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1.
Acta Pharmaceutica Sinica ; (12): 441-445, 2022.
Article in Chinese | WPRIM | ID: wpr-922937

ABSTRACT

Four triterpenoids were isolated and purified from the 95% ethanol extract of Maytenus guangxiensis by silica gel column chromatography, Sephadex LH-20 column chromatography, MCI column chromatography and preparative RP-HPLC. Their structures were determined from their physicochemical properties and spectral data. They were identified as maytguanone A (1), maytguanone B (2), 11α-methoxyurs-12-ene-1β,3β-diol (3), lup-20(29)-ene-3β,11α-diol (4). Compounds 1 and 2 are new triterpenoids, along with compounds 3 and 4 were isolated from M. guangxiensis for the first time. The cytotoxicity of compounds 1, 3 and 4 was evaluated using the MTT procedure with three cancer cell lines. The results show that compound 3 displayed good inhibitory effects against HeLa, with an IC50 of 10.68 μmol·L-1.

2.
Article in Chinese | WPRIM | ID: wpr-888185

ABSTRACT

This study investigated the protective effect of total triterpenoids from Chaenomeles speciosa against Helicobacter pylori(Hp)-induced gastritis in mice and explored its possible mechanism. The chronic atrophic gastritis(CAG) model mice were randomly divided into four groups of model, total triterpenoids from C. speciosa(50 and 100 mg·kg~(-1)) and triple therapy, with C57 BL/6 J mice without Hp infection taken as the normal group. Mice in the treatment groups were given corresponding drugs once a day for 4 weeks. Then the following indexes were detected: the contents of reactive oxygen species(ROS), monocyte chemotactic protein 1(MCP-1), keratinocyte chemokines(KC), TNF-α, IL-1β, IL-6, IL-18, IL-4 and IL-10 in blood and gastric tissue, the activities and contents of LDH, MPO, SOD, GSH-Px, CAT and MDA in gastric tissue and the activities of β-glucuronidase, β-galactosidase, cathepsins B and D in blood, gastric tissue and lysosome. Besides, the mRNA expression levels of Toll-like receptor 4(TLR4), myeloid differentiation factor 88(MyD88), Bcl-2, Bcl-xl, Bax and Bad in gastric tissue were determined by quantitative real-time PCR. Western blot was employed to detect the protein expression levels of TLR4, MyD88, p-IKKβ, p-IκBα, NOD-like receptor 3(NLRP3), apoptosis-associated speck-like protein(ASC), pro-caspase-1, caspase-1, thioredoxin-interacting protein(TXNIP), pro-IL-1β, pro-IL-18, Bcl-2, Bcl-xl, Bax, Bad, cytochrome C, apoptotic protease-activating factor-1(Apaf-1), pro-caspase-9, pro-caspase-3, cleaved-caspase-9, cleaved-caspase-3, poly(ADP-ribose) polymerase 1(PARP-1), cleaved-PARP-1 and cytosol and nucleus NF-κB p65 in gastric tissue. The results indicated that the total triterpenoids from C. speciosa significantly suppressed Hp proliferation, alleviated the damage to gastric mucosa and improved lymphocyte infiltration and gland atrophy. They were also effective in reducing the activities of β-glucuronidase, β-galactosidase, cathepsins B and D in blood and gastric tissue, elevating the activities of β-glucuronidase and cathepsin D in lysosomal organelles, decreasing the contents of ROS, MCP-1, KC, TNF-α, IL-1β, IL-6, IL-18 in blood, MDA content and MPO and LDH activities in gastric tissue and increasing the contents of IL-4 and IL-10 in blood and activities of SOD, CAT and GSH-Px in gastric tissue. Other phenomena were also observed after the treatment with total triterpenoids from C. speciosa, including the down-regulation of the mRNA and protein expression levels of TLR4, MyD88, Bax and Bad, the protein expression levels of p-IKKβ, p-IκBα, NLRP3, ASC, pro-caspase-1, caspase-1, TXNIP, pro-IL-1β, pro-IL-18, cytochrome C, Apaf-1, cleaved-caspase-9, cleaved-caspase-3, cleaved-PARP-1 and nuclear NF-κB p65, reduction of p-IKKβ/IKKβ and p-IκBα/IκBα ratios and up-regulation of the mRNA and protein expression levels of Bcl-2 and Bcl-xl, up-regulation of pro-caspase-9, pro-caspace-3, cytosol NF-κB p65 protein expression levels and Bcl-2/Bax and Bcl-xl/Bad ratios in gastric tissue. These aforementioned results suggest that the total triterpenoids from C. speciosa have significant protective effects against CAG induced by Hp, and its mechanism may be related to enhancing the function of endogenous antioxidant system, suppressing the oxidative stress and inflammatory reaction induced by Hp, correcting lysosomal dysfunction and inflammatory activation of TLR4/NF-κB/NLRP3 inflammasome signaling pathway and thus inhibiting mitochondria-mediated apoptosis.


