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Maghfiroh Gesty Maharani - One of the best experts on this subject based on the ideXlab platform.
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molecular docking studies flavonoid quercetin Isoquercetin and kaempferol of single bulb garlic allium sativum to inhibit lanosterol synthase as anti hypercholesterol therapeutic strategies
International Seminar Metallurgy and Materials, 2020Co-Authors: Maghfiroh Gesty Maharani, Sri Lestari, Betty LukiatiAbstract:Hypercholesterolemia is the highest risk of CVD which is the biggest disease leading death. One of the Indonesian medicinal plants is single bulb garlic with high flavonoids concentration. Lanosterol synthase, an enzyme on the final stage of cholesterol synthesis are the appropriate inhibition stage for drug. This study aimed to analyze the potential of single bulb garlic flavonoids (quercetin, Isoquercetin, and kaempferol) in inhibiting lanosterol synthase. Computational docking analysis was performed using Pyrx, Pymol, Discovery studio, also webserver to predict ADMET and biological activity. Lanosterol synthase was obtained from PDB (PDB ID: IW6J) with RO 48-8071 as native ligand used for control. The results showed binding affinity RO 48-8071 (-10.3 kcal/mol), quercetin (-9.8 kcal/mol), Isoquercetin (-6.8 kcal/mol), and kaempferol (-9.9 kcal/mol). Based on interaction and bonding distance, flavonoids have more stable than control. Flavonoids also have potential as APOA1, HMOX1 enhancers, lipid peroxidase inhibitors, cardioprotectant and hepatoprotectant, high distribution volumes, low toxicity, and clearance. This result indicated that quercetin, Isoquercetin, and kaempferol from single bulb garlic could be potential ligand to treat hypercholesterolemia, and could proceed to in vitro and in vivo study by improving the absorption.
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potensi antihiperkolesterolemik senyawa flavonoid quercetin Isoquercetin dan kaempferol bawang putih tunggal allium sativum terhadap target enzim lanosterol synthase menggunakan teknik molecular docking
SKRIPSI Jurusan Biologi - Fakultas MIPA UM, 2019Co-Authors: Maghfiroh Gesty MaharaniAbstract:Potensi Anti hiperkolesterolemik Senyawa Flavonoid (Quercetin, Isoquercetin, dan Kaempferol) Bawang Putih Tunggal (Allium sativum) Terhadap Target Enzim Lanosterol Synthase MenggunakanTeknik Molecular Docking Maghfiroh Gesty Maharani1, Sri Rahayu Lestari1, Betty Lukiati1 1Jurusan Biologi, FakultasMatematikadanIlmuPengetahuanAlam UniversitasNegeri Malang, Jalan Semarang No 5 Malang, 65145, Indonesia Email koresponden :srirahayulestari@um.ac.id Abstrak : Jantung dan stroke merupakan penyakit penyebab kematian terbesar di duniadengan faktor risiko tertinggi karena hiperkolesterolemia. Penggunaan tanaman herbal sebagai obat hiperkolesterolemia meningkat seiring dengan bertambahnya efek samping obat sintetis dan rekomendasi oleh WHO. Tanaman obat Indonesia, salah satunya adalah bawang putih tunggal. Kandungan utama bawang putih tunggal selain senyawa organosulfur adalah flavonoid. Tahap akhir sintesis kolesterol yang melibatkan enzim lanosterol synthase, merupakan tahapan paling tepat untuk penghambatan obat. Tujuan penelitian ini adalah memprediksi potensi senyawa flavonoid bawang putih tunggal (quercetin, Isoquercetin, dan kaempferol) dalam menghambat enzim lanosterol synthase sebagai antihiperkolesterolemia. Penelitian ini melalui teknik molecular docking dengan software Pyrx, Pymol, Discovery studio serta webserver prediksi potensi dan sifat farmakokinetik. Hasil penelitian menunjukkan senyawa flavonoid bawang putih tunggal memiliki potensi sebagai APOA1 dan HMOX1 enhancer, lipid peroxidase inhibitor, cardioprotectant serta hepatoprotectant, memiliki volume distribusi tinggi (> 0,45 logL/kg), nilai clearance dan toksisitas rendah. Hasil