Phytochemical studies on the whole herb of Sphaerophysa salsula has resulted in the discovery of one new 8-isopentenyl isoflavone derivative, named sphaerosin s2 (3-(8-(2-hydroxypropan-2-yl)-3,4-dihydro-2H-furo[2,3-h]chromen-3-yl)-2,6-dimethoxyphenol) (1), along with four know 8-isopentenyl isoflavone derivatives (2-5). Compounds (2, 4 and 5) were isolated for the first time from this species. Their structures were elucidated on the basis of ESI-MS, UV, IR, 1D NMR and 2D NMR data.
To explore the medication regularity of Tibetan medicine in the treatment of spleen and stomach diseases, analyze the potential drug targets and interactions of the prescriptions, and reveal the mechanism of Tibetan medicine in the treatment of spleen and stomach diseases. The prescriptions in Tibetan medicine for treatment of spleen and stomach diseases were collected, and Traditional Chinese Medicine Inheritance Support System (TCMISS) was used to analyze the association rules between the herbs and discover the core herbs and new prescriptions. The integrated pharmacology platform V1.0 software was used to construct "herb-compound-target" network and investigate the interactions between various herbs and related pathways of Tibetan medicine Wuwei Shiliu powder in the treatment of spleen and stomach diseases. Among the 216 prescriptions of Tibetan medicine in the treatment of spleen and stomach diseases, pomegranate seed was used at a highest frequency (118 times), followed by white cardamom (107 times) and comatose (107 times). 12 new prescriptions were evolved by using the association rules (support>=34%, confidence>=0.85). 5 242 related drug targets and 20 related pathways were obtained from classic formula Wuwei Shiliu Powder (FDR<0.01). It was proposed that Tibetan medicine treatment for spleen and stomach diseases was mainly based on proliferation of "stomach fire" and the main drugs were for regulating Qi-flowing for strengthening spleen. The mechanism may be associated with regulation of digestive juice secretion, proton pump, mitochondria, regulation of intestinal digestion and immunity, the body's immunity to microorganisms function and other multiple targets and pathways to achieve the joint intervention.
Background: Dracocephalum heterophyllum was a traditional Tibetan medicine possesses various pharmacological effects involved in anti-inflammatory, antibacterial activities. However, its anti-hepatitis, antioxidant activity and bioactive compounds have not been reported, the objective of this research work was to investigate the pharmacological activity and bioactive compounds of D. heterophyllum extracts. Results: In the present study, the anti-hepatics and antioxidant activities of four D. heterophyllum extracts (i.e. petroleum ether extracts, ethyl acetate extracts, n-BuOH extracts, and water extracts) were conducted. The main chemical constituent of petroleum ether and ethyl acetate extracts were also isolated using chromatographic techniques and identified by NMR spectroscopic methods. The anti-hepatitis assay showed that the petroleum ether and ethyl acetate extracts of D. heterophyllum significantly prolonged the mean survival times and reduced the mortality of mouse hepatitis model induced by concanavalin A (ConA). The levels of alanine transaminase, aspartate transaminase in blood serum could be decreased obviously by ethyl acetate extracts compared with ConA group (P < 0.01). The histological analysis demonstrated that the ethyl acetate extracts could inhibit apoptosis and necrosis caused by ConA. In addition, the antioxidant activities of the four extracts of D. heterophyllum were measured by DPPH assay, ABTS assay, anti-lipidperoxidation assay, ferric reducing antioxidant power assay, ferrous metal ions chelating assay and determination of total phenolic contents. The results showed that the ethyl acetate extract had the highest antioxidant activities, followed by petroleum ether extract. Finally, nine mainly compounds were isolated from the Petroleum ether and ethyl acetate extracts, including four triterpenes: oleanolic acid ( 1), ursolic acid ( 2), pomolic acid ( 3), 2α- hydroxyl ursolic acid ( 4), three flavonoids: apigenin-7- O-rutinoside ( 5), luteolin ( 8), diosmetin ( 9) and two phenolic acids: rosmarinic acid ( 6), methyl rosmarinate ( 7). Conclusion: The Ethyl acetate extract of D. heterophyllum had the highest anti-hepatitis and antioxidants activities, followed by petroleum ether extract. The bioactive substances may be triterpenes, flavonoids and phenolic acids, the ethyl acetate extracts of D. heterophyllum may be possible candidates in developing anti-hepatitis medicine.
