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Shufang Yang, Ran Wang, Guang Wan, Zhimin Wu, Shujuan Guo, Xingxing Dai, Xinyuan Shi, Yanjiang Qiao
Menthol is a widely used penetration enhancer in clinical medicine due to its high efficiency and relative safety. However, details of the penetration enhancement mechanism of menthol on molecular level is rarely involved in the discussion. In this work, the penetration enhancement (PE) mechanism of menthol is explored by a multiscale method containing molecular dynamics simulations, in vitro penetration experiments and transmission electron microscopy. Osthole is chosen to be the tested drug due to its common-using in external preparations and its representative-accompanying with menthol as a PE in the preparations...
October 21, 2016: Journal of Chemical Information and Modeling
Natalia Karolina Kordulewska, Elżbieta Kostyra, Anna Cieślińska, Ewa Fiedorowicz, Beata Jarmołowska
FXF is a third-generation antihistamine drug and osthole is assumed a natural antihistamine alternative. This paper compares peripheral blood mononuclear cell (PBMC) incubation with FXF and osthole, by studying FXF, osthole and histamine cytokine secretion in PBMC in vitro cultures. Mabtech kits determined the interleukins IL-1β, IL-4, IL-10, IL-13 and TNF-α. The influence of the above active substances on cytokine secretion in PBMC's and serum was assessed: cytokines were IL-1β, IL-4, IL-10, IL-13 and TNF-α; and cytokine levels secreted by untreated PBMCs in pure culture medium formed the absolute control (ctrl)...
October 15, 2016: European Journal of Pharmacology
Yu-Hui Yan, Shao-Heng Li, Hong-Yan Li, Ying Lin, Jing-Xian Yang
In recent years, neural stem cell (NSC) transplantation has been widely explored as a treatment for neurodegenerative diseases. NSCs are special cells that have some capacity for self-renewal and the potential to differentiate into multiple cell types. However, the inflammatory environment of diseased tissue is not conducive to the survival of transplanted cells. Osthole (Ost) is a principal bioactive component of Fructus Cnidii, Radix Angelicae Pubescentis and other traditional Chinese medicines. Ost has a wide range of pharmacological activities, such as anti-inflammation, immunomodulation, and neuroprotection...
October 12, 2016: Neurochemical Research
Lin-Na Luo, De Qiong Xie, Xiao Gang Zhang, Rong Jiang
Renal ischemia-reperfusion (I/R) injury is a major cause of acute kidney injury. The pathogenetic mechanisms underlying renal I/R injury involve inflammation, oxidative stress and apoptosis. Osthole is a coumarin derivative that exhibits potential anti-inflammatory activity. The aim of the present study was to investigate the effect of osthole in renal I/R injury and its underlying mechanism. Renal I/R injury was induced by clamping the left renal artery for 45 min followed by 24 h reperfusion with the contralateral nephrectomy...
October 2016: Experimental and Therapeutic Medicine
Seyed Ebrahim Sajjadi, Abbas-Ali Eskandarian, Yalda Shokoohinia, Hosein-Ali Yousefi, Marjan Mansourian, Hasan Asgarian-Nasab, Negar Mohseni
Leishmaniasis has a wide spectrum of signs and symptoms due to infection to numbers of Leishmania species and makes enormous mortality and morbidity. There are clues of antileishmanial effects of prenylated coumarins. Apiaceae family is one of the most important sources of coumarins. Air-dried aerial parts of Ferulago angulata and fruits of Prangos asperula were extracted with n-hexane, using a soxhlet apparatus. The solvents were evaporated under reduced pressure. Column chromatography and crystallization process resulted to isolation of three prenylated coumarins...
July 2016: Research in Pharmaceutical Sciences
Xiaofeng Li, Chunchun Xue, Libo Wang, Dezhi Tang, Jian Huang, Yongjian Zhao, Yan Chen, Dongfeng Zhao, Qi Shi, Yongjun Wang, Bing Shu
The present study aimed to investigate the effects of osthole on osteoclast formation and bone loss in a mouse model of 5/6 nephrectomy. The mice in control and osthole groups were treated 1 month following 5/6 nephrectomy with either a placebo or osthole, respectively. At 2 months post‑nephrectomy, the L4 vertebrae were harvested. The bone mineral density (BMD) of cancellous bone was measured using micro‑CT and tartrate‑resistant acid phosphatase (TRAP) staining was performed to evaluate osteoclast formation...
October 2016: Molecular Medicine Reports
Ping-Ping Song, Jun Zhao, Zong-Liang Liu, Ya-Bing Duan, Yi-Ping Hou, Chun-Qing Zhao, Min Wu, Min Wei, Nian-He Wang, Ye Lv, Zhao-Jun Han
BACKGROUND: Osthol is a natural coumarin and lead compound that has been developed into commercial fungicides in China. Natural coumarins comprise five major subtypes: simple coumarins, linear furanocoumarins, angular furanocoumarins, linear pyranocoumarins and angular pyranocoumarins. Studies pertaining to the antifungal activities of linear pyranocoumarins are few, and no reports exist for the antifungal activities of angular pyranocoumarins. In order to discover more antifungal natural coumarins, we synthesised a series of simple natural coumarins and isolated several plant-based furanocoumarins and pyranocoumarins using previously described methods...