docking menunjukkan energi ikatan RO 48-8071 (-10,3 kcal/mol), kaempferol (-9,9 kcal/mol), quercetin (-9,8 kcal/mol), Isoquercetin (-6,8 kcal/mol), senyawa flavonoid memiliki ikatan hidrogen dan interaksi hidrofobik, dengan jarak ikatan yang lebih stabil dibandingkan kontrol. Berdasarkan berbagai parameter, senyawa flavonoid memiliki potensi sebagai antihiperkolesterolemia. Hasil prediksi pada penelitian dapat dilanjutkan untuk menguji senyawa flavonoid bawang putih tunggal secara in vitro dan in vivo dengan meningkatkan absorbsi senyawa. Kata Kunci : Antihiperkolesterolemia, Bawang putih tunggal, Flavonoid, Molecular docking. Anti hypercholesterolemic Potential Flavonoid (Quercetin, Isoquercetin, and Kaempferol) of Single Clove Garlic (Allium sativum) Against the Lanosterol Synthase Using Molecular Docking Technique Maghfiroh Gesty Maharani1, Sri Rahayu Lestari1, Betty Lukiati1 1Biology Departement, Faculty Mathematics and Science State University of Malang, St. Semarang 5 Malang, 65145, Indonesia Corresponding author :srirahayulestari@um.ac.id Abstract: Heart and stroke are the biggest cause of death in the world with the highest risk factors due to hypercholesterolemia. The use of herbs as hypercholesterolemia drug increases with increasing side effects of synthetic drugs and recommendations by WHO. Indonesian medicinal plants, one of which is single clove garlic. The main content of single clove garlic beside organosulfur compounds is flavonoids. The final stage of cholesterol synthesis involving the enzyme lanosterol synthase, is the most appropriate stage for drug inhibition. The purpose of this study was to predict the potential of single clove garlic flavonoids (quercetin, Isoquercetin, and kaempferol) in inhibiting the enzyme lanosterol synthase as antihypercholesterolemia. This research is through molecular docking techniques with Pyrx, Pymol software, Discovery studios and web server predictors of potential and pharmacokinetic properties. The results showed that single garlic flavonoids had potential as APOA1 and HMOX1 enhancers, lipid peroxidase inhibitors, cardioprotectant and hepatoprotectant, had high distribution volumes (> 0.45 logL / kg), low clearance and toxicity. The docking result shows RO bond energy 48-8071 (-10.3 kcal / mol), kaempferol (-9.9 kcal / mol), quercetin (-9.8 kcal / mol), Isoquercetin (-6.8 kcal / mol ), flavonoid compounds have hydrogen bonds and hydrophobic interactions, with bonding distances that are more stable than controls. Based on various parameters, flavonoids have the potential to be antihypercholesterolemic. Predicted results in the study can be continued to test single garlic flavonoids in vitro and in vivo by increasing the absorption of compounds. Keywords : Antihypercholesterolemia, Single Clove Garlic, Flavonoids, Molecular docking. 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Potensi Antihiperkolesterolemik Senyawa Flavonoid (Quercetin, Isoquercetin, dan Kaempferol) Bawang Putih Tunggal (Allium sativum) Terhadap Target Enzim Lanosterol Synthase Menggunakan Teknik Molecular Docking
SKRIPSI Jurusan Biologi - Fakultas MIPA UM, 2019Co-Authors: Maghfiroh Gesty MaharaniAbstract:Potensi Anti hiperkolesterolemik Senyawa Flavonoid (Quercetin, Isoquercetin, dan Kaempferol) Bawang Putih Tunggal (Allium sativum) Terhadap Target Enzim Lanosterol Synthase MenggunakanTeknik Molecular DockingMaghfiroh Gesty Maharani1, Sri Rahayu Lestari1, Betty Lukiati1 1Jurusan Biologi, FakultasMatematikadanIlmuPengetahuanAlam UniversitasNegeri Malang, Jalan Semarang No 5 Malang, 65145, IndonesiaEmail koresponden :srirahayulestari@um.ac.id Abstrak: Jantung dan stroke merupakan penyakit penyebab kematian terbesar di duniadengan faktor risiko tertinggi karena hiperkolesterolemia. Penggunaan tanaman herbal sebagai obat hiperkolesterolemia meningkat seiring dengan bertambahnya efek samping