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2.
Front Pharmacol ; 13: 1016004, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36263142

RESUMEN

Obesity is a leading worldwide health threat with ever-growing prevalence, it promotes the incidence of various diseases, particularly cardiovascular disease, metabolic syndrome, diabetes, hypertension, and certain cancers. Traditional Chinese Medicine (TCM) has been used to control body weight and treat obesity for thousands of years, Chinese medicinal herbs provide a rich natural source of effective agents against obesity. However, some problems such as complex active ingredients, poor quality control, and unclear therapeutic mechanisms still need to be investigated and resolved. Prodrugs provide a path forward to overcome TCM deficiencies such as absorption, distribution, metabolism, excretion (ADME) properties, and toxicity. This article aimed to review the possible prodrugs from various medicinal plants that demonstrate beneficial effects on obesity and seek to offer insights on prodrug design as well as a solution to the global obesity issues.

6.
ACS Appl Mater Interfaces ; 13(10): 11588-11596, 2021 Mar 17.
Artículo en Inglés | MEDLINE | ID: mdl-33656316

RESUMEN

Increasing threats from both pathogenic infections and antibiotic resistance highlight the pressing demand for nonantibiotic agents and alternative therapies. Herein, we report several new phenothiazinium-based derivatives, which could be readily synthesized via fragment-based assembly, which exhibited remarkable bactericidal activities both in vitro and in vivo. Importantly, in contrast to numerous clinically and preclinically used antibacterial photosensitizers, these compounds were able to eliminate various types of microorganisms, including Gram-(+) Staphylococcus aureus (S. aureus), Gram-(-) Escherichia coli, multidrug-resistant S. aureus, and their associated biofilms, at low drug and light dosages (e.g., 0.21 ng/mL in vitro and 1.63 ng/cm2 in vivo to eradicate S. aureus at 30 J/cm2). This study thus unveils the potential of these novel phenothiaziniums as potent antimicrobial agents for highly efficient photodynamic antibacterial chemotherapy.


Asunto(s)
Antibacterianos/química , Antibacterianos/farmacología , Fármacos Fotosensibilizantes/química , Fármacos Fotosensibilizantes/farmacología , Animales , Antibacterianos/uso terapéutico , Biopelículas/efectos de los fármacos , Escherichia coli/efectos de los fármacos , Escherichia coli/fisiología , Infecciones por Escherichia coli/tratamiento farmacológico , Humanos , Ratones , Fenotiazinas/química , Fenotiazinas/farmacología , Fenotiazinas/uso terapéutico , Fotoquimioterapia , Fármacos Fotosensibilizantes/uso terapéutico , Infecciones Estafilocócicas/tratamiento farmacológico , Staphylococcus aureus/efectos de los fármacos , Staphylococcus aureus/fisiología
7.
Front Chem ; 8: 559159, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-33363102

RESUMEN

Traditional Chinese medicine (TCM) has been used to treat disorders in China for ~1,000 years. Growing evidence has shown that the active ingredients from TCM have antibacterial, antiproliferative, antioxidant, and apoptosis-inducing features. However, poor solubility and low bioavailability limit clinical application of active compounds from TCM. "Nanoformulations" (NFs) are novel and advanced drug-delivery systems. They show promise for improving the solubility and bioavailability of drugs. In particular, "smart responsive NFs" can respond to the special external and internal stimuli in targeted sites to release loaded drugs, which enables them to control the release of drug within target tissues. Recent studies have demonstrated that smart responsive NFs can achieve targeted release of active compounds from TCM at disease sites to increase their concentrations in diseased tissues and reduce the number of adverse effects. Here, we review "internal stimulus-responsive NFs" (based on pH and redox status) and "external stimulus-responsive NFs" (based on light and magnetic fields) and focus on their application for active compounds from TCM against tumors and infectious diseases, to further boost the development of TCM in modern medicine.

