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1.
Biomed Pharmacother ; 175: 116635, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38653110

RESUMEN

The morbidity and mortality of malignant tumors are progressively rising on an annual basis. Traditional Chinese Medicine (TCM) holds promise as a possible therapeutic agent for the avoidance or therapy of malignant tumors. Salvia miltiorrhiza Bunge (Danshen), a traditional Asian functional food, has therapeutic characteristics in application for the treatment of malignant tumors. Dihydrotanshinone I (DHTS) is the principal lipophilic phenanthraquinone compound found in Salvia miltiorrhiza Bunge, whose anti-tumor effect has attracted widespread attention. The anti-tumor effects include inhibiting cancer cell proliferation, triggering apoptosis of tumor cells, inducing ferroptosis in tumor cells, inhibiting tumor cell invasion and metastasis, and improving drug resistance of tumor cells. In this paper, we summarized and analyzed the mechanisms and targets of anti-tumor effect of DHTS, providing new ideas and establishing a solid theoretical basis for the future advancement and clinical treatment of DHTS.


Asunto(s)
Neoplasias , Fenantrenos , Quinonas , Humanos , Neoplasias/tratamiento farmacológico , Neoplasias/patología , Fenantrenos/farmacología , Fenantrenos/uso terapéutico , Animales , Quinonas/farmacología , Quinonas/uso terapéutico , Apoptosis/efectos de los fármacos , Antineoplásicos Fitogénicos/uso terapéutico , Antineoplásicos Fitogénicos/farmacología , Proliferación Celular/efectos de los fármacos , Medicamentos Herbarios Chinos/uso terapéutico , Medicamentos Herbarios Chinos/farmacología , Salvia miltiorrhiza/química , Resistencia a Antineoplásicos/efectos de los fármacos , Furanos
2.
Molecules ; 28(19)2023 Oct 03.
Artículo en Inglés | MEDLINE | ID: mdl-37836760

RESUMEN

In this paper, liquid-liquid chromatography was introduced for the first time for the separation of fingered citron (Citrus medica L. var. sarcodactylis Swingle). The fingered citron cultivated in Jinhua is of significant industrial and medicinal value, with several major coumarin compounds detected in its extract. Therefore, further separation for higher purity was of necessity. A preparative liquid-liquid chromatographic method was developed by combining two elution modes (isocratic and step-gradient) with selection according to different polarities of the target sample. Five coumarin derivatives-5,7-dimethoxycoumarin (52.6 mg, 99.6%), phellopterin (4.9 mg, 97.1%), 5-prenyloxy-7-methoxycoumarin (6.7 mg, 98.7%), 6-hydroxy-7-methoxycoumarin (7.1 mg, 82.2%), and byakangelicol (10.5 mg, 90.1%)-with similar structures and properties were isolated on a large scale from 100 mg of petroleum ether (PE) extract and 100 mg of ethyl acetate (EA) extract in Jinhua fingered citron. The productivity was much improved. The anti-growth activity of the isolated coumarins was evaluated against three cancer cell lines (HeLa, A549, and MCF7) with an MTT assay. The coumarins demonstrated potential anti-tumor activity on the HeLa cell line, with 5,7-dimethoxycoumarin in particular exhibiting the best anti-growth activity (IC50 = 10.57 ± 0.24 µM) by inhibiting proliferation. It inhibited colony formation and reduced the size of the tumor sphere in a concentration-dependent manner. The main mechanism was confirmed as inducing apoptosis. This work was informative for further studies aimed at exploring new natural-product-based antitumor agents.


Asunto(s)
Citrus , Extractos Vegetales , Humanos , Células HeLa , Extractos Vegetales/farmacología , Extractos Vegetales/química , Cumarinas/farmacología , Citrus/química , Cromatografía Liquida
3.
Zhongguo Zhong Yao Za Zhi ; 48(10): 2679-2698, 2023 May.
Artículo en Chino | MEDLINE | ID: mdl-37282929

RESUMEN

Cytisine derivatives are a group of alkaloids containing the structural core of cytisine, which are mainly distributed in Fabaceae plants with a wide range of pharmacological activities, such as resisting inflammation, tumors, and viruses, and affecting the central nervous system. At present, a total of 193 natural cytisine and its derivatives have been reported, all of which are derived from L-lysine. In this study, natural cytisine derivatives were classified into eight types, namely cytisine type, sparteine type, albine type, angustifoline type, camoensidine type, cytisine-like type, tsukushinamine type, and lupanacosmine type. This study reviewed the research progress on the structures, plant sources, biosynthesis, and pharmacological activities of alkaloids of various types.