obat sintetis dan rekomendasi oleh WHO. Tanaman obat Indonesia, salah satunya adalah bawang putih tunggal. Kandungan utama bawang putih tunggal selain senyawa organosulfur adalah flavonoid. Tahap akhir sintesis kolesterol yang melibatkan enzim lanosterol synthase, merupakan tahapan paling tepat untuk penghambatan obat. Tujuan penelitian ini adalah memprediksi potensi senyawa flavonoid bawang putih tunggal (quercetin, Isoquercetin, dan kaempferol) dalam menghambat enzim lanosterol synthase sebagai antihiperkolesterolemia. Penelitian ini melalui teknik molecular docking dengan software Pyrx, Pymol, Discovery studio serta webserver prediksi potensi dan sifat farmakokinetik. Hasil penelitian menunjukkan senyawa flavonoid bawang putih tunggal memiliki potensi sebagai APOA1 dan HMOX1 enhancer, lipid peroxidase inhibitor, cardioprotectant serta hepatoprotectant, memiliki volume distribusi tinggi (> 0,45 logL/kg), nilai clearance dan toksisitas rendah. Hasil docking menunjukkan energi ikatan RO 48-8071 (-10,3 kcal/mol), kaempferol (-9,9 kcal/mol), quercetin (-9,8 kcal/mol), Isoquercetin (-6,8 kcal/mol), senyawa flavonoid memiliki ikatan hidrogen dan interaksi hidrofobik, dengan jarak ikatan yang lebih stabil dibandingkan kontrol. Berdasarkan berbagai parameter, senyawa flavonoid memiliki potensi sebagai antihiperkolesterolemia. Hasil prediksi pada penelitian dapat dilanjutkan untuk menguji senyawa flavonoid bawang putih tunggal secara in vitro dan in vivo dengan meningkatkan absorbsi senyawa. Kata Kunci: Antihiperkolesterolemia, Bawang putih tunggal, Flavonoid, Molecular docking. Anti hypercholesterolemic Potential Flavonoid (Quercetin, Isoquercetin, and Kaempferol) of Single Clove Garlic (Allium sativum) Against the Lanosterol Synthase Using Molecular Docking TechniqueMaghfiroh Gesty Maharani1, Sri Rahayu Lestari1, Betty Lukiati1 1Biology Departement, Faculty Mathematics and Science State University of Malang, St. Semarang 5 Malang, 65145, IndonesiaCorresponding author :srirahayulestari@um.ac.id Abstract: Heart and stroke are the biggest cause of death in the world with the highest risk factors due to hypercholesterolemia. The use of herbs as hypercholesterolemia drug increases with increasing side effects of synthetic drugs and recommendations by WHO. Indonesian medicinal plants, one of which is single clove garlic. The main content of single clove garlic beside organosulfur compounds is flavonoids. The final stage of cholesterol synthesis involving the enzyme lanosterol synthase, is the most appropriate stage for drug inhibition. The purpose of this study was to predict the potential of single clove garlic flavonoids (quercetin, Isoquercetin, and kaempferol) in inhibiting the enzyme lanosterol synthase as antihypercholesterolemia. This research is through molecular docking techniques with Pyrx, Pymol software, Discovery studios and web server predictors of potential and pharmacokinetic properties. The results showed that single garlic flavonoids had potential as APOA1 and HMOX1 enhancers, lipid peroxidase inhibitors, cardioprotectant and hepatoprotectant, had high distribution volumes (> 0.45 logL / kg), low clearance and toxicity. The docking result shows RO bond energy 48-8071 (-10.3 kcal / mol), kaempferol (-9.9 kcal / mol), quercetin (-9.8 kcal / mol), Isoquercetin (-6.8 kcal / mol ), flavonoid compounds have hydrogen bonds and hydrophobic interactions, with bonding distances that are more stable than controls. Based on various parameters, flavonoids have the potential to be antihypercholesterolemic. Predicted results in the study can be continued to test single garlic flavonoids in vitro and in vivo by increasing the absorption of compounds. Keywords: Antihypercholesterolemia, Single Clove Garlic, Flavonoids, Molecular docking
Cai-ping Wang - One of the best experts on this subject based on the ideXlab platform.
