bluuebunny/crossref_metadata_2025_split huggingface dataset:
Krüppel-like factor 8 promotes aerobic glycolysis in prostate cancer cells by regulating AKT/mTOR signaling pathway
Authors: Zhang Cunming , Chen Song , Song Lide , Ye Haibo , Wang Junwei 
Published: January 2021

Purpose: To investigate the effects of Krüppel-like factor 8 (KLF8) in prostate cancer (PCa) cell viability and glycolysis, and explore its role as a regulatory factor.Methods: Immunoblot assays were conducted to assess the expression of KLF8 and proteins in AKT/mTOR pathway in PCa cell lines PC-3 and DU145. Cell Counting Kit-8 assays were performed to assess the effect of KLF8 on PCa cell viability. The glycolysis capacity of PCa cells was determined by measuring the levels of glucose intake, lactic acid production, and cellular ATP levels.Results: Depletion of KLF8 decreased the survival of PCa cells in vitro (p < 0.05). KLF8 depletion also inhibited aerobic glucose metabolism in PCa cells (p < 0.05). Further studies confirmed that KLF8 contributed to the growth and glycolysis of PCa cells via the regulation of AKT/mTOR pathway.Conclusion: KLF8 regulates glycolysis in PCa cells by regulating AKT/mTOR signaling pathway and is thus a promising therapeutic target for PCa treatment.
Keywords: Krüppel-like factor 8 (KLF8), Prostate cancer (PCa), Aerobic glucose, AKT/mTOR signaling pathway, Therapeutic target
Involvement of TNF-alpha and IL-10 in breast cancer and patient survival
Authors: An Lijuan , Dou Xinman , Wang Mingli , Luo Wenjuan , Ma Qiang , Liu Xiaokang 
Published: January 2021

Purpose: To investigate the involvement of tumor necrosis factor α (TNF-α) and interleukin 10 (IL-10) in the pathogenesis of breast cancer in vivo as well as the activity of ten Chinese herbal compounds in human breast cancer (MCF-7) cell proliferation in vitro.Methods: In the in vivo study, the association of serum TNF-α and IL-10 with breast cancer cell invasiveness and prognosis was determined in female patients (n = 192) with breast cancer, while in the in vitro study, ten herbal Chinese compounds were screened for their effectiveness against MCF-7 cells. The levels of TNF-α, IL-10, estrogen receptor (ER), progesterone receptor (PR) and human epidermal growth factor receptor-2 (HER2/neu) were assayed using their respective enzyme-linked immunosorbent assay (ELISA) kits. Molecular docking was used to determine the lead compound(s) that can effectively inhibit TNF-α and IL-10.Results: Raised serum levels of TNF-α and IL-10 were significantly associated with breast cancer cell invasiveness and poor prognosis (p < 0.05). Moreover, there was a strong association between breast cancer prognosis and the expression levels of ER, PR and HER2/neu. Serum TNF-α and IL-10 levels were significantly elevated in stages II and III patients and in those with lymph node metastasis. Treatment of MCF-7 cells with the herbal compounds significantly reduced the synthesis and release of TNF-α and IL-10 (p < 0.05). The results of molecular docking showed that baicalein and oridonin significantly inhibited TNF- α and IL-10. The two herbal compounds had the highest docking scores for inhibition of cytokines, as well as favorable interaction energies.Conclusion: These results indicate that TNF-α and IL-10 are involved in the pathogenesis of breast cancer, and that baicalein and oridonin effectively inhibit the proliferation of the cells.
Keywords: Baicalein, Breast cancer, Interleukin 10, Oridonin, Tumor necrosis factor alpha
Formulation and characterization of artemether-loaded sodium alginate microcapsules
Authors: Nnamani Petra O. , Echezona Adaeze C. , Metu Obialunamma C. , Onoja Simeon U. , Ogbonna John-Dike N. , Akpa Paul A. , Onunkwo Godswill C. , Nzekwe Ifeanyi T. , Attama Anthony A. 
Published: January 2021

