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Amirsaeed Hosseini, Fatemeh Mirzaee, Ali Davoodi, Hossein Bakhshi Jouybari, Mohammad Azadbakh
Arnebia, a sub cosmopolitan and important genus of the Boraginaceae family, comprises 25 species distributed among the world. Based on the studies of Persian medicine texts, there are some promising bioactivities for this genus that is unknown in modern medicine and some of them are still the basis of new remedies. This article presents Arnebia according to the most important ancient information by the most famous Persian medicine books like Makhzan Al Advieh, Tohfat Al-Momenin, Al-Qanun, Al-Seidaneh and Ekhtiarate Badiei...
February 1, 2018: Medicinski Glasnik
Suoyuan Li, Tao Zhang, Weiguo Xu, Jianxun Ding, Fei Yin, Jing Xu, Wei Sun, Hongsheng Wang, Mengxiong Sun, Zhengdong Cai, Yingqi Hua
PURPOSE: Osteosarcoma is the most common primary bone cancer and is notorious for pulmonary metastasis, representing a major threat to pediatric patients. An effective drug targeting osteosarcoma and its lung metastasis is urgently needed. DESIGN: In this study, a sarcoma-targeting peptide-decorated disulfide-crosslinked polypeptide nanogel (STP-NG) was exploited for enhanced intracellular delivery of shikonin (SHK), an extract of a medicinal herb, to inhibit osteosarcoma progression with minimal systemic toxicity...
2018: Theranostics
Seyed Abbas Mirzaei, Somayeh Reiisi, Parmida Ghiasi Tabari, Abolfazl Shekari, Fatemeh Aliakbari, Elaheh Azadfallah, Fatemeh Elahian
Cytotoxic activities of acetylshikonin and acetoxyisovalerylshikonin alone and in combination with chemotherapeutic agents against parental and drug resistant cell lines were determined using the MTT assay. Effects of Shikonin derivatives on BCRP, MDR1 and MRP transcript and protein levels were relatively measured. Finally, accumulation and efflux kinetics were conducted. The results revealed cell- and concentration-dependency of the cell cytotoxicity. Acetylshikonin and acetoxyisovalerylshikonin transiently made the mRNA ocean turbulent, but FACS analyses using fluorescent-labeled antibodies showed no significant change in the MDR-protein levels...
February 22, 2018: Scientific Reports
Jia-Nan Li, Yun-Feng Cao, Rong-Rong He, Guang-Bo Ge, Bin Guo, Jing-Jing Wu
Shikonin, a natural naphthoquinone compound derived from the herb Lithospermum erythrorhizon, is widely used for its various pharmacological activities. However, its potential interactions with other medications by inhibiting human carboxylesterases 2 (hCE2) remain unknown. In this study, the inhibitory effects of shikonin on the activity of hCE2 in human liver microsomes are investigated by using fluorescein diacetate (FD), N-(2-butyl-1,3-dioxo-2,3-dihydro-1H-phenalen-6-yl)-2-chloroacetamide (NCEN), and CPT-11 as substrates of hCE2...
February 22, 2018: Phytotherapy Research: PTR
Fan Ni, Xianbo Huang, Zhenzhen Chen, Wenbin Qian, Xiangmin Tong
Burkitt's lymphoma (BL) is a highly aggressive malignancy molecularly characterized by deregulation of the C-MYC proto-oncogene. Recently, it has been confirmed that phosphatidylinositol-3-kinase (PI3K) pathway activation is a crucial element in the malignant transformation of the B cells in BL. Despite the better outcome of adults with BL treated with high-intensity chemotherapy regimens, the overall survival rate for patients older than 60 years remains dismal. Shikonin, a natural naphthoquinone derived from Chinese herbal medicine plant, has the potential to induce cell death in a series of human cancer...
February 20, 2018: Scientific Reports
Caimei Huang, Guohua Hu
Shikonin, a natural naphthoquinone isolated from a traditional Chinese medicinal herb, which exerts anti-cancer effects in various cancers. However, the molecular mechanisms underlying the therapeutic effects of shikonin against endometrioid endometrial cancer (EEC) have not yet been fully elucidated. Herein, we investigated anti-cancer effects of shikonin on EEC cells and explored the underlying molecular mechanism. We observed that shikonin inhibits proliferation in human EEC cell lines with in a dose-dependent manner...
February 15, 2018: Bioscience Reports
Hui Wang, Zheng Liu, Xiangchen Li, Ruijie Zhao, Yabin Pu, Handong Wu, Weijun Guan
Shikonin is known to suppress proliferation and induce apoptosis in a variety of cancer cell lines. In the present study, SMMC-7721 human hepatocellular carcinoma cells were treated with shikonin (1, 2 or 4 µM) for 12-48 h. Cell morphological alterations and DNA damage were determined. Furthermore, changes in cell cycle, mitochondrial transmembrane potential, calcium homeostasis and levels of reactive oxygen species were measured. Shikonin-treated SMMC-7721 cells exhibited morphological changes and DNA damage...
