scholarly journals The anti-inflammatory effects of Indonesian and Japanese bitter melon (Momordica charantia L.) fruit extracts on interleukin-1β-treated hepatocytes

2019 ◽  
Vol 9 (1) ◽  
pp. 16 ◽  
Author(s):  
Dinia Rizqi Dwijayanti ◽  
Tetsuya Okuyama ◽  
Tadayoshi Okumura ◽  
Yukinobu Ikeya ◽  
Mikio Nishizawa
Keyword(s):  
Nitric Oxide ◽  
Ethyl Acetate ◽  
Inflammatory Cytokine ◽  
Momordica Charantia ◽  
Interleukin 1Β ◽  
No Production ◽  
Bitter Melon ◽  
Inos Protein ◽  
Ic50 Values ◽  
Anti Inflammatory

Background: Bitter melon, Momordica charantia L. (Cucurbitaceae), grows in tropical to temperate regions in Asia, including Indonesia and Japan. Bitter melon contains triterpenoids, steroidal glycosides, flavonoids, and alkaloids. The green immature fruit of bitter melon is a popular vegetable in Indonesia and Japan and has been used as a traditional Indonesian medicine (Jamu) to treat microbial infections and diabetes mellitus. However, there are currently few reports about the pharmacological effects of the constituents of bitter melon.Objective: To compare the effects of Indonesian and Japanese bitter melon, the production of pro-inflammatory mediators, such as nitric oxide (NO) and pro-inflammatory cytokines, was monitored.Methods: Immature fruits of bitter melons collected from Indonesia and Japan were lyophilized and extracted with methanol. The resultant extracts were fractionated by hydrophobicity into ethyl acetate-soluble (A), n-butanol-soluble (B), and water-soluble (C) fractions. Primary cultured hepatocytes prepared from rat liver were treated with interleukin-1β (IL-1β) and each extract or fraction. Nitrite in the medium was measured, and the half-maximal inhibitory concentration (IC50) value was determined. Lactate dehydrogenase activity in the medium was measured to monitor cytotoxicity. The expression of inducible nitric oxide synthase (iNOS) was detected by western blot analysis. The mRNA levels were measured by reverse transcription-polymerase chain reaction. Results: Indonesian and Japanese bitter melon extracts (BMEs) suppressed NO production by IL-1β-treated hepatocytes without showing cytotoxicity. The IC50 values of the BMEs were 86 μg/mL (Indonesian) and 171 μg/mL (Japanese). Both BMEs suppressed iNOS protein expression. Fractions A and B of both BMEs suppressed NO production. The IC50 values of the Indonesian BME fractions A and B were comparable to those of Japanese BME. Fraction A of both BMEs decreased the levels of iNOS protein and mRNA, as well as those of pro-inflammatory cytokine mRNAs. Fraction C of both BMEs did not affect NO production.Conclusion: The ethyl acetate-soluble fraction (A) of Indonesian and Japanese BMEs exhibited a comparable ability to suppress the induction of the iNOS and pro-inflammatory cytokine genes. These data suggest that hydrophobic constituents in fraction A, such as cucurbitane-type triterpenoids, may be responsible for the observed anti-inflammatory effects of bitter melon from Indonesia and Japan.Keywords: Momordica charantia, nitric oxide, inflammation, Jamu, Goya.

scholarly journals Benzophenone and Benzoylphloroglucinol Derivatives from Hypericum sampsonii with Anti-Inflammatory Mechanism of Otogirinin A

Molecules ◽  
2020 ◽  
Vol 25 (19) ◽  
pp. 4463 ◽  
Author(s):  
Chun-Yi Huang ◽  
Tzu-Cheng Chang ◽  
Yu-Jing Wu ◽  
Yun Chen ◽  
Jih-Jung Chen
Keyword(s):  
Nitric Oxide ◽  
Inhibitory Effect ◽  
No Production ◽  
Necrosis Factor Alpha ◽  
Aerial Parts ◽  
Arginase 1 ◽  
Potent Inhibition ◽  
Ic50 Values ◽  
Cytokine Tumor Necrosis Factor ◽  
Anti Inflammatory