Asunto(s)
Alcaloides , Fabaceae , Alcaloides/farmacología , Alcaloides/química , Quinolizinas/farmacología , Azocinas/farmacología , Azocinas/química
4.
Bioorg Chem ; 131: 106304, 2023 02.
Artículo en Inglés | MEDLINE | ID: mdl-36463590

RESUMEN

Velvet antler is a traditional Chinese medicine with various pharmacological values, which is an important raw material for traditional Chinese medicinal wine. Nevertheless, the chemical compositions and bioactivities of velvet antler residue used for making medicinal wine are rarely reported, leading to a waste of resources. In this study, a velvet antler protein (VA-pro) was extracted from velvet antler residue by simulating the gastrointestinal digestion, and its composition, structural characteristics and in vivo anti-tumor activities were determined and investigated. VA-pro possessed high purity with a relatively low molecular weight as 22.589 kDa under HPLC, one- and two-dimensional electrophoresis, and it contained high contents of Pro, Gly, Glu and Ala. Besides, the secondary structure of VA-pro was dominated by ß-turn and ß-sheet, and VA-pro possessed similar protein sequence, isoelectric point and amino acid compositions to hypothetical protein G4228_020061. The in vivo results substantiated that VA-pro could improve the body weights and immune organ indices, increase the expressions of sera cytokines and regulate the distributions of T and B lymphocytes subsets in peripheral blood of S180 tumor-bearing mice. Furthermore, VA-pro could effectively inhibit solid S180 tumors growth by inducing S phase cell cycle arrest mediated through mitochondria. To summarize, our study provided theoretical support that VA-pro had the potential to be used as an immunopotentiator in immunocompromised or cancer-bearing hosts.


Asunto(s)
Cuernos de Venado , Neoplasias , Ratones , Animales , Cuernos de Venado/química , Cuernos de Venado/metabolismo , Peso Molecular , Proteínas/metabolismo , Aminoácidos/metabolismo , Neoplasias/metabolismo
5.
Zhongguo Zhong Yao Za Zhi ; 47(20): 5574-5583, 2022 Oct.
Artículo en Chino | MEDLINE | ID: mdl-36471975

RESUMEN

Histone lysine-specific demethylase 1(LSD1) has become a promising molecular target for lung cancer therapy. Upon the screening platform for LSD1 activity, some Chinese herbal extracts were screened for LSD1 activity inhibition, and the underlying mechanism was preliminarily investigated at both molecular and cellular levels. The results of LSD1 inhibition showed that Puerariae Lobatae Radix extract can effectively reduce LSD1 expression to elevate the expression of H3 K4 me2 and H3 K9 me2 substrates in H1975 and H1299 cells. Furthermore, Puerariae Lobatae Radix was evaluated for its anti-lung cancer activity. It had a potent inhibitory ability against the proliferation and colony formation of both H1975 and H1299 cells. Flow cytometry and DAPI staining assays indicated that Puerariae Lobatae Radix can induce the apoptosis of lung cancer cells. In addition, it can significantly suppress the migration and reverse the epithelial-mesenchymal transition(EMT) process of lung cancer cells by activating E-cadherin and suppressing the expression of N-cadherin, slug and vimentin. To sum up, Puerariae Lobatae Radix displayed a robust inhibitory activity against lung cancer, and the mechanism may be related to the down-regulation of LSD1 expression to induce the cell apoptosis and suppress the cell migration and EMT process. These findings will provide new insights into the action of Puerariae Lobatae Radix as an anti-lung cancer agent and offer new ideas for the study on the anti-cancer action of Chinese medicine based on the epigenetic modification.


Asunto(s)
Neoplasias , Pueraria , Pueraria/química , Histona Demetilasas/genética , Histona Demetilasas/análisis , Raíces de Plantas/química , Transición Epitelial-Mesenquimal
6.
Protein Pept Lett ; 29(12): 1072-1081, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36098412