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Isoquercetin improves inflammatory response in rats following ischemic stroke
Frontiers in Neuroscience, 2021Co-Authors: Yun-wei Shi, Xin Miao Liang, Xinyi Chen, Jiaxing Liu, Xingjuan Fan, Ying Jin, Jiale Liang, Cai-ping WangAbstract:Inflammatory response contributes to brain injury after ischemia and reperfusion (I/R). Our previous literature has shown Isoquercetin plays an important role in protecting against cerebral I/R injury. The present study was conducted to further investigate the effect of Isoquercetin on inflammation-induced neuronal injury in I/R rats with the involvement of cyclic adenosine monophosphate (cAMP)/protein kinase A (PKA) and inhibitor of NF-κB (I-κB)/nuclear factor-kappa B (NF-κB) signaling pathway mediated by Toll-like receptor 4 (TLR4) and C5a receptor 1 (C5aR1). In vivo middle cerebral artery occlusion and reperfusion (MCAO/R) rat model and in vitro oxygen-glucose deprivation and reperfusion (OGD/R) neuron model were used. MCAO/R induced neurological deficits, cell apoptosis, and release of cytokines such as tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-6 in ischemic brain in rats. Simultaneously, the expression of TLR4 and C5aR1 was significantly up-regulated in both MCAO/R rats and OGD/R neurons, accompanied with the inhibition of cAMP/PKA signaling and activation of I-κB/NF-κB signaling in the cortex of MCAO/R rats. Over-expression of C5aR1 in neurons induced decrease of cell viability, exerting similar effects with OGD/R injury. Isoquercetin acted as a neuroprotective agent against I/R brain injury to suppress inflammatory response and improve cell recovery by inhibiting TLR4 and C5aR1 expression, promoting cAMP/PKA activation, and inhibiting I-κB/NF-κB activation and Caspase 3 expression. TLR4 and C5aR1 contributed to inflammation and apoptosis via activating cAMP/PKA/I-κB/NF-κB signaling during cerebral I/R, suggesting that this signaling pathway may be a potent therapeutic target in ischemic stroke. Isoquercetin was identified as a neuroprotective agent, which maybe a promising therapeutic agent used for the treatment of ischemic stroke and related diseases.