Purpose: To increase the solubility of artemether (ART) in Transcutol® HP through microencapsulation in sodium alginate polymer to achieve sustained in vivo release.Method: Graded concentrations of ART (0.00, 0.25, 0.50, 0.75, and 1.00 g) microcapsules were produced using Tween® 80 by the cold homogenization method at 24 x 1000 rpm for 15 min. Characterization based on yield, encapsulation efficiency (EE), particle size, pH stability, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR) and in vivo release using Peter’s four-day suppressive protocol in Wistar mice infected with Plasmodium berghei, were determined.Results: The results obtained indicate that 0.5 g ART-loaded microcapsules (AMC) showed the highest yield of 96.85 %. The EE of 88.3 % corresponded to 0.75 g ART-loaded microcapsules. DSC results revealed that there was a significant reduction in enthalpy in all the formulations compared to the crystalline drug, but no strong bond interaction occurred except for the blank microcapsules. The AMC1.0 showed high dose-dependent plasmodial growth inhibition of 88.75 % while AMC0.25 had the least (68.13 %).Conclusion: The artemether microcapsules showed sustained release characteristics for oral delivery of artemether and therefore may reduce some of the adverse effects associated with high dose artemether therapy in conventional oral tablets.
Keywords: Malaria, Artemether, Transcutol® HP, Sustained-release, RBC count, Antiplasmodial activity
Effect of penehyclidine hydrochloride on IL-6, TNF-α, HIF- 1α and oxidative stress in lung tissue of young rats with acute lung injury
Authors: Shu Jihong , Fang Zhenjiao , Xiong Xinjun 
Published: January 2021

Purpose: To investigate the effect of penehyclidine hydrochloride (PHC) on interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), hypoxia inducible factor-1α (HIF-1α), and oxidative stress levels in lung tissues of acute lung injury (ALI) neonatal rats.Methods: 40 male Sprague-Dawley (SD) rats were assigned to model, low-dose PHC, high-dose PHC, and control groups (n = 10). Levels of IL-6, TNF-α and HIF-1α were evaluated by enzyme-linked immunosorbent assay (ELISA). Pulmonary lesions were determined histologically using H&E staining.Results: The lung tissue levels of IL-6, TNF-α and HIF-1α were significantly higher in model rats than in control rats, and significantly lower in PHC-treated rats than in model group, with decrease in levels as PHC dose increased (p < 0.05). The lung tissue activity of MPO and level of MDA in model rats were significantly higher than those in control rats, but significantly lower in the lung tissues of the two PHC groups than in the model group; decrease in levels occurred as PHC dose increased (p < 0.05).Conclusion: PHC decreases the lung and serum levels of IL-6, TNF-α and HIF-1α in a rat model of ALI, and mitigates pulmonary oxidative stress and lung tissue damage. Thus, penehyclidine hydrochloride may be useful to mitigate ALI-induced damage in patients. However, further studies and clinical trials are required to ascertain this
Keywords: Penehyclidine hydrochloride, Alveolar septum, Acute lung injury, Inflammatory cells, IL-6, TNF-α, HIF-1α, Oxidative stress
Z-ligustilide reduces cisplatin-induced nephrotoxicity via activation of NRF2/HO-1 signaling pathways
Authors: Chen Xu , Cao Yingjie , Guo Naifeng , Lu Guoyuan 
Published: January 2021

