scholarly journals Metabolites Identification of Chemical Constituents From the Eggplant (Solanum melongena L.) Calyx in Rats by UPLC/ESI/qTOF-MS Analysis and Their Cytotoxic Activities

2021 ◽  
Vol 12 ◽  
Author(s):  
Yuanyuan Song ◽  
Ting Mei ◽  
Yan Liu ◽  
Shengnan Kong ◽  
Jincheng Zhang ◽  
...  

Eggplant (Solanum melongena L.) Calyx is a medicinal and edible traditional Chinese medicine with anti-inflammatory, anti-oxidant, and anti-cancer properties. However, the pharmacodynamic components and metabolic characteristics remain unclear. Amide and phenylpropanoid were the two main constituents, and four amides, including n-trans-p-coumaroyltyramine (1), n-trans-p-coumaroyloctopamine (2), n-trans-p-coumaroylnoradrenline (3), n-trans-feruloyloctopamine (4), and a phenylpropanoid neochlorogenic acid (5) were selected. In this study, these five representative compounds showed cytotoxic activities on A549, HCT116, and MCF7 cells. In addition, the metabolites of 1–5 from the eggplant calyx in rats were identified. In total, 23, 37, 29, and 17 metabolites were separately characterized in rat plasma, urine, feces, and livers, by UPLC/ESI/qTOF-MS analysis. The metabolism of amides and phenylpropanoid was mainly involved in hydroxylation, methylation, glucuronidation, or sulfation reactions. Two hydroxylated metabolites (1-M2 and 2-M3) were clearly identified by comparison with reference standards. Rat liver microsome incubation experiments indicated that P450 enzymes could hydroxylate 1–5, and the methylation reaction of the 7-hydroxyl was also observed. This is the first study on the in vivo metabolism of these compounds, which lays a foundation for follow-up studies on pharmacodynamic evaluations and mechanisms.

Author(s):  
Pavani C H

Hyperlipidemia is the immediate results of the excessive fat intake in food. This results in the elevated levels of cholesterol and triglycerides in the blood. This leads to heart conditions like CAD, hypertension, congestive heart failure as risk factors which can be lethal. There are many drugs to treat and control the lipids levels in the body. These drugs are either designed to prevent LDL accumulation and VLDL synthesis. Some drugs also lower the elevated levels of saturated lipids in the body. But many drugs are known to cause side effects and adverse effects; therefore, alternatives to the drugs are the subjects for current investigations. Herbs and medicinal plants are used as treatment sources for many years. They have been used in the Indian medical systems like Ayurveda, Siddha etc. As the application of herbs in the treatment is growing, there is an urgent need for the establishment of Pharmacological reasoning and standardization of the activity of the medicinal plants. Chloris paraguaiensis Steud. is Poyaceae member that is called locally as Uppugaddi. Traditionally it is used to treat Rheumatism, Diabetes, fever and diarrhoea. The chemical constituents are known to have anti-oxidant properties and most of the anti-oxidants have anti-hyperlipidemic activity too. Since the plant has abundant flavonoid and phenol content, the current research focusses on the investigation of the anti-hyperlipidemic activity of the plant Chloris extracts. Extracts of Chloris at 200mg/kg showed a comparably similar anti hyperlipidemia activity to that of the standard drug. The extracts showed a dose based increase in the activity at 100 and 200mg/kg body weight.


2021 ◽  
Author(s):  
Zhe Li ◽  
Lkhaasuren Ryenchindorj ◽  
Bonan Liu ◽  
Ji SHI ◽  
Chao Zhang ◽  
...  

Abstract Background: Chinese materia medica processing is a distinguished and unique pharmaceutical technique in traditional Chinese Medicien (TCM), which has played an important role in reducing side effects, increasing medical potencies, altering the properties and even changing the curative effects of raw herbs.The efficacy improvement in medicinal plants is mainly caused by changes in the key substances through an optimized processing procedure.The effect of invigorating the kidney-yang for rice wine-steamed Cistancha deserticola was more strengthened than raw C. deserticola (CD). Methods: To evaluate the effect of processing, a comparative analysis was conducted by utilizing the UPLC-Q-TOF-MSE with the UNIFI informatics platform. In vitro studies were performed for the characterization of constituents as well as metabolites in vivo , and chemical components were determined in CD and its processed products. The multivariate statistical analyses were conducted to evaluate variations between them. OPLS-DA was used for pairwise comparison which revealed their marked differences. Results: In this study, the obtained results revealed considerable variations in phenylethanoid glycosides (PhGs) and iridoids after processing. The detection of 97 compounds was carried out in the extracts of CD and its processed product. In an in-vivo study, 10 prototype components and 44 metabolites were evaluated in rat plasma, feces, and urine. The obtained results revealed that processing leads to the considerable variation in the chemical constituents of CD and affects the disposition of the compounds in-vivo, and phase II metabolic processes were the key cascades of each compound and most of the metabolites were associated with echinacoside or acteoside. Conclusions: According to our literature search, the existing study reveals a comparative study of raw and processed CD for the first time. The obtained data help us to understand the impact of CD processing for further studies.