9.
Food Sci Technol Int ; 26(8): 696-705, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-32380848

RESUMEN

In this study, the disinfection effect of curcumin-mediated photodynamic therapy on the contact surfaces of fresh fruit was investigated. Our results showed that the optimum concentration of curcumin and the energy density required were 0.5 µM and 7.2 J/cm2, respectively. Photodynamic therapy showed an excellent disinfection rate for the fresh fruits with a reduction of more than 80% in the total bacteria and coliform counts. The photodynamic therapy inhibited species that belonged to the categories of gram-negative and facultative anaerobic bacteria, except for two species of the Trichoderma fungus. Importantly, photodynamic therapy prolonged the shelf-life of grapes for two days at room temperature. Therefore, photodynamic therapy should be commercialized as a high efficiency and non-thermal sterilization technology for use in the food industry.


Asunto(s)
Curcumina , Desinfección , Microbiología de Alimentos , Frutas , Viabilidad Microbiana , Fotoquimioterapia , Antiinfecciosos/farmacología , Bacterias/efectos de los fármacos , Curcumina/farmacología , Desinfección/métodos , Microbiología de Alimentos/métodos , Frutas/microbiología , Hongos/efectos de los fármacos
10.
Artif Cells Nanomed Biotechnol ; 48(1): 542-559, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-32054336

RESUMEN

Celastrol is used in traditional Chinese medicine for treating cancers. However, its low water solubility and poor tumour selection represent major pitfalls for clinical application. In the present study, gold nanoparticle (AuNP) firstly was conjugated with PVP-co-2-dimethylaminoethyl methacrylate (Polymer) and celastrol then modified by folic acid. The as-prepared folate receptor-targeted celastrol AuNP (FCA) was characterized using attenuated total reflection Fourier transform infrared spectroscopy, UV-Vis spectrometry, transmission electron microscope, and inductively coupled plasma mass spectrometry. The physical properties of FCA were also determined in solubility, drug encapsulation and in vitro drug release. Its anticancer activities were assessed in the 2D and 3D breast cancer models. The results showed that FCA was synthesized successfully with good solubility, high encapsulation efficiency and loading content. FCA showed the optimal cumulative release at pH 5.0 and high cellular uptake and exhibited significant inhibition on breast cancer cells. FCA also induced more significant apoptosis either in 2D and 3D breast cancer model than the celastrol AuNP and celastrol alone. These findings demonstrate that FCA improves water solubility of celastrol and enhances its anticancer activities against breast cancer. FCA might be a potential candidate of anticancer drug for breast cancer in the future if further development.


Asunto(s)
Antineoplásicos/farmacología , Neoplasias de la Mama , Ácido Fólico/química , Nanopartículas del Metal/química , Triterpenos/química , Antineoplásicos/síntesis química , Antineoplásicos/química , Antineoplásicos/metabolismo , Apoptosis/efectos de los fármacos , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/patología , Cápsulas , Supervivencia Celular/efectos de los fármacos , Estabilidad de Medicamentos , Receptores de Folato Anclados a GPI/metabolismo , Ácido Fólico/metabolismo , Ácido Fólico/farmacología , Oro/química , Oro/farmacología , Humanos , Células MCF-7 , Nanopartículas del Metal/toxicidad , Estructura Molecular , Tamaño de la Partícula , Triterpenos Pentacíclicos , Polímeros/química , Polímeros/farmacología , Solubilidad , Esferoides Celulares/efectos de los fármacos , Triterpenos/farmacología
11.
Food Chem ; 274: 415-421, 2019 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-30372959

RESUMEN

Photodynamic treatment (PDT) is an innovative technology with non-thermal and environmentally sound merits, but the evaluation on the storage qualities of fresh produce was scarce. In this study, the effects of curcumin-based PDT on the quality of fresh-cut 'Fuji' apple slices during storage at 4 °C were investigated. The impacts on the survival of Escherichia coli, color and weight loss were examined under different curcumin concentrations, illumination time or incubation time. Curcumin-based photodynamic inactivation of E. coli on the surface of apple slices reached 0.95 log. Curcumin-based PDT was proven to prevent browning and weight loss. Additionally, PDT significantly reduced the activity of polyphenol oxidase and peroxidases to 48% and 51%, respectively. Moreover, there were few negative changes in total phenolic, ascorbic acid content and anti-oxidant activity of the treated apples. These results indicated that curcumin-based PDT was a viable and promising non-thermal technology to preserve the quality of fresh produce.