RESUMEN

BACKGROUND: Accumulating evidence has demonstrated the immunomodulatory effects of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) in rheumatoid arthritis and the tumor microenvironment, besides its known capacity of specifically inducing the apoptosis of cancer cells. Mice are common available animal models for studying the roles of TRAIL. However, mice express only a single TRAIL receptor (mTRAILR) with an intracellular death domain, in contrast to the two TRAIL receptors (TRAILR1 and TRAILR2) in humans. Moreover, human TRAIL binds weakly to mTRAILR, whereas mouse TRAIL has a high affinity for human TRAIL-Rs. Therefore, we considered that murine TRAIL would be more suitable than human TRAIL for exploring the immunoregulatory effect of TRAIL in immunocompetent mice or when using mouse cells as the target. To our knowledge, the detailed method for the production of recombinant murine TRAIL has not been reported. OBJECTIVE: In this study, we aimed to design and express two soluble forms of murine TRAIL and verify the properties of the protein. METHODS: Recombinant murine TRAILs were expressed in Escherichia coli BL21 (DE3, and Nichelating affinity chromatography was used for protein purification. SDS-PAGE, GDS-PAGE and HPLC were applied to analyze the protein structure. The cytotoxicity of our purified murine TRAILs was evaluated in the TRAIL-sensitive human breast cancer ZR-75-30 cells and murine breast cancer 4T1 cells. Finally, validation of the tumor-killing ability of the murine protein in vivo. RESULTS: Two soluble forms of murine TRAILs (mT_N99 and mT_N188) were purified and demonstrated with high purity and trimeric structure. In addition, Zn2+ supplement was essential to produce soluble murine TRAILs in E.coli BL21 (DE3). The two purified soluble mTRAILs showed similar cytotoxicity to cancer cells, moreover, mT_N99 also showed a good anti-tumor effect in vivo and is more suitable for the treatment of murine tumor models. CONCLUSION: A production approach for recombinant murine TRAIL was determined, which covered the design of shortened forms, expression, purification and characterization.


Asunto(s)
Ligando Inductor de Apoptosis Relacionado con TNF , Animales , Femenino , Humanos , Ratones , Apoptosis , Línea Celular Tumoral , Suplementos Dietéticos , Escherichia coli/genética , Escherichia coli/metabolismo , Ligando Inductor de Apoptosis Relacionado con TNF/biosíntesis , Ligando Inductor de Apoptosis Relacionado con TNF/farmacología , Microambiente Tumoral , Zinc/farmacología
7.
Zhongguo Zhong Yao Za Zhi ; 47(13): 3526-3529, 2022 Jul.
Artículo en Chino | MEDLINE | ID: mdl-35850805

RESUMEN

One new phenylethanoid glycoside was isolated from the ethyl acetate fraction of the 75% EtOH extract of Forsythiae Fructus by various column chromatographies(HP20, silica gel, ODS) and preparative HPLC.Its structure was identified as forsythiayanoside E(1) by physicochemical properties and extensive spectroscopic analysis(HR-ESI-MS, 1 D and 2 D NMR).Compound 1 was evaluated for cytotoxic activities by MTT assay and showed weak cytotoxic activity against MCF-7 and A-375 cell lines with inhibition rates of 39.85% and 43.38% at 40 µmol·L~(-1), and no cytotoxic activity against PC-3 and HepG2 cell lines at 100 µmol·L~(-1).


Asunto(s)
Glicósidos Cardíacos , Glicósidos , Glicósidos Cardíacos/análisis , Cromatografía Líquida de Alta Presión , Frutas/química , Glicósidos/análisis , Glicósidos/farmacología , Estructura Molecular , Extractos Vegetales/química
8.
J Ethnopharmacol ; 296: 115488, 2022 Oct 05.
Artículo en Inglés | MEDLINE | ID: mdl-35728712

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Licorice is a well-known herbal medicine, and we previously found that several licorice prenylated flavonoids could cause death of SW480 colorectal cancer cells by promoting autophagy. Given many kinds of prenylated flavonoids in licorice, the activities of other compounds deserve further investigation. In addition, the contribution of isoprenyl groups on the autophagy promotion activities has not been clarified. AIM OF THE STUDY: This study aimed to investigate whether lupalbigenin (LPB) and 6,8-diprenylgenistein (DPG), two licorice diprenylated flavonoids, could induce autophagic cell death of SW480 cells, and clarify the contribution of isoprenyl groups. MATERIALS AND METHODS: Cytotoxic activities of LPB and DPG were tested by using an MTT method, and apoptosis induction effects were evaluated by PI-Annexin V staining-based flow cytometry and protein levels of caspase-3 and PARP-1. Autophagy promotion effects of LPB and DPG were assessed by protein levels of LC3, p62, Akt and mTOR as well as number of autophagosomes in cells, and autophagy inhibitor chloroquine (CQ) was involved to identify the role of autophagy on LPB or DPG-caused death of SW480 cells. In addition, two groups of structurally similar diprenylated, mono-prenylated and free flavonoids were obtained from licorice, which were used to investigate the contribution of isoprenyl groups on their autophagy promotion activities. RESULTS: Both LPB and DPG significantly induced apoptosis of SW480 cells with strong cytotoxic activities, and meanwhile, they also promoted autophagy probably through the Akt/mTOR signaling pathway. Further studies indicated that LPB and DPG could induce autophagic cell death of SW480 cells. Moreover, isoprenyl groups contributed mainly to the cytotoxic and autophagy promotion activities of licorice prenylated flavonoids. CONCLUSION: This study reported for the first time that licorice diprenylated flavonoids LPB and DPG induced death of SW480 cells by promoting autophagy, which was mainly attributed to the isoprenyl groups. The results provided theoretical basis for researches on anti-colorectal cancer drugs and their structural modification.


