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1.
A simple and sensitive HPLC–UV method was developed to determine ligustilide in rat brain samples after nasal administration. The lower limit of quantification (LLOQ) was 245 ng/ml for ligustilide. The calibration curve was linear over a concentration range of 245–4900 ng/ml. Brain samples were obtained at regular time intervals after nasal administration of ligustilide (45 mg/kg). Ligustilide could be detected in rat brain only after 5 min of nasal administration; which showed that ligustilide may have a rapid onset of action. This result illustrates that intranasal administration of ligustilide may act as a promising alternative to conventional routes of administration. 相似文献
2.
Soni VK Yadav DK Bano N Dixit P Pathak M Maurya R Sahai M Jain SK Misra-Bhattacharya S 《Fitoterapia》2012,83(1):110-116
Annona squamosa (AS) has traditionally been used as ethnomedicine. We have earlier extracted and fractionated the twigs of AS based upon its bioactivity and observed its immune potentiating activity that was localized in its three fractions. Present communication deals with the phytochemical analysis and pharmacological investigation of the most active chloroform fraction that led to isolation and identification of a number of compounds whose structures were elucidated using 1D and 2D NMR spectroscopic analysis. Amongst the twelve pure compounds isolated, five compounds Lanuginosine (1), (+) -O- methylarmepavine (2), (+)-anomuricine (3), Isocorydine (4), and N-methyl-6, 7-dimethoxyisoquinolone (5) were evaluated in vivo for their immune modifier activities in BALB/c mice after oral administration at three log doses of 0.3, 1.0 and 3.0 mg/kg for 14 consecutive days. Of these, three compounds (1, 2 and 5) showed dose dependent immune stimulating activity. However, the uppermost activity was noted in the compound N-methyl-6, 7-dimethoxyisoquinolone at the 3.0 mg/kg oral dose. The activity was assessed in the form of increased splenic T and B cellular proliferation, up-regulated CD4+, CD8+ and CD19+ cell population and accentuation in the peritoneal macrophage function. The compound possibly acted modifying the expression of Th1- and Th2- cytokines via stimulation of pro-inflammatory Th1 cytokines IL-2 and IFN-γ. These results warrant the use of the above compounds as an efficient immune-stimulant or immune-adjuvant against diseases with immune suppression. The analogs of the compound may further be chemically synthesized to achieve desired immune modifying activity. 相似文献
3.
The majority of bioactive principles in a complex matrix such as natural products and botanical medicines are secondary rather than primary metabolites. In addition to being chemically diverse, the bioactivity of an ethnobotanical can comprise from one to several bioactive compounds, present in a complex mixture. Conventional discovery efforts utilize bioassay-guided fractionation (BGF) to isolate individual active compounds. When applied to complex natural products, BGF is often challenged by an apparent loss of activity during fractionation, resulting in weakly active isolated compounds. Metabolomic analysis can potentially complement existing the BGF paradigm by capturing the chemical complexity of the metabolites. The proposed biochemometric approach establishes a link between the chemistry of a secondary metabolome and a deserved health impact, using a high-throughput, high-resolution capable biological endpoint. The proof of principle is demonstrated for the anti-tuberculosis (TB) activity of the Alaskan ethnobotanical, Oplopanax horridus. Biochemometric analysis identified the 100 most active constituents from thousands of metabolites in the active extract by means of 2D orthogonal chromatography using countercurrent and GC-MS methods. Previously isolated O. horridus phytoconstituents were used as reference markers of known structure and bio (in)activity. Positive correlations allowed distinction of anti-TB actives from inactive compounds. A total of 29 bioactives from 3 main structural classes were assigned based on MS data. Biochemometric analysis is a new tool for the standardization of herbal medicines and ethnobotanicals, as well as for drug discovery from nature. The method can assign multiple active compounds in complex mixtures without their prior isolation or structure elucidation, while still providing an interface to structural information. 相似文献
4.
