The Experts below are selected from a list of 405 Experts worldwide ranked by ideXlab platform
Salman Khan - One of the best experts on this subject based on the ideXlab platform.
-
Anti-hyperalgesic properties of a Flavanone Derivative Poncirin in acute and chronic inflammatory pain models in mice
BMC Pharmacology and Toxicology, 2019Co-Authors: Ruqayya Afridi, Ashraf Ullah Khan, Sidra Khalid, Bushra Shal, Hina Rasheed, Muhammad Zia Ullah, Omer Shehzad, Yeong Shik Kim, Salman KhanAbstract:Background Poncirin is Flavanone Derivative (isolated from Poncirus trifoliata ) with known pharmacological activities such as anti-tumor, anti-osteoporotic, anti-inflammatory and anti-colitic. The present study aimed to explore the anti-allodynic and anti-hyperalgesic potentials of poncirin in murine models of inflammatory pain. Methods The analgesic potential of poncirin was evaluated in formalin-, acetic acid-, carrageenan- and Complete Freund’s Adjuvant (CFA)-induced inflammatory pain models in mice. Anti-allodynic and anti-hyperalgesic activities were measured using Von Frey filaments, Randall Selitto, hotplate and cold acetone tests. The serum nitrite levels were determined using Griess reagent. The Quantitative Real-time PCR (qRT-PCR) was performed to assess the effect of poncirin on mRNA expression levels of inflammatory cytokines and anti-oxidant enzymes. Results Intraperitoneal administration of poncirin (30 mg/kg) markedly reduced the pain behavior in both acetic acid-induced visceral pain and formalin-induced tonic pain models used as preliminary screening tools. The poncirin (30 mg/kg) treatment considerably inhibited the mechanical hyperalgesia and allodynia as well as thermal hyperalgesia and cold allodynia. The qRT-PCR analysis showed noticeable inhibition of pro-inflammatory cytokines (mRNA expression levels of TNF-α, IL-1β and IL-6) ( p
-
Anti-hyperalgesic properties of a Flavanone Derivative Poncirin in acute and chronic inflammatory pain models in mice.
BMC pharmacology & toxicology, 2019Co-Authors: Ruqayya Afridi, Ashraf Ullah Khan, Sidra Khalid, Bushra Shal, Hina Rasheed, Muhammad Zia Ullah, Omer Shehzad, Yeong Shik Kim, Salman KhanAbstract:Poncirin is Flavanone Derivative (isolated from Poncirus trifoliata) with known pharmacological activities such as anti-tumor, anti-osteoporotic, anti-inflammatory and anti-colitic. The present study aimed to explore the anti-allodynic and anti-hyperalgesic potentials of poncirin in murine models of inflammatory pain. The analgesic potential of poncirin was evaluated in formalin-, acetic acid-, carrageenan- and Complete Freund’s Adjuvant (CFA)-induced inflammatory pain models in mice. Anti-allodynic and anti-hyperalgesic activities were measured using Von Frey filaments, Randall Selitto, hotplate and cold acetone tests. The serum nitrite levels were determined using Griess reagent. The Quantitative Real-time PCR (qRT-PCR) was performed to assess the effect of poncirin on mRNA expression levels of inflammatory cytokines and anti-oxidant enzymes. Intraperitoneal administration of poncirin (30 mg/kg) markedly reduced the pain behavior in both acetic acid-induced visceral pain and formalin-induced tonic pain models used as preliminary screening tools. The poncirin (30 mg/kg) treatment considerably inhibited the mechanical hyperalgesia and allodynia as well as thermal hyperalgesia and cold allodynia. The qRT-PCR analysis showed noticeable inhibition of pro-inflammatory cytokines (mRNA expression levels of TNF-α, IL-1β and IL-6) (p
-
anti hyperalgesic properties of a Flavanone Derivative poncirin in acute and chronic inflammatory pain models in mice