Three new compounds, 4-geranyloxy-2-hydroxy-6-isoprenyloxybenzophenone (1), hypericumone A (2) and hypericumone B (3), were obtained from the aerial parts of Hypericum sampsonii, along with six known compounds (4–9). The structures of these compounds were determined through spectroscopic and MS analyses. Hypericumone A (2), sampsonione J (8) and otogirinin A (9) exhibited potent inhibition (IC50 values ≤ 40.32 μM) against lipopolysaccharide (LPS)-induced nitric oxide (NO) generation. Otogirinin A (9) possessed the highest inhibitory effect on NO production with IC50 value of 32.87 ± 1.60 μM. The well-known proinflammatory cytokine, tumor necrosis factor-alpha (TNF-α) was also inhibited by otogirinin A (9). Western blot results demonstrated that otogirinin A (9) downregulated the high expression of inducible nitric oxide synthase (iNOS). Further investigations on the mechanism showed that otogirinin A (9) blocked the phosphorylation of MAPK/JNK and IκBα, whereas it showed no effect on the phosphorylation of MAPKs/ERK and p38. In addition, otogirinin A (9) stimulated anti-inflammatory M2 phenotype by elevating the expression of arginase 1 and Krüppel-like factor 4 (KLF4). The above results suggested that otogirinin A (9) could be considered as potential compound for further development of NO production-targeted anti-inflammatory agent.

scholarly journals Chemical Profiles and Anti-inflammatory Activity of the Essential Oils from Seseli gummiferum and Seseli corymbosum subsp. corymbosum

2016 ◽  
Vol 11 (10) ◽  
pp. 1934578X1601101
Author(s):  
Alev Tosun ◽  
Jaemoo Chun ◽  
Igor Jerković ◽  
Zvonimir Marijanović ◽  
Maurizio A. Fenu ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Essential Oils ◽  
Inflammatory Activity ◽  
Raw 264.7 Cells ◽  
No Production ◽  
Raw 264.7 ◽  
Gene Assay ◽  
Germacrene D ◽  
Ic50 Values ◽  
Anti Inflammatory

The anti-inflammatory activity of the essential oils from Seseli corymbosum subsp. corymbosum Pall. ex Sm. (SC) and Seseli gummiferum Boiss. & Heldr. subsp. corymbosum (SG) was investigated for the first time on lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. The main constituents (determined by GC-FID and GC-MS analyses) were germacrene D (54.1%) and sabinene (22.4%) in SG oil and β-phellandrene (29.2%), α-phellandrene (8.2%) and germacrene D (2.5%) in SC oil. SC and SG oils inhibited nitric oxide (NO) production with IC50 values of 56.1 and 108.2 μg/mL, respectively. The oils also inhibited prostaglandin E2 (PGE2) with IC50 values of 49.4 μg/mL (SC oil) and 95.5 μg/mL (SG oil). The inhibitory effect of SC and SG oils was accompanied by dose-dependent decreases of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) protein expressions in LPS-induced RAW 264.7 cells. The research of the reporter gene assay on nuclear factor κB (NF-κB) showed that SC and SG oils inhibited NF-κB transcriptional activity. The obtained results suggest that SC and SG oils exert the anti-inflammatory effects in LPS-stimulated RAW 264.7 cells by suppressing NF-κB activation.

scholarly journals Nitric oxide (NO) radical inhibitory of hedyotis philippinensis and its marker compound, asperuloside

2014 ◽  
Vol 10 (1) ◽  
Author(s):  
Emi Norzehan Mohamad Mahbob ◽  
Rohaya Ahmad ◽  
Syahida Ahmad
Keyword(s):  
Nitric Oxide ◽  
Folk Medicine ◽  
No Production ◽  
Marker Compound ◽  
Methanolic Extracts ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Anti Inflammatory ◽  
Dose Dependent ◽  
Raw264.7 Macrophage