Generally, berberine, coptisine, palmatine, and jatrorrhizine were considered as the main bio-active compounds in Rhizoma Coptis (RC). Little attention was paid to investigate the pharmacological activity of minor constituents in RC. The present study was designed to separate the minor compounds, and the cytotoxicity and antihyperglycemic effect of these compounds in HepG2 cells were also studied. Palmatine (1), berberine (2), coptisine (3), epiberberine (4), columbamine (5), and jatrorrhizine (6) from RC ethanol extract were isolated by high speed counter current chromatography (HSCCC) in one run. The remaining fraction (about 50% of extract in HSCCC) was further isolated by traditional column chromatography methods to yield magnoflorine (7), ferulic acid (8), and choline (9). Another four alkaloids, namely groenlandicine (10), berberrubine (11), oxyberberine (12), 8-oxo-coptisine (13), also were obtained from CHCl3 extracts. Especially, choline was first isolated from RC. Cell assay indicated that the minor fractions excluding compounds 1-6 showed obvious glucose lowering activity. In addition, the minor monomers also exhibited moderate glucose lowering activity. The combination of berberine and ferulic acid showed synergistic effect on antihyperglycemic. The combination of alkaloids 1-6 was same so. All compounds had different cytotoxicity in HepG2 cells within the test concentration. Of them, berberrubine showed the strongest cytotoxicity. The results suggested that combined action of variety constituents contributed to the antihyperglycemic effets and low cytotoxicity of RC extract in HepG2 cells. 相似文献
5.
《Fitoterapia》2014
Nerve growth factor (NGF) and analog reagents to promote the neurite outgrowth of nerve cells against the neuron degeneration are expected to be potentially useful for the medical treatment of Alzheimer's disease. In our focus on the discovery of bioactive diterpenes, we investigated the chemical constituents of the plant Croton yanhuii. This investigation led to the isolation and identification of two novel clerodane diterpenes (1 and 2). Their structures were elucidated on the basis of extensive 1D and 2D NMR (COSY, HMQC, HMBC, and NOESY) and mass (ESIMS and HR-ESIMS) spectroscopic data analyses. Further biological screenings showed that both of the compounds enhanced NGF-mediated neurite outgrowth from PC12 cells. 相似文献
6.
Investigation of characteristic constituents of Salicornia bigelovii Torr. led to isolation of two new 30-nortriterpenoid glycosides, Bigelovii A (1), Bigelovii B (2), together with two known 30-nortriterpenoid glycosides 3-4 and three known oleanane-type triterpenoid glycosides 5-7. The structures of new compounds were elucidated by extensive 1D and 2D NMR, and MS spectroscopic analysis, and chemical evidences. All compounds were isolated for the first time from Chenopodiaceae. Thus compounds 1-4 were evaluated for their cytotoxicity and compouds 1, 3 showed moderate activity against four cell lines, HL-60 (promyelocytic leukemia), MCF-7 (breast carcinoma), HepG2 (liver carcinoma) and A549 (lung carcinoma), with IC(50) values of 6.18, 78.08, 13.64 and >100μM for 1; 31.87, >100, ~100, >100μM for 3, respectively. 相似文献
7.
