Diagnostic ion filtering targeted screening and isolation of anti‐inflammatory iridoid glycosides from Hedyotis diffusa

Author(s):  
Fangying Shi ◽  
Chaoying Tong ◽  
Chengxin He ◽  
Shuyun Shi ◽  
Yuanxin Cao ◽  
...  
Author(s):  
Jyoti Vandana ◽  
Gupta A K ◽  
Alok Mukerjee

  Objective: This study aims to perform phytochemical screening and investigate anti-inflammatory activity of extract from aerial part of the plant Plantago major L.Methods: Preliminary phytochemical screening of plant extract was carried out using standard qualitative procedures and anti-inflammatory activity was evaluated using carrageenan-induced paw edema model in male Wistar albino rats using plethysmometer. Diclofenac sodium (10 mg/kg, b.w.) was used as standard drug.Results: Preliminary phytochemical screening of the different extracts revealed that they were rich in secondary metabolite compounds such as carbohydrates, tannins, steroids, flavonoids, terpenoids, glycosides, fats and oils, alkaloids, phenolic compounds, and iridoid glycosides. The anti-inflammatory activity was evaluated using carrageenan-induced paw edema models in Wistar albino rats. The anti-inflammatory activity of methanolic extract (ME) was found to be dose dependent in carrageenan-induced paw edema model. The ME has shown significant (p<0.05) inhibition of paw edema, 61.11% and 55.55% on 4th hr at the doses of 900 and 600 mg/kg, respectively.Conclusion: The results of the present study demonstrate that ME of the aerial parts of the plant possess significant (p<0.05) anti-inflammatory potential.


2018 ◽  
Vol 2018 ◽  
pp. 1-11 ◽  
Author(s):  
Yuan Xu ◽  
Xiao-Xia Chen ◽  
Yi-Xin Jiang ◽  
Dan-Dan Zhang

Hedyotis diffusa Willd and Scutellaria barbata D. Don (HDSB) were the core couplet in medicines that were commonly used for the purpose of anti-inflammation and anticancer treatments in China. However, biological properties of this couplet have not been fully elucidated. In this study, we screened fractions of HDSB for their anti-inflammatory activities and explored pertinent molecular mechanisms on murine macrophage RAW264.7 cell model. Ethyl acetate fraction from the aqueous extract of the couplet at equal weight ratio (EA11) showed the strongest inhibition of the nitrite accumulation in supernatant of RAW264.7 cells stimulated with lipopolysaccharide (LPS)/interferon-γ (IFN-γ). In addition, EA11 inhibited iNOS and IL-1β expression in a concentration-dependent manner while promoting the expression of HO-1 and PPAR-γ. Anti-inflammatory capability is most likely facilitated by its inhibitory effect on JNK signaling pathway and miR-155 expression. This study suggests that EA11 may be represented as a potential anti-inflammatory therapeutic candidate.


2022 ◽  
Vol 22 (1) ◽  
Author(s):  
Quhuan Ma ◽  
Yanmei Lu ◽  
Yi Deng ◽  
Xiaodong Hu ◽  
Wanyu Li ◽  
...  

Abstract Background Patrinia scabra Bunge is a well-known herbal medicine for its favorable treatment on inflammatory diseases owing to its effective ingredients, in which iridoid glycoside plays an extremely significant role. This article aimed to improve the content of total iridoid glycosides in crude extract through a series optimization of extraction procedure. Moreover, considering that both pain and inflammation are two correlated responses triggered in response to injury, irritants or pathogen, the article investigated the anti-inflammatory and analgesic activities of P. scabra to screen out the active fraction. Method P. scabra was extracted by ultrasonic-microwave synergistic extraction (UMSE) to obtain total iridoid glycosides (PSI), during which a series of conditions were investigated based on single-factor experiments. The extraction process was further optimized by a reliable statistical method of response surface methodology (RSM). The elution fractions of P. scabra extract were prepared by macroporous resin column chromatography. Through the various animal experiment including acetic acid-induced writhing test, formalin induced licking and flinching, carrageenan-induced mice paw oedema test and xylene-induced ear edema in mice, the active fractions with favorable analgesic and anti-inflammatory effect were reasonably screen out. Results The content of PSI could reach up to 81.42 ± 0.31 mg/g under the optimum conditions as follows: ethanol concentration of 52%, material-to-liquid ratio of 1:18 g/mL, microwave power at 610 W and extraction time of 45 min. After gradient elution by the macroporous resin, the content of PSI increased significantly. Compared with other concentrations of elution liquid, the content of PSI in 30 and 50% ethanol eluate was increased to reach 497.65 and 506.90 mg/g, respectively. Owing to the pharmacology experiment, it was reasonably revealed that 30 and 50% ethanol elution fractions of P. scabra could relieve pain centrally and peripherally, exhibiting good analgesic and anti-inflammatory activities. Conclusion Patrinia scabra possessed rich iridoids and exhibited significant analgesic and anti-inflammatory activities.


Molecules ◽  
2019 ◽  
Vol 24 (1) ◽  
pp. 197 ◽  
Author(s):  
Ran Yang ◽  
Lei Fang ◽  
Jia Li ◽  
Zhenhua Zhao ◽  
Hua Zhang ◽  
...  