Asunto(s)
Curcumina/farmacología , Calidad de los Alimentos , Almacenamiento de Alimentos , Malus/efectos de los fármacos , Malus/efectos de la radiación , Color , Escherichia coli/efectos de los fármacos , Escherichia coli/fisiología , Escherichia coli/efectos de la radiación , Malus/enzimología , Malus/microbiología , Fotoquimioterapia
12.
Front Pharmacol ; 9: 1374, 2018.
Artículo en Inglés | MEDLINE | ID: mdl-30538634

RESUMEN

Cancer is still a severe threat to the health of people worldwide. Chemotherapy is one of main therapeutic approaches to combat cancer. However, chemotherapy only has a limited success with severe side effects, especially causing damage to normal tissues such as bone marrow, gastrointestine, heart, liver, renal, neuron, and auditory tissues, etc. The side-effects limit clinical outcome of chemotherapy and lower patients' quality of life, and even make many patients discontinue the chemotherapy. Thus, there is a need to explore effective adjuvant strategies to prevent and reduce the chemotherapy-induced side effects. Naturally occurring products provide a rich source for exploring effective adjuvant agents to prevent and reduce the side effects in anticancer chemotherapy. Curcumin is an active compound from natural plant Curcuma longa L., which is widely used as a coloring and flavoring agent in food industry and a herbal medicine in Asian countries for thousands of years to treat vomiting, headache, diarrhea, etc. Modern pharmacological studies have revealed that curcumin has strong antioxidative, anti-microbial, anti-inflammatory and anticancer activities. Growing evidence shows that curcumin is able to prevent carcinogenesis, sensitize cancer cells to chemotherapy, and protect normal cells from chemotherapy-induced damages. In the present article, we review the preventive effect of curcumin against chemotherapy-induced myelosuppression, gastrointestinal toxicity, cardiotoxicity, hepatotoxicity, nephrotoxicity, neurotoxicity, ototoxicity, and genotoxicity, and discuss its action mechanisms.

13.
Fitoterapia ; 127: 245-251, 2018 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-29496564

RESUMEN

Six new cassaine diterpenoids (1, 3-7), along with three known ones (2, 8-9) were isolated from the seeds of Erythrophleum fordii. Their structures were elucidated by extensive spectroscopic methods and acid hydrolysis. Compound 2 was tested to be the most potent one and showed more sensitive activities on MCF-7 and A549 cancer cells with IC50 values of 3.66 ±â€¯1.20 and 2.87 ±â€¯0.46 µM, respectively. Furthermore, compound 2 reduced the number of cell colonies significantly in a dose-dependent manner in the colony formation assay and triggered apoptosis of MCF-7 cell.


Asunto(s)
Alcaloides/aislamiento & purificación , Antineoplásicos Fitogénicos/aislamiento & purificación , Diterpenos/aislamiento & purificación , Fabaceae/química , Abietanos , Alcaloides/farmacología , Antineoplásicos Fitogénicos/farmacología , Línea Celular Tumoral , Diterpenos/farmacología , Humanos , Estructura Molecular , Extractos Vegetales/química , Semillas/química
14.
ACS Appl Mater Interfaces ; 9(31): 25706-25716, 2017 Aug 09.
Artículo en Inglés | MEDLINE | ID: mdl-28741924