Subject(s)
Animals , Gastritis/drug therapy , Helicobacter pylori , Mice , NF-kappa B/genetics , Rosaceae , Triterpenes
3.
Article in Chinese | WPRIM | ID: wpr-888052

ABSTRACT

The chemical constituents from the leaves of Ilex guayusa were investigated. Sixteen triterpenoids were isolated from the 95% ethanol extract of dried leaves of I. guayusa by silica gel, Sephadex LH-20, and ODS column chromatographies and semi-prepa-rative HPLC. Those triterpenoids were identified by NMR, HR-MS, and literature analysis: 3β-hydroxy-11α,12α-epoxy-24-nor-urs-4(23)-ene-28,13β-olide(1), 3β-hydroxy-24-nor-4(23),12-oleanadien-28-methyl ester(2), oleanolic acid(3), 3β,28-dihydroxy-12-oleanene(4), 2α,3β-dihydroxy-11α,12α-epoxy-24-'nor-olean-4(23)-ene-28,13β-olide(5), ursolic acid(6), 3β,23-dihydroxy ursolic acid(7), 3β,28-dihydroxy-12-ursene(8), 3β-28-nor-urs-12-ene-3,17-diol(9), 3β-hydroxyurs-11-ene-28,13β-olide(10), 13β,28-epoxy-3β-hydroxy-11-ursene(11), 3β-hydroxy-28,28-dimethoxy-12-ursene(12), 3β-hydroxy-24-nor-urs-4(23),12-dien-28-oic acid(13), 3β-hydroxy-24-nor-urs-4(23),12-dien-28-methyl ester(14), 2α,3β-dihydroxy-11α,12α-epoxy-24-nor-urs-4(23)-ene-28,13β-olide(15) and 2α,3β-dihydroxy-11α,12α-epoxy-24-nor-urs-4(23),20(30)-dien-28,13β-olide(16). Compounds 1-2 were new compounds, and compounds 4-5, 7 and 9-16 were isolated from I. guayusa for the first time.


Subject(s)
Drugs, Chinese Herbal , Ilex guayusa , Molecular Structure , Oleanolic Acid , Plant Leaves , Triterpenes
4.
Article in Chinese | WPRIM | ID: wpr-879019