Phytochemical investigation of Annona squamosa twigs, resulted in isolation and identification of twelve known (1-12) compounds among them one 1-(4-β-D-glucopyranosyloxyphenyl)-2-(β-D-glucopyranosyloxy)-ethane (11) is synthetically known but first time isolated from natural sources. Their structures were elucidated using 1D and 2D NMR spectroscopic analysis. The isolated compounds (2-8, 11) were evaluated for H+ K+-ATPase activity. Three of these compounds (+)-O-methylarmepavine (2), N-methylcorydaldine (3), isocorydine (6) showed promising anti-secretory activity. Activity of these compounds, comparable to the standard drug omeprazole is novel to our finding. Moreover, there is no information accessible regarding the pharmacological effect of A. squamosa on the gastrointestinal system. This study is the first of its kind to show the significant anti-ulcer effect of A. squamosa. The present study aimed to evaluate the gastroprotective effect of A. squamosa (AS) and to identify its active constituents. Anti-ulcer activity was evaluated against cold restraint (CRU), pyloric ligation (PL), aspirin (ASP), alcohol (AL) induced gastric ulcer and histamine (HA) induced duodenal ulcer model and further confirmed through in vitro assay of H+ K+-ATPase activity and plasma gastrin level. AS and its chloroform and hexane fraction attenuated ulcer formation in CRU, PL, HA model and displayed anti-secretory activity in vivo through reduced free, total acidity and pepsin in PL, confirmed by in vitro inhibition of H+ K+-ATPase activity with corresponding decrease in plasma gastrin level. Cytoprotection of AS was apparent with protection in AL, ASP models and enhanced mucin level in PL. 相似文献
8.
Sesquiterpenes from Vladimiria souliei and their inhibitory effects on NO production 总被引：1，自引：0，他引：1
As a part of our ongoing search for plant-derived compounds that inhibit nitric oxide production, the methanol extract of the roots of Vladimiria souliei was found to show significant inhibitory effects on INF-γ-induced nitric oxide production in murine macrophage RAW264.7 cells. Bioactivity-guided isolation of the extract yielded two most active sesquiterpenes, including a new compound, named souliene A (1) and alismol (2). Their structures were elucidated by spectroscopic methods (IR, ESIMS, HRESIMS, 1D and 2D NMR). Two isolates showed promising inhibitory effects on INF-γ-induced nitric oxide production in murine macrophage RAW264.7 cells. 相似文献
9.
Two new triterpenoids (1, 2), together with one flavonoid glycoside and thirteen known triterpenoids were isolated from the roots of Actinidia chinensis Planch (Actinidiaceae). The structures of the new constituents were elucidated as 12α-chloro-2α, 3β, 13β, 23-tetrahydroxyolean-28-oic acid-13-lactone (1), 2α, 3α, 19α, 23, 24-pentahydroxyurs-12-en-28-oic acid (2). Structure elucidation was accomplished by 1D, 2D NMR spectra (HMQC, HMBC, 1H-1H COSY, TOCSY, and NOESY) and mass spectrometry (ESIMS). Moreover, two known triterpenoids showed positive cytotoxic activity against LOVO and HepG2 cell lines. 相似文献
10.
Borges-Argáez R Canche-Chay CI Peña-Rodríguez LM Said-Fernández S Molina-Salinas GM 《Fitoterapia》2007,78(5):370-372
Leaves, root and stem bark of Diospyros anisandra were screened against two strains of Mycobacterium tuberculosis, one resistant and one susceptible to antibiotics, using the microplate Alamar blue assay test. The lypophylic fractions of the root and bark showed significant inhibitory activity against both strains, with the hexane fraction of the bark showing the strongest activity (MIC 6.25 microg/ml) against the resistant strain and a significant antimicrobial activity against Staphylococcus aureus, Bacillus subtilis, Candida albicans, Aspergillus niger, and Colletotrichum gloeosporioides. The bioassay-guided purification of the bioactive hexane fraction resulted in the isolation and identification of the naphthoquinone plumbagin as one of the metabolites responsible for the biological activity. 相似文献
11.
In this paper, microdialysis combined with ultra performance liquid chromatography/mass spectrometry (UPLC-MS) was applied for the determination of ligustilide in freely moving rats' brain. The extracellular unbound ligustilide could be detected in rat brain within the first time interval (0-20 min) after nasal administration but not after oral administration. This result showed that ligustilide could quickly enter the brain after nasal administration; which implied that ligustilide may have a rapid onset of action. This work demonstrated the potential application of microdialysis combined with UPLC-MS in pharmacokinetic studies. Furthermore, the advantage that fewer animals used in the microdialysis experiment was confirmed. 相似文献
12.