Asunto(s)
Glycyrrhiza , Neoplasias , Apoptosis , Autofagia , Línea Celular Tumoral , Flavonoides/farmacología , Genisteína/análogos & derivados , Isoflavonas , Extractos Vegetales/farmacología , Proteínas Proto-Oncogénicas c-akt/metabolismo , Serina-Treonina Quinasas TOR
9.
J Ethnopharmacol ; 293: 115285, 2022 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-35429621

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Marsdenia tenacissima (Roxb.) Moon, (M. tenacissima) a traditional herbal medicine, has been used for thousands of years. It is noted in Dian Nan Ben Cao that M. tenacissima is bitter in flavor and cold in property, and extracts possess diverse pharmacological effects, including immunomodulation and anti-tumor activities. AIM OF THE STUDY: The anti-tumor effects of M. tenacissima extracts (MTE) have been repeatedly confirmed, and this medicine has also been extensively applied in cancer treatment or prognostic adjuvant therapy, with significant curative effect. This study aims to comprehensively analyze the anti-tumor mechanism of M. tenacissima starting from the key features of traditional Chinese medicine and by studying the main active components individually to identify anti-tumor targets in the context of hepatocellular carcinoma. MATERIALS AND METHODS: Molecular network profiling and multi-omic joint analyses were conducted using an H22 mouse model of hepatocellular carcinoma to determine the main active ingredients in MTE and the underlying anti-tumor mechanisms. RESULTS: Tenacissosides I, H, and G (TI,TH and TG) were found to be the likely active ingredients of MTE in the treatment of hepatocellular carcinoma. These compounds were shown to promote apoptosis, inhibit angiogenesis and improve immune function through targeting P53, JAK-1 and HIF1α, respectively. CONCLUSIONS: For the first time, based on the theory that multiple components and multiple targets synergistically exert the beneficial effects of a traditional Chinese medicine, this paper comprehensively analyzes the mechanisms of action of M. tenacissima and provides a novel strategy for the subsequent development of anti-tumor therapies.


Asunto(s)
Carcinoma Hepatocelular , Neoplasias Hepáticas , Marsdenia , Animales , Carcinoma Hepatocelular/tratamiento farmacológico , Neoplasias Hepáticas/tratamiento farmacológico , Medicina Tradicional China , Ratones , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico
10.
J Nat Med ; 76(3): 670-674, 2022 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-35249209

RESUMEN

To explore useful natural compounds from indigenous medicinal plants, the cytotoxic properties from a methanolic extract of Boehmeria sieboldiana leaves against human cancer cell lines were isolated in the present study. After purification of the extract, seco-dehydroantofine B (1) together with two known phenanthroindolizine alkaloids, seco-dehydroantofine A (2) and septicine (3), were isolated. The structure of seco-dehydroantofine B was elucidated by performing comprehensive one- and two-dimensional nuclear magnetic resonance spectroscopy and high-resolution electrospray ionization mass spectrometry. The cytotoxicity of these compounds against five human tumor cell lines was evaluated. Compound 3 exhibited anti-tumor activity at IC50 values of 50.0, 66.9, 50.0, and 153.7 µM against MKN1, SAS, HL-60, and THP-1 cells, respectively.


Asunto(s)
Alcaloides , Antineoplásicos Fitogénicos , Boehmeria , Neoplasias , Alcaloides/química , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Línea Celular Tumoral , Humanos , Estructura Molecular , Extractos Vegetales/análisis , Extractos Vegetales/farmacología , Hojas de la Planta/química
11.
Int J Biol Macromol ; 205: 615-625, 2022 Apr 30.
Artículo en Inglés | MEDLINE | ID: mdl-35202635

