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1.

Background

Isodon rugosus is used traditionally in the management of hypertension, rheumatism, tooth-ache and pyrexia. Present study was arranged to investigate I. rugosus for phytoconstituents, phytotoxic and cytotoxic activities to explore its toxicological, pharmacological potentials and to rationalize its ethnomedicinal uses. Briefly, qualitative phytochemical analysis of the plant extracts were carried out for the existence of alkaloids, flavonoids, saponins, oils, glycosides, anthraquinones, terpenoids, sterols and tannins. Plant crude methanolic extract (Ir.Cr), its subsequent fractions; n-hexane (Ir.Hex), chloroform (Ir.Chf), ethyl acetate (Ir.EtAc), aqueous (Ir.Aq) and saponins (Ir.Sp) in different concentrations were tested for phytotoxic and cytotoxic activities using radish seeds and brine shrimps (Artemia salina) respectively. The phytotoxic activity was determined by percent root length inhibition (RLI) and percent seeds germination inhibition (SGI) while the cytotoxicity was obtained with percent lethality of the brine shrimps.

Results

Ir.Cr was tested positive for the presence of alkaloids, glycosides, flavonoids, oils, terpenoids, saponins, tannins and anthraquinones. Among different fractions Ir.Sp, Ir.Chf, Ir.EtAc, and Ir.Cr were most effective causing 93.55, 89.32, 81.32 and 58.68% inhibition of seeds in phytotoxicity assay, with IC50 values of 0.1, 0.1, 0.1 and 52 μg/ml respectively. Similarly, among all the tested samples, Ir.Sp exhibited the highest phytotoxic effect causing 91.33% root length inhibition with IC50 of 0.1 μg/ml. Ir.Sp and Ir.Chf were most effective against brine shrimps showing 92.23 and 76.67% lethality with LC50 values of 10 and 12 μg/ml respectively.

Conclusions

It may be inferred from the current investigations that I. rugosus contains different secondary metabolites and is a potential source for the isolation of natural anticancer and herbicidal drug molecules. Different fractions exhibited phytotoxic and cytotoxic activities, thus providing pharmacological basis for ethnomedicinal uses of this plant.  相似文献   

2.
For the first time a finger print analysis via high-performance thin layer chromatography (HPTLC) of Boswellia Sp. Burseraceae was accomplished. A preliminary investigation of the Boswellia Sp. Burseraceae displayed the presence of chemical constituents that could be involved in the production of innovative pharmaceuticals for an array of antiviral, anticancer, and antibacterial uses. Moreover, the finger print analysis would deem useful for establishing HPTLC standardization for natural and herbal photochemical constituents.  相似文献   

3.
BackgroundCissampelos sympodialis Eichl. (Menispermaceae) is used in folk medicine for the treatment of respiratory conditions such as bronchitis and asthma. The aqueous fraction of the hydroalcoholic extract of its leaves has shown immunomodulatory, bronchodilator and anti-inflammatory activities. However, there is no data available on the pharmacognostic quality control of its leaves.ObjectiveThe aim of the present study was to characterize the drug material obtained from the leaves of C. sympodialis, with the determination of WHO recommended assays, histochemistry of leaf sections and HPLC determination of its main bioactive alkaloid, warifteine.Materials and methodsThree batches of leaves were collected and histochemical and phytochemical analyses were performed to screen for alkaloids, phenolics, terpenoids, lipids, polysacharides and saponins. Pharmacopeial assays for the plant material were also conducted and the bisbenzylisoquinoline alkaloid warifteine was quantified by HPLC analysis.ResultsThe histochemistry of leaf sections from C. sympodialis revealed the presence of lipids, polysaccharides, phenolic compounds and alkaloids, mainly as part of idioblast secretions. These results were confirmed by general phytochemical screening reactions conducted with the leaf hydroalcoholic extract (presence of alkaloids, steroids, tannins, flavonoids and saponins). General pharmacopeial tests conducted with the leaves were within accepted standards. The warifteine content was similar for the three batches tested (0.004–0.006%).ConclusionThe physicochemical parameters and the morphological results presented in this paper can be used as basis for the preparation of a monograph on C. sympodialis leaves.  相似文献   