ABSTRACT

Triterpenoids are one of the most active constituents in Ligustri Lucidi Fructus, but only oleanolic acid has been mostly studied. In recent years, a growing number of studies have shown that other triterpenes from Ligustri Lucidi Fructus also have various biological activities, so it is necessary to build up a detailed profile of the triterpenoids in Ligustri Lucidi Fructus. The chromatographic separation was performed on a C_(18) column(4.6 mm×250 mm, 5 μm) with mobile phase of methanol-acetonitrile-0.2% formic acid for gradient elution. The detection wavelength was set at 210 nm, with a flow rate of 0.5 mL·min~(-1), and the column temperature of 25 ℃. The HPLC fingerprint of triterpenoids in Ligustri Lucidi Fructus was built by testing 21 batches of samples from different sources. The structures of the total 15 common chromatographic peaks were elucidated with UHPLC-ESI-Orbitrap-MS/MS technique and six of them were identified as tormentic acid, pomolic acid, maslinic acid, botulin, oleanolic acid and ursolic acid by comparison to the reference substances. Under the same chromatographic condition, four main triterpenes(podocarboxylic acid, hawthorn acid, oleanolic acid and ursolic acid) were quantified and the results of system adaptability and methodology investigation all met the requirements of content determination. Meanwhile, with oleanolic acid(A) as the internal reference substance, quantitative analysis of multi-components by single marker(QAMS) method was used to analyze the above four components. The relative correction factor of oleanolic acid(B), hawthorn acid(C) and ursolic acid(D) to oleanolic acid was f_(B/A)=1.12, f_(C/A)=1.02 and f_(D/A)=0.88, respectively, and the relative retention values of these three to oleanolic acid was RRV_(B/A)=0.46, RRV_(C/A)=0.70 and RRV_(D/A)=1.03, respectively. The contents determined by two methods were similar. In conclusion, the method built in this paper is proved to be simple, reliable and specific for the simultaneous qualitative and quantitative analysis of the triterpenoids in Ligustri Lucidi Fructus, which can lay foundation for further assays of the triterpenoids in Ligustri Lucidi Fructus and the relative products.


Subject(s)
Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Fruit , Ligustrum , Tandem Mass Spectrometry , Triterpenes
5.
Acta Pharmaceutica Sinica B ; (6): 1676-1685, 2021.
Article in English | WPRIM | ID: wpr-888828

ABSTRACT

Fusidane-type antibiotics, represented by helvolic acid, fusidic acid and cephalosporin P

6.
Article in English | WPRIM | ID: wpr-888799

ABSTRACT

Six new tirucallane-type triterpenoids (1-6), along with ten known triterpenoids, were isolated from methylene chloride extract of the resin of Boswellia carterii Birdw. By the application of the comprehensive spectroscopic data, the structures of the compounds were clarified. The experimental electronic circular dichroism spectra were compared with those calculated, which allowed to assign the absolute configurations. Compounds 5 and 6 possesed a 2, 3-seco tirucallane-type triterpenoid skeleton, which were first reported. Their inhibitory activity against NO formation in LPS-activated BV-2 cells were evaluated. Compound 9 showed appreciable inhibitory effect, with an IC

7.
Article in Chinese | WPRIM | ID: wpr-862672

ABSTRACT

Objective::To analysis the chemical constituents in Sancao Baogan decoction by ultra-high performance liquid chromatography coupled with hybrid quadrupole-orbitrap mass spectrometry (UPLC-ESI-HRMSn). Method::The separation was performed on an ACQUITY UPLC BEH C18 column (2.1 mm×100 mm, 1.7 μm) by a gradient elution of methanol (A)-0.1% formic acid solution (B) (0-2 min, 5%A; 2-20 min, 5%-12%A; 20-35 min, 12%-40%A; 35-38 min, 40%A; 38-48 min, 40%-80%A; 48-50 min, 80%A). The flow rate was 0.3 mL·min-1 and the column temperature was set at 30 ℃, the injection volume was 10 μL. Electrospray ionization was applied and the data were collected via positive and negative ion modes. By using Xcalibur 3.0 software, the chemical constituents were analyzed based on the relative retention time, excimer ion peak and fragment ion peak of the compounds, as well as comparison with human metabolome database (HMDB), reference substances and literature data. Result::A total of 40 chemical components were identified from Sancao Baogan decoction, including 16 phenolic acids, 19 flavonoids, 2 anthraquinones, 1 triterpenoid, 1 sterol, and 1 monoterpenoid. Six compounds (dansensu, α-pinene, epigallocatechin, 2, 5-dihydroxybenzoic acid, naringenin and emodin) were reported for the first time from Sancao Baogan decoction. Conclusion::The established UPLC-ESI-HRMSn can quickly, accurately and comprehensively analyze the chemical constituents of Sancao Baogan decoction, which lays a foundation for the basic research of pharmacodynamic substances and quality control of this formula.