August 28, 2016: Pest Management Science
Guoqiang Jiang, Jia Liu, Baoyin Ren, Yawei Tang, Lawrence Owusu, Man Li, Jing Zhang, Likun Liu, Weiling Li
ETHNOPHARMACOLOGICAL RELEVANCE: Cnidium monnieri (L.) Cusson is a commonly used traditional Chinese medicine to treat gynecological disease in some countries. Osthole, an active O-methylated coumadin isolated from Cnidium monnieri (L.) Cusson, has been shown to induce various beneficial biochemical effects such as anti-seizure and anti-inflammatory effects. However, the anti-tumor mechanism of osthole is not well known. AIM OF STUDY: Here, we show that osthole inhibited the proliferation and migration of two widely used ovarian cancer cell lines, A2780 and OV2008 cells, in a dose-dependent manner...
August 23, 2016: Journal of Ethnopharmacology
Ming-Zhi Zhang, Rong-Rong Zhang, Jia-Qun Wang, Xiang Yu, Ya-Ling Zhang, Qing-Qing Wang, Wei-Hua Zhang
Based on the microwave-assisted synthetic protocol developed in our previous work, we have synthesized a series of novel furo[3,2-c]coumarins as fused Osthole derivatives, via the reaction of 4-hydroxycoumarins and β-ketoesters catalyzed by DMAP. All the target compounds were evaluated in vitro for their antifungal activity against six phytopathogenic fungi, some compounds exhibited potential activity in the primary assays. Especially compounds 6c, 7b, 8b and 8c (shown in Fig. 1) were the most active ones, EC50 values of these four compounds against Colletotrichum capsica, Botrytis cinerea and Rhizoctonia solani were further investigated...
August 9, 2016: European Journal of Medicinal Chemistry
Xingxing Dai, Qianqian Yin, Guang Wan, Ran Wang, Xinyuan Shi, Yanjiang Qiao
Borneol is a natural permeation enhancer that is effective in drugs used in traditional clinical practices as well as in modern scientific research. However, its molecular mechanism is not fully understood. In this study, a mixed coarse-grained model of stratum corneum (SC) lipid bilayer comprised of Ceramide-N-sphingosine (CER NS) 24:0, cholesterol (CHOL) and free fatty acids (FFA) 24:0 (2:2:1) was used to examine the permeation enhancing mechanism of borneol on the model drug osthole. We found two different mechanisms that were dependent on concentrations levels of borneol...
2016: International Journal of Molecular Sciences
Zhongrong Zhang, Wing Nang Leung, Gang Li, Yau Ming Lai, Chun Wai Chan
Osthole has been found to restore bone mass in preclinical osteoporotic models. In the present study, we investigated the effects of osthole on bone fracture repair in mice. Adult C57BL/6 mice were subjected to transverse femoral fractures and administrated orally with 20 mg/kg osthole and vehicle solvent daily from week 1 post-operation. Fracture callus were analyzed by plain radiography, micro-computed tomography, histology, molecular imaging and immunohistochemistry and tartrate-resistant acid phosphatase staining...
August 18, 2016: Calcified Tissue International
Miaomiao Yuan, Yanping Luo, Qi Xin, Haijun Gao, Guochao Zhang, Tao Jing
Echinococcosis is a zoonotic infection caused by cestode species of the genus Echinococcus; in addition, this zoonosis has long been neglected as a parasitic disease and has limited treatment options. Clinical drugs such as benzimidazole derivatives have limited treatment efficacy. The current study evaluated a novel drug, osthole, with low toxicity and high activity against Echinococcus in vitro and in vivo. The results in vitro indicated that the viability of Echinococcus granulosus protoscoleces in the group treated with osthole (120μM) decreased by 100% within 3days...
August 15, 2016: Veterinary Parasitology
Min Jia, Yuan Li, Hai-Liang Xin, Ting-Ting Hou, Nai-Dai Zhang, Hong-Tao Xu, Qiao-Yan Zhang, Lu-Ping Qin
There is an increasing interest in phytoestrogens due to their potential medical usage in hormone replacement therapy (HRT). The present study was designed to investigate the in vitro effects of estrogen-like activities of two widespread coumarins, osthole and imperatorin, using the MCF-7 cell proliferation assay and their alkaline phosphatase (ALP) activities in osteoblasts Saos-2 cells. The two compounds were found to strongly stimulate the proliferation of MCF-7 cells. The estrogen receptor-regulated ERα, progesterone receptor (PR) and PS2 mRNA levels were increased by treatment with osthole and imperatorin...