BMC Clinical Pharmacology, 2019Co-Authors: Ruqayya Afridi, Ashraf Ullah Khan, Sidra Khalid, Bushra Shal, Hina Rasheed, Muhammad Zia Ullah, Omer Shehzad, Yeong Shik Kim, Salman KhanAbstract:Poncirin is Flavanone Derivative (isolated from Poncirus trifoliata) with known pharmacological activities such as anti-tumor, anti-osteoporotic, anti-inflammatory and anti-colitic. The present study aimed to explore the anti-allodynic and anti-hyperalgesic potentials of poncirin in murine models of inflammatory pain. The analgesic potential of poncirin was evaluated in formalin-, acetic acid-, carrageenan- and Complete Freund’s Adjuvant (CFA)-induced inflammatory pain models in mice. Anti-allodynic and anti-hyperalgesic activities were measured using Von Frey filaments, Randall Selitto, hotplate and cold acetone tests. The serum nitrite levels were determined using Griess reagent. The Quantitative Real-time PCR (qRT-PCR) was performed to assess the effect of poncirin on mRNA expression levels of inflammatory cytokines and anti-oxidant enzymes. Intraperitoneal administration of poncirin (30 mg/kg) markedly reduced the pain behavior in both acetic acid-induced visceral pain and formalin-induced tonic pain models used as preliminary screening tools. The poncirin (30 mg/kg) treatment considerably inhibited the mechanical hyperalgesia and allodynia as well as thermal hyperalgesia and cold allodynia. The qRT-PCR analysis showed noticeable inhibition of pro-inflammatory cytokines (mRNA expression levels of TNF-α, IL-1β and IL-6) (p < 0.05) in poncirin treated group. Similarly, poncirin treatment also enhanced the mRNA expressions levels of anti-oxidant enzymes such as transcription factor such as nuclear factor (erythroid-derived 2)-like 2 (Nrf2) (p < 0.05), heme oxygenase (HO-1) (p < 0.05) and superoxide dismutase (SOD2) (p < 0.05). Chronic treatment of poncirin for 6 days did not confer any significant hepatic and renal toxicity. Furthermore, poncirin treatment did not altered the motor coordination and muscle strength in CFA-induced chronic inflammatory pain model. The present study demonstrated that poncirin treatment significantly reduced pain behaviors in all experimental models of inflammatory pain, suggesting the promising analgesic potential of poncirin in inflammatory pain conditions.
Jin Sook Kim - One of the best experts on this subject based on the ideXlab platform.
-
Cytoprotection against hydrogen peroxide-induced cell death in cultured mouse mesangial cells by erigeroFlavanone, a novel compound from the flowers of Erigeron annuus.
Chemico-biological interactions, 2009Co-Authors: Ohn Soon Kim, Nam Hee Yoo, Dae Sik Jang, Young Sook Kim, Jin Sook KimAbstract:Hyperglycemia-induced oxidative stress has been suggested as a mechanism underlying diabetic complications. Oxidative stress triggers cell death in various cell types, including glomerular mesangial cells which play important roles in diabetic nephropathy. In the present study, we investigated the potential cytoprotective effect of erigeroFlavanone, a novel Flavanone Derivative from the flowers of Erigeron annuus, in cultured mouse mesangial cells using hydrogen peroxide (H2O2) as an oxidative stress inducer. Our data show that hydrogen peroxide induced a decrease in cell viability that was attenuated by erigeroFlavanone. Hydrogen peroxide treatment increased formation of dichlorofluorescein (DCF)-sensitive intracellular reactive oxygen species (ROS). This enhanced ROS formation was significantly reduced by pretreatment with erigeroFlavanone in a dose-dependent manner. Hydrogen peroxide treatment also induced phosphorylation of the mitogen-activated protein kinases (MAPKs), c-Jun terminal kinase (JNK), extracellular-regulated kinase (ERK) and p38, and activated caspase-3. Pretreatment with erigeroFlavanone inhibited hydrogen peroxide-induced activation of MAPKs and caspase-3. From these data we conclude that erigeroFlavanone provides a protective effect against oxidative stress-induced cell death in mesangial cells that is associated with its antioxidant action and inhibition of MAPKs and caspase-3. These results suggest that erigeroFlavanone has potential as a therapeutic agent in the treatment of renal diabetic complications.