4.
The aqueous extract of Hemidesmus indicus roots was investigated for its in vivo antigenotoxic effect against cisplatin-induced cytogenetic damage. Swiss albino mice were administered with various doses of the extract either singly (50, 100 and 200 mg/kg body weight) or as split doses (10, 20 and 40 mg/kg bw/day) for five consecutive days by oral gavage. As endpoints, chromosome aberrations, micronuclei in polychromatic erythrocytes, mitotic index and PCE/NCE ratio were estimated. The extract protected the bone marrow cells from cisplatin-induced genotoxicity in an inverse dose-dependent manner. However, the extract was cytotoxic at all doses. But, under split dose regime it conferred a higher level of genoprotection and was not cytotoxic at the lower two doses. The presence of saponins, tannins, phenols, terpenoids, flavonoids and coumarins in the crude extract could explain these effects.  相似文献   

5.
Twenty five plant species from the Maruthamalai hills, Coimbatore, were screened for the presence of phytoconstituents. Among 25 plants, 19 gave positive tests for flavonoids, 23 for alkaloids, 20 for saponins, 25 for tannins, 22 for steroids and terpenoids, 23 for phenolic compounds, and tests indicated the presence of rotenoids in all the plants.  相似文献   

6.
Transthyretin (TTR) is an amyloidogenic protein, the amyloidogenic potential of which is enhanced by a number of specific point mutations. The ability to inhibit TTR fibrillogenesis is known for several classes of compounds, including natural polyphenols, which protect the native state of TTR by specifically interacting with its thyroxine binding sites. Comparative analyses of the interaction and of the ability to protect the TTR native state for polyphenols, both stilbenoids and flavonoids, and some of their main metabolites have been carried out. A main finding of this investigation was the highly preferential binding of resveratrol and thyroxine, both characterized by negative binding cooperativity, to distinct sites in TTR, consistent with the data of x-ray analysis of TTR in complex with both ligands. Although revealing the ability of the two thyroxine binding sites of TTR to discriminate between different ligands, this feature has allowed us to evaluate the interactions of polyphenols with both resveratrol and thyroxine preferential binding sites, by using resveratrol and radiolabeled T4 as probes. Among flavonoids, genistein and apigenin were able to effectively displace resveratrol from its preferential binding site, whereas genistein also showed the ability to interact, albeit weakly, with the preferential thyroxine binding site. Several glucuronidated polyphenol metabolites did not exhibit significant competition for resveratrol and thyroxine preferential binding sites and lacked the ability to stabilize TTR. However, resveratrol-3-O-sulfate was able to significantly protect the protein native state. A rationale for the in vitro properties found for polyphenol metabolites was provided by x-ray analysis of their complexes with TTR.  相似文献   

7.
Glycyrrhiza glabra, commonly known as licorice, is a popular herbal supplement used for the treatment of chronic inflammatory conditions and possesses anticancer and antiviral activities. This species contains a plethora of phytochemicals including terpenoids, saponins, flavonoids, polyamines and polysaccharides. The full complement of bioactive compounds has yet to be elucidated, a step necessary in order to explain its medicinal use. There are over 30 species in the Glycyrrhiza genus world-wide, most of which have been little characterized in terms of phytochemical or pharmacological properties. Here, large scale multi-targeted metabolic profiling and fingerprinting techniques were utilized to help gain a broader insight into Glycyrrhiza species chemical composition. UV, MS and NMR spectra of extracted components were connected with NMR, MS, and multivariate analyses data from Glycyrrhiza glabra, Glycyrrhiza uralensis, Glycyrrhiza inflata and Glycyrrhiza echinata. Major peaks in 1H NMR and MS spectra contributing to the discrimination among species were assigned as those of glycyrrhizin, 4-hydroxyphenyl acetic acid, and glycosidic conjugates of liquiritigenin/isoliquiritigenin. Primary metabolites profiling using GC–MS revealed the presence of cadaverine, an amino acid, exclusively found in G. inflata roots. Both LC–MS and NMR were found effective techniques in sample classification based on genetic and or geographical origin as revealed from derived PCA analysis.  相似文献   

