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1.
Molecules ; 26(3)2021 Jan 30.
Artículo en Inglés | MEDLINE | ID: mdl-33573318

RESUMEN

During the time of the novel coronavirus disease 2019 (COVID-19) pandemic, it has been crucial to search for novel antiviral drugs from plants and well as other natural sources as alternatives for prophylaxis. This work reviews the antiviral potential of plant extracts, and the results of previous research for the treatment and prophylaxis of coronavirus disease and previous kinds of representative coronaviruses group. Detailed descriptions of medicinal herbs and crops based on their origin native area, plant parts used, and their antiviral potentials have been conducted. The possible role of plant-derived natural antiviral compounds for the development of plant-based drugs against coronavirus has been described. To identify useful scientific trends, VOSviewer visualization of presented scientific data analysis was used.


Asunto(s)
Antivirales/uso terapéutico , Extractos Vegetales/uso terapéutico , Alcaloides/química , Alcaloides/farmacología , Antivirales/química , Visualización de Datos , Flavonoides/química , Flavonoides/farmacología , Humanos , Extractos Vegetales/química , Extractos Vegetales/farmacología , Plantas Medicinales/química , Terpenos/química , Terpenos/farmacología
2.
BMC Complement Med Ther ; 21(1): 64, 2021 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-33588819

RESUMEN

BACKGROUND: The disparity of harvesting locations can influence the chemical composition of a plant species, which could affect its quality and bioactivity. Terminalia albida is widely used in traditional Guinean medicine whose activity against malaria has been validated in vitro and in murine models. The present work investigated the antimalarial properties and chemical composition of two samples of T. albida collected from different locations in Guinea. METHOD: T. albida samples were collected in different locations in Guinea, in Dubréka prefecture (West maritime Guinea) and in Kankan prefecture (eastern Guinea). The identity of the samples was confirmed by molecular analysis. In vitro antiplasmodial activity of the two extracts was determined against the chloroquine resistant strain PfK1. In vivo, extracts (100 mg/kg) were tested in two experimental murine models, respectively infected with P. chabaudi chabaudi and P. berghei ANKA. The chemical composition of the two samples was assessed by ultra-high-performance liquid chromatography coupled to high resolution mass spectrometry. RESULTS: In vitro, the Dubréka sample (TaD) was more active with an IC50 of 1.5 µg/mL versus 8.5 µg/mL for the extract from Kankan (TaK). In vivo, the antiparasitic effect of TaD was substantial with 56% of parasite inhibition at Day 10 post-infection in P. chabaudi infection and 61% at Day 8 in P. berghei model, compared to 14 and 19% inhibition respectively for the treatment with TaK. In addition, treatment with TaD further improved the survival of P. berghei infected-mice by 50% at Day 20, while the mortality rate of mice treated with Tak was similar to the untreated group. The LC/MS analysis of the two extracts identified 38 compounds, 15 of which were common to both samples while 9 and 14 other compounds were unique to TaD and TaK respectively. CONCLUSION: This study highlights the variability in the chemical composition of the species T. albida when collected in different geographical locations. These chemical disparities were associated with variable antimalarial effects. From a public health perspective, these results underline the importance of defining chemical fingerprints related to botanical species identification and to biological activity, for the plants most commonly used in traditional medicine.


Asunto(s)
Antimaláricos/química , Malaria/tratamiento farmacológico , Fitoterapia , Extractos Vegetales/química , Plasmodium/efectos de los fármacos , Terminalia/química , Animales , Antimaláricos/farmacología , Antimaláricos/uso terapéutico , Femenino , Guinea , Malaria/parasitología , Masculino , Medicina Tradicional Africana , Ratones Endogámicos C57BL , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Especificidad de la Especie , Terminalia/clasificación
3.
Viruses ; 13(2)2021 02 02.
Artículo en Inglés | MEDLINE | ID: mdl-33540713

RESUMEN

The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has spread globally. Although measures to control SARS-CoV-2, namely, vaccination, medication, and chemical disinfectants are being investigated, there is an increase in the demand for auxiliary antiviral approaches using natural compounds. Here we have focused on hydroxytyrosol (HT)-rich aqueous olive pulp extract (HIDROX®) and evaluated its SARS-CoV-2-inactivating activity in vitro. We showed that the HIDROX solution exhibits time- and concentration-dependent SARS-CoV-2-inactivating activities, and that HIDROX has more potent virucidal activity than pure HT. The evaluation of the mechanism of action suggested that both HIDROX and HT induced structural changes in SARS-CoV-2, which changed the molecular weight of the spike proteins. Even though the spike protein is highly glycosylated, this change was induced regardless of the glycosylation status. In addition, HIDROX or HT treatment disrupted the viral genome. Moreover, the HIDROX-containing cream applied on film showed time- and concentration-dependent SARS-CoV-2-inactivating activities. Thus, the HIDROX-containing cream can be applied topically as an antiviral hand cream. Our findings suggest that HIDROX contributes to improving SARS-CoV-2 control measures.