Background: Hypecoum leptocarpum Hook. f. et Thoms., which is used in traditional Tibetan medicine as an antipyretic, antitussive, analgesic, and anti-inflammatory agent, contains a variety of alkaloids that could be responsible for its analgesic and anti-inflammatory properties. Objective: The present study was designed to investigate the anti-inflammatory activity of the total alkaloids from H. leptocarpum (AHL) in vitro and to elucidate the chemical structure of the anti-inflammatory components in AHL. Materials and Methods: Chemical characterization was performed using liquid chromatography/quadrupole-time-of-flight mass and diode-array detector-high performance liquid chromatography. The anti-inflammatory effects of AHL were investigated by measuring the production of inflammatory cytokines using enzyme-linked immunosorbent assay and mRNA expression by real-time polymerase chain reaction in lipopolysaccharide-induced RAW 264.7 macrophages. Results: Chemical analysis of AHL revealed the presence of seven alkaloids, protopine (13.3%), cryptopine (1.5%), leptopidinine, leptocarpine, corydamine, dihydroleptopine, and oxohydrastinine. AHL significantly suppressed the production of nitric oxide (NO), interleukin-1 beta (IL-1 β), IL-6, and tumor necrosis factor-alpha (TNF-α) in LPS-induced RAW 264.7 cells. The maximum levels of suppression of NO, IL-1 β, IL-6, and TNF-α were 86.8% ± 2.2%, 70.1% ± 1.5%, 100.1% ± 2.5%, and 50.8% ± 3.6%, respectively. IC50values of suppression of cytokine production by AHL were 7.47 ± 2.81 μg/mL (NO), 0.12 ± 0.28 μg/mL (IL-1 β), 0.56 ± 0.37 μg/mL (IL-6), and 18.95 ± 5.23 μg/mL (TNF-α). AHL was also shown to downregulate mRNA expression of inducible NO synthase, IL-1 β, IL-6, and TNF-α in vitro. Conclusion: The study provides convincing evidence that AHL has strong anti-inflammatory activity. The potent activity is likely a result of synergy between the different alkaloids. Abbreviations used: The total alkaloids from H. leptocarpum: AHL; Nitric oxide: NO; Interleukin-1 beta IL-1β; Interleukin-6: IL-6; Tumor necrosis factor-alpha: TNF-α; Prostaglandin E2: PGE2; Inducible nitric oxide synthase: iNOS; Nonsteroidal anti-inflammatory drugs: NSAIDs; lipopolysaccharide: LPS; The total ion chromatograms: TIC; The liquid chromatography/quadrupole-time of flight: LC/Q-TOF; Nuclear factor-kappa B: NF-κB; Janus kinase-signal transducers and activators of transcription: JAK-STAT. [ABSTRACT FROM AUTHOR]
Bioactive equivalent combinatorial components play a critical role in herbal medicines. However, how to discover and enrich them efficiently is a question for herbal pharmaceuticals researchers. In our work, a novel two-dimensional reversed-phase/hydrophilic interaction high-performance liquid chromatography method was established to perform real-time components trapping and combining for preparation and isolation of coeluting components. Arenaria kansuensis was taken as an example, and solid-phase extraction coupled with liquid-liquid extraction as a simple and efficient method for enriching trace components, reversed phase column coupled with hydrophilic interaction liquid chromatography XAmide column as two-dimensional chromatography technology for isolation and preparation of coeluting constituents, enzyme-linked immune-sorbent assay as bio-guided assay, and anti-inflammatory bioactivity evaluation for bioactive constituents. A combination of 12 β-carboline alkaloids was identified as anti-inflammatory bioactive equivalent combinatorial components from A. kansuensis, which accounts for 1.9% w/w of original A. kansuensis. This work answers the key question of which are real anti-inflammatory components from A. kansuensis and provides a fast and efficient approach for discovering and enriching trace β-carboline alkaloids from herbal medicines for the first time. More importantly, the discovery of bioactive equivalent combinatorial components could improve the quality control of herbal products and inspire a herbal medicine based on combinatorial therapeutics.