2017 ◽  
Vol 2017 ◽  
pp. 1-13 ◽  
Author(s):  
Yunshuang Fan ◽  
Yamei Li ◽  
Yuanyuan Wu ◽  
Lixin Li ◽  
Yuming Wang ◽  
...  

Simiao Wan (SMW), an important multiherbal formula used in traditional Chinese medicine, is extensively used to treat rheumatoid arthritis. However, the knowledge of the bioactive components of SMW remains unclear. Thus, gas chromatography–mass spectrometry (GC-MS) and liquid chromatography–mass spectrometry (LC-MS) were used to analyze the chemical constituents of volatile and nonvolatile extracts of SMW, as well as its absorbed components in rat plasma after oral SMW administration. Identification of several compounds was enabled by comparison of retention times, MS spectra, and MS/MS spectral data with the standard substance and reference materials reported in the literature. In the volatile extracts, GC-MS identified 26 compounds in vitro, three of which observed in blood by GC-MS. In the nonvolatile extracts, LC-MS identified 49 compounds in SMW; 18 compounds containing 7 prototype compounds, 5 metabolites, and 6 unknown compounds were absorbed by blood. The proposed GC-MS and LC-MS method was appropriate not only for the rapid screening and identification of multiple components of an SMW extract but also for screening its bioactive constituents in vivo. The proposed method could be a promising tool for the quality control of other Chinese herbal medicines.


2020 ◽  
Vol 11 (4) ◽  
pp. 6066-6078
Author(s):  
Greeshma G Nair ◽  
Sathianarayanan S

The objective of this review is to document briefly about the chemical constituents, pharmacognostical evaluation and biological activities of Syzygium samarangense belongs to the family Myrtaceae. It is generally called Java Apple, Wax Apple, Blume, Chambekka etc. Syzygium samarangense traditionally used as an astringent. It is also used to treat fever and halt diarrhea. The whole plant contains flavonoids, terpenoids, tannins, phenolic compounds, gallic acid, ellagic acid, squalene, botulin, lupeol, sitosterol, mixture of cycloartenol stearate, lupenyl stearate, β-sitosterol stearate, vitamins and minerals which bearing anti-oxidant, anti- microbial, hypoglycemic, anti-inflammatory, Immunomodulatory, CNS, Anti- diarrheal, anthelmintic and cytotoxic activities. In this review, different parts of the plant, their phytochemical constituents and their corresponding biological activities have been explored. The literatures reported that the fruit part contains carotene, anthocyanin and vescalagin which is used as antioxidant, anti- microbial and hypoglycemic effect. The leaf part contains myricetin, strobopinine, epigallocatechin, aurentiacin which bearing anti-inflammatory and immunomodulatory effect. The alcoholic extracts of leaves, seeds, root bearing analgesic, anti- inflammatory effect in lipopolysaccharide, antioxidant, cytotoxic activity against human colon cancer cell, the studies revealed that the extracts showed a potent anti- microbial activity against salmonella typhi, Escherichia coli, pseudomonas aeruginosa, bacillus subtilis, candida albicans etc. The aqueous extract of fruit prevents diabetes mellitus in rats.