8.
Mangifera longipes and Quercus gomeziana both is an ethnomedicinally important Asian herb that has been known for numerous healing activity of tribal people. The present research aims to investigate the phytochemical analysis with in vitro, in vivo possibilities of the soluble ethanol extract of M. longipes root (EEMLR) and Q. gomeziana leaves (EEQGL) by an experimental approach. The plant extract of EEMLR and EEQGL was found secondary metabolites, notably steroids, glycosides, tannins, flavonoids, saponins, gums, and alkaloids. Additionally, the extract showed significant activity in antioxidant, antipyretic, anti-inflammatory, membrane stabilization, cytotoxic, thrombolytic, and analgesic activities while no response in antibacterial activity. Our findings reveal that soluble ethanol extract of EEMLR and EEQGL is safe, which can be an effective source for exploring new medicinal products. This research's outcomes may provide potentials for mitigating pyrexia, inflammation, pain, cellular toxicity, and coagulation.  相似文献   

9.
Medicinal plants have therapeutic potential and are used worldwide to treat various diseases. In this study, the corm of Caladium x hortulanum was extracted with various solvents and implied the availability of phytochemicals such as flavonoids, alkaloids, tannins, steroids, phenols, glycosides, saponins and terpenoids. The solvent extracts of the corm showed antibacterial and antifungal activity with the growth inhibition zone ranged 0–24?mm. The isolation of phytochemicals was carried out using gel column chromatography, Thin Layer Chromatography followed by High Performance Liquid Chromatography. Gas Chromatography and Mass Spectrophotometry analysis was used to determine the phytochemicals. The corm extract showed potent antidiabetic activity on Hep G2 cell lines and CCl4 induced toxicity was elucidated. This possessed antiinflammatory property on murine monocyclic macrophage cell line RAW 264.7 showed 45.85?±?1.8% inhibition of cyclooxygenase activity. The corm extract showed hepatoprotective activity. The CCl4 incorporated Hep G2 cells showed 19.629?±?1.5% viability, whereas viability increased as 78.82?±?1.9% at 100?µg/ml of extract.  相似文献   

10.
Legumes produce a high diversity of secondary metabolites which serve as defence compounds against herbivores and microbes, but also as signal compounds to attract pollinating and fruit-dispersing animals. As nitrogen-fixing organisms, legumes produce more nitrogen containing secondary metabolites than other plant families. Compounds with nitrogen include alkaloids and amines (quinolizidine, pyrrolizidine, indolizidine, piperidine, pyridine, pyrrolidine, simple indole, Erythrina, simple isoquinoline, and imidazole alkaloids; polyamines, phenylethylamine, tyramine, and tryptamine derivatives), non-protein amino acids (NPAA), cyanogenic glucosides, and peptides (lectins, trypsin inhibitors, antimicrobial peptides, cyclotides). Secondary metabolites without nitrogen are phenolics (phenylpropanoids, flavonoids, isoflavones, catechins, anthocyanins, tannins, lignans, coumarins and furanocoumarins), polyketides (anthraquinones), and terpenoids (especially triterpenoid, steroidal saponins, tetraterpenes). While some secondary metabolites have a wide distribution (flavonoids, triterpenes, pinitol), however, others occur in a limited number of taxa. The distributions of secondary metabolites with an irregular occurrence are mapped on a molecular phylogeny of the Fabaceae, reconstructed from a combined data set of nucleotide sequences from rbcL, matK and ITS genes. In most cases, the distribution patterns of secondary metabolites do not agree with the phylogeny of the plants producing them. In contrary, the distribution of many secondary metabolites is patchy and irregular. Thus, the use of phytochemical data to reconstruct a phylogeny of plants is often not informative and can be misleading. The patchy distribution may be due to convergent evolution, a contribution of endophytic fungi or more likely, to an early acquisition of the key genes of secondary metabolism in the evolution of land plants among others by horizontal gene transfer from bacteria. Thus it would be a matter of gene regulation whether these genes are active in some but not all taxa.  相似文献   