Hedyotis spesies have been used in Chinese folk medicine as a treatment for colds, stomatitis and various inflammations. In this study, three methanolic extracts of Hedyotis species (Hedyotis corymbosa, Hedyotis havilandii and Hedyotis philippinensis) were screened for their anti-inflammatory activity. The plant extracts along with asperuloside, the marker compound of H. philippinensis were tested for their anti-inflammatory effect against lipopolysaccharide (LPS) and interferon- (IFN-)-induced nitric oxide (NO) production using RAW264.7 macrophage cells. Among the three species, H. philippinensis (leaves and stems) showed good NO radical inhibitory activity (with IC50 values of 139.76±12.50 and 176.21±2.48 g/ml, respectively). Asperuloside, isolated as a major compound from the plant moderately inhibited LPS/IFN--induced NO production by 63% at a concentration of 100 M (45% cell viability) compared to L-NAME (77 %). Its IC50 value was found to be 75.45±2.25 M. Its inhibition was also found to be dose-dependent.

scholarly journals Anti-Inflammatory Activity of the Phlorotannin Trifuhalol A Using LPS-Stimulated RAW264.7 Cells Through NF-κB and MAPK Main Signaling Pathways

2019 ◽  
Vol 14 (5) ◽  
pp. 1934578X1984979 ◽  
Author(s):  
Kasira Phasanasophon ◽  
Sang Moo Kim
Keyword(s):  
Nitric Oxide ◽  
Ethyl Acetate ◽  
Signaling Pathways ◽  
Ethyl Acetate Fraction ◽  
Inflammatory Activity ◽  
Raw264.7 Cells ◽  
No Production ◽  
Mitogen Activated Protein ◽  
Anti Inflammatory ◽  
Factor Α

Trifuhalol A, a phlorotannin, was extracted from Agarum cribrosum with ethyl acetate and fractionated using Sephadex LH-20 column chromatography (SF1-SF6). The ethyl acetate fraction (EAF) and SF5-containing trifuhalol A exhibited strong inhibitory activity against hyaluronidase. The anti-inflammatory activity of the phlorotannin, EAF, and SF5 was determined through the inhibition of nitric oxide (NO) production in lipopolysaccharide-stimulated RAW264.7 cells. Furthermore, the inhibition of NO production was validated by confirming the appreciable downregulation of inducible nitric oxide synthase expression. Agarum cribrosum phlorotannin also markedly suppressed the expression of cyclooxygenase-2, interleukin (IL)-1β, IL-6, and tumor necrosis factor-α. In addition, the anti-inflammatory action was verified by examining its effects on proinflammatory signaling pathways. The activation of nuclear factor (NF)-κB and mitogen-activated protein kinases (MAPKs) was attenuated via the inhibition of NF-κB p-65, c-Jun N-terminal kinase, extracellular signal-regulated kinase 1/2, and p38 MAPK phosphorylation. Therefore, trifuhalol A is a potential source for either the prevention or the treatment of inflammation.

scholarly journals Ethyl Acetate Extract ofArtemisia anomalaS. Moore Displays Potent Anti-Inflammatory Effect

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Xi Tan ◽  
Yuan-Lai Wang ◽  
Xiao-Lu Yang ◽  
Dan-Dan Zhang
Keyword(s):  
Nitric Oxide ◽  
Ethyl Acetate ◽  
Ethyl Acetate Extract ◽  
Mapk Signaling ◽  
Raw264.7 Cells ◽  
Heme Oxygenase 1 ◽  
No Production ◽  
Dependent Manner ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Artemisia anomalaS. Moore has been widely used in China to treat inflammatory diseases for hundreds of years. However, mechanisms associated with its anti-inflammatory effect are not clear. In this study, we prepared ethyl acetate, petroleum ether,n-BuOH, and aqueous extracts from ethanol extract ofArtemisia anomalaS. Moore. Comparing anti-inflammatory effects of these extracts, we found that ethyl acetate extract of this herb (EAFA) exhibited the strongest inhibitory effect on nitric oxide (NO) production in LPS/IFNγ-stimulated RAW264.7 cells. EAFA suppressed the production of NO in a time- and dose-dependent manner without eliciting cytotoxicity to RAW264.7 cells. To understand the molecular mechanism underlying EAFA’s anti-inflammatory effect, we showed that EAFA increased total cellular anti-oxidant capacity while reducing the amount of inducible nitric oxide synthase (iNOS) in stimulated RAW264.7 cells. EAFA also suppressed the expression of IL-1βand IL-6, whereas it elevates the level of heme oxygenase-1. These EAFA-induced events were apparently associated with NF-κB and MAPK signaling pathways because the DNA binding activity of p50/p65 was impaired and the activities of both ERK and JNK were decreased in EFEA-treated cells comparing to untreated cells. Our findings suggest that EAFA exerts its anti-inflammatory effect by inhibiting the expression of iNOS.