8.
Chinese Pharmaceutical Journal ; (24): 1512-1516, 2020.
Article in Chinese | WPRIM | ID: wpr-857584

ABSTRACT

OBJECTIVEP: To investigate the effect of flavonoids and triterpenoids on the function of organic anion transporting polypeptide 1B3. METHODS: Natural products such as flavonoids and triterpenoids are widely present in traditional Chinese medicine and daily diets. In the present study, CHO cells stably expressing OATP1B3 and its fluorescent substrate fluorescein methotrexate were employed to investigate the effect of 21 natural products on the function of OATP1B3. RESULTS: Mulberrin, glycyrrhetinic acid, glycyrrhizic acid, quercitrin, quercetin, and chrysanthemum stem-leaf flavonoids showed significant inhibitory effects on OATP1B3-mediated uptake of fluorescein methotrexate, with IC50 values being of 3.6, 3.8, 7.5, 9.0, 10.1 μmol•L-1, and 4.1 μg•mL-1, respectively. The IC50 value of glycyrrhetinic acid on OATP1B3 was comparable to its blood concentration in clinics, indicating an OATP1B3-mediated drug-drug interaction could occur. CONCLUSION: Some flavonoids and triterpenoids are OATP1B3 inhibitors. When patients take medications of OATP1B3 substrates, care should be taken to avoid coadmistration of drugs or food containing these inhibitors to circumvent the occurrence of adverse drug interactions.

9.
Article in Chinese | WPRIM | ID: wpr-846595

ABSTRACT

Objective: To compare the effects of different drying methods on the quality of Trichosanthis Pericarpium, and screen the suitable drying methods for its modern drying processing. Methods: The fresh Trichosanthis Pericarpium collected from Anhui were processed by traditional and modern drying processing methods [hot air drying (40, 50, 60, 70 ℃), microwave vacuum drying (40, 50, 60, 70 ℃; vacuum -0.08 MPa), short-wave infrared drying (50, 60, 70 ℃), vacuum -80 ℃ lyophilization, traditional solar drying, shadow drying]. Combined with the appearance of the samples after drying, the composition and content of the 40 resource chemical compositions [five kinds of flavonoids (rutin, luteoloside, apigenin-7-O-glucuronide, apigenin, tangeretin), three kinds of triterpenoids (cucurbitacin D, cucurbitacin B, cucurbitacin E)] and nutritional nourishing ingredients [two kinds of saccharides (glucose, fructose), eighteen kinds of amino acids (phenylalanine, L-leucine, iso-leucine, L-tryptophan, γ-aminobutyric acid, L-methionine, L-valine, L-proline, L-tyrosine, trans-4-hydroxy-L-proline, L-threonine, L-glutamic acid, L-glutamine, L-serine, L-asparagine, L-citrulline, L-arginine, L-lysine), and twelve kinds of nucleosides (thymidine, 2’-deoxyuridine, adenine, uridine, adenosine, 2’-deoxyinosine, inosine, cytosine, guanine, 2’-deoxyguanosine, cytidine, guanosine)] were evaluated for comprehensively evaluating the quality of the different samples. The best modern drying method for Trichosanthis Pericarpium was preferred by principal component analysis. Results: Among different dry samples, the content of medicinal ingredients and nutrient nourishing ingredients varied greatly, among which fructose and glucose content ranged from 9.78% to 21.32% and 4.46% to 15.63%, respectively. Samples of 70 ℃ microwave vacuum drying had the highest total amount of flavonoids and tetracyclic triterpenoids, while those of 40 ℃ hot air drying treatment were the lowest. Through comprehensive evaluation of 14 kinds of Trichosanthis Pericarpium samples obtained by different drying methods, it was found that samples of 70 ℃ hot air drying, 70 ℃ short-wave infrared drying, vacuum -80 ℃ lyophilization, 50 ℃ microwave vacuum drying and 60 ℃ hot air drying were better than the traditional solar drying. Conclusion: Combined with the appearance of the medicinal properties, color, texture, drying time and functional ingredients, it was recommended that 70 ℃ hot air drying method was the preferred conditions for production based on the current state of the equipment of company. Based on the development of new equipment in the future, short-wave infrared 70 ℃ drying can be used as the development direction of Trichosanthis Pericarpium. The study provided reference for the standardization and quality characteristics of production of Trichosanthis Pericarpium.