A high-speed counter-current chromatography (HSCCC) method, using a two-phase solvent system composed of ethyl acetate/n-butanol/methanol/water (5:1:1:5, v/v/v/v), was successfully established to separate the five iridoid glucosides 7-O-ethyl sweroside (1), secologanin dimethylacetal (2), adinoside F (3), (7R)-secologain n-butyl methyl acetal (4) and adinoside G (5) from Lonicerae Japonicae Flos. Their purities were 96.8%, 98.5%, 93.3%, 98.0% and 99.9%, respectively. All the iridoid glucosides were identified by HR-ESI-MS, 1D and 2D NMR. Compounds 3 and 5 are new iridoid glucosides. The anti-inflammatory tests showed that compounds 1–5 all expressed moderate inhibitory effects on β-glucuronidase release in rat polymorphonuclear leukocytes (PMNs) induced by platelet-activating factor (PAF) with IC50 values ranging from 4.52 to 6.50 µM, while the antibacterial assays demonstrated that all the compounds displayed mild inhibitory activities against Staphylococcus aureus ATCC 25923 with MIC values ranging from 13.7 to 26.0 µg/mL.


2007 ◽  
Vol 62 (11-12) ◽  
pp. 813-820 ◽  
Author(s):  
Esra Küpeli Akkol ◽  
I. Irem Tatli ◽  
Zeliha S. Akdemir

The anti-inflammatory and antinociceptive properties of four major compounds from the flowers of Verbascum pterocalycinum var. mutense were investigated. Saponin glycosides called ilwensisaponin A and C and iridoid glycosides known as ajugol and picroside IV were isolated from the methanolic extract. A dose-related anti-inflammatory and antinociceptive response were obtained in this study at doses of 100 and 200 mg/kg. The results of the evaluation of the anti-inflammatory activity induced by carrageenan and PGE1 showed that this species possesses active constituents that could diminish the cyclooxygenase activitiy. No effects were observed in the 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced ear edema model. Our results support the anti-inflammatory and analgesic effects of Verbascum pterocalycinum var. mutense. Ilwensisaponins A and C could explain in part the anti-inflammatory and analgesic activities of this species. Although antinociceptive and anti-inflammatory activities of ajugol and picroside IV were found insignificant in the statistical analysis, ilwensisaponin A and C showed notable activity without inducing any apparent acute toxicity as well as gastric damage.


Molecules ◽  
2020 ◽  
Vol 25 (24) ◽  
pp. 5867
Author(s):  
Jun Hee Park ◽  
Wan Kyunn Whang

Previous studies have reported that Hedyotis diffusa Willdenow extract shows various biological activities on cerebropathia, such as neuroprotection and short-term memory enhancement. However, there has been a lack of studies on the inhibitory activity on neurodegenerative diseases such as Alzheimer’s disease (AD) through enzyme assays of H. diffusa. Therefore, H. diffusa extract and fractions were evaluated for their inhibitory effects through assays of enzymes related to AD, including acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE1), and on the formation of advanced glycation end-product (AGE). In this study, ten bioactive compounds, including nine iridoid glycosides 1–9 and one flavonol glycoside 10, were isolated from the ethyl acetate and n-butanol fractions of H. diffusa using a bioassay-guided approach. Compound 10 was the strongest inhibitor of cholinesterase, BACE1, and the formation of AGEs of all isolated compounds, while compound 5 had the lowest inhibitory activity. Compounds 3, 6, and 9 exhibited better inhibitory activity than other compounds on AChE, and two pairs of diastereomeric iridoid glycoside structures (compounds 4, 8, and 6, 7) showed higher inhibitory activity than others on BChE. In the BACE1 inhibitory assay, compounds 1–3 were good inhibitors, and compound 10 showed higher inhibitory activity than quercetin, the positive control. Moreover, compounds 1 and 3 were stronger inhibitors of the formation of AGE than aminoguanidine (AMG), the positive control. In conclusion, this study is significant since it demonstrated that the potential inhibitory activity of H. diffusa on enzymes related to AD and showed the potential use for further study as a natural medicine for AD treatment on the basis of the bioactive components isolated from H. diffusa.


Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1684 ◽  
Author(s):  
Seyed Mostafa Goldansaz ◽  
Carmen Festa ◽  
Ester Pagano ◽  
Simona De Marino ◽  
Claudia Finamore ◽  
...  

The n-butanolic extract, from an Iranian specimen of Nepeta asterotricha Rech. f. (NABE), displayed anti-inflammatory effects on lipopolysaccharide (LPS)-stimulated J774A.1 macrophages, which reduced nitrites and cytokines production. Bioassay guided fractionation of the extract led to the isolation of four iridoid glycosides, including a new one known as nepetamoside (1), one hexenyl-diglycoside, and some polyphenol and flavonoid components. None of the isolated iridoid components displayed significant effects on nitrites formation in an in vitro LPS-induced model of inflammation, thus suggesting that the plant anti-inflammatory effect is probably due to a synergistic action among its constituents.


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