RESUMEN

Targeting drug delivery remains a challenge in various disease treatment including cancer. The local drug deposit could be greatly enhanced by some external stimuli-responsive systems. Here we develop pluronic P123/F127 polymeric micelles (M) encapsulating curcumin (Cur) that are permeabilized directly by focused ultrasound, in which ultrasound triggers drug release. Tumor preferential accumulation and site-specific sonochemotherapy were then evaluated. Cur-loaded P123/F127 mixed micelles (Cur-M) exhibited longer circulating time and increased cellular uptake compared to free Cur. With the assistance of focused ultrasound treatment, Cur-M showed tumor-targeting deposition in a time-dependent manner following systemic administration. This was due to enhanced permeabilization of tumor regions and increased penetration of Cur-M in irradiated tumor cells by ultrasound sonoporation. Furthermore, Cur-M self-assembly could be regulated by ultrasound irradiation. In vitro Cur release from mixed micelles was greatly dependent on ultrasound intensity but not on duration, suggesting the cavitational threshold was necessary to initiate subsequent sonochemotherapy. In vivo site-specific drug release was demonstrated in dual-tumor models, which showed spatial-temporal release of entrapped drugs following intratumoral injection. The sonoporation-assisted site-specific chemotherapy significantly inhibited tumor growth and the decrease in tumor weight was approximately 6.5-fold more than without exposure to ultrasound irradiation. In conclusion, the established ultrasound-guided nanomedicine targeting deposit and local release may represent a new strategy to improve chemotherapy efficiency.


Asunto(s)
Polímeros/química , Antineoplásicos , Línea Celular Tumoral , Curcumina , Portadores de Fármacos , Sistemas de Liberación de Medicamentos , Liberación de Fármacos , Humanos , Micelas
15.
Parkinsons Dis ; 2017: 4764212, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-28607800

RESUMEN

Progressive degeneration of dopaminergic neurons in the substantia nigra (SN) is implicated in Parkinson's disease (PD). The efficacy of these currently used drugs is limited while traditional Chinese medicine (TCM) has been used in the management of neurodegenerative diseases for many years. This study was designed to evaluate the effect of a modified traditional Chinese herbal medicine decoction, Cong Rong Jing (CRJ), on cell survival and apoptosis of 1-methyl-4-phenylpyridinium- (MPP+-) treated MES23.5 dopaminergic cells. CRJ was prepared as a decoction from three Chinese herbs, namely, Herba Cistanches, Herba Epimedii, and Rhizoma Polygonati. We reported here that CRJ significantly enhanced the cell survival of MES23.5 cells after the exposure of MPP+ and inhibited the production of intracellular reactive oxygen species (ROS) induced by MPP+. CRJ also prevented the MPP+-treated MES23.5 cells from apoptosis by reducing the externalization of phosphatidylserine and enhancing the Bcl-2/Bax protein expression ratio. Signaling proteins such as JAK2, STAT3, and ERK1/2 were also involved in the action of CRJ. Taken together, these results provide a preliminary mechanism to support clinical application of the TCM formulation in PD and possibly other neurodegenerative diseases associated with ROS injury and apoptosis.

16.
J Mater Chem B ; 5(10): 1980-1987, 2017 Mar 14.
Artículo en Inglés | MEDLINE | ID: mdl-32263952

RESUMEN

Photodynamic therapy (PDT) is a promising modality, which uses light energy to activate a nontoxic photosensitizer to treat various diseases like cancer and infectious diseases. Hypocrellin B (HB) is a naturally occurring photosensitizer isolated from traditional Chinese medicine Hypocrella bambusea. However, the high hydrophobicity and poor selectivity severely limit its application. Apoferritin, a macromolecular protein, can serve as an attractive nanocage to carry HB while improving its water solubility and tumor selectivity. In this study, novel HB-apoferritin nanoparticles (HB-AFT NPs) were successfully developed by assembling HB within the apoferritin nanocage. The self-assembled HB-AFT NPs have a narrow size distribution and smooth surface with an average diameter of 12 nm and a HB encapsulation efficiency of 85%. The morphological observation and circular dichroism analysis showed that the encapsulation strategy of HB did not impair apoferritin structure, and thus it potentially maintained the tumor targeting ability of apoferritin. Compared with free HB solution, HB-AFT NPs exhibited more pronounced photodynamic activity on MDA-MB-231 cells due to the higher intracellular uptake, increased reactive oxygen species (ROS) production and excellent tumor-targeting. All these results suggest that the self-assembled HB-AFT NPs can be considered as a potential photosensitive drug for tumor targeting photodynamic therapy.