-
erigeroFlavanone a Flavanone Derivative from the flowers of erigeron annuus with protein glycation and aldose reductase inhibitory activity
Journal of Natural Products, 2008Co-Authors: Nam Hee Yoo, Dae Sik Jang, Jeong Lim Yoo, Yun Mi Lee, Young Sook Kim, Junghee Cho, Jin Sook KimAbstract:A novel 2,3-dioxygenated Flavanone, erigeroFlavanone (1), as well as eight known flavonoids and two known γ-pyranone Derivatives, were isolated from an ethyl acetate-soluble extract of the flowers of Erigeron annuus. The structure of compound 1 was elucidated by interpretation of spectroscopic data. All of the isolates were subjected to in vitro bioassays to evaluate their inhibitory activity against advanced glycation end products formation and rat lens aldose reductase.
Aty Widyawaruyanti - One of the best experts on this subject based on the ideXlab platform.
-
Flavonoids with antiplasmodial and cytotoxic activities of Macaranga triloba
Fitoterapia, 2012Co-Authors: Ishak Zakaria, Norizan Ahmat, Faridahanim Mohd Jaafar, Aty WidyawaruyantiAbstract:Abstract A new Flavanone Derivative, malaysianone A ( 1 ), four prenylated Flavanones, 6-prenyl-3′-methoxyeriodictyol ( 2 ), nymphaeol B ( 3 ), nymphaeol C ( 4 ) and 6-farnesyl-3′,4′,5,7-tetrahydroxyFlavanone ( 5 ), and two coumarins, 5,7-dihydroxycoumarin ( 6 ) and scopoletin ( 7 ), were isolated from the dichloromethane extract of the inflorescences of Macaranga triloba . The structures of these compounds were elucidated based on spectroscopic methods including nuclear magnetic resonance (NMR-1D and 2D), UV, IR and mass spectrometry. The cytotoxic activity of the compounds was tested against several cell lines, with 5 inhibiting very strongly the growth of HeLa and HL-60 cells (IC 50 : 1.3 μg/ml and 3.3 μg/ml, respectively). Compound 5 also showed strong antiplasmodial activity (IC 50 : 0.06 μM).
Bo Yang - One of the best experts on this subject based on the ideXlab platform.
-
MSFTZ, a Flavanone Derivative, Induces Human Hepatoma Cell Apoptosis via a Reactive Oxygen Species- and Caspase-Dependent Mitochondrial Pathway
The Journal of pharmacology and experimental therapeutics, 2008Co-Authors: Meidan Ying, Huazhou Ying, Bo YangAbstract:Hepatocellular carcinoma (HCC) is the most common malignancy of the liver. It is unfortunate that HCCs are highly refractory to conventional chemotherapy, radiation therapy, and even immunotherapy. Thus, novel therapeutic targets need to be sought for the successful treatment of HCCs. We now report that (+/-)-(3aRS,4SR)-2-(2-chloro-4-methylsulfonylphenyl)-4'-chloro-3alpha,4-diethoxy-flavane[4,3-d]-D1,9b-1,2,3-thiadiazoline (MSFTZ), a synthesized Flavanone Derivative, induced growth arrest and apoptosis of HCCs both in vitro and in vivo. MSFTZ induced a time- and dose-dependent increase in HCC apoptosis through caspase-3 activation and poly(ADP-ribose) polymerase-1 cleavage. Activation of caspase-9 induced by MSFTZ suggested that MSFTZ-induced signaling was mediated through a mitochondrial death pathway. In addition, we observed an elevation of reactive oxygen species (ROS) and a consequent loss of mitochondrial membrane potential, further suggesting that MSFTZ-induced death signaling was mediated through a mitochondrial oxygen stress pathway. These events were associated with a decrease and increase in Bcl-2 and Bax expression, respectively, as well as phosphorylation of mitogen-activated protein kinase (MAPK) and activation of p53-MDM2 pathway. However, the antioxidant N-acetylcysteine opposed MSFTZ-mediated mitochondrial dysfunction, caspase activation, Bcl-2/Bax modulation, and apoptosis, supporting the role of ROS in the apoptotic process. We were surprised that we failed to observe the protective effect of N-acetylcysteine against MSFTZ-induced MAPK activation. Furthermore, MSFTZ had an antitumor effect in vivo by 34.8 to 78.7% reduction of tumor size in SMMC-7721-xenografted nude mice. We conclude that MSFTZ induces HCC cell apoptosis both in vivo and in vitro via caspase- and ROS-dependent mitochondrial pathway. In addition, MSFTZ has potential as a novel therapeutic agent for the treatment of HCC.