Purpose: To investigate the effect of Z-ligustilide (Z-lig) on cisplatin-induced nephrotoxicity and examine whether NRF2 signaling mediates the underlying mechanism of action.Methods: Human proximal tubular epithelial cells (HK-2) were pretreated with 20 or 100 μM Z-lig for 2 h, followed by 10 μM cisplatin treatment for 24 h. Cell viability was measured using (3-(4,5- dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. A commercial kit was used todetermine lactate dehydrogenase (LDH) release. Apoptosis was determined by flow cytometry while Western blotting was used to evaluate protein levels. Levels of malondialdehyde (MDA), superoxide dismutase (SOD), glutathione (GSH), and glutathione peroxidase (GSH-Px) were assessed by enzymelinked immunosorbent assay (ELISA).Results: Cisplatin decreased HK-2 cell viability and increased LDH release, while Z-lig increased cell viability and decreased LDH release in a dose-dependent manner (p < 0.05). Moreover, Z-lig reduced cisplatin-induced apoptosis (p < 0.01), and alleviated cellular oxidative stress caused by cisplatin (p < 0.05). Furthermore, Z-lig activated NRF2/HO-1 signaling in cells treated with cisplatin (p < 0.05).Conclusion: Z-lig reduces cisplatin-induced nephrotoxicity via activation of NRF2/HO-1 signaling. Thus, Z-lig is a potential drug for the treatment of nephrotoxicity caused by cisplatin.
Keywords: Z-ligustilide, Cisplatin, Nephrotoxicity, Oxidative stress, Apoptosis, Nuclear factor erythroid 2-related factor 2, Heme oxygenase-1
Ginsenoside induces cell death in breast cancer cells via ROS/PI3K/Akt signaling pathway
Authors: He Lihong , Wang Xiaorui , Ma Qing , Zhao Weipeng , Jia Yongsheng , Dong Guolei , Zhu Yuehong , Jia Xiaochen , Tong Zhongsheng 
Published: January 2021

Purpose: To study the influence of ginsenoside on breast carcinoma, and the mechanism of action involved.Methods: Different concentrations of ginsenoside were used to treat MCF-7 breast cancer cell line. Cell viability was measured by MTT assay, while protein expressions of p-Akt and p-PI3K were determined using Western blotting. The concentrations of reactive oxidative reactants and reactive oxygen species (ROS) were assessed using fluorescence immunoassay and immunofluorescence assay. The mechanism of action involved in ginsenoside-mediated apoptosis was determined based on ROS/PI3K/Akt signaling pathway.Results: There was no change in the inhibition of MCF-7 cell proliferation in control cells with time (p > 0.05). However, inhibition of MCF-7 cell proliferation in ginsenoside group was significantly higher than that in the control group (p < 0.05); furthermore, it increased with time and ginsenoside concentration. Apoptosis was markedly and concentration-dependently higher in ginsenoside-treated MCF-7 cells than in controls (p > 0.05). There were lower protein levels of p-PI3K and p-Akt in ginsenoside-exposed MCF-7 cells than in control group; the protein expressions decreased with increase in ginsenoside concentration (p < 0.05). The expressions of ROS in ginsenoside-treated MCF-7 cells declined, relative to the untreated group; in addition, the expressions decreased with increase in ginsenoside concentration (p < 0.05).Conclusion: Ginsenoside suppresses proliferation of MCF-7 cell line, and exerts apoptotic effect on the cells via inhibition of the ROS/PI3K/Akt signal pathway. This provides a new approach to treat breast cancer.
Keywords: Breast cancer cells, Ginsenoside, Apoptosis, ROS/PI3K/Akt signaling pathway
Suppressive efficiency of Kojic acid from Aspergillus tamarii MM11 against HepG-2 cell line derived from human liver cancer
Authors: El-Metwally Mohammad M. , ElBealy Eman R. , Beltagy Doha M. , Shaaban Mohamed , El-kott Attalla F. 
Published: January 2021