11.
BackgroundCyclooxygenase-2 (COX-2) is an important enzyme with numerous biological functions. Overexpression of COX-2 has been associated with various inflammatory-related diseases and therefore, projected as an important pharmacological target.PurposeWe aimed to investigate the inhibitory potential of isolated bioactive compounds, 3-caffeoyl-4-dihydrocaffeoyl quinic acid (CDQ) and isorhamnetin 3-O-β-d-glucopyranoside (IDG), from Salicornia herbacea against COX-2 using both computational and in vitro approaches.MethodsComputational analysis, including molecular docking, molecular dynamics (MD) simulations, and post-simulations analysis, were employed to estimate the binding affinity and stability of CDQ and IDG in the catalytic pocket of COX-2 against Celecoxib as positive control. These predictions were further evaluated using in vitro enzyme inhibition as well as gene expression mediation in macrophages cells.ResultsMolecular docking analysis revealed substantial binding energy of CDQ (-6.1 kcal/mol) and IDG (-5.9 kcal/mol) with COX-2, which are lower than Celecoxib (-8.1 kcal/mol). MD simulations (100 ns) and post simulation analysis exhibited the substantial stability and binding affinity of docked CDQ and IDG compounds with COX-2. In vitro assays indicated significant COX-2 inhibition by CDQ (IC50 = 76.91 ± 2.33 μM) and IDG (IC50 = 126.06 ± 9.44 μM). This result supported the inhibitory potential of isolated bioactive compounds against COX-2. Also, a cellular level study revealed a downregulation of COX-2 expression in tumor necrosis factor-alpha stimulated RAW 264.7 macrophages treated with CDQ and IDG.ConclusionComputational and experimental analysis of CDQ and IDG from S. herbacea established their potential in the inhibition and mediation of COX-2. Hence, CDQ and IDG can be considered for therapeutic development against COX-2 linked disorders, such as inflammation and cancer. Furthermore, CDQ and IDG structures can be served as a lead compound for the development of advanced novel anti-inflammatory drugs.  相似文献   

12.
Due to the negative consequences carried by the usage of synthetic insecticides, a global interest into finding substitutes for these chemical compounds through natural products has arisen. When yielded to external attacks, plants generally produce metabolites to defend themselves. The physicochemical characteristics of this kind of compounds have allowed their usage as potential bioinsecticides. The Hymenaea courbaril L. (algarrobo) has proven to be a plant rich in metabolites with outstanding biological activity, in such a way that some of its extracts have been tested as insecticides. The goal of this study was to know the phytochemical composition of Hymenaea courbaril L.’s resin and perform evaluations in vivo of its toxic and genotoxic effects in the biological model Drosophila melanogaster. For this, two resin extracts were prepared and both a phytochemical analysis were carried out on them, having found in the ethanolic total extract the presence of terpenes, flavonoids and coumarins, while in the partial ethanolic extract only presence of terpenes and flavonoids was found. Drosophila larvae were submitted to different concentrations of the extracts and both the survival and the sexual ratio were evaluated, finding that larvae are more sensitive to the partial ethanolic extract. Subsequently, the induction of somatic mutation and mitotic recombination (SMART) was evaluated in the flies’ eyes. The most significant affectations at a genotoxic level were found when larvae were tested with the partial extract, indicating that possibly the coumarins absence makes this insect more susceptible to damages at a genetic material level.  相似文献   