10.
Article in Chinese | WPRIM | ID: wpr-846575

ABSTRACT

Rhododendron molle is a plant of the Ericaceae family. It is commonly used in the treatment of rheumatoid arthritis. Modern pharmacological studies have confirmed that its diterpenoids are main medicinal ingredients with anti-inflammatory, analgesic and other pharmacological effects. Through reviewing domestic and foreign literatures, this review aims to provide a comprehensive overview of the research progress in the chemical constituents and pharmacological effects of R. molle, and briefly prospects research of the titled plant.

11.
Article in Chinese | WPRIM | ID: wpr-846554

ABSTRACT

Objective: To study the chemical constituents from Rhynchosia volubilis. Methods: The compounds were isolated and purified by a combination of various chromatographic techniques including silica gel, ODS, Toyopearl HW-40C, Sephadex LH-20, and semi-preparative HPLC chromatography. Their structures were identified by physicochemical properties and spectroscopic data. Results: Thirteen compounds were isolated from the petroleum ether extracts of R. volubilis and their structures were elucidated as (-)-sigmoidin E (1), lupinifolin (2), precatorin B (3), cajanone (4), sophoraisoflavanone B (5), 5,3’-dihydroxy-4’-methoxy-5’- γ,γ-dimethylallyl-2″,2″-dimethylpyrano [5,6:6,7] isoflavanone (6), genistein (7), licoisoflavone A (8), erylatissin B (9), neo-bavaisoflavone (10), lupeol (11), betulinic aldehyde (12), and clionasterol (13). Compounds 1-10 were all prenylated flavonoids, of which compounds 1-2 were dihydroflavones, compounds 3-6 were dihydroisoflavones, and compounds 7-10 were isoflavones. Compounds 11-12 were lupine triterpenoids, and compounds 13 was a sterol. Conclusion: Compounds 1, 5-6, 8-10, 12 and 13 are isolated from the genus for the first time, while compounds 1-3 and 5-13 are separated from this plant for the first time.

12.
Article in Chinese | WPRIM | ID: wpr-846521

ABSTRACT

Objective: Identification of chemical constituents from Gengen Qinlian Decoction by UPLC-LTQ-Orbitrap-MS. Methods: The analysis was performed on Dikma Endeavorsil C18 (100 mm × 2.1 mm, 1.8 μm) with mobile phase of 0.1% formic acid water solution (A)-acetonitrile (B) for gradient elution at a flow rate of 0.3 mL/min. The UPLC-LTQ-Orbitrap-MS was equipped with an Electrospray ionization ion probe and MS1 and MS2 data of samples were collected in positive and negative ion mode, respectively. Results: A total of 67 constituents were identified from Gegen Qinlian Decoction by reference substance identification, software prediction analysis and related literature reports, including 36 flavonoids, 12 alkaloids, four triterpenoids and triterpenoid saponins, and 15 other ingredients. Conclusion: In this study, UPLC-LTQ-Orbitrap-MS was used to systematically elucidate the chemical constituents of Gegen Qinlian Decoction, and the fragmentation characteristics of its main chemical constituents were preliminarily explained and summarized, which provided a reference for the quality control and mechanism research of Gegen Qinlian Decoction.