Purpose: To evaluate the antioxidant and cytotoxic properties of Kojic acid (KOJIC ACID) from Aspergillus tamarii MM11 against HepG-2 cell line derived from human liver cancer.Methods: The crude extract of A. tamarii MM11 was dissolved in a mixture of CH2Cl2/MeOH (85:15) and separation was done using silica gel chromatography using gradient size exclusion chromatograph. The non-polar oily fractions were subjected to gas chromatography-mass spectrometric (GC-MS) analysis. Kojic acid structure was identified by x-beam crystallography and spectroscopic methods. Total antioxidant properties of KOJIC ACID were evaluated by using 1,1-diphenyl-2- picrylhydrazyl (DPPH) against ascorbic acid as a reference. The cytotoxic activity of KOJIC ACID from A. tamarii MM11 was investigated on the human cell line of liver cancer (HepG-2) using a sulforhodamine B (SRB) assay based on a cell density determination by the measurement of cellular protein content.Result: Highly bioactive Kojic acid was isolated as the main product. A. tamarii MM11 Kojic acid showed good antioxidant activity with half-maximal inhibitory concentration of IC50 at concentrations of 10.34 compared to 6.79 μg/mL for ascorbic acid. Kojic acid also showed good cytotoxic activity against HepG-2 cell line of human liver cancer with IC50 at 6.20 compared to 3.25 μg/mL of reference drug doxorubicin.Conclusion: Kojic acid produced naturally from A. tamarii MM11 shows good antioxidant and cytotoxic activity against HepG-2 cell line derived from human liver cancer. These findings suggest that Kojic acid can be therapeutically used as an antitumor drug after further in vivo studies.
Keywords: Aspergillus tamarii, Secondary metabolites, Kojic acid, Anticancer, Liver cancer
Anti-cancer effects of Vernonia amygdalina: A systematic review
Authors: Joseph Julia , Lim Vuanghao , Rahman Heshu Sulaiman , Othman Hemn Hassan , Samad Nozlena Abdul 
Published: January 2021

Purpose: To systematically review all the studies that have addressed the anti-cancer activities of the VA leaf extract in vitro to determine the strength of evidence of its anti-cancer effects and whether it can be used as an effective cancer therapy.Methods: The databases of Scopus, Science Direct, PubMed, Springer, and Directory of Open Access Journals were searched for relevant articles. Only articles published in the English language from January 2000 to November 2018 were selected for full-text retrieval and review, before being included in the final review.Results: From a total of 28 articles identified for full-text retrieval, only 17 fulfilled the inclusion criteria. The papers reviewed showed that VA decreases cell viability, inhibits DNA synthesis and causes DNA damage in cancer cells. VA also induces apoptosis and cell cycle arrest in cancer cells via gene regulation. All in all, there is evidence showing that VA possesses time- and concentration-dependent anti-cancer activity.Conclusion: The VA leaf extract has the potential to be developed into cancer therapeutics. However, more research is needed on its effect on normal cells before VA is developed into a cancer therapeutic.
Keywords: Vernonia amygdalina, Anti-cancer effect, DNA damage, Apoptosis
Enhancement of solubility and dissolution rate of ebastine fast-disintegrating tablets by solid dispersion method
Authors: Islam Nayyer , Irfan Muhammad , Abbas Nasir , Syed Haroon Khalid , Iqbal Muhammad Shahid , Khan Ikram ullah , Rasul Akhtar , Inam Sana , Hussain Amjad , Mohsin Noor ul Amin , Arshad Mohammad Sohail , Ali Mohsin 
Published: January 2021

Purpose: To investigate the efficiency of different solubilizing agents in improving solubility as well as dissolution rate of ebastine (a BCS class II drug) by incorporating prepared solid dispersion into fast disintegrating tablets.Method: The solubility of ebastine was determined in distilled water, lipids and solubilizing agents. Subsequently, the binary solid dispersions were prepared by kneading method using varying weight ratios of ebastine and solubilizing agents. The solid dispersions were then incorporated into fast disintegrating tablets (SD-FDT). Central composite rotatable design (CCD) was used to determine the impact of super disintegrating agents on disintegration time and friability of tablets. The solubility and dissolution rate of developed SD-FDT were compared with a marketed brand. The solid dispersion particles were characterized by Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder x-ray diffraction (P-XRD) and scanning electron microscopy (SEM).Results: The saturated solubility of pure ebastine in water was 0.002 ± 0.041 mg/ml while the aqueous solubility of EBT/poloxamer solid dispersion SET3 (P) was 0.018 ± 2.510 mg/ml; on the other hand, EBT/soluplus solid dispersion SET1(S) has an aqueous solubility of 0.242 ± 1.390 mg/ml. Within 30 min, drug release was 14.00 ± 1.77, 78.00 ± 2.31 and 98.70 ± 2.54 % from pure EBT, SET3 (P) and SET1(S), respectively.Conclusion: The solubility and dissolution rate of ebastine has been successfully enhanced by incorporating its solid dispersion in fast-disintegrating tablets (SD-FDT).
Keywords: Ebastine, Solid dispersion, Poloxamer 188, Soluplus, Solubility, Dissolution
Ameliorative and anti-arthritic potential of arjunolic acid against complete Freund’s adjuvant-induced arthritis in rats
Authors: Fan Yi , Zhang Cheng , Zheng Guotao , Wu Shuai , Wang Yujie , Bian Jinsong 
Published: January 2021

