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JOURNAL OF ETHNOPHARMACOLOGY · 2024 · IF 4.8

Efficacy of spilanthol and Acmella oleracea (L.) R. K. Jansen (Asteraceae) extract against Schistosoma mansoni infection

Danilo de Souza Costa,Rayssa A. Cajas,Carla Monteiro Leal,Lara S. Aleixo de Carvalho,Lara Cruz de Souza,Lucas Fukui-Silva,Josué de Moraes,Ademar A. Da Silva Filho

Ethnopharmacological relevance Acmella oleracea (L.) R. K. Jansen, commonly referred to as “Jambu”, is a valuable medicinal plant native to the Amazon regions. Inflorescences of A. oleracea is utilized as local anesthetic properties and for its insecticidal, antiparasitic, and anthelmintic attributes. Aims of this study This study aimed to evaluate the in vitro and in vivo antiparasitic properties of A. oleracea extract and spilanthol (SPL) against Schistosoma mansoni . Materials and methods The ethanolic extract of A. oleracea inflorescences (AoE) was prepared, analyzed by HPLC-DAD, and characterized by UHPLC-HRMS/MS. SPL was isolated from AoE by chromatographic fractionation. The antischistosomal properties of AoE and SPL were evaluated in vitro against adult schistosomes and in preclinical assays using murine models of patent S. mansoni infection. Results Through UHPLC-HRMS/MS analysis, 14 alkamides were annotated in AoE. HPLC-DAD analysis of AoE revealed a peak with a substantial relative area of ∼85%, which was isolated and identified as SPL. AoE and SPL caused mortality of adult schistosomes ex vivo , showing EC 50 values of 32.6 μg/mL and 27.8 μM, respectively, without affected Vero cells or Caenorhabditis elegans . In preclinical studies, the oral administration (400 mg/kg) of AoE and SPL resulted in significant reductions in worm burden of 28% and ∼42%, respectively. Additionally, SPL exhibits remarkable effects on oogram, decreasing egg burden and the number of immature eggs by over 80%, while also promoting significant reductions in hepato- and splenomegaly. Conclusions The research underscores the antischistosomal activity of A. oleracea highlighting the potential of SPL as a lead for the development of new schistosomicidal drugs and encouraging further studies to validate the traditional anthelmintic use of A. oleracea inflorescences.

CAS / MDL: 64-19-7 64-18-6
研究领域: 药理学 · 寄生虫学 · 药物开发
✓ 已验证 产品关联 DOI PubMed 高影响因子
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NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY · 2024 · IF 3.1

Exploring the anti-NSCLC mechanism of phillyrin targeting inhibition of the HSP90-AKT pathway

Duan Qiong,Li Ruochen,Wang Mingxiao,Cui Zhenting,Zhu Xia,Chen Fanghong,Han Feng,Ma Jianxin

Phillyrin (PHN), derived from the dried fruit of Forsythia suspensa (Thunb.) Vahl, is a kind of Chinese herbal medicine with the effect of clearing heat, and has been used in China for thousands of years in treating various tumors. However, the mechanism of its main components on non-small cell lung cancer (NSCLC) remains unclear. PHN is a distinct component extracted from Forsythia suspensa with promising anti-cancer activity against various tumor types. This study sought to elucidate the promising effects of PHN on NSCLC. Based on network pharmacology results, we identified potential PHN targets and pathways for NSCLC treatment. CCK-8 assay, wound healing assay, apoptosis assay, western blot, and in vivo experiments verified the inhibitory effect of PHN on NSCLC. Network pharmacology identified 160 potential PHN targets, 955 NSCLC-related targets, and 54 common targets, along with 132 pathways and 2 core genes. Biological experiments demonstrated that PHN significantly inhibited the growth and migration of A549 and LLC cells while promoting their apoptosis. Western blot analysis revealed down-regulation of AKT, HSP90AA1, and CDC37 expression, suggesting that PHN inhibits A549 and LLC cell proliferation by down-regulating the HSP90-AKT pathway. In vivo experiments confirmed that PHN significantly inhibited NSCLC growth with low toxicity. This study, using network pharmacology and biological experiments, verified the effectiveness of PHN against NSCLC through the HSP90-AKT pathway. These findings provide a foundation for further research and analysis.