June 2016: Chinese Journal of Natural Medicines
Shaoheng Li, Yuhui Yan, Yanan Jiao, Zhong Gao, Yang Xia, Liang Kong, Yingjia Yao, Zhenyu Tao, Jie Song, Yaping Yan, Guangxian Zhang, Jingxian Yang
Accumulation of β-amyloid peptide (Aβ) in the brain plays an important role in the pathogenesis of Alzheimer's disease (AD). It has been reported that osthole exerts its neuroprotective effect on neuronal synapses, but its exact mechanism is obscure. Recently, microRNAs have been demonstrated to play a crucial role in inducing synaptotoxicity by Aβ, implying that targeting microRNAs could be a therapeutic approach of AD. In the present study, we investigated the neuroprotective effects of osthole on a cell model of AD by transducing APP695 Swedish mutant (APP695swe, APP) into mouse cortical neurons and human SH-SY5Y cells...
September 2016: Journal of Molecular Neuroscience: MN
Zhi-qiang Pan, Long-long Liang, Zhao-qin Fang, Xiao-mei Liu, Wen-li Lu, Yuan-yuan Zhang
OBJECTIVE: To study the effect of osthole (Ost) on adrenocortical function in Y1 mouse adrenocortical tumor cells. METHODS: Y1 mouse adrenocortical tumor cells were taken as subjects in this experiment. In 10.0%, 1.0%, and 0.1% serum DMEM-F12 medium, Y1 cells were treated with 1, 10, 25, 50, 100, and 200 micromol/L Ost for 24 and 48 h. 0.1% Dimethyl Sulfoxide (DMSO) was taken as negative control group and 1 mmol/L (Bu) 2cAMP as positive control group. Cell growth morphology was observed under inverted microscope...
May 2016: Chinese Journal of Integrated Traditional and Western Medicine
Shu Meng, Chong Zhang, Wei Shi, Xiao-Wei Zhang, Dan-Hua Liu, Ping Wang, Jian-Xin Li, Ying Jin
The main objective of the present research was to evaluate the flexible nano-vesicles for transdermal delivery of osthole. The nano-vesicles were formulated, characterized and evaluated for their physicochemical properties, in vitro skin permeation and in vivo plasma concentration. The encapsulation efficiency of osthole in ethosome and transfersome was measured to be 83.3±4.8% and 80.9±3.6%, respectively. In vitro studies showed that osthole ethosome provided an enhanced transdermal flux of 6.98±1.6μg/cm(2)/h and a decreased lag time of 2...
September 20, 2016: European Journal of Pharmaceutical Sciences
Hongyang Hu, Min Chen, Guangzu Dai, Guoqing Du, Xuezong Wang, Jie He, Yongfang Zhao, Dapeng Han, Yuelong Cao, Yuxin Zheng, Daofang Ding
BACKGROUND/AIMS: Bone marrow-derived mesenchymal stem cells (MSCs) are responsible for new bone formation during adulthood. Accumulating evidences showed that Osthole promotes the osteogenic differentiation in primary osteoblasts. The aim of this study was to investigate whether Osthole exhibits a potential to stimulate the osteogenic differentiation of MSCs and the underlying mechanism. METHODS: MSCs were treated with a gradient concentration of Osthole (6.25 µM, 12...
2016: Cellular Physiology and Biochemistry
Krystyna Skalicka-Woźniak, Tomasz Mroczek, Magdalena Walasek, Kazimierz Głowniak
For the first time, the separation of coumarin derivatives from the petroleum ether extract of the fruits of Mutellina purpurea through high-performance countercurrent chromatography (HPCCC) is described. Four compounds, pteryxin (1; 2.72 mg), hyuganin C (2; 7.94 mg), osthol (3; 4.30 mg), and hyuganin A (4; 3.09 mg), were obtained in a single run following the injection of crude extract (300 mg). Additionally, auraptenol (5) and hyuganin D (6) were identified using LC-ESI-(Q)TOF-MS. The structures of the isolated compounds were elucidated through spectroscopic (NMR and MS) methods...
July 2016: Planta Medica
Jun Liu, Ran Xu, Xiaokun Zhao
OBJECTIVE: To investigate the effect of osthole on epidermal growth factor receptor tyrosine kinase (EGFR-TPK), matrix-metalloproteinase-2 (MMP-2), aminopeptidase N (APN) in bladder cancer cell and the underlying mechanism.
 METHODS: The T24 cell lines were cultured. The inhibitory effects of osthole on EGFR-TPK, APN and MMP-2 were evaluated by spectrophotometric and MTT assay. The caspase-3 activity and the expression COX-2 and VEGF in T24 were examined. The activity of NF-κB was determined by electrophoretic mobility shift assay...
April 2016: Zhong Nan da Xue Xue Bao. Yi Xue Ban, Journal of Central South University. Medical Sciences
Lu Wang, Lei Yang, Ying Lu, Yingzhun Chen, Tianhua Liu, Yanli Peng, Yuhong Zhou, Yang Cao, Zhenggang Bi, Tianyi Liu, Zhenhong Liu, Hongli Shan
BACKGROUND/AIMS: Osteosarcoma is the second highest cause of cancer-related death in children and adolescents. Majority of osteosarcoma patients (90%) show metastasis. Previous reports revealed that osthole showed antitumor activities via induction of apoptosis and inhibition of proliferation. However, the potential effects and detailed molecular mechanisms involved remained unclear. METHODS: Cell viability was analyzed by MTT assay in osteosarcoma cell lines MG-63 and SAOS-2...
2016: Cellular Physiology and Biochemistry
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