13.
Article in Chinese | WPRIM | ID: wpr-846422

ABSTRACT

Terminalia chebula is a traditional Chinese herbal medicine, which distributed in Yunnan, Guangdong, Guangxi, Tibet and etc. T. chebula is widely used in the clinical medicine of Chinese medicine and it plays a significant role in the Mongolian medicine and the Tibetan medicine. The chemical composition of T. chebula is rich and diverse, including phenolic acids, tannins, triterpenoids, aliphatics, flavonoids, volatile oils, amino acids, trace elements, carbohydrates and so on. Modern pharmacological studies have shown that T. chebula extract has many pharmacological activities, such as anti-oxidation, anti-cancer, anti-tumor, detoxification, antibacterial, strong heart, anti-inflammation, immunomodulation, anti-microbial, and promoting bronchial smooth muscle contraction. From the aspects of textual research, chemical composition characteristics, pharmacological action and so on, this paper expounds the research progress of T. chebula. According to the core concept of Q-marker, we predicted and analyzed the quality markers of T. chebula from the aspects of chemical composition characteristics, traditional efficacy, medicinal properties, pharmacokinetics, new clinical use and measurable composition. It provides reference for the quality evaluation of T. chebula.

14.
Article in Chinese | WPRIM | ID: wpr-846374

ABSTRACT

Ligustrum plants are important ornamental plants and medicinal plants, with important ornamental value and medicinal value. Ligustrum plants are complicated in chemical constituents and extensive pharmacological activities. The review is to present an overview about studies on chemical constituents and pharmacological activities of the Ligustrum plants, which can provide some foundations and references for the further study.

15.
Chinese Herbal Medicines ; (4): 214-223, 2020.
Article in Chinese | WPRIM | ID: wpr-842010

ABSTRACT

Kadsura coccinea belongs to medicinally important genus Kadsura from the Schisandraceae family. It has been used in traditional Chinese medicine (TCM) for the treatment of rheumatoid arthritis and gastroenteric disorders. The initial phytochemical work focused on the identification of some structurally novel and diverse natural products, which turned the attention of many researchers towards this plant. Thus far, 202 compounds have been reported in this plant. Lignans and terpenoids were found as the main chemical constituents of this plant. Some of the triterpenoids and sesquiterpenoids with novel structures are of particular interest for natural product researchers. The isolated compounds of this plant have shown different bioactivities including anti-tumor, anti-HIV, anti-inflammatory, nitric oxide (NO) production inhibitory and other pharmacological effects. This review systematically summarizes all the phytochemical and pharmacological work done so far on K. coccinea, and can be used as a reference for future research on this plant.

16.
Article in Chinese | WPRIM | ID: wpr-828405

ABSTRACT

The tirucallane-type triterpenoids, composed of six isoprene units, belong to a group of tetracyclic triterpenoids. Although the naturally-derived tirucallane-type triterpenoids were found in a small amount, the kind of compounds showed various structures, which consist of apo-type, linear said-chain-type and cyclolike said-chain-type and broad bioactivities, such as cytotoxicity, anti-inflammation, antioxidation and anti-plasmin, etc. This paper summarized origins, structures and bioactivities of tirucallane-type triterpenoids in recent ten years. The future research and exploration of tirucallane-type triterpenoids were discussed and prospected.


Subject(s)
Antineoplastic Agents, Phytogenic , Molecular Structure , Triterpenes
17.
Article in English | WPRIM | ID: wpr-827791

ABSTRACT

Triterpenoids have been described in Andrographis paniculata. Oleanolic acid exhibits high biological activity and is widely used in the clinic, and β-sitosterol not only has good biological activity but also plays an important physiological role in plants. However, analysis of the biosynthetic pathway of triterpenoids in Andrographis paniculata has not been reported. Here, we provide the first report of the isolation and identification of nine 2, 3-oxidosqualene cyclases (ApOSC3 to ApOSC11) from A. paniculata. The results showed that ApOSC4 represented a monofunctional synthase that could convert 2, 3-oxidosqualene to β-amyrin. ApOSC5 as a bifunctional 2, 3-oxidosqualene cyclases, could transfer 2, 3-oxidosqualene to β-amyrin and α-amyrin. ApOSC6 to ApOSC8 composed the multifunctional 2, 3-oxidosqualene cyclases that could convert 2, 3-oxidosqualene to β-amyrin, α-amyrin and one or two undetermined triterpenoids. This study provides a better understanding of the biosynthetic pathway of triterpenoids in A. paniculata, and the discovery of multifunctional 2, 3-oxidosqualene cyclases ApOSC5 to ApOSC8 of the facilitates knowledge of the compounds diversity in A. paniculata.