CAS / MDL: 487-41-2
研究领域: 肿瘤学 · 药理学 · 分子生物学 · 中药学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ONCOLOGY REPORTS · 2018 ·Vol. 39 ·期 6 ·3055-3063 · IF 2.976

Huaier suppresses proliferative and metastatic potential of prostate cancer PC3 cells via downregulation of Lamin B1 and induction of autophagy

Ailin Yang,Yanan Zhao,Ying Wang,Xiaojun Zha,Yunfang Zhao,Pengfei Tu,Zhongdong Hu

Prostate cancer is one of the most common malignancies occurring in males. Although large advances have been made in the pathogenesis of prostate cancer, the development of drugs with high efficacy and low toxicity for the treatment of prostate cancer is urgently needed. Recently, more and more attention has been paid to the antitumor effect of Traditional Chinese Medicine (TCM) worldwide. Trametes robiniophila Murr. (Huaier) has been applied as a type of TCM drug for ~1,600 years. Huaier exhibits excellent clinical efficacy in the treatment of cancer, including prostate cancer. However, the mechanisms underlying the anti-prostate cancer effect of Huaier remain largely unclear. In the present study, we revealed that Huaier aqueous extract inhibited the proliferative and metastatic capabilities of human prostate cancer PC3 cells through CCK-8 assay, in vitro scratch assay and Transwell assay. Moreover, decreased Lamin B1 was implicated in Huaier-induced suppression of proliferative and metastatic potential of PC3 cells. Intriguingly, we demonstrated that Huaier treatment induced autophagic cell death in PC3 cells. This study sheds new light on the mechanisms underlying the activity of Huaier against prostate cancer and provides a new theoretical basis for the clinical application of Huaier in prostate cancer.

CAS / MDL: 88899-55-2
研究领域: 肿瘤学 · 中药学 · 细胞生物学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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TISSUE & CELL · 2021 · IF 2.466

miR-934 promotes breast cancer metastasis by regulation of PTEN and epithelial–mesenchymal transition

Yexia Lu,Xiuxiu Hu,Xueyi Yang

Breast cancer (BC) is the most commonly diagnosed malignancy and the leading cause of cancer-related mortality among females. Over 90 % of the cases of death in BC patients are attributed to tumor cell metastasis. Therefore, it is urgently needed to investigate the molecular mechanisms of BC metastasis. The expression of miRNA in BC was evaluated by qRT-PCR and bioinformatics analysis. Clone formation, EdU assays, and subcutaneous xenograft model were used to test the growth of BC cells. Wound healing, transwell assays, and lung-metastasis model were used to explore the effect of miR-934 knockdown on cell metastasis. The miR-934 targets in BC were identified through bioinformatics analysis and luciferase reporter assays. The expression of protein was tested by western blot. The binding of mRNA and RNA-binding-protein was verified using RIP assays. miR-934 expression was significantly elevated in BC tissues, especially in those with lymph node metastasis and associated with poor patient prognosis. Experiments in vitro and in vivo showed that that upregulated miR-934 was not necessarily required for the growth of BC cells. However, miR-934 knockdown significantly inhibited the migration and invasion abilities of BC cells. Moreover, PTEN as identified as the direct target of miR-934 in BC, and miR-934 could promote BC cell metastasis by regulation of PTEN and epithelial–mesenchymal transition (EMT). Our results suggested that targeting miR-934 may be a practical treatment for BC cell metastasis.

CAS / MDL: 30525-89-4 67-56-1
研究领域: 肿瘤学 · 分子生物学 · 癌症研究
✓ 已验证 产品关联 DOI PubMed 高影响因子
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American Journal of Translational Research · 2021 ·Vol. 13 ·期 4 ·2111-2126 · IF 4.06

NEAT1 promotes the repair of abdominal aortic aneurysms of endothelial progenitor cells via regulating miR-204-5p/Ang-1.