Chemical composition and antimicrobial activity of Momordica charantia seed essential oil 总被引：1，自引：0，他引：1
The essential oil obtained from the seeds of Momordica charantia was analyzed by GC/MS. Twenty-five components, representing 90.9% of the oil, were identified. The main constituents were trans-nerolidol, apiole, cis-dihydrocarveol and germacrene D. Furthermore, the oil was tested for its antibacterial and antifungal activities. Staphylococcus aureus was found to be the most sensitive microorganism with MIC values <500 microg/ml. 相似文献
13.
Phytochemical investigation of the ethanolic extract of twigs of Kigelia pinnata DC. afforded one new iridoid 7-hydroxy eucommiol (1), and nine known compounds (2-10). The structure of compounds was elucidated by extensive spectroscopic methods, including 1D, 2D NMR experiments and MS analysis. All these compounds were evaluated for GLUT4 translocation modulatory effect in skeletal muscle cells. Four of the tested compounds 1, 5, 6 and 7 showed significant stimulation of GLUT4 translocation to cell surface in skeletal muscle cells without any adverse effect on cell viability. Effect of these four compounds was concentration-dependent and comparable to standard drug rosiglitazone. These findings indicate that constituents of K. pinnata may provide leads for the therapeutics for insulin resistance and diabetes. 相似文献
14.
Natural products chemistry is the discipline that lies at the heart of modern pharmacognosy. The field encompasses qualitative and quantitative analytical tools that range from spectroscopy and spectrometry to chromatography. Among other things, modern research on crude botanicals is engaged in the discovery of the phytochemical constituents necessary for therapeutic efficacy, including the synergistic effects of components of complex mixtures in the botanical matrix. In the phytomedicine field, these botanicals and their contained mixtures are considered the active pharmaceutical ingredient (API), and pharmacognosists are increasingly called upon to supplement their molecular discovery work by assisting in the development and utilization of analytical tools for assessing the quality and safety of these products. Unlike single-chemical entity APIs, botanical raw materials and their derived products are highly variable because their chemistry and morphology depend on the genotypic and phenotypic variation, geographical origin and weather exposure, harvesting practices, and processing conditions of the source material. Unless controlled, this inherent variability in the raw material stream can result in inconsistent finished products that are under-potent, over-potent, and/or contaminated. Over the decades, natural product chemists have routinely developed quantitative analytical methods for phytochemicals of interest. Quantitative methods for the determination of product quality bear the weight of regulatory scrutiny. These methods must be accurate, precise, and reproducible. Accordingly, this review discusses the principles of accuracy (relationship between experimental and true value), precision (distribution of data values), and reliability in the quantitation of phytochemicals in natural products. 相似文献
15.
Studies on the chemical constituents of leaves of Camellia oleifera Abel. led to the isolation of 3 new bibenzyl glycosides. Their structures have been elucidated as 1-(3′,5′-dihydroxy)phenyl-2-(4″-O-β-D-glucopyranosyl)phenylethane (1), 1-(3′,5′-dimethoxy)phenyl-2-(4″-O-β-D-glucopyranosyl)phenylethane (2) and 1-(3′,5′-dimethoxy)phenyl-2-[4″-O-β-D-glucopyranosyl(6→1)-O-α-L-rhamnopyranosyl]phenylethane (3) through spectral studies including HR-ESI-MS, 1H NMR, 13C NMR and 2D NMR experiments. All the above 3 bibenzyl glycosides showed cytotoxic activities to Hela and hep2 cell lines. 相似文献
16.