• <b>Saxifraga tangutica</b> Engl. is a promising source of antioxidants against DPPH and FRAP. • The 50% ethanol extract of S. <b>tangutica</b> showed strong antioxidative activity against DPPH and FRAP. • Eight phenols were isolated from S. <b>tangutica</b>; all of the compounds are reported for the first time from this plant. • The antioxidative S. <b>tangutica</b> extracts and isolated phenols supports the antioxidant of this plant.<br><b>Saxifraga tangutica</b> Engl., is a medicinal herb that grows on the Qinghai-Tibet Plateau. Extracts and phenols from the Qinghai population have been subjected to antioxidative assays against DPPH radical-scavenging and reducing power (FRAP). The 50% ethanol extract showed strong antioxidative activity against DPPH and FRAP, with IC50 ± SEM [μg/mL] values of 9.38 ± 0.46 and 15.46 ± 0.52, respectively. The antioxidative activity-guided fractionations were performed according to the DPPH and FRAP screening results. Fourteen fractions from the 50% ethanol extract showed dissimilar antioxidative activity against DPPH and FRAP of 8.16 ± 0.76 ∼ 38.42 ± 0.58 μg/mL and 13.22 ± 0.68 ∼ 61.47 ± 0.49 μg/mL. The chemical assay-guided separation of the active fractions (fractions 3, 6, 7 and 8) led to eight phenols: protocatechuic aldehyde (<b>1</b>), ethyl gallate (<b>2</b>), rhododendrin (<b>3</b>), <b>p</b>-hydroxyacetophenone (<b>4</b>), rhododendrol (<b>5</b>), protocatechuic acid ethyl ester (<b>6</b>), frambinone (<b>7</b>) and ethylparaben (<b>8</b>). All phenols are reported here for the first time from <b>S. tangutica</b> Engl. Protocatechuic aldehyde (<b>1</b>), ethyl gallate (<b>2</b>), rhododendrin (<b>3</b>) and protocatechuic acid ethyl ester (<b>6</b>) showed strong antioxidative activities (IC50 ± SEM [mM] between 8.79 ± 0.15 and 4.25 ± 0.47 and between 6.15 ± 0.48 and 2.83 ± 0.49) against DPPH and FRAP.
BACKGROUND: Radix Gentianae Macrophyllae, commonly known as Qinjiao (in Chinese), is dried roots of medicinal plants that belong to Gentianaceae family and Gentiana genus. It has medically been used for the treatment of various diseases such as arthritis, stroke, facial paralysis, and scapulohumeral periarthritis in China since ancient times.PURPOSE: The aim of this paper is to provide a comprehensive and constructive overview of Qinjiao mainly containing Gentiana macrophylla Pall., Gentiana straminea Maxim., Gentiana crasicaulis Duthie ex Burk., and Gentiana daurica Fisch. in botany, traditional use, phytochemicals, pharmacology (biological activities and pharmacokinetics), quality control, and authentication according to the up-to-date data of available scientific literatures.
MATERIALS AND METHODS: All information regarding these four plants was collected from various academic search engines for example Google, Google Scholar, Web of Science, SciFinder, Pubmed, CNKI, and Wanfang. Additional information was obtained from botanical books, Chinese classic texts, and medical monographs.