RESUMEN

Recently, more and more attention has been paid to the structure and application of tea polysaccharides. Herein, a water-soluble homogeneous polysaccharide (DTP-1) from dark brick tea was purified, characterized, and investigated its anti-tumor activity in vitro. The DTP-1 with a molecular weight of 11,805 Da is mainly composed of glucose, galactose and arabinose. It has a backbone, which is composed of →4)-α-D-Glcp-(1→, →5)-α-L-Araf-(1→, →6)-ß-D-Galp-(1→, →2)-α-L-Araf-(1→, →3)-ß-D-Galp-(1→, with →4,6)-ß-D-Galp-(1 â†’ as branching point and →1)-ß-D-Glcp as terminal. In addition, DTP-1 could significantly affect the viability of A549 and SMMC7721 cells with an inhibition rate of 31.71% and 33.38% (600 µg/mL, 24 h), respectively, by inducing apoptosis and inhibiting cell migration. Moreover, DTP-1 had no effect on corresponding normal cells. Therefore, DTP-1 showed great potential to become a functional food and an anti-tumor drug.


Asunto(s)
Polisacáridos , Agua , Galactosa , Peso Molecular , Polisacáridos/química , Polisacáridos/farmacología ,
12.
Exp Cell Res ; 410(1): 112948, 2022 01 01.
Artículo en Inglés | MEDLINE | ID: mdl-34826423

RESUMEN

Honey-processed Astragalus is a dosage form of Radix Astragalus mixed with honey by a traditional Chinese medicine processing method which improves immune activity. This pharmacological activity of honey-processed Astragalus polysaccharide (HP-APS) might be due to structural changes during the honey roasting process. Previously, we have prepared and characterized HP-APS and preliminarily found its anti-inflammatory effects. However, whether the pharmacodynamic activity of HP-APS induces tumor cell apoptosis and the mechanisms responsible for the immunogenic death (ICD) have not been elucidated. Here, A549, MC38 and B16 cells were used to evaluate the cells viability, apoptosis and cell cycles, respectively. Cellular immunogenic cell death-related molecules calreticulin (CRT), Heat Shock Proteins (HSP)70, major histocompatibility complex I (MHC-I), and co-stimulator molecules CD80/CD86 were determined by flow cytometry. The extracellular ATP release was also detected. B16-OVA and MC38-OVA cells were treated with HP-APS and co-cultivated with OT1 mouse of CD3+T cells for assessment of proliferation, in mice model, and the establishment of C57BL/B6 mouse model bearing B16 cells for assessment of HP-APS the regulation of immune activity in vivo. Our results showed that HP-APS has an inhibitory effect on tumor cell proliferation, which induces tumor cell apoptosis, preventing cells-transforming from G1 phase to S phase in cell cycles. Furthermore, HP-APS could effectively increase the expression of HSP70, CRT, MHC-I, CD86, CD80 and ATP release. T cell proliferation index is significantly improved. CD3 cell proliferation in OT1 mice was significantly increased from the 4th generation to the 5th generation. Moreover, the results have also shown that HP-APS could inhibit tumor growth by increasing immune cell infiltration in the tumor tissues. In the mouse melanoma model with HP-APS treatment, the tumor weight and volume were significantly reduced, and the growth of melanoma was inhibited. CD8+ T is significantly increased. The ratio of CD4+ T and CD8+ T cells numbers are also significantly increased in mouse spleen, but it is less than PD-1 alone treatment separately. Altogether, these findings suggest that HP-APS exerts anti-tumor effects, and that its underlying mechanisms might be associated with the expression of immunogenicity cell death related molecules and the immunomodulatory effects of immune cells.


Asunto(s)
Planta del Astrágalo/química , Medicamentos Herbarios Chinos/farmacología , Muerte Celular Inmunogénica/efectos de los fármacos , Neoplasias/tratamiento farmacológico , Células A549 , Animales , Apoptosis/efectos de los fármacos , Astragalus propinquus/química , Linfocitos T CD8-positivos/efectos de los fármacos , Linfocitos T CD8-positivos/inmunología , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Medicamentos Herbarios Chinos/química , Regulación Neoplásica de la Expresión Génica/efectos de los fármacos , Miel/análisis , Humanos , Muerte Celular Inmunogénica/inmunología , Inmunomodulación/efectos de los fármacos , Inmunomodulación/inmunología , Activación de Linfocitos/efectos de los fármacos , Melanoma Experimental , Ratones , Proteínas de Neoplasias/genética , Neoplasias/genética , Neoplasias/inmunología , Neoplasias/patología , Polisacáridos/química , Polisacáridos/farmacología
13.
Zhongguo Zhong Yao Za Zhi ; 46(17): 4360-4366, 2021 Sep.
Artículo en Chino | MEDLINE | ID: mdl-34581038