scholarly journals Total Alkaloids from Bamboo Shoots and Bamboo Shoot Shells of Pleioblastus amarus (Keng) Keng f. and Their Anti-Inflammatory Activities

Molecules ◽  
2019 ◽  
Vol 24 (15) ◽  
pp. 2699 ◽  
Author(s):  
Yan Ren ◽  
Yisha Ma ◽  
Zhidan Zhang ◽  
Liying Qiu ◽  
Huanhuan Zhai ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Raw264.7 Cells ◽  
No Production ◽  
Bamboo Shoot ◽  
Edible Plant ◽  
Protein Levels ◽  
Total Alkaloids ◽  
Bamboo Shoots ◽  
Ic50 Values ◽  
Anti Inflammatory

The bamboo shoot of Pleioblastus amarus (Keng) Keng f. is a medicinal and edible plant product in China. In this study, the chemical composition of the total alkaloids from bamboo shoots and bamboo shoot shells of P. amarus (Keng) Keng f. (ABSP and ABSSP, respectively) were separated and investigated by UHPLC/QTOF-MS/MS. The results showed that a total of 32 alkaloids were extracted, with 15 common to both ABSP and ABSSP and 10 and 7 alkaloids distinct to ABSP and ABSSP, respectively. ABSP and ABSSP both decreased the lipopolysaccharide (LPS, 0.5 μg/mL)-induced nitric oxide (NO) production in RAW264.7 murine macrophages with half maximal inhibitory concentration (IC50) values of 78 and 55 μg/mL, respectively. We also found that ABSP and ABSSP (100 μg/mL) could decrease the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) at both mRNA and protein levels in LPS-exposed RAW264.7 cells. Moreover, 100 μg/mL of ABSP and ABSSP also significantly inhibited LPS-induced mRNA expression of interleukin 1β (IL-1β) and tumor necrosis factor α (TNF-α). Additionally, ABSP and ABSSP (100 μg/mL) decreased the phosphorylation of extracellular regulated protein kinase (ERK) in LPS-stimulated RAW264.7 cells. Collectively, the total alkaloids from the bamboo shoots and shells of P. amarus exhibit anti-inflammatory effects in LPS-activated RAW264.7 cells through the inhibition of ERK signaling. This result can provide support for the medicinal use and further study of P. amarus.

scholarly journals Inflammatory and Cytotoxic Activities of Abietane Terpenoids from Nepeta bracteata Benth.

Molecules ◽  
2021 ◽  
Vol 26 (18) ◽  
pp. 5603
Author(s):  
Manli Zhang ◽  
Meiying Chen ◽  
Yong Hou ◽  
Congzhao Fan ◽  
Hongyan Wei ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Silica Gel ◽  
Raw 264.7 Cells ◽  
Cytotoxic Activities ◽  
No Production ◽  
Raw 264.7 ◽  
Material Basis ◽  
Ic50 Values ◽  
Anti Inflammatory ◽  
Macrophage Viability