18.
China Pharmacy ; (12): 2196-2201, 2020.
Article in Chinese | WPRIM | ID: wpr-825647

ABSTRACT

OBJECTIVE:To i mprove the transfer rate and purity of oleanolic acid and ursolic acid in total triterpenoids from Ligustrum lucidum ,so as to optimize the purification technology. METHODS :Oleanolic acid and ursolic acid were used as representative components of total triterpenoids ,and their contents were determined by HPLC. The determination was performed on Thermo BDS Hypersil C 18 column with mobile phase consisted of methanol- 0.02% ammonium acetate solution (80∶20,V/V)at the flow rate of 1.0 mL/min. The detection wavelength was set at 210 nm,and column temperature was 30 ℃. The sample size was 20 μ L. In single factor tests,using transfer rate of oleanolic acid and ursolic acid as index ,the effects of water precipitation temperature and time ,the amount of redissolved ethanol on the purification technology was investigated ;using transfer rate and purity of two components as indexes ,the effects of the amount of activated carbon and volume fraction of crystallization ethanol were investigated. Based on it ,using the amount of redissolved ethanol and activated carbon ,volume fraction of crystallization ethanol as factors ,Box-Behnken response surface methodology was used to optimize the purification technology ,and validation tests were performed. RESULTS :The optimal purification technology was adding 4-fold(mL/g,the same below )water in L. lucidum concentrated solution ,placing for 2 hours at 0 ℃(water precipitation );adding 1-fold ethanol to dissolve (redissolution); adding 4% activated carbon (edulcoration);finally adding water to adjust the volume fraction of ethanol to 80%,placing at 4 ℃ for 12 hours(crystallization),centrifuging and drying. The results of 3 times of validation tests showed that the transfer rates of oleanolic acid and ursolic acid in total triterpenoids prepared by optimized technology were 61.11% and 65.78%,the purities of them were 53.44% and 19.79%,and RSDs were both lower than 3%. CONCLUSIONS :The optimized purification technology has high extraction efficiency and simple operation ,which can be used for industrial production of purification of total triterpenoids from L. lucidum and the development of corresponding preparations.

19.
China Pharmacy ; (12): 2101-2106, 2020.
Article in Chinese | WPRIM | ID: wpr-825189

ABSTRACT

OBJECTIVE:To establish a method for th e content determination of 7 kinds of triterpenoids in Poria cocos ,and to compare the differences of the above components in P. cocos from different habitats ,so as to provide reference for the quality control of P. cocos . METHODS :Using 36 batches of P. cocos from different habitats as samples ,HPLC method was used for content determination of dehydrotomorphic acid , polyporhinic acid C , 3-epidehydrotomorphic acid , 3-O-acetyl-16 α-hydroxy-hydrogenolysaccharic acid ,dehydrotomorphic acid ,pachymic acid and dehydrotrametenolic acid. The column was performed on Thermo Acclaim 120 C18 with mobile phase consisted of acetonitrile-phosphoric acid water (gradient elution )at the flow rate of 1 mL/min. The detection wavelength was set at 210 nm. The column temperature was 30 ℃,and the injection volume was 20 μL. SPSS 21.0 statistical software was used for cluster analysis of 36 batches of P. cocos from different habitats. RESULTS : The linearity of 7 triterpenoids was good in the range of their mass concentration (all r≥0.999 0);average recoveries were 96.74%-104.04%(RSD=0.54%-1.55%,n=6). RSDs of precision ,and reproducibility stability (24 h)tests were all lower than 3.0%(n=6). RSD of durability test was lower than 5.0%(n=2). There were some differences in the single content of 7 indicator components among samples from different habitats ,but the total content difference was not obvious (the total content of most samples was in the range of 1.3-1.9 mg/g). After cluster analysis ,36 batches of sample were clustered into 5 categories,i.e. S 27 was clustered into class Ⅰ;S30 and S 34 were clustered into class Ⅱ;S2,S8 and S 9 were clustered into class Ⅲ;S10,S11,S12 and S 14 were clustered into class Ⅳ;and the remaining 26 batches of samples were clustered into class Ⅴ. CONCLUSIONS :The method is simple ,and has good precision ,repeatability and durability. It can be used for the simultaneous determination of above 7 components in P. cocos . There has no significant difference in the quality of P. cocos from different habitats. The content of P. cocos in most producing areas is uniform in content and stable in quality ,only a few of them are different. Δ 基金项目 :国家重点研发计划中医药现代化研究重点专项