RESULTS: So far 166 compounds have been isolated and identified from Qinjiao plants together with Gentiana tibetica King ex Hook. f., Gentiana siphonantha Maxim., Gentiana officinalis H. Smith, and Gentiana waltonii Burk. Their constituents are mainly classified into iridoid glycosides, triterpenes, flavones, sterols, benzene derivatives, etc. The pharmacological studies demonstrate that Qinjiao plants display a wide range of bioactivities e.g. anti-inflammatory, anti-oxidant, hepato-protective, cardio- and neuro-protective, insecticidal, and anti-influenza effects. The conventional quality control is performed by determination of the concentration of some compounds, e.g., gentiopicroside, or establishment of the fingerprint. In addition to seed propagation, tissue culture technology has been used to address the limited supplies and guarantee the sustainable development of Qinjiao in the experimental scale.
CONCLUSIONS: Although the identification of compounds from Qinjiao and demonstration of medicinal uses in vitro and in vivo have been carried out, various other studies on these plants should deserve our more attention. More efforts should be concentrated on the underlying mechanisms of their beneficial bioactivities. The proper toxic evaluation is indispensable to guarantee the safety, efficacy, and eligibility for medical use. To sum up, the summarized achievements could highlight the importance of Qinjiao and provide a solid foundation for scientists not only to further exploit the therapeutic potentials, but also possibly develop novel drugs in the subsequent research.
BACKGROUND: Radix Gentianae Macrophyllae, commonly known as Qinjiao (in Chinese), is dried roots of medicinal plants that belong to Gentianaceae family and Gentiana genus. It has medically been used for the treatment of various diseases such as arthritis, stroke, facial paralysis, and scapulohumeral periarthritis in China since ancient times. PURPOSE: The aim of this paper is to provide a comprehensive and constructive overview of Qinjiao mainly containing Gentiana macrophylla Pall., Gentiana straminea Maxim., Gentiana crasicaulis Duthie ex Burk., and Gentiana daurica Fisch. in botany, traditional use, phytochemicals, pharmacology (biological activities and pharmacokinetics), quality control, and authentication according to the up-to-date data of available scientific literatures. MATERIALS AND METHODS: All information regarding these four plants was collected from various academic search engines for example Google, Google Scholar, Web of Science, SciFinder, Pubmed, CNKI, and Wanfang. Additional information was obtained from botanical books, Chinese classic texts, and medical monographs. RESULTS: So far 166 compounds have been isolated and identified from Qinjiao plants together with Gentiana tibetica King ex Hook. f., Gentiana siphonantha Maxim., Gentiana officinalis H. Smith, and Gentiana waltonii Burk. Their constituents are mainly classified into iridoid glycosides, triterpenes, flavones, sterols, benzene derivatives, etc. The pharmacological studies demonstrate that Qinjiao plants display a wide range of bioactivities e.g. anti-inflammatory, anti-oxidant, hepato-protective, cardio- and neuro-protective, insecticidal, and anti-influenza effects. The conventional quality control is performed by determination of the concentration of some compounds, e.g., gentiopicroside, or establishment of the fingerprint. In addition to seed propagation, tissue culture technology has been used to address the limited supplies and guarantee the sustainable development of Qinjiao in the experimental scale. CONCLUSIONS: Although the identification of compounds from Qinjiao and demonstration of medicinal uses in vitro and in vivo have been carried out, various other studies on these plants should deserve our more attention. More efforts should be concentrated on the underlying mechanisms of their beneficial bioactivities. The proper toxic evaluation is indispensable to guarantee the safety, efficacy, and eligibility for medical use. To sum up, the summarized achievements could highlight the importance of Qinjiao and provide a solid foundation for scientists not only to further exploit the therapeutic potentials, but also possibly develop novel drugs in the subsequent research.