February 2018: Experimental and Therapeutic Medicine
Kuo-Hua Lin, Ming-Yii Huang, Wei-Chung Cheng, Shu-Chi Wang, Shih-Hua Fang, Hung-Pin Tu, Chia-Cheng Su, Yung-Li Hung, Po-Len Liu, Chi-Shuo Chen, Yu-Ting Wang, Chia-Yang Li
Shikonin is a naphthoquinone isolated from the dried root of Lithospermum erythrorhizon, an herb used in Chinese medicine. Although several studies have indicated that shikonin exhibits antitumor activity in breast cancer, the mechanism of action remains unclear. In the present study, we performed transcriptome analysis using RNA-seq and explored the mechanism of action of shikonin in regulating the growth of different types of breast cancer cells. The IC50 of shikonin on MCF-7, SKBR-3 and MDA-MB-231 cells were 10...
February 8, 2018: Scientific Reports
Chin-Shiu Huang, Haw-Wen Chen, Tzu-Yu Lin, Ai-Hsuan Lin, Chong-Kuei Lii
ETHNOPHARMACOLOGICAL RELEVANCE: Shikonin, a naphthoquinone pigment abundant in the root of the Chinese herb Lithospermum erythrorhizon, has been widely used to treat inflammatory diseases for thousands of years. Whether shikonin changes drug metabolism remains unclear. AIM OF THE STUDY: We investigated whether shikonin modulates the expression of hepatic drug-metabolizing enzymes and transporters as well as the possible mechanisms of this action. MATERIALS AND METHODS: Primary hepatocytes isolated from Sprague-Dawley rats were treated with 0-2 μM shikonin and the protein and mRNA levels of drug-metabolizing enzymes and transporters as well as the activation of aryl hydrocarbon receptor (AhR) and NF-E2-related factor 2 (Nrf2) were determined...
January 25, 2018: Journal of Ethnopharmacology
Mani Shankar Babu, Sailendra Mahanta, Alexander J Lakhter, Takashi Hato, Subhankar Paul, Samisubbu R Naidu
Reliance on aerobic glycolysis is one of the hallmarks of cancer. Although pyruvate kinase M2 (PKM2) is a key mediator of glycolysis in cancer cells, lack of selective agents that target PKM2 remains a challenge in exploiting metabolic pathways for cancer therapy. We report that unlike its structural analog shikonin, a known inhibitor of PKM2, lapachol failed to induce non-apoptotic cell death ferroxitosis in hypoxia. However, melanoma cells treated with lapachol showed a dose-dependent inhibition of glycolysis and a corresponding increase in oxygen consumption...
2018: PloS One
Yue Zhang, Bin Sun, Zhi Huang, Dai-Wei Zhao, Qingfan Zeng
BACKGROUND Shikonin is a component of Chinese herbal medicine. The aim of this study was to investigate the effects of shikonin on cell migration of papillary thyroid cancer cells of the TPC-1 cell line in vitro and expression levels of the phosphate and tensin homolog deleted on chromosome 10 (PTEN) and DNA methyltransferase 1 (DNMT1) genes. MATERIAL AND METHODS The Cell Counting Kit-8 (CCK-8) assay was performed to evaluate the proliferation of TPC-1 papillary thyroid cancer cells, and the normal thyroid cells, HTori-3, in vitro...
February 1, 2018: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
Xianchun Wen, Jiping Li, Defu Cai, Liling Yue, Qi Wang, Li Zhou, Li Fan, Jianwen Sun, Yonghui Wu
Shikonin (SHK) has been proven to have a good anti-tumor effect. However, poor water solubility and low bioavailability limit its wide application in clinical practice. In this study, to overcome these drawbacks, RGD-modified shikonin-loaded liposomes (RGD-SSLs-SHK) were successfully prepared. It exhibited excellent physicochemical characteristics including particle size, zeta potential, encapsulation efficiency, and delayed release time. Meanwhile, the targeting activity of the RGD-modified liposomes was demonstrated by flow cytometry and confocal microscopy in the αvβ₃-positive MDA-MB-231 cells...
January 29, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Wenquan Liang, Jianxin Cui, Kecheng Zhang, Hongqing Xi, Aizhen Cai, Jiyang Li, Yunhe Gao, Chong Hu, Yi Liu, Yixun Lu, Ning Wang, Xiaosong Wu, Bo Wei, Lin Chen
Colon cancer is the third most common malignancy worldwide, and chemotherapy is a widely used strategy in clinical therapy. Chemotherapy-resistant of colon cancer is the main cause of recurrence and progression. Novel drugs with efficacy and safety in treating colon cancer are urgently needed. Shikonin, a naphthoquinone derived from the roots of the herbal plant Lithospermum erythrorhizon, has been determined to be a potent anti-tumor agent. The aim of the present study was to detect the underlying anti-tumor mechanism of shikonin in colon cancer...
