropis falcate total flavonoids ointment after transdermal administration in rats. METHODS: The content of 2',4'-dihydroxychalcone (TFC) in plasma was determined by high performance liquid chromatography. The concentration was determined at various time and the data was processed by 3P97. RESULTS: TFC behaved as a one-compartment and a two-compartment model after transdermal administration of total Oxytropis falcate total flavonoids ointment and solution, respectively. And the C(max) of ointment was improved about 3 times compared with that of the solution. CONCLUSION: The results show that the ointment possesses sustained release property and significantly prolong the degradation half life of TFC. The ointment is benefit to improve the analgesic and anti-inflammatory activity after transdermal administration.


Subject(s)
Chalcones/pharmacokinetics , Flavonoids/pharmacokinetics , Ointments , Oxytropis/chemistry , Skin/metabolism , Administration, Cutaneous , Animals , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Area Under Curve , Biological Availability , Chalcones/administration & dosage , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal/chemistry , Drugs, Chinese Herbal/pharmacokinetics , Flavonoids/administration & dosage , Flavonoids/pharmacology , Rats , Skin Absorption , Solutions , Time Factors
20.
Zhong Yao Cai ; 34(3): 415-20, 2011 Mar.
Article in Zh | MEDLINE | ID: mdl-21823462

ABSTRACT

OBJECTIVE: To study the protective effects of the cream of the total flavonoids from Oxytropis falcata on the destructed skin of mice induced by moderate-wave ultraviolet (UVB) irradiation. METHODS: Dorsal skin of Wistar mice were treated with the cream of the total flavonoids from Oxytropis falcata and then irradiated with UVB in the dosage of 5 min once a day for one week. The tissue of skin was pathological diagnosed and the activities or contents of superoxide dismutase (SOD), malondialdehyde (MDA), hydroxyproline (Hyp), glutathione peroxidease (GSH-Px), glutathione (GSH), glutathion-s-transferase (GST), catalase (CAT) and hydroxy radical (*OH) were determined with chromatometry. RESULTS: The ultraviolet protective effects of the cream could be observed with appearance and pathology examine. The cream could increase the activities of SOD (P < 0.001), GSH-Px (P < 0.001), GST (P < 0.05) and CAT (P < 0.01), raise the content of Hyp (P < 0.001) significantly. The cream could also decrease the contents of MDA and *OH (P < 0.001), and the activities of GSH significantly (P < 0.001). CONCLUSION: The cream of the total flavonoids from Oxytropis falcata has protective effect on the destructed skin of mice induced by moderate-wave ultraviolet (UVB) irradiation.


Subject(s)
Antioxidants/pharmacology , Flavonoids/pharmacology , Radiation-Protective Agents/pharmacology , Skin/drug effects , Skin/radiation effects , Ultraviolet Rays/adverse effects , Animals , Antioxidants/administration & dosage , Body Weight/drug effects , Disease Models, Animal , Female , Glutathione Peroxidase/metabolism , Glutathione Transferase/metabolism , Hydrogen Peroxide/metabolism , Malondialdehyde/metabolism , Oxidative Stress , Oxytropis/chemistry , Random Allocation , Rats , Rats, Wistar , Skin/metabolism , Skin/pathology , Superoxide Dismutase/metabolism
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