13.
Cyperus scariosus (R.Br) belongs to the family Cyperaceae and it has a diverse medicinal importance. To identify human cyclooxegenase-2 (COX-2) inhibitors from C. scariosus, the rhizome powder was exhaustively extracted with various solvents based on the increasing polarity. Based on the presence and absence of secondary metabolites, we have selected the methanolic extract to evaluate the anti-oxidant and anti-inflammatory activity. The same extract was further subjected to gas chromatography-mass spectroscopy (GC-MS) analysis to identify the active compounds. Binding affinities of these compounds towards anti-inflammatory protein COX-2 were analyzed using molecular docking interaction studies. Phytochemical analysis showed that methanol extract is positive for all secondary metabolites. The antioxidant activity of the C. scariosus rhizomes methanolic extract (CSRME) is half to that of ascorbic acid at 50 µg/ml. The anti-inflammatory activity of CSRME is higher than that of diclofenac sodium salt at high concentration, which is evident from the dose dependent inhibition of bovine serum albumin denaturation at 40 µg/ml–5 mg/ml. GC-MS analysis showed the presence of nine compounds, among all N-methyl-1-adamantaneacetamide and 1,5,diphenyl-2H-1,2,4- triazine form a hydrogen bond interactions with Ser-530 and Tyr-385 respectively and found similar interactions with crystal structure of diclofenac bound COX-2 protein. Benzene-1, 2-diol, 4-(4-bromo-3 chlorophenyl iminomethyl forms hydrogen bond interactions with Thr-199 and Thr-200 as similar to crystallized COX-2 protein with valdecoxib. Collectively our results suggest that CSRME contains medicinally important anti-inflammatory compounds and this justifies the use of this plant as a folklore medicine for preventing inflammation associated disorders.  相似文献   

14.
Trillium govanianum rhizomes are traditionally consumed as a raw powder and decoction for the treatment of health complications. Hence, the present study aimed to investigate whether aqueous and alcoholic extracts of T. govanianum rhizomes under hot and cold extraction conditions have similar or dissimilar chemical, nutrient, and antioxidant profiles. The total phenolics, flavonoids, carbohydrates, proteins, fats, and energy values were estimated in all the conditionally prepared samples. The total phenolics (21.23±1.4 mg GAE/g extract), flavonoids (70.57±3.24 mg RE/g extract) were found higher in hot ethanolic extract (TGHEt), while cold water extract (TGGC) showed higher nutrients including amino acids (10.545±0.219 mg/g) and nucleosides (1.803±0.018 mg/g). The nutrient energy value (2.60 and 2.49 Kcal/g extract) was higher in cold and hot ethanolic extracts. Further, TGHEt scavenged the DPPH. (IC50; 870±22 μg/mL) and ABTS.+ (IC50; 80±1.49 μg/mL) effectively and proved its highest antioxidant activity compared to other samples. In LC/MS/MS-based metabolite profiling, twenty-six metabolites (fatty acids, steroidal saponins, triterpene saponins, ecdysteroid hormones) were confirmed with mass fragmentation and literature, while one hundred nine metabolites were identified using the METLIN database. The principal component analysis showed clustering of hot condition extracts while cold extracts were differentially located in quadrants. The heatmaps exhibited the associations and differences between metabolite composition, solvents, and extraction conditions. The identified metabolites speculatively predicted the biosynthesis pathway of T. govanianum. Findings also illustrated that T. govanianum is a source of bioactive nutritional components and saponins. The current metabolite profiling of T. govanianum will help in its agricultural and biotechnological interventions for higher quality produce.  相似文献   

15.
16.
In-depth characterization of specialized metabolites in the endemic Gypsophila perfoliata L. “tekirae” (G. tekirae Stef.) by liquid chromatography – quadrupol-Orbitrap mass spectrometry allowed dereplication/annotation of 22 flavonoids including 11 2″-O-pentosyl/deoxyhexosyl/hexosyl-C-hexosyl-flavones in the aerial parts and 23 gypsogenin- and quillaic acid-bidesmosides in the roots. Saponins were mainly mono-and diacetyl, and methoxycinnamoyl derivatives of 16 core structures forming isobaric isomers. Three acetylated derivatives of 2″-O-deoxyhexosyl-6-C-hexosyl-flavones are annotated for the first time in the genus Gypsophila together with five quillaic acid-based saponins. Aerial parts extract revealed prominent antioxidant and tyrosinase inhibitory activity, while roots demonstrated higher capacity against acetylcholinesterase, butyrylcholinesterase and α-glucosidase. The chemophenetic significance of acetylated 2″-O-glycosyl-6-C-hexosyl-flavones and GOTCAB saponins with methoxycinnamoyl-substituted α-chains was discussed.  相似文献   