Chao Shi,Chongwen Shen,Ge Liu,Shaofeng Yang,Fenglin Ye,Jinjin Meng,Youmin Pan

Purpose To clarify the regulatory effect of Nuclear-enriched abundant transcript 1 (NEAT1) on abdominal aortic aneurysm (AAA) model rats and isolated endothelial progenitor cells (EPCs). Methods The AAA rat model was established by CaCl 2 stimulation, and overexpressed NEAT1 was injected into rats through tail vein. Abdominal aorta lesions and numbers of EPCs in tissues and peripheral blood were examined by hematoxylin-eosin, immunofluorescence and flow cytometry. The extracted EPCs were identified by microscopy, DiI-ac-LDL staining and flow cytometry. Effect of overexpressed/silencing NEAT1 on the viability, migration, tube formation and VEGF content of EPCs was investigated by MTT-, wound-healing, tube formation assays and ELISA, respectively. The expressions of NEAT1, miR-204-5p, Angiopoietin-1 (Ang-1)/ERK pathway were determined by qRT-PCR and Western blot as needed. The targeting relationships between NEAT1 and miR-204-5p, and miR-204-5p and Ang-1 were predicted on starBase, TargetScan and confirmed by dual-luciferase experiments. The mutual regulation effect was studied through rescue experiments. Results Overexpressed NEAT1 not only reduced inflammatory infiltration and increased the number of EPCs in abdominal aorta and peripheral blood, but also promoted the viability, migration, tube formation of EPCs, increased VEGF content and upregulated the expression of the Ang-1/ERK pathway in EPCs. However, silencing NEAT1 produced opposite results. NEAT1 targeting miR-204-5p inhibited the functional effects of miR-204-5p on of EPCs. Overexpressed/silencing Ang-1 partially reversed the effects of NEAT1 or miR-204-5p on the characteristics of EPCs. Conclusion NEAT1 competitively binds with miR-204-5p and up-regulates Ang-1 expression in EPCs to effectively improve the proliferation, migration and angiogenesis of EPCs.

CAS / MDL: 67-63-0
研究领域: 分子生物学 · 心血管疾病 · 细胞生物学 · 基因调控
✓ 已验证 产品关联 DOI PubMed 高影响因子
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NEUROENDOCRINOLOGY · 2023 ·Vol. 113 ·期 6 ·641-656 · IF 4.1

5-Iodotubercidin Inhibits the Growth of Insulinoma Cells by Inducing Apoptosis

Zheng Biaolin,Chen Xiubing,Chen Fengping,Liao Xiaomin,Wang Feng,Yang Zhe,Yi Nan,Shi Xiaoyan,Qin Shanyu,Jiang Haixing

Introduction: 5-Iodotubercidin, a type of purine derivative, has attracted increasing attention in tumor chemotherapy because of its potential as an antitumor agent in recent years. In this study, we confirmed the effects on apoptosis in insulinoma cell lines induced by 5-iodotubercidin and tried to illuminate the underlying mechanisms. Methods: We used 5-iodotubercidin in the treatment of insulinoma cells and the cell proliferation was examined using CCK-8 assay, colony-forming assays, and insulinoma animal models. Cell apoptosis was examined using TUNEL assays and Western blotting. Cellular DNA damage was shown by comet assay and immunofluorescence. The expression of apoptosis-regulating proteins and DNA damage biomarker was investigated by Western blotting. Subcutaneous inoculation of the insulinoma cells into nude mice was to measure blood glucose, insulin levels, and tumor growth. ATM siRNA and p53 siRNA were used as loss-of-function targets to evaluate 5-iodotubercidin treatment. Results: 5-Iodotubercidin inhibited the proliferation of insulinoma cells and induced DNA damage and cell apoptosis. Moreover, 5-iodotubercidin induced ATM and p53 activated. In vivo, 5-iodotubercidin inhibited the growth of Ins-1 and Min-6 cells xenografts in nude mice. Conclusion: 5-Iodotubercidin induces DNA damage leading to insulinoma cells apoptosis by activating ATM/p53 pathway. Therefore, this is a potential strategy for treating insulinoma

研究领域: 肿瘤学 · 分子生物学 · 细胞生物学 · 药理学
✓ 已验证 DOI PubMed 高影响因子
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Foods · 2025 ·Vol. 14 ·期 10 ·1702 · IF 5.1

Characterization of Key Factors Associated with Flavor Characteristics in Lager Beer Based on Flavor Matrix

Jiaxin Hong,Huayang Wei,Ruiyang Yin,Jiang Xie,He Huang,Liyun Guo,Dongrui Zhao,Yumei Song,Jinyuan Sun,Mingquan Huang,Baoguo Sun

Lager beer has the characteristics of a refreshing aroma, clean and less intense taste, as well as a low alcohol degree, which is suitable for daily drinking. This study aimed to clarify the relationship between important flavor compounds and flavor profiles for lager beer. Headspace solid-phase microextraction, solvent-assisted flavor evaporation combined with comprehensive two-dimensional gas chromatography–mass spectrometry, gas chromatography–mass spectrometry, and gas chromatography-olfactometry–mass spectrometry were applied for the qualitative and quantitative analysis of the trace components in lager beer. Furthermore, the recombination experiment was successfully applied to simulate the flavor profile, and the omission experiment was conducted to study the effects of flavor compounds on the flavor profile. A total of nine compounds were identified as the key flavor compounds, and their contribution to the flavor characteristics of lager beer was verified according to validation experiments. It was found that the influence of the key flavor compounds on the sensory attributes such as malty aroma, fruity aroma, sweetness, and bitterness varied with their concentration. These findings might provide ideas for the research regarding the flavor compounds and flavor profile of lager beer, and contribute to the development of different types of beer in the future.