Nepeta bracteata Benth. is used clinically to treat tracheal inflammation, coughs, asthma, colds, fevers, adverse urination, and other symptoms, along with functions in clearing heat and removing dampness. However, there have been few studies characterizing the material basis of its efficacy. Therefore, the aim of this study was to screen for compounds with anti-inflammatory activities in N. bracteata Benth. Using silica gel, ODS C18, and Sephadex LH-20 column chromatography, as well as semipreparative HPLC, 10 compounds were separated from N. bracteata Benth. extract, including four new diterpenoids (1–4), one amide alkaloid (5), and five known diterpenoids (6–10). The structures of all the isolates were elucidated by HR-ESI-MS, NMR, and CD analyses. Using lipopolysaccharide (LPS)-stimulated RAW 264.7 cells, we investigated the anti-inflammatory activities of compounds 1–10. It is worth noting that all were able to inhibit nitric oxide (NO) production with IC50 values < 50 μM and little effect on RAW 264.7 macrophage viability. Compounds 2 and 4 displayed remarkable inhibition with IC50 values of 19.2 and 18.8 μM, respectively. Meanwhile, screening on HCT-8 cells demonstrated that compounds 2 and 4 also had moderate cytotoxic activities with IC50 values of 36.3 and 41.4 μM, respectively, which is related to their anti-inflammatory effects.

scholarly journals Structural Characterization and Assessment of Anti-Inflammatory and Anti-Tyrosinase Activities of Polyphenols from Melastoma normale

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3913
Author(s):  
Rui-Jie He ◽  
Jun Li ◽  
Yong-Lin Huang ◽  
Ya-Feng Wang ◽  
Bing-Yuan Yang ◽  
...  
Keyword(s):  
Enzyme Inhibitors ◽  
Enzyme Inhibitor ◽  
Structure Identification ◽  
No Production ◽  
Protective Effects ◽  
Successful Isolation ◽  
Ic50 Values ◽  
Development And Utilization ◽  
Inhibitory Activities ◽  
Anti Inflammatory

Polyphenols, widely distributed in the genus Melastoma plants, possess extensive cellular protective effects such as anti-inflammatory, anti-tyrosinase, and anti-obesity, which makes it a potential anti-inflammatory drug or enzyme inhibitor. Therefore, the aim of this study is to screen for the anti-inflammatory and enzyme inhibitory activities of compounds from title plant. Using silica gel, MCI, ODS C18, and Sephadex LH-20 column chromatography, as well as semipreparative HPLC, the extract of Melastoma normale roots was separated. Four new ellagitannins, Whiskey tannin C (1), 1-O-(4-methoxygalloyl)-6-O-galloyl-2,3-O-(S)-hexahydroxydiphenoyl-β-d-glucose (2), 1-O-galloyl-6-O-(3-methoxygalloyl)-2,3-O-(S)-hexahydroxydiphenoyl-β-d-glucose (3), and 1-O-galloyl-6-O-vanilloyl-2,3-O-(S)-hexahydroxydiphenoyl-β-d-glucose (4), along with eight known polyphenols were firstly obtained from this plant. The structures of all isolates were elucidated by HRMS, NMR, and CD analyses. Using lipopolysaccharide (LPS)-stimulated RAW2 64.7 cells, we investigated the anti-inflammatory activities of compounds 1–4, unfortunately, none of them exhibit inhibit nitric oxide (NO) production, their IC50 values are all > 50 μM. Anti-tyrosinase activity assays was done by tyrosinase inhibition activity screening model. Compound 1 showed weak tyrosinase inhibitory activity with IC50 values of 426.02 ± 11.31 μM. Compounds 2–4 displayed moderate tyrosinase inhibitory activities with IC50 values in the range of 124.74 ± 3.12–241.41 ± 6.23 μM. The structure–activity relationships indicate that hydroxylation at C-3′, C-4′, and C-3 in the flavones were key to their anti-tyrosinase activities. The successful isolation and structure identification of ellagitannin provide materials for the screening of anti-inflammatory drugs and enzyme inhibitors, and also contribute to the development and utilization of M. normale.