Purpose: To determine the anti-arthritic effect of arjunolic acid against complete Freund’s adjuvant (CFA)-induced arthritis in rats.Methods: Arthritis was induced in male Sprague Dawley rats by intradermal injection of 0.1 mL of CFA at the right footpad. Upon induction of osteoarthritis, arjunolic acid was administered via oral gavage at doses of 40 and 80 mg/kg once daily for 25 successive days. Indomethacin was used as reference drug at a dose of 3 mg/kg via gavage twice weekly for 25 days. Changes in paw swelling, serum hematology, antioxidant enzymes, serum inflammatory mediators, and histopathology were determined using standard procedures.Results: Paw swelling and weight loss in CFA-induced arthritic rats were significantly reversed (p < 0.01) by arjunolic acid. Malondialdehyde (MDA) levels, spleen index and thymus index were significantly reduced in CFA-induced arthritic rats (p < 0.01). Moreover, arjunolic significantly increased superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx) activities, while downregulating the expressions of TNF-α, IL-1β and IL-6 in serum (p < 0.01). The hematological and histopathological changes due to CFA-induced arthritis were ameliorated by arjunolic acid.Conclusion: The results obtained in this study indicate that arjunolic acid may possess therapeutic potentials for the management of arthritis.
Keywords: Arjunolic acid, Triterpenoid; Oxidative stress, osteoarthritis, Inflammation
Glycyrrhizin inhibits the invasion and metastasis of breast cancer cells via upregulation of expressions of miR-200c and e-cadherin
Authors: He Lihong , Wang Xiaorui , Ma Qing , Zhao Weipeng , Jia Yongsheng , Dong Guolei , Zhu Yuehong , Jia Xiaochen , Tong Zhongsheng 
Published: January 2021

Purpose: To determine the inhibitory effect of glycyrrhizin (GLA) on cell invasion and metastasis in mammary carcinoma cells, and the mechanisms of actions involved.Methods: The effect of GLA at different concentrations on proliferation of breast cancer MDA-MB-231 and BT549 cells was assayed by MTT method. Transwell assay was used to determine the effect of GLA at different concentrations on invasiveness and metastasis of breast cancer MDA-MB-231 and BT549 cells. The influence of LGA on expressions of microRNA-200c and miR-200c was assayed by reverse transcriptase-polymerase chain reaction (RT-PCR).Results: There was no statistically significant difference in cell proliferation amongst cells treated with 5 and 20 μM GLA and untreated breast cancer cells. However, the proliferation of cells treated with 40 μM GLA was significantly reduced (p < 0.05). In the cell invasion and migration experiments, cell population transferred to the base of Transwell chamber in the two cell lines treated with GLA was markedly decreased, relative to cells without GLA treatment, while the number of cells decreased with increase in GLA concentration (p < 0.05). Results from image-pro-plus analysis revealed that the population of cells quantitatively crossing the Transwell compartment membrane decreased with increase in GLA concentration (p < 0.05). The expression of e-cadherin was increased by GLA treatment in a concentration-dependent manner. Moreover, GLA treatment led to significant changes in amounts of miR-200s a, b and c, with changes in miR-200c being the most significant (p < 0.05).Conclusion: GLA suppresses the invasiveness and metastasis of breast cancer MDA-MB-231 and BT549 cells via upregulation of the expressions of miR-200c and e-cadherin. These findings provide a theoretical basis for the development of new breast cancer drugs.
Keywords: Glycyrrhiza, GLA, miR-200c, E-cadherin, Inhibition, Breast cancer cells, Invasion, Metastasis
Coenzyme Q10 attenuates airway inflammation and oxidative stress in neonatal asthmatic rats
Authors: Peng Jingwei , Ma Jilong , Zhang Lan , Lu Banghao 
Published: January 2021