CAS / MDL: 64-17-5 75-09-2
研究领域: 食品科学 · 分析化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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FOOD RESEARCH INTERNATIONAL · 2025 · IF 8

Unraveling the mysterious jujube-like aroma in Pu-erh tea: Decoding the material basis for distinctive aroma formation

Guohe Chen,Wanling Xiao,Zhichao Lin,Mengzhen Xia,Yajie Xue,Jing Zhang,Sudu Bao,Junye Zhu,He Xie,Jianan Huang,Zhonghua Liu,Chao Wang

Abstact The jujube-like aroma is widely regarded as a noble aroma of Pu-erh tea (PET), but the key odor-active compounds remain unclear. Thus, the molecular sensory science approaches were used to decode the key odor-active compounds of PET with jujube-like aroma. Sixty-eight volatiles were identified in both PETs and jujube sample. Among them, 19 odor-active compounds were identified by relative odor activity value (ROAV) and Pearson correlation analysis. Aroma recombination experiment successfully reproduced the characteristic jujube-like aroma of PET. Omission experiments identified 17 aroma compounds have significant contributions ( p  < 0.05), with 9 key odor-active compounds including 1-octen-3-ol, hexanal, etc. ( p  < 0.001). This study elucidates the key odor-active compounds of jujube-like aroma in PET, to provide a theoretical reference for the targeting process regulation of the product.

研究领域: 食品科学 · 植物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Journal of the Taiwan Institute of Chemical Engineers · 2016 · IF 2.848

In vitro and in vivo antitumor effects of the extract of Sapindus spp.

Xiao-Wen Zhu,Min-Ping Wei,De-Ping Xu,Ya-Hui Guo,Yun-Fei Xie,Wei-Rong Yao

This study evaluated the antitumor effect of some fractions extracted from Sapindus spp. on breast cancer. Four water-extracted fractions (I, II, III, IV) were isolated from the pericarp of Sapindus spp. using X-5 and AB-8 macroporous resin columns and MCI gel column. The in vitro effect was determined using the MTT assay. Our results indicated that fractions I-IV did not exhibit significant cytotoxic effects towards the normal cell MDA-kb2; Fraction II and IV inhibited the growth of MCF-7 (estrogen receptor positive), MDA-MB-231 (estrogen receptor negative), and MDA-MB-435   s human breast cancer cell lines; of these, MDA-MB-435   s cell line was the most sensitive, and the IC 50 of Fraction II and IV against this cell line were 33.11 and 30.06   µg/mL, respectively. In the in vivo experiment, Fraction II and IV showed a strong antitumor effect at a dose of 162.5   mg/kg/d, with inhibition rate of 40.43% and 38.77%. Fraction II and IV also induced apoptosis of tumor cells, activations of Bax (Fraction II) and inhibition of Bcl-2 (Fraction II and IV). Our results underscore the pharmacological potential of Sapindus spp. extracts.

CAS / MDL: 298-93-1
研究领域: 药理学 · 肿瘤学 · 植物化学
✓ 已验证 产品关联 DOI 高影响因子
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2020 · IF 4.389

Stimulation of in vitro and in vivo osteogenesis by Ti-Mg alloys with the sustained-release function of magnesium ions

Luxin Liang,Qianli Huang,Hong Wu,Zhengxiao Ouyang,Tang Liu,Hao He,Jian Xiao,Guanghua Lei,Kun Zhou

Magnesium (Mg) is well-known for its bioactivity and degradability. However, due to its low evaporation temperature and limited solubility in titanium (Ti), the fabrication of Ti-Mg alloys remains a huge challenge. In this study, Ti-xMg (x = 0.312, 0.625, 1.25 and 2.5 wt.%) alloys were fabricated by the combination of mechanical alloying (MA) and spark plasma sintering (SPS). Mg mainly existed as a solid solute element in the Ti matrix, while it also existed as second-phase particles due to its precipitation and dispersion during the SPS process. At a low content of 0.625 wt.%, Mg could increase the mechanical strength of Ti by the solid solution strengthening. However, it was detrimental to material mechanical properties when the Mg content increased to 1.25 wt.%. Being immersed in phosphate buffered solution (PBS), Ti-Mg alloys exhibited a burst Mg 2+ release behavior within the first day, and then the rates of Mg 2+ release gradually decreased within the following 27 days. The results suggested that the cell viability was dependent on the content of Mg in the Ti-Mg alloys. The high Mg content (2.5 wt.%) in the Ti-Mg alloys could lead to significant cytotoxicity. However, appropriate Mg content (0.312∼0.625 wt.%) could promote cell attachment, proliferation and differentiation. The Ti-0.625Mg alloy exhibited the best in vitro biological performance among all groups. In vivo results obtained by implanting the Ti-0.625Mg alloy in the femurs of rats further revealed its enhanced regenerative potential and osteointegration compared to pure Ti implants.