20.
Article in Chinese | WPRIM | ID: wpr-773089

ABSTRACT

The aim of this paper was to observe the combination therapy with total triterpenoids of Chaenomeles speciosa and omeprazole on indomethacin-induced gastric ulcer in rats, and explore its possible mechanism. Rats were randomly divided into normal group, model group, omeprazole monotherapy(3.6 mg·kg~(-1)) group, total triterpenoids of C. speciosa monotherapy(100 mg·kg~(-1)) group, total triterpenoids of C. speciosa and omeprazole combination therapy(100 mg·kg~(-1)+3.6 mg·kg~(-1)) group. Except for the normal group, the other groups were given indomethacin(20 mg·kg~(-1)) by oral once a day for 7 consecutive days. Then the treated groups were given corresponding drugs by gavage, once a day for 14 consecutive days. The next day after the last administration, half of the rats in each group were measured the gastric mucosal blood flow, gastric juice volume and serum TNF-α, IL-1β, IL-6, IL-4 and IL-10. After the remaining rats in each group were underwent pyloric ligation 4 hours after the last administration, the gastric endocrine volume, pH value and total acidity of gastric secretion were measured, then histological analysis was performed, MPO activity, cAMP content and histomorphological analysis were conducted. Real-time PCR was applied to detect the mRNA expressions of gastric tissue TNF-α,IL-1β, IL-6, IL-4, IL-10, VEGFA, A_(2A)R; the protein expressions of VEGFA, A_(2A)R, PKA, p-PKA, CREB, p-CREB, EGF, EGFR, p-EGFR, MUC6, TFF2 in gastric tissue were detected by Western blot. The results indicated that total triterpenoids of C. speciosa and omeprazole combination therapy might significantly increase gastric mucosal blood flow, gastric mucus volume, reduce gastric endocrine volume, secretion acidity and mucosal damage, decrease the levels of TNF-α,IL-1β and IL-6, increase the levels of IL-4 and IL-10 in blood and gastric tissue, inhibit the activity of MPO, increase the content of cAMP in gastric tissue, up-regulate the mRNA expressions of VEGFA, A_(2A)R and protein expressions of VEGFA, A_(2A)R, PKA, p-PKA, CREB, p-CREB, EGF, EGFR, p-EGFR, MUC6, TFF2 in gastric tissue, elevate p-PKA/PKA, p-CREB/CREB and p-EFGR/EFGR. Moreover, the combination therapy with total triterpenoids of C. speciosa and omeprazole was more obvious than those of two monotherapies. These aforementioned findings suggested that the combination therapy with total triterpenoids of C. speciosa and omeprazole on indomethacin-induced gastric ulcer have significant therapeutic effect on indomethacin induced gastric ulcer in rats, its mechanism might be related to regulating A_(2A)R/AKT/CREB, A_(2A)R/VEGFA, EGF/EGFR and MUC6/TFF2 signaling pathways, inhibiting pro-inflammatory factors, increasing gastric mucosal blood flow, up-regulating mucosal cell proliferation factors and promoting mucosal protective factors.


Subject(s)
Animals , Cytokines , Gastric Mucosa , Indomethacin , Omeprazole , Pharmacology , Phytochemicals , Pharmacology , Random Allocation , Rats , Rosaceae , Chemistry , Stomach Ulcer , Drug Therapy , Triterpenes , Pharmacology , Tumor Necrosis Factor-alpha
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