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Isoquercetin Ameliorates Cerebral Impairment in Focal Ischemia Through Anti-Oxidative, Anti-Inflammatory, and Anti-Apoptotic Effects in Primary Culture of Rat Hippocampal Neurons and Hippocampal CA1 Region of Rats
Molecular Neurobiology, 2017Co-Authors: Cai-ping Wang, Yun-wei Shi, Xiao-chuan Zhang, Xin Miao Liang, Miao Tang, Yun Gu, Zhi-wei Wang, Fei DingAbstract:Ischemic stroke is a major disability and cause of death worldwide due to its narrow therapeutic time window. Neuroprotective agent is a promising strategy to salvage acutely ischemic brain tissue and extend the therapeutic time window for stroke treatment. In this study, we aimed to evaluate the neuroprotective effects of Isoquercetin in (1) primary culture of rat hippocampal neurons exposure on oxygen and glucose deprivation and reperfusion (OGD/R) injury and (2) rats subjected to transient middle cerebral artery occlusion and reperfusion (MCAO/R) injury. The results showed that Isoquercetin post-treatment reduced the infarct size, number of apoptotic cells, oxidative stress, and inflammatory response after ischemia and reperfusion injury. The underlying mechanism study indicated that the neuroprotective effects of Isoquercetin were elicited via suppressing the activation of toll-like receptor 4 (TLR4), nuclear factor-kappa B (NF-κB) and caspase-1; the phosphorylation of ERK1/2, JNK1/2, and p38 mitogen-activated protein kinase (MAPK); and the secretion of tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), and IL-6. In addition, Isoquercetin also effectively alleviated hippocampus neuron apoptosis by regulation of cyclic AMP responsive element-binding protein (CREB), Bax, Bcl-2, and caspase-3. Our report provided new considerations into the therapeutic action and the underlying mechanisms of Isoquercetin to improve brain injury in individuals who have suffered from ischemic stroke. As a potent anti-inflammatory and anti-oxidative compound with neuroprotective capacities, the beneficial effects of Isoquercetin when used to treat ischemic stroke and related diseases in humans warrant further studies.
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Isoquercetin protects cortical neurons from oxygen glucose deprivation reperfusion induced injury via suppression of tlr4 nf кb signal pathway
Neurochemistry International, 2013Co-Authors: Cai-ping Wang, Xiao-chuan Zhang, Xin Miao Liang, Zhi-wei Wang, Fei Ding, Luzhong ZhangAbstract:In the present study, oxygen-glucose deprivation followed by reperfusion (OGD/R), an in vitro model of ischemia, was used to evaluate the neuroprotective effect of Isoquercetin in primary culture of rat cortical neuronal cells. It was found that Isoquercetin administered prior to the insult could prevent OGD/R-induced intracellular calcium concentrations ([Ca2+](i)) increase, lactate dehydrogenase (LDH) release and cell viability decrease. For the first time, Isoquercetin is described as a neuroprotective agent that potentially explains the alleviation and prevention from OGD/R-induced injury in neurons. Mechanistic studies showed that the neuroprotective effect of Isoquercetin was carried out by anti-inflammatory signaling pathway of inhibiting protein expression of toll-like receptor 4 (TLR4) and nuclear factor-kappa B (NF-kappa B), and mRNA expression of TNF-alpha and IL-6, accompanied by the anti-apoptotic signaling pathway of deactivation of extracellular-regulated kinase (ERK), Jun kinase (JNK) and p38, and inhibition of activity of caspase-3. Therefore, these studies highlighted the confirmation of Isoquercetin, a flavonoid compound, as an anti-inflammation and anti-apoptosis factor which might be used as a therapeutic strategy for the ischemia/reperfusion (I/R) brain injury and related diseases. (C) 2013 Elsevier Ltd. All rights reserved.
Zhi-wei Wang - One of the best experts on this subject based on the ideXlab platform.