-
Antileukemia activity of MSFTZ-a novel Flavanone analog.
Anti-cancer drugs, 2006Co-Authors: Liang Fang, Huazhou Ying, Bo YangAbstract:A newly synthesized Flavanone Derivative, (+/-)-(3aRS,4SR)-2-(2-chloro-4-methyl- sulfonylphenyl)-4'-chloro-3a,4-diethoxy-flavane[4,3-d]-Delta-1,2,3-thiadiazoline (MSFTZ), was investigated for its antileukemia activity and molecular mechanisms. Cytotoxicity assay confirmed the high antiproliferative efficiency of MSFTZ in six leukemia cell lines (including two drug-resistant cell lines), with 50% inhibition of cell viability values ranging from 1.0 to 9.2 micromol/l. The results of flow cytometry assay showed that the percentage of apoptotic HL-60 cells was 68.3% after 48 h treatment with MSFTZ, suggesting that the activation of the apoptosis pathway was an anticancer property of MSFTZ. Furthermore, the protein changes related to apoptosis were investigated. Exposure of HL-60 cells to MSFTZ induced pro-caspase-9 and pro-caspase-3 cleavage, X-linked inhibitor of apoptosis protein and Bcl-X(L) downregulation, and poly(ADP-ribose) polymerase degradation. Treatment of cells with MSFTZ resulted in a time-dependent reduction in phosphorylation (activation) of extracellular signal-regulated kinase 1/2 and an increase in phosphorylation (activation) of Jun N-terminal kinase. Taken together, our results demonstrated that activation of mitogen-activated protein kinase and apoptotic cascade is involved in MSFTZ-induced antileukemia activity. All data suggest that MSFTZ is a promising chemotherapy drug.
Ruqayya Afridi - One of the best experts on this subject based on the ideXlab platform.
-
Anti-hyperalgesic properties of a Flavanone Derivative Poncirin in acute and chronic inflammatory pain models in mice
BMC Pharmacology and Toxicology, 2019Co-Authors: Ruqayya Afridi, Ashraf Ullah Khan, Sidra Khalid, Bushra Shal, Hina Rasheed, Muhammad Zia Ullah, Omer Shehzad, Yeong Shik Kim, Salman KhanAbstract:Background Poncirin is Flavanone Derivative (isolated from Poncirus trifoliata ) with known pharmacological activities such as anti-tumor, anti-osteoporotic, anti-inflammatory and anti-colitic. The present study aimed to explore the anti-allodynic and anti-hyperalgesic potentials of poncirin in murine models of inflammatory pain. Methods The analgesic potential of poncirin was evaluated in formalin-, acetic acid-, carrageenan- and Complete Freund’s Adjuvant (CFA)-induced inflammatory pain models in mice. Anti-allodynic and anti-hyperalgesic activities were measured using Von Frey filaments, Randall Selitto, hotplate and cold acetone tests. The serum nitrite levels were determined using Griess reagent. The Quantitative Real-time PCR (qRT-PCR) was performed to assess the effect of poncirin on mRNA expression levels of inflammatory cytokines and anti-oxidant enzymes. Results Intraperitoneal administration of poncirin (30 mg/kg) markedly reduced the pain behavior in both acetic acid-induced visceral pain and formalin-induced tonic pain models used as preliminary screening tools. The poncirin (30 mg/kg) treatment considerably inhibited the mechanical hyperalgesia and allodynia as well as thermal hyperalgesia and cold allodynia. The qRT-PCR analysis showed noticeable inhibition of pro-inflammatory cytokines (mRNA expression levels of TNF-α, IL-1β and IL-6) ( p
-
Anti-hyperalgesic properties of a Flavanone Derivative Poncirin in acute and chronic inflammatory pain models in mice.