CAS / MDL: 7439-95-4
研究领域: 生物材料学 · 组织工程学 · 医学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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CHEMISTRY & BIODIVERSITY · 2018 ·Vol. 15 ·期 4 ·e1800024 · IF 1.617

ent-Sauchinone as Potential Anticancer Agent Inhibiting Migration and Invasion of Human Liver Cancer Cells via Suppressing the STAT3 Signaling Pathway

Qi-Zhe Gong,Di Xiao,Feng Feng,Xiao-Dong Wen,Wei Qu

ent -Sauchinone, a lignan isolated from Saururus chinensis ( Lour .) Baill ., was reported that it could modulate the expression of signal transducer and activator of transcription 3 (STAT3). Since STAT3 plays a key role in invasion, migration, and metastasis of cancer, we investigated whether ent -sauchinone could exert promising inhibitory effects on the invasion and migration of the metastatic human liver cancer cell line SMMC-7721 in the present study. ent -Sauchinone was extracted from dried herbs of Saururus chinensis ( Lour .) Baill . Human liver cancer cell lines SMMC-7721 and HCCLM3 were used to test the effect of ent -sauchinone on cell viability. The IC 50 values and time-dependent effect of ent -sauchinone were determined by MTT assay. Cell migration and invasion of SMMC-7721 were evaluated by the wound healing test and transwell assay respectively, the known anti-metastasis agent curcumin was used as a positive control. Western blotting assay was used to investigate relevant molecular mechanisms of cell invasion and migration. Though ent -sauchinone didn't show high cytotoxicity, the wound healing assay and transwell migration assay revealed a profound impairment in the metastatic potential of SMMC-7721 cells due to down-regulation of N-cadherin, MMP-2, and MMP-9 proteins induced by inhibiting the phosphorylation of STAT3. These findings suggest that ent -sauchinone could be used as a promising agent to treat cancer metastasis.

CAS / MDL: 458-37-7
研究领域: 肿瘤学 · 药理学 · 细胞生物学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Cancer Biomarkers · 2019 ·Vol. 24 ·期 4 ·469-475 · IF 2.859

Relationship between p-cofilin and cisplatin resistance in patients with ovarian cancer and the role of p-cofilin in prognosis

Qin Yujing,Li Wenxue,Long Yingli,Zhan Zhijia

OBJECTIVE: This study aims to determine the correlation between p-cofilin expression and cisplatin resistance in patients with ovarian cancer, and also to investigate the role of p-cofilin in prognosis. PATIENTS AND METHODS: The ovarian cancer cell line A2780/DDP resistant to cisplatin was prepared. The cell resistance to cisplatin was measured via MTT assay. The cell invasion capacity was identified via Transwell assay. The mRNA expression and protein level was evaluated via semi-quantitative PCR and Western blot, respectively. The tumor tissues of patients with cisplatin-resistant ovarian cancer were collected. The relationship between prognosis and p-cofilin expression was analyzed. RESULTS: The growth rate of A2780 was similar to that of A2780/DDP. The sensitivity of A2780 to cisplatin was significantly higher than that of A2780/DDP (p< 0.01). The migration capacity of A2780/DDP was significantly increased compared to that of A2780 (p< 0.01), indicating that the cisplatin-resistant cell lines were successfully constructed. Both CFL1 mRNA level and p-cofilin level in A2780/DDP was significantly higher than that in A2780 (p< 0.01). The p-cofilin level in cancer tissues in patients with cisplatin-resistant ovarian cancer was significantly higher than that in patients with cisplatin-sensitive ovarian cancer (p< 0.01). The cisplatin resistance was positively correlated with the p-cofilin expression level (r= 0.802, p= 0.023). The survival time of patients with normal or low level of p-cofilin was significantly longer than that of patients with high expression. CONCLUSION: The cisplatin resistance of ovarian cancer is closely related to the expression level of p-cofilin, which affects the prognosis of patients with ovarian cancer.

CAS / MDL: 14913-33-8
研究领域: 肿瘤学 · 分子生物学 · 癌症研究
✓ 已验证 产品关联 DOI PubMed 高影响因子
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