2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Nidal Jaradat ◽  
Mohammed Hawash ◽  
Gada Dass

Abstract Background Rumex rothschildianus is the sole member of a unique section of the genus Rumex, in the family Polygonaceae. This species is a very rare small dioecious annual, endemic to Palestine that is traditionally used as food and for the treatment of various diseases. Therefore, the current investigation aimed to screen the chemical constituents, antioxidants, anti-α-amylase, anti-α-glucosidase, antilipase, and cytotoxic effects of four solvents fractions of R. rothschildianus leaves. Methods Dried powder of R. rothschildianus leaves was extracted in four solvents with different polarities. Several qualitative and quantitative phytochemical tests were performed to determine the components of the extracts. The colorimetric analysis was used for the quantitative determination of phenols, flavonoids, and tannins. In-vitro assays were performed to evaluate the extracts for antioxidant, anti-α-amylase, anti-α-glucosidase, and antilipase inhibitory activities, as well as cytotoxicity by MTS assay against cervical carcinoma cells line (HeLa) and breast cancer cell line (MCF7). Results The acetone fraction of R. rothschildianus leaves showed the most significant antioxidant activity, due to having the highest content of flavonoids and phenolics, with an IC50 value of 6.3 ± 0.4 μg/ml, compared to 3.1 ± 0.9 μg/ml for Trolox, and regarding lipase inhibition activity the acetone fraction showed the most potent activity with an IC50 value of 26.3 ± 0.6 μg/ml, in comparison with orlistat positive control IC50 12.3 μg/ml. The same extract was the most potent inhibitor of α-amylase and α-glucosidase, with IC50 values of 19.1 ± 0.7 μg/ml and 54.9 ± 0.3 μg/ml, respectively, compared to 28.8, 37.1 ± 0.3 μg/ml of acarbose, respectively. The hexane fraction showed 99.9% inhibition of HeLa cells and 97.4% inhibition for MCF7 cells. Conclusion The acetone fraction of R. rothschildianus leaves might provide a source of bioactive compounds for the treatment of oxidative stress. Similarly, the hexane fraction indicates the promising antitumor potential of R. rothschildianus. Clearly, these initial indications need further purification of potentially active compounds, and ultimately, in-vivo studies to determine their effectiveness.


2014 ◽  
Vol 6 (17) ◽  
pp. 7075 ◽  
Author(s):  
Hardik Chandasana ◽  
Yashpal S. Chhonker ◽  
Veenu Bala ◽  
Yarra Durga Prasad ◽  
Vishnu L. Sharma ◽  
...  

2021 ◽  
Vol 16 (1) ◽  
Author(s):  
Zhe Li ◽  
Lkhaasuren Ryenchindorj ◽  
Bonan Liu ◽  
Ji Shi ◽  
Chao Zhang ◽  
...  

Abstract Background Chinese materia medica processing is a distinguished and unique pharmaceutical technique in Traditional Chinese Medicine (TCM) used for reducing side effects, and increasing or even changing therapeutic efficacy of the raw herbs.Changes in the essential components induced by an optimized processing procedure are primarily responsible for the increased efficacy of medicinal plants.The kidney-yang invigorating effect of rice wine-steamed Cistancha deserticola (C. deserticola) was stronger than raw C. deserticola (CD). Methods A comparison analysis was carried out using the UPLC-Q-TOF-MSE with the UNIFI informatics platform to determine the influence of processing. In vitro studies were performed for the characterization of constituents as well as metabolites in vivo. The chemical components were determined in CD and its processed products. The multivariate statistical analyses were conducted to evaluate variations between them while OPLS-DA was used for pairwise comparison. Results The results of this study revealed considerable variations in phenylethanoid glycosides (PhGs) and iridoids after processing. A total of 97 compounds were detected in the extracts of CD and its processed product. PhGs having 4'-O-caffeoyl group in the 8-O-β-d-glucopyranosyl part, like acteoside, cistanoside C, campneoside II, osmanthuside decreased after being processed, while PhGs with 6'-O-caffeoyl group in the 8-O-β-d-glucopyranosyl part, such as isoacetoside, isocistanoside C, isocampneoside I, isomartynoside increased, especially in the CD-NP group. The intensity of echinacoside and cistanoside B whose structure possess 6'-O-β-d-glucopyranosyl moiety also increased. In in vivo study, 10 prototype components and 44 metabolites were detected in rat plasma, feces, and urine. The obtained results revealed that processing leads to the considerable variation in the chemical constituents of CD and affected the disposition of the compounds in vivo, and phase II metabolic processes are the key cascades of each compound and most of the metabolites are associated with echinacoside or acteoside. Conclusions This is the first global comparison research of raw and processed CD. These findings add to our understanding of the impact of CD processing and give important data for future efficacy investigations.


1996 ◽  
Vol 75 (01) ◽  
pp. 118-126 ◽  
Author(s):  
T Abrahamsson ◽  
V Nerme ◽  
M Strömqvist ◽  
B Åkerblom ◽  
A Legnehed ◽  
...  