RESUMEN

Diosgenin is widely distributed in many plants, such as Polygonatum sibiricum, Paris polyphylla, Dioscorea oppositifolia, Trigonella foenum-graecum, Costus speciosus, Tacca chantrieri, which has good anti-tumor activity and preferable effects on preventing atherosclerosis, protecting the heart, treating diabetes, etc. This review combed through the anti-tumor mechanisms of diosgenin encompassing lung, breast, gallbladder, liver, oral cavity, stomach, bladder, bone marrow, etc. Besides, it was discovered that diosgenin mainly exerts its effect by inhibiting tumor cell migration, suppressing tumor cell proliferation and growth, and inducing cell apoptosis. However, problems like low yield and bioavailability frequently exist in natural diosgenin. This review introduced methods such as structural modification, dosage form optimization and combination medication to improve the yield and anti-tumor activity of diosgenin. Via the summary of this paper, it is expected to provide theoretical basis for the rational exploitation and utilization of diosgenin.


Asunto(s)
Productos Biológicos , Diosgenina , Trigonella , Apoptosis , Proliferación Celular , Diosgenina/farmacología
14.
Carbohydr Polym ; 273: 118496, 2021 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-34560937

RESUMEN

A homogeneous polysaccharide, EJP90-1, was isolated from the leaves of E. japonica by hot water extraction in this study. EJP90-1 (7702 Da) was a heteropolysaccharide mainly consisting of →5)-linked-α-L-Araf-(1→, →4)-linked-ß-D-Manp-(1→, →2,4)-linked-α-L-Rhap-(1→, →4)-linked-α-D-Xylp-(1→, →4)-linked-ß-D-Galp-(1→, →2)-linked-ß-D-Galp-(1→, →6)-linked-ß-D-Glcp-(1→, α-D-Glcp-(4→, and t-linked-α-L-Araf. EJP90-1 was found to show moderate anti-tumor activity at the cellular level. In order to improve the anti-tumor activity and the potential applications of EJP90-1, a typical sodium selenite-nitric acid (Na2SeO3-HNO3) modification on EJP90-1 was carried out. X-ray photoelectron spectroscopy (XPS) and energy dispersive spectrometer (EDS) analysis confirmed that Se was successfully introduced into the polymer chain of EJP90-1. The subsequent in vitro cytotoxicity evaluation showed the selenylation modification derivative (EJP90-1-Se) possessed significant antiproliferative activity against cancer cells (HepG2 and A549 cells) through inducing cell apoptosis. The anti-tumor activity of EJP90-1-Se was further confirmed by zebrafish models, which inhibited the proliferation and migration of HepG2 cells and the angiogenesis.


Asunto(s)
Antineoplásicos/farmacología , Eriobotrya/química , Neoplasias/tratamiento farmacológico , Polisacáridos/farmacología , Selenio/química , Células A549 , Animales , Apoptosis/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Células Hep G2 , Humanos , Neoplasias/metabolismo , Neovascularización Patológica/metabolismo , Ácido Nítrico/química , Espectroscopía de Fotoelectrones/métodos , Hojas de la Planta/química , Polisacáridos/química , Pez Cebra
15.
Carbohydr Polym ; 270: 118365, 2021 Oct 15.
Artículo en Inglés | MEDLINE | ID: mdl-34364610

RESUMEN

In this study, an inulin fructan (TMP50-2) with moderate anti-tumor activity was obtained from dandelion. To further improve the anti-tumor activity of TMP50-2, a monodisperse and stable spherical nanoparticle (Tw-TMP-SeNP, 50 nm) was fabricated. Physico-chemical analysis revealed that TMP50-2 and Tween 80 were tightly wrapped on the surface of SeNPs by forming CO⋯Se bonds or through hydrogen bonding interaction (OH⋯Se). In vitro anti-tumor assay showed that Tw-TMP-SeNP treatment could significantly inhibit the proliferation of cancer cells (HepG2, A549, and HeLa) in a dose-dependent manner, while HepG2 cells were more susceptible to Tw-TMP-SeNP with an IC50 value of 46.8 µg/mL. The apoptosis induction of HepG2 cells by Tw-TMP-SeNP was evidenced by increasing the proportion of apoptotic cells ranging from 12.5% to 27.4%. Furthermore, in vivo zebrafish model confirmed the anti-tumor activity of Tw-TMP-SeNP by inhibiting the proliferation and migration of tumor cells as well as the angiogenesis of zebrafish embryos.