17.
Aging Dis ; 8(6): 792-811, 2017 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-29344417

RESUMEN

Neural stem cells (NSCs) are special types of cells with the potential for self-renewal and multi-directional differentiation. NSCs are regulated by multiple pathways and pathway related transcription factors during the process of proliferation and differentiation. Numerous studies have shown that the compound medicinal preparations, single herbs, and herb extracts in traditional Chinese medicine (TCM) have specific roles in regulating the proliferation and differentiation of NSCs. In this study, we investigate the markers of NSCs in various stages of differentiation, the related pathways regulating the proliferation and differentiation, and the corresponding transcription factors in the pathways. We also review the influence of TCM on NSC proliferation and differentiation, to facilitate the development of TCM in neural regeneration and neurodegenerative diseases.

18.
Photodiagnosis Photodyn Ther ; 15: 133-8, 2016 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-27444887

RESUMEN

Breast cancer is one of the commonest malignant tumors threatening to women. The present study aims to investigate the effect of photodynamic action of palmatine hydrochloride (PaH), a naturally occurring photosensitizer isolated from traditional Chinese medicine (TCM), on apoptosis of breast cancer cells. Firstly, cellular uptake of PaH in MCF-7 cells was measured and the cytotoxicity of PaH itself on breast cancer MCF-7 cells was estimated using the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. Subcellular localization of PaH in MCF-7 cells was observed using confocal laser scanning microscopy (CLSM). For photodynamic treatment, MCF-7 cells were incubated with PaH and then irradiated by visible light (470nm) from a LED light source. Photocytotoxicity was investigated 24h after photodynamic treatment using MTT assay. Cell apoptosis was analyzed 18h after photodynamic treatment using flow cytometry with Annexin V/PI staining. Nuclear was stained using Hoechst 33342 and observed under a fluorescence microscope. Intracellular production of reactive oxygen species (ROS) was studied by measuring the fluorescence of 2, 7-dichlorofluorescein (DCF) using a flow cytometry. Results showed that PaH treatment alone had no or minimum cytotoxicity to MCF-7 cells after incubation for 24h in the dark. After incubation for 40min, the cellular uptake of PaH reached to the maximum, and PaH mainly located in mitochondria and endoplasmic reticulum of MCF-7 cells. Photodynamic treatment of PaH demonstrated a significant photocytotoxicity on MCF-7 cells, induced remarkable cell apoptosis and significantly increased intracellular ROS level. Our findings demonstrated that PaH as a naturally occurring photosensitizer induced cell apoptosis and significantly killed MCF-7 cells.


Asunto(s)
Apoptosis/efectos de los fármacos , Apoptosis/efectos de la radiación , Alcaloides de Berberina/administración & dosificación , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/patología , Fotoquimioterapia/métodos , Relación Dosis-Respuesta a Droga , Relación Dosis-Respuesta en la Radiación , Humanos , Luz , Células MCF-7 , Fármacos Fotosensibilizantes/administración & dosificación , Resultado del Tratamiento
19.
Photodiagnosis Photodyn Ther ; 15: 53-8, 2016 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-27181460