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Isoquercetin Ameliorates Cerebral Impairment in Focal Ischemia Through Anti-Oxidative, Anti-Inflammatory, and Anti-Apoptotic Effects in Primary Culture of Rat Hippocampal Neurons and Hippocampal CA1 Region of Rats
Molecular Neurobiology, 2017Co-Authors: Cai-ping Wang, Yun-wei Shi, Xiao-chuan Zhang, Xin Miao Liang, Miao Tang, Yun Gu, Zhi-wei Wang, Fei DingAbstract:Ischemic stroke is a major disability and cause of death worldwide due to its narrow therapeutic time window. Neuroprotective agent is a promising strategy to salvage acutely ischemic brain tissue and extend the therapeutic time window for stroke treatment. In this study, we aimed to evaluate the neuroprotective effects of Isoquercetin in (1) primary culture of rat hippocampal neurons exposure on oxygen and glucose deprivation and reperfusion (OGD/R) injury and (2) rats subjected to transient middle cerebral artery occlusion and reperfusion (MCAO/R) injury. The results showed that Isoquercetin post-treatment reduced the infarct size, number of apoptotic cells, oxidative stress, and inflammatory response after ischemia and reperfusion injury. The underlying mechanism study indicated that the neuroprotective effects of Isoquercetin were elicited via suppressing the activation of toll-like receptor 4 (TLR4), nuclear factor-kappa B (NF-κB) and caspase-1; the phosphorylation of ERK1/2, JNK1/2, and p38 mitogen-activated protein kinase (MAPK); and the secretion of tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), and IL-6. In addition, Isoquercetin also effectively alleviated hippocampus neuron apoptosis by regulation of cyclic AMP responsive element-binding protein (CREB), Bax, Bcl-2, and caspase-3. Our report provided new considerations into the therapeutic action and the underlying mechanisms of Isoquercetin to improve brain injury in individuals who have suffered from ischemic stroke. As a potent anti-inflammatory and anti-oxidative compound with neuroprotective capacities, the beneficial effects of Isoquercetin when used to treat ischemic stroke and related diseases in humans warrant further studies.
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Isoquercetin protects cortical neurons from oxygen glucose deprivation reperfusion induced injury via suppression of tlr4 nf кb signal pathway
Neurochemistry International, 2013Co-Authors: Cai-ping Wang, Xiao-chuan Zhang, Xin Miao Liang, Zhi-wei Wang, Fei Ding, Luzhong ZhangAbstract:In the present study, oxygen-glucose deprivation followed by reperfusion (OGD/R), an in vitro model of ischemia, was used to evaluate the neuroprotective effect of Isoquercetin in primary culture of rat cortical neuronal cells. It was found that Isoquercetin administered prior to the insult could prevent OGD/R-induced intracellular calcium concentrations ([Ca2+](i)) increase, lactate dehydrogenase (LDH) release and cell viability decrease. For the first time, Isoquercetin is described as a neuroprotective agent that potentially explains the alleviation and prevention from OGD/R-induced injury in neurons. Mechanistic studies showed that the neuroprotective effect of Isoquercetin was carried out by anti-inflammatory signaling pathway of inhibiting protein expression of toll-like receptor 4 (TLR4) and nuclear factor-kappa B (NF-kappa B), and mRNA expression of TNF-alpha and IL-6, accompanied by the anti-apoptotic signaling pathway of deactivation of extracellular-regulated kinase (ERK), Jun kinase (JNK) and p38, and inhibition of activity of caspase-3. Therefore, these studies highlighted the confirmation of Isoquercetin, a flavonoid compound, as an anti-inflammation and anti-apoptosis factor which might be used as a therapeutic strategy for the ischemia/reperfusion (I/R) brain injury and related diseases. (C) 2013 Elsevier Ltd. All rights reserved.
Fang Shan - One of the best experts on this subject based on the ideXlab platform.
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flavonoid composition antibacterial and antioxidant properties of tartary buckwheat bran extract
Industrial Crops and Products, 2013Co-Authors: Lijun Wang, Xiushi Yang, Fang ShanAbstract:Abstract The tartary buckwheat [Fagopyrum tataricum (L.) Gaench] bran, which is an important by-product during the production of tartary buckwheat tea, is a good source of flavonoids but has not been made full use of. Some studies reveal its antioxidant activity. However no research is found for its antibacterial activities against Propionibacterium and Staphylococci species. The 60% (v/v) EtOH extract of the tartary buckwheat bran (TBBE) was prepared at room temperature and the flavonoids content was determined by HPLC. Rutin (541.3 ± 9.3 mg/g), Isoquercetin (9.33 ± 0.16 mg/g) and quercetin (66.3 ± 1.14 mg/g) were detected in the TBBE. The inhibition zone of TBBE against four bacterial strains varied from 7.6 mm to 11.6 mm; minimum inhibition concentration (MIC) values were from 512 μg/mL to 2048 μg/mL. IC50 of DPPH scavenging activity and relative ORAC values were 8.36 ± 0.27 μg/mL and 11,090 ± 1278 μmol TE/g, respectively. For the constituents of TBBE querectin showed higher antioxidant and antibacterial properties than TBBE and its glycosides (Isoquercetin and rutin). These results suggest that TBBE might be useful to develop new types of antibacterial substance and new skin care cosmetics to prevent or improve acne.