17.
Due to the negative consequences carried by the usage of synthetic insecticides, a global interest into finding substitutes for these chemical compounds through natural products has arisen. When yielded to external attacks, plants generally produce metabolites to defend themselves. The physicochemical characteristics of this kind of compounds have allowed their usage as potential bioinsecticides. The Hymenaea courbaril L. (algarrobo) has proven to be a plant rich in metabolites with outstanding biological activity, in such a way that some of its extracts have been tested as insecticides. The goal of this study was to know the phytochemical composition of Hymenaea courbaril L.’s resin and perform evaluations in vivo of its toxic and genotoxic effects in the biological model Drosophila melanogaster. For this, two resin extracts were prepared and both a phytochemical analysis were carried out on them, having found in the ethanolic total extract the presence of terpenes, flavonoids and coumarins, while in the partial ethanolic extract only presence of terpenes and flavonoids was found. Drosophila larvae were submitted to different concentrations of the extracts and both the survival and the sexual ratio were evaluated, finding that larvae are more sensitive to the partial ethanolic extract. Subsequently, the induction of somatic mutation and mitotic recombination (SMART) was evaluated in the flies’ eyes. The most significant affectations at a genotoxic level were found when larvae were tested with the partial extract, indicating that possibly the coumarins absence makes this insect more susceptible to damages at a genetic material level.  相似文献   

18.
Screening of phytochemical Ephedra alte crude extract by GC–MS and HPLC analysis indicated the presence of alkaloids, tannins, flavonoids, terpenoids, and phenolic acid in the extract. The total phenolic content of E. alte methanol extract was 39.43 mg of Gallic acid eq/g, crude E. alte with 56.74, and 2.42 µg Trolox equivalent antioxidant capacity (TEAC)/g of plant extract according to DPPH and FRAP assay, respectively. The antimicrobial activity of E. alte against Staphylococcus aureus, staphylococcus epidermidis, Escherichia coli, and Klebsiellaoxytoca demonstrated a mean zone diameter of inhibition ranging from 0 to 17 mm. The MIC of the extracts ranged from 0.5 to 1.0 mg/mL. E. alte extract inhibits pepsin enzyme activity with IC50 values of 213.67 µg/ml. This study revealed that E. alte extract has pepsin enzyme inhibitory, antibacterial, antioxidant activities. The current outcomes indicate that E. alte might be employed as a natural agent for managing GERD and infectious diseases.  相似文献   

19.
Forsythiae Fructus, the fruit of Forsythia suspense is a traditional Chinese hebal medicine that has the antiviral and antioxidant effects in China. Modern analytical chemistry studies showed that the extracts of Forsythiae Fructus contain many bioactive components, such as flavonoids, lignans, phenolic acids, and terpenoids, which can be used to anti-inflammatory and treat toxicity, tonsillitis, ulcers, pharyngitis and acute nephritis. In order to study the types and quantities of metabolites in Forsythiae Fructus, we isolated, identified and analysed metabolites between two varieties of Forsythiae Fructus using UPLC/ESI-Q TRAP-MS/MS. The results showed that a total of 407 metabolites were identified in Forsythiae Fructus using UPLC/ESI-Q TRAP-MS/MS, including 21 terpenoids, 68 phenolic acids, 63 flavonoids, 43 amino acids and derivatives, 22 alkaloids, 55 lipids, 24 lignans and coumarins, 31 nucleotides and derivatives, 29 organic acids, and 51 other metabolites. Among, lignans and coumarins, terpenoids, organic acids, lipids, and phenolic acids were rich in Forsythiae Fructus, which accounted for more than 60% of the total metabolite content. Differential metabolite analysis revealed that 80 metabolites differed significantly between the two types of Forsythiae Fructus. Our results greatly enrich the Forsythiae Fructus phytochemical composition database and provide valuable information for further study of the metabolites of Forsythiae Fructus.  相似文献   

20.
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