RESUMEN

Palmatine hydrochloride (PaH) is a natural active compound from a traditional Chinese medicine (TCM). The present study aims to evaluate the effect of PaH as a new photosensitizer on colon adenocarcinoma HT-29 cells upon light irradiation. Firstly, the absorption and fluorescence spectra of PaH were measured using a UV-vis spectrophotometer and RF-1500PC spectrophotometer, respectively. Singlet oxygen ((1)O2) production of PaH was determined using 1, 3-diphenylisobenzofuran (DPBF). Dark toxicity of PaH was estimated using the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. Cellular uptake of PaH in HT-29 cells was detected at different time intervals. Subellular localization of PaH in HT-29 cells was observed using confocal laser fluorescence microscopy. For photodynamic treatment, HT-29 cells were incubated with PaH and then irradiated by visible light (470nm) from a LED light source. Photocytotoxicity was investigated 24h after photodynamic treatment using MTT assay. Cell apoptosis was observed 18h after photodynamic treatment using a flow cytometry with Annexin V/PI staining. Results showed that PaH has an absorption peak in the visible region from 400nm to 500nm and a fluorescence emission peak at 406nm with an excitation wavelength of 365nm. PaH was activated by the 470nm visible light from a LED light source to produce (1)O2. Dark toxicity showed that PaH alone treatment had no cytotoxicity to HT-29 cancer cells and NIH-3T3 normal cells after incubation for 24h. After incubation for 40min, the cellular uptake of PaH reached to the maximum and PaH was located in mitochondria. Photodynamic treatment of PaH demonstrated a significant photocytotoxicity on HT-29 cells. The rate of cell death increased significantly in a PaH concentration-dependent and light dose-dependent manner. Further evaluation revealed that the early and late apoptotic rate of HT-29 cells increased remarkably up to 21.54% and 5.39% after photodynamic treatment of PaH at the concentration of 5µM and energy density of 10.8J/cm(2). Our findings demonstrated that PaH as a naturally occurring photosensitizer has potential in photodynamic therapy on colon adenocarcinoma.


Asunto(s)
Alcaloides de Berberina/administración & dosificación , Neoplasias Experimentales/tratamiento farmacológico , Neoplasias Experimentales/patología , Fotoquimioterapia/métodos , Apoptosis/efectos de los fármacos , Apoptosis/efectos de la radiación , Supervivencia Celular/efectos de los fármacos , Supervivencia Celular/efectos de la radiación , Relación Dosis-Respuesta a Droga , Relación Dosis-Respuesta en la Radiación , Células HT29 , Humanos , Luz , Fármacos Fotosensibilizantes/administración & dosificación
20.
Photodiagnosis Photodyn Ther ; 12(3): 385-92, 2015 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-26117199

RESUMEN

Norovirus (NoV) is one of the most important seafood- and water-borne viruses, and is a major cause of acute gastroenteritis outbreaks. In the present study we investigated the effect of curcumin as a sensitizer to photodynamic treatment both in buffer and in oysters against murine norovirus 1 (MNV-1), a surrogate of NoV. MNV-1 cultured in buffer and MNV-1 bio-accumulated in oysters were irradiated with a novel LED light source with a wavelength of 470nm and an energy of 3.6J/cm(2). Inactivation of MNV-1 was investigated by plaque assays. After virus was extracted from the gut of oysters treated over a range of curcumin concentrations, the ultrastructural morphology of the virus was observed using electron microscopy, and the integrity of viral nucleic acids and stability of viral capsid proteins were also determined. Results showed that the infectivity of MNV-1 was significantly inhibited by 1-3logPFU/ml, with significant damage to viral nucleic acids in a curcumin dose-dependent manner after photodynamic activation. Virus morphology was altered after the photodynamic treatment with curcumin, presumably due to the change of the viral capsid protein structures. The data suggest that treatment of oysters with photodynamic activation of curcumin is a potentially efficacious and cost-effective method to inactivate food-borne NoV. Further studies are necessary to evaluate the toxicology of this approach in detail and perform sensory evaluation of the treated product.


Asunto(s)
Curcumina/farmacología , Norovirus/efectos de los fármacos , Ostreidae , Fotoquimioterapia/métodos , Fármacos Fotosensibilizantes/farmacología , Animales , Ratones , Viabilidad Microbiana/efectos de los fármacos , Microscopía Electrónica de Transmisión , Reacción en Cadena de la Polimerasa de Transcriptasa Inversa , Inactivación de Virus/efectos de los fármacos
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