Objective: To investigate the chemical constituent from the roots of Gentiana straminea.; Methods: The constituents were separated by microporous resin,silica gel,Sephadex LH-20 and preparative column chromatography and their structures were elucidated by NMR and MS spectral methods.; Results: Twelve chemical constituents were isolated from the roots of Gentiana straminea and their structures were identified as daucosterol( 1),β-sitosterol( 2),ursolic acid( 3),sweroside( 4),swertiamarin( 5),gentiopicroside( 6),6’-O-acetyl-gentiopicroside( 7),6’-O-β-D-glucopyranosyl-sweroside( 8),protocatech uic aldehyde( 9),protocatechuic acid( 10),methyl gallate( 11) and dibutyl phthalate( 12).; Conclusion: The compounds 8,9,10,11 and 12 are obtained from this plant for the first time.;
A phytochemical investigation of <b>Saxifraga tangutica</b> led to the isolation of 11 compounds, including eight diarylheptanoids (<b>1</b>-<b>6</b>, <b>10</b> and <b>11</b>) and three phenylpropanoids (<b>7</b>-<b>9</b>). The chemical structures were established by extensive analysis of their MS and NMR spectroscopic data or comparison with literature data. In the present research, we report the isolated compounds <b>1</b>-<b>11</b>, for the first time, in the species <b>S. tangutica</b>. Moreover, compounds <b>1</b>, <b>2</b> and <b>4</b>-<b>11</b> have not been reported from any species in Saxifragaceae family. Furthermore, we discuss the chemotaxonomic significance of the isolated compounds.<br>• Eight diarylheptanoids and three phenylpropanoids have been isolated from <b>Saxifraga tangutica.</b> • Compounds <b>1</b>-<b>11</b> are firstly reported in the species <b>Saxifraga tangutica.</b> • Compounds <b>1</b>, <b>2</b> and <b>4</b>-<b>11</b> are firstly isolated from genus <b>Saxifraga</b> or family Saxifragaceae.
ETHNOPHARMACOLOGICAL RELEVANCE: Dioscorea zingiberensis C. H. Wright (D. zingiberensis), Dioscoreaceae, is used extensively in traditional Chinese medicines. The aim of the current review paper is to give a comprehensive overview of the traditional usage and phytochemistry of the plant. Clinical studies performed and products prepared from the plant and active principles will be mentioned. In addition a review of the taxonomy of the genus Dioscorea is given.MATERIALS AND METHODS: A systematic search on literature has been performed in databases like Google Scholar, Science Direct, Scifinder, Web of Science, and in Chinese databases (China Knowledge Resource Integrated, i.e., CNKI and Wanfang) including Ph.D. and M.Sc. dissertations. These from the period 1983-2016 have been searched.
RESULTS: D. zingiberensis is an endemic plant in China widely distributed in some provinces, especially Hubei and Shaanxi. The rhizomes are the medicinal part in Dun-Ye-Guan-Xin-Ning tablets and are used for isolation of diosgenin. Steroidal saponins are believed to be the active principles. More than 70 compounds have been identified. Several of these have been tested in preclinical assays and clinical trials. A wide spectrum of biological effects including cardiovascular, anti-thrombosis, hyperlipidemia, neuroprotection, anti-inflammatory, and anthelmintic effect has been verified.
CONCLUSIONS: Because of the promising results from the investigations on the plant material of D. zingiberensis, further in depth analyses ought to be performed to evaluate its potential as either a traditional drug or a source of bioactive principle. The presently performed studies do not explain mechanism of action, pharmacokinetics (ADME properties), or toxicity. All of these topics need more elaborate investigations.
An efficient preparative procedure for the separation of four antibacterial diterpenes from a Salvia prattii crude diterpenes-rich sample was developed. Firstly, the XION hydrophilic stationary phase was chosen to separate the antibacterial crude diterpenes-rich sample (18.0 g) into three fractions with a recovery of 46.1%. Then, the antibacterial fractions I (200 mg), II (200 mg), and III (150 g) were separated by the Megress C18 preparative column, and compounds tanshinone IIA (80.0 mg), salvinolone (62.0 mg), cryptotanshinone (70.0 mg), and ferruginol (68.0 mg) were produced with purities greater than 98%. The procedure achieved large-scale preparation of the four diterpenes with high purity, and it could act as a reference for the efficient preparation of active diterpenes from other plant extracts.