December 12, 2017: Oncotarget
Yuna Tong, Lan Bai, Rong Gong, Junlan Chuan, Xingmei Duan, Yuxuan Zhu
Excessive accumulation of β-amyloid (Aβ) is thought to be a major causative factor in the pathogenesis of Alzheimer's disease (AD). Pretreating Aβ-induced neurotoxicity is a potential therapeutic approach to ameliorate the progression and development of AD. The present study aimed to investigate the neuroprotective effect of shikonin, a naphthoquinone pigment isolated from the roots of the traditional Chinese herb Lithospermum erythrorhizon, on Aβ1-42-treated neurotoxicity in PC12 cells. Pretreating cells with shikonin strongly improved cell viability, decreased the malondialdehyde and reactive oxygen species (ROS) content, and stabilized the mitochondrial membrane potential in Aβ1-42-induced PC12 cells...
January 8, 2018: Scientific Reports
Yuna Tong, Junlan Chuan, Lan Bai, Jianyou Shi, Lei Zhong, Xingmei Duan, Yuxuan Zhu
Hyperglycemia-induced oxidative stress is thought to play a critical role in the pathogenesis of diabetic nephropathy (DN). Treating high-glucose (HG)-induced proximal tubule injury has become a patential therapeutic option to attenuate the onset and progression of DN. The present study aimed to investigate the renoprotective effect of shikonin, the chief active compound extracted from the roots of the traditional Chinese herb Lithospermum erythrorhizon, on HG-induced cytotoxicity in NRK-52E cells. Treating cells with HG significantly reduce cell viability while also significantly increasing content of reactive oxygen species (ROS)...
January 2, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Jian-Cai Tang, Jia Zhao, Feng Long, Jian-Ye Chen, Bo Mu, Zhen Jiang, Yonggan Ren, Jian Yang
Increasing evidences indicate that shikonin can suppress the tumor growth. However, the mechanisms remain elusive. In the present study, we investigated the effects and mechanisms of shikonin against esophageal cancer. The expression of hypoxia inducible factor 1α (HIF1α) and pyruvate kinase M2 (PKM2) in esophageal cancer tissues and cells was detected by immunohistochemistry and Western blot. CCK-8 was used to examine the esophageal cancer cell viability. Apoptosis and cell cycle were analyzed by flow cytometry...
2018: Journal of Cancer
Hélio Nitta Matsuura, Sonia Malik, Fernanda de Costa, Morteza Yousefzadi, Mohammad Hossein Mirjalili, Randolph Arroo, Avninder S Bhambra, Miroslav Strnad, Mercedes Bonfill, Arthur Germano Fett-Neto
Plant secondary metabolism evolved in the context of highly organized and differentiated cells and tissues, featuring massive chemical complexity operating under tight environmental, developmental and genetic control. Biotechnological demand for natural products has been continuously increasing because of their significant value and new applications, mainly as pharmaceuticals. Aseptic production systems of plant secondary metabolites have improved considerably, constituting an attractive tool for increased, stable and large-scale supply of valuable molecules...
December 30, 2017: Molecular Biotechnology
Yali Zhang, Tingting Xu, Zheer Pan, Xiangting Ge, Chuchu Sun, Chun Lu, Hongjin Chen, Zhongxiang Xiao, Bing Zhang, Yuanrong Dai, Guang Liang
BACKGROUND AND PURPOSE: Acute lung injury (ALI) is a challenging clinical syndrome which manifests as an acute inflammatory response. Myeloid differentiation protein 2 (MD2) has an important role in mediating lipopolysaccharide (LPS)-induced inflammation. Currently, there are no effective molecular-based therapies for ALI or viable biomarkers for predicting the severity of disease. Recent preclinical studies have shown that shikonin (SHI), a natural naphthoquinone, prevents LPS-inflammation...
December 15, 2017: British Journal of Pharmacology
Nami Shimada, Ryoko Takasawa, Sei-Ichi Tanuma
Many cancer cells undergo metabolic reprogramming known as the Warburg effect, which is characterized by a greater dependence on glycolysis for ATP generation, even under normoxic conditions. Glyoxalase I (GLO I) is a rate-limiting enzyme involved in the detoxification of cytotoxic methylglyoxal formed in glycolysis and which is known to be highly expressed in many cancer cells. Thus, specific inhibitors of GLO I are expected to be effective anticancer drugs. We previously discovered a novel GLO I inhibitor named TLSC702...
January 15, 2018: Archives of Biochemistry and Biophysics
Miaomiao Li, Xuan Chen, Shuang Hu, Runqin Wang, Xiaoli Peng, Xiaohong Bai
Oil-in-salt hollow fiber liquid phase microextraction coupled with high performance liquid chromatography ultraviolet detection (HPLC-UV) was developed for determination of the blood concentrations of the main active compounds, hesperidin, honokiol, shikonin, magnolol, emodin and β,β'-dimethylacrylshikonin, after oral administration of Zi-Cao-Cheng-Qi decoction (ZCCQD) and their total plasma protein binding rates. In the procedure, a hollow fiber segment was immersed in organic solvent to fill the solvent in the fiber lumen and wall pore, and then the fiber was immersed into sodium chloride solution to cover a thin salt membrane on the fiber wall pore filling organic solvent...
January 1, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
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