Asunto(s)
Nanopartículas/química , Neoplasias/tratamiento farmacológico , Polisacáridos/farmacología , Selenio/farmacología , Taraxacum/química , Células A549 , Animales , Antineoplásicos/farmacología , Apoptosis/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Fructanos/química , Fructanos/farmacología , Células HeLa , Células Hep G2 , Humanos , Enlace de Hidrógeno , Neoplasias/metabolismo , Neoplasias/patología , Polisacáridos/química , Selenio/química , Pez Cebra
16.
Front Chem ; 9: 666280, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33996757

RESUMEN

Vaccaria segetalis is a dry mature seed of Vaccaria hispanica (Mill.) Rauschert, which belongs to the genus V. segetalis (Neck.) Garcke. There are multiple medicinal parts of V. segetalis, according to the records, including roots, stems, leaves, flowers, and seeds, which should be used together. Currently, V. segetalis is most frequently used in the treatment of menstruation, dysmenorrhea, breast milk stoppages, and chylorrhea. Numerous studies present historical evidence of the use of V. segetalis to treat several diseases and describe its beneficial effects including prolactin- (PRL-) like, estrogen-like, antitumor, antiangiogenesis, and antioxidant activity. We summarized the period from January 1980 to December 2019 regarding V. segetalis. This review paper indicates that V. segetalis has promising clinical applications. The main active ingredients of the plant have been elucidated in recent years. We summarized the previously and newly discovered pharmacological effects of V. segetalis in addition to its active ingredients, ethnopharmacological uses, and toxicological properties, and provided a focus for future research.

17.
BMC Pharmacol Toxicol ; 22(1): 1, 2021 01 06.
Artículo en Inglés | MEDLINE | ID: mdl-33407916

RESUMEN

BACKGROUND: The development of novel and effective drugs for targeted human hepatocellular carcinoma still remains a great challenge. The alkaloid nitidine chloride (NC), a component of a traditional Chinese medicine, has been shown to have anticancer properties, but doses at therapeutic levels have unacceptable side effects. Here we investigate folic acid modified D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS-FA) as a potential carrier for controlled delivery of the drug. METHODS: Synthesized TPGS-FA was characterized by FTIR, UV-visible and 1H NMR spectroscopy, and TPGS loaded with NC was evaluated for its ability to induce apoptosis in Huh7 cells by Annexin V/PI and MTT assays, and observed by laser scanning confocal microscopy and inverted phase contrast microscopy. RESULTS: TPGS-FA/NC complexes were prepared successfully, and were homogenious with a uniform size of ~ 14 nm diameter. NC was released from the TPGS-FA/NC complexes in a controlled and sustained manner under physiological conditions (pH 7.4). Furthermore, its cytotoxicity to hepatocarcinoma cells was greater than that of free NC. CONCLUSIONS: TPGS-FA is shown to be useful carrier for drugs such as NC, and TPGS-FA/NC could potentially be a potent and safe drug for the treatment of hepatocellular carcinoma.


Asunto(s)
Antineoplásicos/administración & dosificación , Benzofenantridinas/administración & dosificación , Carcinoma Hepatocelular/tratamiento farmacológico , Portadores de Fármacos/administración & dosificación , Ácido Fólico/administración & dosificación , Neoplasias Hepáticas/tratamiento farmacológico , Nanopartículas/administración & dosificación , Vitamina E/administración & dosificación , Antineoplásicos/química , Apoptosis/efectos de los fármacos , Benzofenantridinas/química , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Portadores de Fármacos/química , Liberación de Fármacos , Ácido Fólico/química , Humanos , Micelas , Nanopartículas/química , Vitamina E/química
18.
Bioengineered ; 12(1): 382-391, 2021 12.
Artículo en Inglés | MEDLINE | ID: mdl-33472492