BMC pharmacology & toxicology, 2019Co-Authors: Ruqayya Afridi, Ashraf Ullah Khan, Sidra Khalid, Bushra Shal, Hina Rasheed, Muhammad Zia Ullah, Omer Shehzad, Yeong Shik Kim, Salman KhanAbstract:Poncirin is Flavanone Derivative (isolated from Poncirus trifoliata) with known pharmacological activities such as anti-tumor, anti-osteoporotic, anti-inflammatory and anti-colitic. The present study aimed to explore the anti-allodynic and anti-hyperalgesic potentials of poncirin in murine models of inflammatory pain. The analgesic potential of poncirin was evaluated in formalin-, acetic acid-, carrageenan- and Complete Freund’s Adjuvant (CFA)-induced inflammatory pain models in mice. Anti-allodynic and anti-hyperalgesic activities were measured using Von Frey filaments, Randall Selitto, hotplate and cold acetone tests. The serum nitrite levels were determined using Griess reagent. The Quantitative Real-time PCR (qRT-PCR) was performed to assess the effect of poncirin on mRNA expression levels of inflammatory cytokines and anti-oxidant enzymes. Intraperitoneal administration of poncirin (30 mg/kg) markedly reduced the pain behavior in both acetic acid-induced visceral pain and formalin-induced tonic pain models used as preliminary screening tools. The poncirin (30 mg/kg) treatment considerably inhibited the mechanical hyperalgesia and allodynia as well as thermal hyperalgesia and cold allodynia. The qRT-PCR analysis showed noticeable inhibition of pro-inflammatory cytokines (mRNA expression levels of TNF-α, IL-1β and IL-6) (p
-
anti hyperalgesic properties of a Flavanone Derivative poncirin in acute and chronic inflammatory pain models in mice
BMC Clinical Pharmacology, 2019Co-Authors: Ruqayya Afridi, Ashraf Ullah Khan, Sidra Khalid, Bushra Shal, Hina Rasheed, Muhammad Zia Ullah, Omer Shehzad, Yeong Shik Kim, Salman KhanAbstract:Poncirin is Flavanone Derivative (isolated from Poncirus trifoliata) with known pharmacological activities such as anti-tumor, anti-osteoporotic, anti-inflammatory and anti-colitic. The present study aimed to explore the anti-allodynic and anti-hyperalgesic potentials of poncirin in murine models of inflammatory pain. The analgesic potential of poncirin was evaluated in formalin-, acetic acid-, carrageenan- and Complete Freund’s Adjuvant (CFA)-induced inflammatory pain models in mice. Anti-allodynic and anti-hyperalgesic activities were measured using Von Frey filaments, Randall Selitto, hotplate and cold acetone tests. The serum nitrite levels were determined using Griess reagent. The Quantitative Real-time PCR (qRT-PCR) was performed to assess the effect of poncirin on mRNA expression levels of inflammatory cytokines and anti-oxidant enzymes. Intraperitoneal administration of poncirin (30 mg/kg) markedly reduced the pain behavior in both acetic acid-induced visceral pain and formalin-induced tonic pain models used as preliminary screening tools. The poncirin (30 mg/kg) treatment considerably inhibited the mechanical hyperalgesia and allodynia as well as thermal hyperalgesia and cold allodynia. The qRT-PCR analysis showed noticeable inhibition of pro-inflammatory cytokines (mRNA expression levels of TNF-α, IL-1β and IL-6) (p < 0.05) in poncirin treated group. Similarly, poncirin treatment also enhanced the mRNA expressions levels of anti-oxidant enzymes such as transcription factor such as nuclear factor (erythroid-derived 2)-like 2 (Nrf2) (p < 0.05), heme oxygenase (HO-1) (p < 0.05) and superoxide dismutase (SOD2) (p < 0.05). Chronic treatment of poncirin for 6 days did not confer any significant hepatic and renal toxicity. Furthermore, poncirin treatment did not altered the motor coordination and muscle strength in CFA-induced chronic inflammatory pain model. The present study demonstrated that poncirin treatment significantly reduced pain behaviors in all experimental models of inflammatory pain, suggesting the promising analgesic potential of poncirin in inflammatory pain conditions.