Antitumor activities of water extract (fraction A), ethanol extract (fraction B), ethyl acetate extract (fraction C), non-ethyl acetate extract (fraction D) and compound diosbulbin B isolated from Dioscorea bulbifera L. (DB) were investigated in vivo in this present study. The results showed that fractions B and C both decreased tumor weight in S180 and H22 tumor cells bearing mice, while fractions A and D had no such effect. Furthermore, fraction C altered the weight of spleen and thymus, and the amounts of total leukocytes, lymphocytes and neutrophils in tumor-bearing mice. Further results showed that compound diosbulbin B demonstrated anti-tumor effects in the dose-dependent manner at the dosage of 2 to 16 mg/kg without significant toxicity in vivo. Furthermore, on the basis of chemical analysis of the above extracts by high-performance liquid chromatography (HPLC) with a diode array detector (DAD), diosbulbin B was found to be the major antitumor bioactive component of DB. These results suggest that DB has potential anti-tumor effects which may be related to influencing the immune system for the first time, and the compound diosbulbin B is the major antitumor component of DB. 相似文献
17.
以红树林植物来源内生真菌构巢曲霉MA143为研究对象,对其ICI培养基发酵粗提物的化学成分进行初步研究,以期从红树林植物中分离得到具有显著生物活性的新化合物,用于如抗肿瘤、抗真菌等医药用途。采用萃取法、硅胶柱层析、Sephadex LH-20凝胶柱层析、RP-18反相柱层析等技术从中分离纯化得到了3个化合物。结合碳谱(13C-NMR)、氢谱(1HNMR)、质谱(ESI-MS)等波谱学技术及相关数据库检索鉴定出这3个化合物分别为:sterigmatocystin、Versicolorin A、Averufanin。红树林植物开发新型生物活性物质的潜能不可低估,开发其药物价值,发挥其经济效益与生态效益,促进海岸居民对其加以保护和种植,具有非常重要的现实意义。 相似文献
18.
Junji Akaki Yasunori Matsui Hiroaki Kojima Satomi Nakajima Kaeko Kamei Makoto Tamesada 《Fitoterapia》2009
It has been reported that mycelia of the Cordyceps sinensis (CS) can function as an immunostimulant. However, the active constituents of the mycelia are not well known. In this study, we investigated which components of the mycelia of CS induce monocyte activation and then structurally analyzed the active components. 相似文献
19.
Four new chamigrane derivatives, laurecomin A (1), laurecomin B (2), laurecomin C (3), and laurecomin D (4), one new naturally occurring sesquiterpene, 2,10-dibromo-3-chloro-7-chamigren-9-ol acetate (5), and three known halogenated structures, deoxyprepacifenol (6), 1-bromoselin-4(14),11-diene (7), and 9-bromoselin-4(14),11-diene (8), were isolated from the marine red alga Laurencia composita collected from Pingtan Island, China. The structures of these compounds were unambiguously established by 1D, 2D NMR and mass spectroscopic techniques. The bioassay results showed that 2 was active against both brine shrimp and fungus Colletotrichum lagenarium. 相似文献
20.
Oil production from the seeds of Camellia oleifera Abel. causes a great waste of shells which contain a lot of bioactive components. The aim of this research was to isolate flavonoid from the shells of C. oleifera Abel. and evaluate its uses. The shells were extracted by 70% methanol, hydrolyzed by 2 M hydrochloric acid, and further crystallized in acetone, the corresponding yield of flavonoid was up to 2.1% (purity: 93.8%). The procedure is concise, quick and proper for industrial utilization of the shells. Flavonoid was identified as bimolecular kaempferol structure by UV, MS, 1H NMR and 13C NMR spectra, which is a new biflavonoid and first found in C. oleifera Abel. It showed stronger scavenging activity of DPPH and ABTS radicals than kaempferol. MDA decreased, and SOD and GSH-Px activities increased significantly in serum (P < 0.01) and brain tissue (P < 0.05) of mice after intragastric administration of biflavonoid at 200 mg/kg/d for 30 d. Its effects in vivo are superior to vitamin C and similar to kaempferol. Thus biflavonoid can be used as a prospective antioxidant to protect brain cells against damage from free radicals. 相似文献