Anti-inflammatory assessment of 3-Acetylmyricadiol in LPS-Stimulated Raw 264.7 Macrophages

2021 ◽  
Vol 24 ◽  
Author(s):  
Gazanfar Ahmad ◽  
Reyaz Hassan ◽  
Neerupma Dhiman ◽  
Asif Ali
Keyword(s):  
Nitric Oxide ◽  
Cell Viability ◽  
Ethyl Acetate ◽  
Mtt Assay ◽  
Bark Extract ◽  
Maximum Effect ◽  
Potential Candidate ◽  
Tnf Α ◽  
Anti Inflammatory ◽  
Inflammatory Action

Background: Pentacyclic triterpenoids are a biologically active class of phytoconstituents with diverse pharmacological activity including anti-inflammatory action. Objective: In the current study, we isolated 3-Acetylmyricadiol, a pentacyclic triterpenoid, from the ethyl acetate bark-extract of Myrica esculenta and evaluated it for anti-inflammatory potential. Methods: The ethyl acetate bark-extract of the M. esculenta was subjected to column chromatography to isolate 3-Acetylmyricadiol. MTT assay was performed to check cell viability. The production of proinflammatory mediators like Nitric oxide, IL-6, TNF-α was observed after administration of 5, 10, 20 μM of 3-Acetylmyricadiol in LPS-activated Raw 246.7 macrophages by the reported methods. Results: MTT assay indicated more than 90% cell viability up to 20 μM of 3-Acetylmyricadiol. The administration of 3-Acetylmyricadiol inhibited the production of Nitric oxide, IL-6, TNF-α in a dose-dependent manner significantly in comparison to LPS treated cells. The maximum effect was observed at 20 μM of 3-Acetylmyricadiol which resulted in 52.37, 63.10, 55.37 % inhibition of Nitric oxide, IL-6, TNF-α respectively. Conclusion: Our study demonstrated the anti-inflammatory action of 3-Acetylmyricadiol and can serve as a potential candidate in the development of the clinically efficient anti-inflammatory molecule.

scholarly journals Anti-Inflammatory Activities of Compounds Isolated from the Rhizome of Anemarrhena asphodeloides

Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2631 ◽  
Author(s):  
Zeyuan Wang ◽  
Jianfeng Cai ◽  
Qing Fu ◽  
Lingping Cheng ◽  
Lehao Wu ◽  
...  
Keyword(s):  
Nuclear Factor Κb ◽  
Microglial Cells ◽  
No Production ◽  
Dependent Manner ◽  
Platycodin D ◽  
Protein Levels ◽  
Chemical Structures ◽  
Ic50 Values ◽  
Anti Inflammatory ◽  
Anemarrhena Asphodeloides

Fifteen unreported compounds in Anemarrhena asphodeloides, iriflophene (3), hostaplantagineoside C (7), tuberoside G (8), spicatoside B (9), platycodin D (14), platycoside A (15), platycodin D2 (16), polygalacin D2 (17), platycodin D3 (18), isovitexin (20), vitexin (21), 3,4-dihydroxyallylbenzene-3-O-α-l-rhamnopyranosyl(1→6)-β-d-glucopyranoside (22), iryptophan (24), adenosine (25), α-d-Glucose monoallyl ether (26), together with eleven known compounds (1, 2, 4–6, 10–13, 19 and 23), were isolated from the rhizomes of Anemarrhena asphodeloides. The chemical structures of these compounds were characterized using HRMS and NMR. The anti-inflammatory activities of the compounds were evaluated by investigating their ability to inhibit LPS-induced NO production in N9 microglial cells. Timosaponin BIII (TBIII) and trans-hinokiresinol (t-HL) exhibited significant inhibitory effects on the NO production in a dose-dependent manner with IC50 values of 11.91 and 39.08 μM, respectively. Immunoblotting demonstrated that TBIII and t-HL suppressed NO production by inhibiting the expressions of iNOS in LPS-stimulated N9 microglial cells. Further results revealed that pretreatment of N9 microglial cells with TBIII and t-HL attenuated the LPS-induced expression tumor necrosis factor (TNF)-α and interleukin-6 (IL-6) at mRNAs and protein levels. Moreover, the activation of nuclear factor-κB (NF-κB) and phosphatidylinositol 3-kinase (PI3K)/Akt signaling pathways were inhibited by TBIII and t-HL, respectively. Our findings indicate that the therapeutic implication of TBIII and t-HL for neurogenerative disease associated with neuroinflammation.

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