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comparative evaluation of quercetin Isoquercetin and rutin as inhibitors of α glucosidase
Journal of Agricultural and Food Chemistry, 2009Co-Authors: Feng Chao Zhou, Fei Gao, Jun Sheng Bian, Fang ShanAbstract:Three flavonoids from tartary buckwheat bran, namely, quercetin (Que), Isoquercetin (Iso) and rutin (Rut), have been evaluated as α-glucosidase inhibitors by fluorescence spectroscopy and enzymatic kinetics and have also been compared with the market diabetes healer, acarbose. The results indicated that Que, Iso and Rut could bind α-glucosidase to form a new complex, which exhibited a strong static fluorescence quenching via nonradiation energy transfer, and an obvious blue shift of maximum fluorescence. The sequence of binding constants (KA) was Que > Iso > Rut, and the number of binding sites was one for all of the three cases. The thermodynamic parameters were obtained by calculations based on data of binding constants. They revealed that the main driving force of the above-mentioned interaction was hydrophobic. Enzymatic kinetics measurements showed that all of the three compounds were effective inhibitors against α-glucosidase. Inhibitory modes all belonged to a mixed type of noncompetitive and antic...
Xin Miao Liang - One of the best experts on this subject based on the ideXlab platform.
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Isoquercetin improves inflammatory response in rats following ischemic stroke
Frontiers in Neuroscience, 2021Co-Authors: Yun-wei Shi, Xin Miao Liang, Xinyi Chen, Jiaxing Liu, Xingjuan Fan, Ying Jin, Jiale Liang, Cai-ping WangAbstract:Inflammatory response contributes to brain injury after ischemia and reperfusion (I/R). Our previous literature has shown Isoquercetin plays an important role in protecting against cerebral I/R injury. The present study was conducted to further investigate the effect of Isoquercetin on inflammation-induced neuronal injury in I/R rats with the involvement of cyclic adenosine monophosphate (cAMP)/protein kinase A (PKA) and inhibitor of NF-κB (I-κB)/nuclear factor-kappa B (NF-κB) signaling pathway mediated by Toll-like receptor 4 (TLR4) and C5a receptor 1 (C5aR1). In vivo middle cerebral artery occlusion and reperfusion (MCAO/R) rat model and in vitro oxygen-glucose deprivation and reperfusion (OGD/R) neuron model were used. MCAO/R induced neurological deficits, cell apoptosis, and release of cytokines such as tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-6 in ischemic brain in rats. Simultaneously, the expression of TLR4 and C5aR1 was significantly up-regulated in both MCAO/R rats and OGD/R neurons, accompanied with the inhibition of cAMP/PKA signaling and activation of I-κB/NF-κB signaling in the cortex of MCAO/R rats. Over-expression of C5aR1 in neurons induced decrease of cell viability, exerting similar effects with OGD/R injury. Isoquercetin acted as a neuroprotective agent against I/R brain injury to suppress inflammatory response and improve cell recovery by inhibiting TLR4 and C5aR1 expression, promoting cAMP/PKA activation, and inhibiting I-κB/NF-κB activation and Caspase 3 expression. TLR4 and C5aR1 contributed to inflammation and apoptosis via activating cAMP/PKA/I-κB/NF-κB signaling during cerebral I/R, suggesting that this signaling pathway may be a potent therapeutic target in ischemic stroke. Isoquercetin was identified as a neuroprotective agent, which maybe a promising therapeutic agent used for the treatment of ischemic stroke and related diseases.