SummaryThe aim of this study was to investigate the anti-thrombotic effects of an inhibitor of the plasminogen activator inhibitor-1 (PAI-1) in rats given endotoxin. In studies in vitro, PRAP-1, a Fab-fragment of a polyclonal antibody against human PAI-1, was shown to inhibit PAI-1 activity in rat plasma as well as to stimulate clot-lysis of the euglobulin fraction derived from rat plasma. Endotoxin administered to anaesthetised rats produced a marked increase in plasma PAI-1 activity. To study fibrin formation and lysis in vivo after intravenous (i. v.) injection of the coagulant enzyme batroxobin, 125I-fibrinogen was administered to the animals. The thrombi formed by batroxobin were rapidly lysed in control animals, while the rate of lysis was markedly attenuated in rats given endotoxin. PRAP-1 was administered i.v. (bolus + infusion) to rats given endotoxin and batroxobin and the PAI-1 inhibitor caused a dose-dependent decrease in the 125I-fibrin deposition in the lungs. An immunohistochemical technique was used to confirm this decrease in density of fibrin clots in the tissue. Furthermore, PRAP-1 decreased plasma PAI-1 activity in the rats and this reduction was correlated to the decrease in lung 125I-fibrin deposition at the corresponding time point. It is concluded that in this experimental model the PAI-1 antibody PRAP-1 may indeed inhibit thrombosis in animals exposed to endotoxin.


2020 ◽  
Vol 11 (4) ◽  
pp. 5059-5066
Author(s):  
Sushma B K ◽  
Raveesha H R

The present work is aimed to determine the chemical constituents in Baliospermum montanum methanolic extracts. An in vitro regenerated procedure was developed for the induction of callus from stem explant cultured on Murashige and Skoog (MS) medium fortified with various concentration and permutations of 2, 4-dichloro phenoxy acetic acid, 1-naphthalene acetic acid, 6-benzyl amino purine and gibberellic acid. FTIR & GC-MS analysis was done according to standard procedure. The quantitative estimation of β-sitosterol was done by HPLC method. Maximum fresh and dry weight of callus was estimated in the combination of GA3 (0.5 mg/L) + NAA (2 mg/L) compared to other concentration. The FTIR analysis showed various functional compounds with different characteristic peak values in the extracts. Major bioactive constituents were recognized in the GC-MS analysis. Root extract revealed the existence of 1-hexadecanol, pentanoic acid, 2-(aminooxy)- and 1-hexacosanol. Leaf extract showed the presence of propanoic acid, 2-oxo-, trimethylsilyl ester, 9,12-octadecadienoic acid (z,z)-, trimethylsilyl ester, docosane, 1,22-dibromo- and pentatriacontane. Stem and stem derived callus exhibit the presence of 1,6,3,4-dihydro-2-deoxy-beta-d-lyxo-hexopyranose, n-hexadecanoic acid and pentanoic acid, 2-(aminooxy). The methanolic extract of leaf exhibited 0.2149 % of β-sitosterol content. There were no peaks observed in the root, stem and stem derived callus. Further studies are necessary for the isolation and characterization of bioactive compounds from B. montanum.


2020 ◽  
Vol 11 (3) ◽  
pp. 3384-3390
Author(s):  
Ashish ◽  
Anjali ◽  
Dixit Praveen K ◽  
Nagarajan K ◽  
Sahoo Jagannath

Justicia gendarussa Burm .f. (family Acanthaceae) which is also known as willow-leaves and commonly known as Nili-Nirgundi, it is very commonly found nearby to China and its availability is very common in larger parts of India and Andaman islands. Traditionally it is used to treat various sorts of disorders such as wound healing, anti-inflammatory, anti-oxidant, antiproliferative, anti-arthritic etc. Justicia gendarussa is one of the crucial herbs which has been used in the Ayurveda. Majorly leaves parts of the plant shows the pharmacological activity but the root of the plant Justicia gendarussa is also have the important medicinal values. A large variety of pharmacologically active constituents i.e., alkaloids, flavonoids, saponin, carbohydrates, steroids, triterpenoids, carotenoids, aminoacids, tannins, phenolics, coumarines and anthaquinones are also present in this plant and they makes the plant pharmacologically important. The activity of the plant is also dependent on the solvent which is used for the extraction the various vital chemical constituents. The different- different parts of the plants having the different medicinal values also differ in the chemical values. This review is not only focused on the essential phytochemical constituents which is available in the plant but it also explains their necessary medicinal value to shows the essential biological action and phytopharmacological actions of various parts of the plant.


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