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.
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.
Lycium ruthenicum Murr. (LRM, Solanaceae), also called "black wolfberry" in China, is extremely tolerant drought. Although black wolfberry has seeds that are rich in oil, being considered as a potential alternative for edible oil production, little information has been found regarding its characterization. The present study evaluated the fatty acid profile of the seed oil and its phytosterol contents. Moreover, its antioxidant potential and its inhibition activities on pancreatic lipase, and cholesterol esterase (CEase) were also determined. The key fatty acids of studied oil were linoleic (74.58%), oleic (11.82%), γ-linolenic (6.60%), palmitic (4.88%), and stearic (1.40%) acids, which together comprised 99.28% of the total fatty acids. Phytosterols including 24-methylenecholesterol, campesterol, stigmasterol, dihydrolanosterol, 24-methyldesmosterol, β-sitosterol, Δ5 -avenasterol, cycloartenol, and Δ7- avenasterol were identified for the 1st time. The inhibition values (IC50 ) for the DPPH and ABTS radical scavenging capacities of the oil were 7.86 and 15.49 mg/mL, respectively. Additionally, LRM seed oil was also demonstrated to possess strong pancreatic lipase, and CEase inhibition activities with IC50 values of 12.38 and 2.63 mg/mL, respectively. The mechanism study indicated that the inhibitory manner of the oil on CEase belonged to uncompetitive inhibition of reversible inhibition. The results derived from above studies suggest that LRM seed oil could be a potential source of high value phytochemicals for developing novel functional food.
Diosgenin wastewater produced from <b>Dioscorea zingiberensis</b> C. H. Wright in diosgenin enterprise is the by-product of numerous operations chiefly including washing raw materials, acid hydrolysis, and cleaning the apparatus with water. It requires the removal of high concentrations of various organic and inorganic contaminants from this wastewater in order to avoid pollution to the environment and fresh water system. Currently, several different methods such as chemical, physicochemical, biological recovery resource, constructed wetland, and integrated methods of these processes are being applied for treating diosgenin wastewater. Aiming to get a comprehensive overview, available reports from experimental scale to industry scale about the treatment of this wastewater were collected and summarized. Therefore, this review paper will provide appropriate choice for the efficient treatment of diosgenin wastewater and supportive information for the other scientists who want to continue this valuable research in the future.<br><br>Display Omitted<br>• Studies of diosgenin wastewater treatment between 2003 and 2016 are reviewed. • Characteristics of diosgenin wastewater are presented. • These methods used for diosgenin wastewater are compared. • Merits and demerits of each approach to cope with diosgenin wastewater are stated. • Future promising ways should be updated based on currently available ones.
A new diarylheptanoid, (5S)-1,7-bis-(3,4-dihydroxyphenyl)-5-hydroxyheptan-3-one-5-O-β-D-6-Oacetylglucoside (<i>1</i>), together with two known diarylheptanoids, (5S)-1,7-bis-(3,4-dihydroxyphenyl)-5-hydroxyheptan-3-one-5-O-β-D-glucopyranoside (<i>2</i>) and hirsutanonol (<i>3</i>), were isolated from Saxifraga tangutica. The structures of <i>1-3</i> were elucidated using 1D and 2D NMR spectral data, including high-resolution mass spectra (HR-ESI-MS). It was found that the new compound was acetyl-substituted (5S)-1,7-bis-(3,4-dihydroxyphenyl)-5-hydroxyheptan-3-one-5-O-β-D-glucopyranoside.
A new isocoumarin, along with 10 known compounds, was isolated from the aerial parts of Aconitum gymnandrum. Their structures were elucidated by spectroscopic methods including extensive 1D and 2D NMR techniques. Among the known compounds, compound 11 was obtained as a natural product for the first time, which was previously reported as a synthetic product. In addition, compounds 1-5, 7 and 9 were tested for their cytotoxicity against four human cancer cell lines. The results showed that compounds 3, 4 and 7 displayed cytotoxicity against lung cancer A549 and gastric cancer MGC80, respectively, whereas 5 and 9 showed selective cytotoxicity against hepatocellular carcinoma HepG2.