RESUMEN

The trypsin-assisted extraction of polysaccharides from Allium cepa L. was optimized using the response surface methodology (RSM). The optimum extraction conditions were extraction temperature, extraction time, extraction pH, and enzyme amount of 37.16°C, 180 min, 8.57, and 5.16%, respectively. Under the optimized conditions, the yield of A. cepa L. polysaccharides (ACP) reached 9.69%, which was comparable with the predicted yield (9.73%). Mid- and high-dose ACP significantly inhibited the tumor growth (43.93%) and the tumor inhibition percentage (38.05%), which were more than 30%. The ACP could extend the survival time of H22 ascites tumor-bearing mice. Furthermore, the ACP could reduce the thymus and the spleen atrophy and significantly promoted the Con A-induced proliferation of splenocytes and elevated the serum IFN-γ and IL-2 levels. Therefore, the ACP could inhibit the tumor growth in tumor-bearing mice and regulated the immune function of mice. Practical ApplicationsThe trypsin-assisted extraction has high efficiency, is carried out through the polysaccharide extraction and the deproteinization at the same time, and is more convenient and fast than traditional methods. No detailed study on the optimization of the trypsin extraction of onion polysaccharides is available. Thus, this experiment aims to use the BBD (4 factors and 3 levels) to optimize the roles of extraction temperature, extraction time, extraction pH, and amount of enzyme on the yield of polysaccharides obtained from the fruit of A. cepa L. In addition, when looking for high-quality biological functional principles for the pharmaceutical industry, the antitumor activity of ACP was evaluated. A. cepa L. is one of the most widely cultivated and consumed crops worldwide. Polysaccharides are the main active ingredient, and studies have shown that a high intake of Allium vegetables is associated with reduced risk of cancers.


Asunto(s)
Antineoplásicos Fitogénicos , Cebollas/química , Fitoquímicos , Polisacáridos , Tripsina/metabolismo , Animales , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Antineoplásicos Fitogénicos/farmacología , Proliferación Celular , Citocinas/metabolismo , Femenino , Inmunomodulación , Masculino , Ratones , Neoplasias Experimentales , Cebollas/metabolismo , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Polisacáridos/química , Polisacáridos/aislamiento & purificación , Polisacáridos/farmacología , Proyectos de Investigación
19.
Anticancer Agents Med Chem ; 21(5): 611-620, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-32748757

RESUMEN

BACKGROUND: Deoxypodophyllotoxin, isolated from the Traditional Chinese Medicine Anthriscus sylvestris, is well-known because of its significant anti-tumor activity with strong toxicity in vitro and in vivo. OBJECTIVE: In this article, a series of deoxypodophyllotoxin derivatives were synthesized and their anti-tumor effectiveness was evaluated. METHODS: The anti-tumor activity of deoxypodophyllotoxin derivatives was investigated by the MTT assay method. Apoptosis percentage was measured by flow cytometer analysis using Annexin-V-FITC. RESULTS: The derivatives revealed obvious cytotoxicity in the MTT assay by decreasing the number of late cancer cells. The decrease of Bcl-2/Bax could be observed in MCF-7, HepG2, HT-29, and MG-63 using Annexin V-FITC. The ratio of Bcl-2/Bax in the administration group was decreased, which was determined by the ELISA kit. CONCLUSION: The derivatives of deoxypodophyllotoxin could induce apoptosis in tumor cell lines by influencing Bcl-2/Bax.


Asunto(s)
Antineoplásicos/farmacología , Apoptosis/efectos de los fármacos , Medicamentos Herbarios Chinos/farmacología , Podofilotoxina/análogos & derivados , Proteínas Proto-Oncogénicas c-bcl-2/antagonistas & inhibidores , Proteína X Asociada a bcl-2/antagonistas & inhibidores , Antineoplásicos/síntesis química , Antineoplásicos/química , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Medicamentos Herbarios Chinos/síntesis química , Medicamentos Herbarios Chinos/química , Humanos , Estructura Molecular , Podofilotoxina/síntesis química , Podofilotoxina/química , Podofilotoxina/farmacología , Proteínas Proto-Oncogénicas c-bcl-2/genética , Proteínas Proto-Oncogénicas c-bcl-2/metabolismo , Relación Estructura-Actividad , Células Tumorales Cultivadas , Proteína X Asociada a bcl-2/genética , Proteína X Asociada a bcl-2/metabolismo
20.
Acta Pharmaceutica Sinica ; (12): 1856-1864, 2021.
Artículo en Chino | WPRIM | ID: wpr-887003

RESUMEN

Increasing research have found a high correlation between senescence and tumor. Cellular senescence can inhibit tumorigenesis while the cellular microenvironment altered by senescent cells can promote the proliferation and metastasis of tumor cells. Some cellular signaling pathways are commonly involved in aging process and carcinogenesis. The deregulation and imbalance of these pathways results into senescence and tumor development. Thus, agents that balance these pathways may effective for anti-aging and anti-tumor. Traditional Chinese medicine (TCM) has been used for the activation of multiple signaling pathways and molecular targets both associated with aging and tumor, with few side effects. Therefore, the article reviewed the cellular signalings that cross between the aging and tumors, and on this basis, summarized the current effective components of TCM with anti-aging and anti-cancer properties, as well as the potential mechanisms of these components in the cross signalings, to provide new research strategies and perspectives for effective components of TCM to treat aging and tumors.

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