Purpose: To determine the therapeutic effect of coenzyme Q10 (CoQ10) on ovalbumin (OVA)-provoked asthma in neonatal rats.Methods: Asthma was induced by exposing neonatal rats to OVA. The levels of SOD, CAT, GPx, GSH, MDA and MPO were estimated using standard biochemical kits, while ELISA was used to measure the concentrations of Ig E and Th2 cytokines. Gene expressions were assayed with qRT-PCR, and protein expressions were determined with western blotting.Results: OVA treatment led to increases in levels of BALF inflammatory cells, lipid peroxidation, serum IgE and BALF Th2 cytokines, but it decreased antioxidant levels. Furthermore, the protein expression of NF-κB and mRNA expression levels of proinflammatory cytokines and inducible nitric oxide synthase (iNOS) were upregulated in the asthmatic rats (p < 0.05). However, coenzyme Q10 supplementation significantly decreased lipid peroxidation, and reduced inflammatory cells and IgE levels, while the antioxidant levels were enhanced (p < 0.05). Moreover, coenzyme Q10 reduced the levels of Th2 cytokines and downregulated the expressions of NF-κB, TNF-α, IL-6, and iNOS in the neonatal asthmatic rats (p < 0.05).Conclusion: Coenzyme Q10 attenuates airway inflammation and oxidative stress in neonatal asthmatic rats. Thus, coenzyme Q10 has promising therapeutic potential in the management of asthma.
Keywords: Asthma, Neonatal, Coenzyme Q10, Th2, cytokines, Oxidative stress, Antiinflammation
Methyl 4-(β-D-glucopyranosyloxy)-3-hydroxy-5- methoxybenzoate, isolated from Sanguisorba officinalis, inhibits CpG-DNA-induced inflammation
Authors: Rahman Mohammad Saydur , Ali Irshad , Arooj Madeeha , Su Xiang Dong , Yang Seo Young , Kim Young Ho , Koh Young-Sang 
Published: January 2021

Purpose: To evaluate the anti-inflammatory effect of methyl-4-(β-D-glucopyranosyloxy)-3-hydroxy-5-methoxybenzoate (comp-1) on immune cells.Methods: Comp-1 was isolated from Sanguisorba officinalis. After treating with comp-1, cell viability and levels of pro-inflammatory cytokines were assessed utilizing MTT assay and ELISA, respectively. Besides, the effects of comp-1 on nuclear factor kappa B (NF-κB), mitogen-activated protein kinase (MAPK), and iNOS were determined using western blotting. Moreover, nitric oxide production was assessed using the Griess reagent.Results: Treatment of dendritic cells (DCs) with CpG DNA upregulated cytokine expression. Comp-1 markedly downregulated the expressions of IL-12 p40, IL-6, and TNF-α, with 50% inhibitory concentrations (IC50) of 1.077 ± 0.04 (p < 0.01), 0.28 ± 0.01 (p < 0.01), and 0.79 ± 0.02 μM (p < 0.01),respectively. Treatment of DCs with CpG DNA upregulated NF-κB and MAPK activation. However, pretreatment of the cells with Comp-1 suppressed CpG DNA-induced NF-κB and MAPK activation. Moreover, comp-1 exhibited a strong anti-inflammatory effect by inhibiting nitric oxide production and iNOS expression.Conclusion: These results reveal that comp-1 has significant anti-inflammatory effect on immune cells.
Keywords: Natural compound, Inflammation, Pro-inflammatory cytokine, Toll-like receptor9