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Yingchang Ma, Yang Zhang, Yuanjuan Zhai, Zhenhua Zhu, Ying Pan, Dawei Qian, Shulan Su, Xinsheng Fan, Jinao Duan
Haizao Yuhu Decoction (HYD) has been used for approximately 500 years and is well-known in Traditional Chinese Medicine for its efficacy in the treatment of thyroid-related diseases. In this study, a rapid liquid chromatography-tandem mass spectrometry method was developed for the determination of liquiritin, naringin, hesperidin, peimine, liquiritigenin, glycyrrhizic acid, bergapten, nobiletin, osthole, and glycyrrhetinic acid in rat plasma to investigate the pharmacokinetic profile of different HYD prescriptions in a rat model of hypothyroidism...
December 22, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Ruili Li, Chao Zhao, Minna Yao, Ying Song, Yin Wu, Aidong Wen
ETHNOPHARMACOLOGICAL RELEVANCE: Coumarins from Radix angelicae pubescentis (CRAP) are a major active component that are isolated from dried roots of Angelica biserrata Yuan et Shan, which has been used clinically to cure headaches for a long period of time, and it is an effective treatment for pain. The aim of the present study was to investigate the analgesic effect of CRAP on a spared nerve injury (SNI) model of neuropathy. MATERIALS AND METHODS: Antinociceptive effects of CRAP were assessed in Sprague-Dawley male rats using a spared nerve injury model of neuropathic pain...
January 4, 2017: Journal of Ethnopharmacology
Chen Yu, Peng Li, Dong Qi, Lei Wang, Hong-Lin Qu, Yue-Juan Zhang, Xue-Kai Wang, Hua-Ying Fan
BACKGROUND AND PURPOSE: As a natural coumarin derivative from the Cnidium monnieri(L)Cusson fruit, osthole consists of 7-methoxy-8-isopentenoxy-coumarin. The purpose of this research is to study the mechanism and effect of osthole on sepsis-induced acute kidney injury. EXPERIMENTAL APPROACH: The protective effect of osthole on mouse macrophage RAW 264.7 and HK-2 cells induced by LPS in vitro and on acute kidney injury model induced by sepsis and established by puncture and cecal ligation (CLP) in vivo were tested...
November 25, 2016: Oncotarget
Xiao-Man Xu, Man-Li Zhang, Yi Zhang, Li Zhao
In the present study, we investigated the effects and mechanisms of Osthole on the apoptosis of non-small cell lung cancer (NSCLC) cells and its synergistic effect with Embelin. Our results revealed that treatment with both Osthole and Embelin inhibited cell proliferation. Notably, combination treatment of Osthole and Embelin inhibited cell proliferation more significantly compared with monotherapy. In addition, morphological analysis and Annexin V/propidium iodide analysis revealed that the combination of Osthole and Embelin enhanced their effect on cell apoptosis...
November 2016: Oncology Letters
Shui Liu, Bowen Liu, Zhao-Qing Luo, Jiaming Qiu, Xuan Zhou, Gen Li, Bing Zhang, Xuming Deng, Zhenguo Yang, Jianfeng Wang
We reported the inhibition of α-Hemolysin (Hla) production in methicillin-resistant Staphylococcus aureus USA300 by osthole and further investigated the combination of osthole and baicalin in the treatment of staphylococcal pneumonia. Using cytotoxicity assays and a mouse model of intranasal lung infection, we evaluated the effect of combined therapy. Our results suggest that the combination of osthole and baicalin alleviated S. aureus-mediated A549 cell injury and protected mice from S. aureus pneumonia.
January 2017: World Journal of Microbiology & Biotechnology
Jin-Cheng Liu, Feng Wang, Mei-Lin Xie, Zong-Qi Cheng, Qiong Qin, Lin Chen, Rong Chen
BACKGROUND: Osthole, a natural coumarin and bioactive compound isolated from the fruit of Cnidium monnieri (L.) Cusson, was reported to prevent isoprenaline-induced myocardial fibrosis in mice by inhibiting the transforming growth factor-β1 (TGF-β1) expression, but the underlying mechanism is still unclear. The aim of this study is to illuminate whether the mechanism of osthole inhibiting collagen I and III expressions is associated with Smad signaling pathway in mouse cardiac fibroblasts (CFs) treated with TGF-β1...
February 1, 2017: International Journal of Cardiology
Natalia Karolina Kordulewska, Elżbieta Kostyra, Anna Cieślińska, Michał Matysiewicz, Ewa Fiedorowicz, Edyta Sienkiewicz-Szłapka
INTRODUCTION: Fexofenadine (FXF) is a third-generation antihistamine drug and osthole is assumed as a natural antihistamine alternative. This paper compares results of histamine, FXF and osthole impact on HRH-1, COX-2, NF-κB-p50, CCR1 mRNA expression. We also measured mRNA expression of IL-1β and CCL5/RANTES in incubated peripheral blood mononuclear cells (PBMC) to compared how histamine, FXF and osthole had influence on expression level and interacts on product secretion. OBJECTIVE: The purpose was to investigate expression pattern in asthma PBMC...
November 10, 2016: Immunobiology
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 the 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 use in external preparations and because it often accompanies menthol as a PE in the preparations...
November 28, 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)...
November 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...
January 2017: 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...
December 4, 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...
November 29, 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...
August 18, 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...
December 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
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