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Isoquercetin Ameliorates Cerebral Impairment in Focal Ischemia Through Anti-Oxidative, Anti-Inflammatory, and Anti-Apoptotic Effects in Primary Culture of Rat Hippocampal Neurons and Hippocampal CA1 Region of Rats
Molecular Neurobiology, 2017Co-Authors: Cai-ping Wang, Yun-wei Shi, Xiao-chuan Zhang, Xin Miao Liang, Miao Tang, Yun Gu, Zhi-wei Wang, Fei DingAbstract:Ischemic stroke is a major disability and cause of death worldwide due to its narrow therapeutic time window. Neuroprotective agent is a promising strategy to salvage acutely ischemic brain tissue and extend the therapeutic time window for stroke treatment. In this study, we aimed to evaluate the neuroprotective effects of Isoquercetin in (1) primary culture of rat hippocampal neurons exposure on oxygen and glucose deprivation and reperfusion (OGD/R) injury and (2) rats subjected to transient middle cerebral artery occlusion and reperfusion (MCAO/R) injury. The results showed that Isoquercetin post-treatment reduced the infarct size, number of apoptotic cells, oxidative stress, and inflammatory response after ischemia and reperfusion injury. The underlying mechanism study indicated that the neuroprotective effects of Isoquercetin were elicited via suppressing the activation of toll-like receptor 4 (TLR4), nuclear factor-kappa B (NF-κB) and caspase-1; the phosphorylation of ERK1/2, JNK1/2, and p38 mitogen-activated protein kinase (MAPK); and the secretion of tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), and IL-6. In addition, Isoquercetin also effectively alleviated hippocampus neuron apoptosis by regulation of cyclic AMP responsive element-binding protein (CREB), Bax, Bcl-2, and caspase-3. Our report provided new considerations into the therapeutic action and the underlying mechanisms of Isoquercetin to improve brain injury in individuals who have suffered from ischemic stroke. As a potent anti-inflammatory and anti-oxidative compound with neuroprotective capacities, the beneficial effects of Isoquercetin when used to treat ischemic stroke and related diseases in humans warrant further studies.
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Isoquercetin protects cortical neurons from oxygen glucose deprivation reperfusion induced injury via suppression of tlr4 nf кb signal pathway
Neurochemistry International, 2013Co-Authors: Cai-ping Wang, Xiao-chuan Zhang, Xin Miao Liang, Zhi-wei Wang, Fei Ding, Luzhong ZhangAbstract:In the present study, oxygen-glucose deprivation followed by reperfusion (OGD/R), an in vitro model of ischemia, was used to evaluate the neuroprotective effect of Isoquercetin in primary culture of rat cortical neuronal cells. It was found that Isoquercetin administered prior to the insult could prevent OGD/R-induced intracellular calcium concentrations ([Ca2+](i)) increase, lactate dehydrogenase (LDH) release and cell viability decrease. For the first time, Isoquercetin is described as a neuroprotective agent that potentially explains the alleviation and prevention from OGD/R-induced injury in neurons. Mechanistic studies showed that the neuroprotective effect of Isoquercetin was carried out by anti-inflammatory signaling pathway of inhibiting protein expression of toll-like receptor 4 (TLR4) and nuclear factor-kappa B (NF-kappa B), and mRNA expression of TNF-alpha and IL-6, accompanied by the anti-apoptotic signaling pathway of deactivation of extracellular-regulated kinase (ERK), Jun kinase (JNK) and p38, and inhibition of activity of caspase-3. Therefore, these studies highlighted the confirmation of Isoquercetin, a flavonoid compound, as an anti-inflammation and anti-apoptosis factor which might be used as a therapeutic strategy for the ischemia/reperfusion (I/R) brain injury and related diseases. (C) 2013 Elsevier Ltd. All rights reserved.