A new isocoumarin, along with 10 known compounds, was isolated from the aerial parts of Aconitum gymnandrum. Their structures were elucidated by spectroscopic methods including extensive 1D and 2D NMR techniques. Among the known compounds, compound 11 was obtained as a natural product for the first time, which was previously reported as a synthetic product. In addition, compounds 1-5, 7 and 9 were tested for their cytotoxicity against four human cancer cell lines. The results showed that compounds 3, 4 and 7 displayed cytotoxicity against lung cancer A549 and gastric cancer MGC80, respectively, whereas 5 and 9 showed selective cytotoxicity against hepatocellular carcinoma HepG2.
Abstract Lancea tibetica is an important traditional Tibetan medicinal plant that grows on the Qinghai-Tibet Plateau with great development potential in pharmaceutical industry. In this study, a combinative method using HPLC-DPPH and two-dimensional liquid chromatography has been developed to identify and separate antioxidants from Lancea tibetica. Under the target-guidance of HPLC-DPPH experiment, three antioxidant fractions from Lancea tibetica were recognized. Then, separation of the three fractions using two-dimensional semi-preparation liquid chromatography led to seven phenylpropanoids: (+)-pinoresinol-β-D-glucoside (1), isoacteoside (2), acteoside (3), tibeticoside (4),epipinoresinol (5), anthelminthicol (6) and phillygenol (7). As a result, seven major antioxidants in Lancea tibetica were isolated with more than 96% purity. Furthermore, in vitro bioassay against DPPH revealed compounds 1 – 7 with IC 50 values ranging from 6.16 ± 0.08 to 25.09 ± 0.11 (μM) and compounds 1 , 2 and 3 showed activities stronger than the two reference antioxidants (vitamin C, rutin), with IC 50 values of 6.16 ± 0.08, 8.93 ± 0.06 and 7.98 ± 0.05 (μM), respectively. Results of the present study indicated that the method was an efficient technique to systematically screen and isolate antioxidants from medicine crops. Graphical abstract Unlabelled Image Highlights • A novel screen and separation method for purification of antioxidants directly. • Seven antioxidants isolated from Lancea tibetica bioactivity-guided. • Isolated antioxidants with IC 50 values from 6.16 ± 0.08 to 25.09 ± 0.11 (μM). • The first report on antioxidant capacity of the compounds from Lancea tibetica.
Lancea tibetica is an important traditional Tibetan medicinal plant that grows on the Qinghai-Tibet Plateau with great development potential in pharmaceutical industry. In this study, a combinative method using HPLC-DPPH and two-dimensional liquid chromatography has been developed to identify and separate antioxidants from Lancea tibetica. Under the target-guidance of HPLC-DPPH experiment, three antioxidant fractions from Lancea tibetica were recognized. Then, separation of the three fractions using two-dimensional semi-preparation liquid chromatography led to seven phenylpropanoids: (+)-pinoresinol-β-D-glucoside (1), isoacteoside (2), acteoside (3), tibeticoside (4),epipinoresinol (5), anthelminthicol (6) and phillygenol (7). As a result, seven major antioxidants in Lancea tibetica were isolated with more than 96% purity. Furthermore, in vitro bioassay against DPPH revealed compounds 1-7 with IC50 values ranging from 6.16 ± 0.08 to 25.09 ± 0.11 (μM) and compounds 1, 2 and 3 showed activities stronger than the two reference antioxidants (vitamin C, rutin), with IC50 values of 6.16 ± 0.08, 8.93 ± 0.06 and 7.98 ± 0.05 (μM), respectively. Results of the present study indicated that the method was an efficient technique to systematically screen and isolate antioxidants from medicine crops.
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