Asunto(s)
Antivirales/farmacología , Olea , Alcohol Feniletílico/análogos & derivados , Extractos Vegetales/farmacología , /efectos de los fármacos , Administración Tópica , Animales , Antivirales/química , Carbohidratos/química , Chlorocebus aethiops , Genoma Viral/efectos de los fármacos , Glicosilación , Pruebas de Sensibilidad Microbiana , Alcohol Feniletílico/administración & dosificación , Alcohol Feniletílico/farmacología , Fosfoproteínas/química , Extractos Vegetales/química , /fisiología , Crema para la Piel , Glicoproteína de la Espiga del Coronavirus/química , Células Vero , Inactivación de Virus/efectos de los fármacos
4.
Acta Cir Bras ; 36(1): e360102, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33605307

RESUMEN

PURPOSE: To study the Periplaneta americana L. extract Ento-B on the treatment of chronic ulcerative colitis induced by 2,4-dinitrochlorobenzene and acetic acid in rats and to explore its primary mechanism of action. METHODS: Using 2,4-dinitrochlorobenzene combined with acetic acid to induce chronic ulcerative colitis (chronic UC) in rats. The sulfasalazine (400 mg/kg) and Ento-B (200 mg/kg, 100 mg/kg,50 mg/kg) were given by intragastric administration and the effect was evaluated according to the disease activity index (DAI) score, colon mucosal injury index (CMDI) score, histopathological score (HS) and the serum levels of Interleukin-4(IL-4), Interleukin-10(IL-10), Tumor necrosis factor-α(TNF-α), Malondialdehyde(MDA), Superoxide dismutase(SOD) and Inducible nitric oxide synthase(iNOS.). RESULTS: Compared with the model group, all doses of Ento-B could reduce the score of CMDI (p < 0.05), HS(p < 0.05 or p < 0.01), significantly increased the expression of IL-4, IL-10, SOD (p < 0.01) and decreased the levels of TNF-α, MDA, iNOS in serum of UC rats, significantly improving the degree of colon lesionsin UC rats. CONCLUSIONS: Ento-B may play an important role in the treatment of ulcerative colitis induced byUC rats. The mechanism may be related to the increased expression of IL-4, IL-10, SOD and reduced expression of TNF-α, MDA, iNOS.


Asunto(s)
Colitis Ulcerosa , Periplaneta , Ácido Acético , Animales , Colitis Ulcerosa/inducido químicamente , Colitis Ulcerosa/tratamiento farmacológico , Colon , Dinitroclorobenceno , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Ratas , Factor de Necrosis Tumoral alfa
5.
BMC Complement Med Ther ; 21(1): 71, 2021 Feb 19.
Artículo en Inglés | MEDLINE | ID: mdl-33607987

RESUMEN

BACKGROUND: In previous studies, Cassia spectabilis DC leaf has shown a good antiplasmodial activity. Therefore, this study is a follow-up study of the extract of leaf of C. spectabilis DC on its in vitro and in vivo antiplasmodial activity and mechanism as an antimalarial. METHODS: The extract was fractionated, sub-fractionated and isolated to obtain the purified compound. In vitro antiplasmodial activity test against Plasmodium falciparum to find out the active compound. In vivo test against P. berghei ANKA-infected mice was conducted to determine prophylactic activity and antiplasmodial activity either alone or in combination with artesunate. The inhibition of heme detoxification test as one of the antimalarial mechanisms was carried out using the Basilico method. RESULTS: The results showed that active antimalarial compound isolated from C. spectabilis DC leaf had a structural pattern that was identical to (-)-7-hydroxycassine. Prophylactic test of 90% ethanolic extract of C. spectabilis DC leaf alone against P. berghei ANKA-infected mice obtained the highest percentage inhibition was 68.61%, while positive control (doxycycline 13 mg/kg) was 73.54%. In combination with artesunate, 150 mg/kg three times a day of C. spectabilis DC (D0-D2) + artesunate (D2) was better than the standard combination of amodiaquine + artesunate where the inhibition percentages were 99.18 and 92.88%, respectively. The IC50 of the extract for the inhibitory activity of heme detoxification was 0.375 mg/ml which was better than chloroquine diphosphate (0.682 mg/ml). CONCLUSION: C. spectabilis DC leaf possessed potent antiplasmodial activity and may offer a potential agent for effective and affordable antimalarial phytomedicine.


Asunto(s)
Antimaláricos/farmacología , Cassia/química , Hemo/metabolismo , Malaria/parasitología , Extractos Vegetales/farmacología , Plasmodium berghei/efectos de los fármacos , Plasmodium falciparum/efectos de los fármacos , Animales , Antimaláricos/aislamiento & purificación , Antimaláricos/uso terapéutico , Artesunato/uso terapéutico , Cloroquina/análogos & derivados , Cloroquina/farmacología , Cetonas , Malaria/tratamiento farmacológico , Masculino , Ratones Endogámicos BALB C , Fitoterapia , Piperidinas , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico , Hojas de la Planta/química , Plasmodium berghei/metabolismo , Plasmodium falciparum/metabolismo
6.
BMC Complement Med Ther ; 21(1): 69, 2021 Feb 19.
Artículo en Inglés | MEDLINE | ID: mdl-33607999

RESUMEN

BACKGROUND: Endoplasmic reticulum stress (ERS) is one of the main mechanisms of spinal cord injury (SCI) pathology and can affect the physiological state of neurons. Icariin (ICA), the main pharmacological component of Epimedium, can relieve the symptoms of patients with SCI and has obvious protective effects on neurons through ERS. METHODS: PC12 cells were induced to differentiate into neurons by nerve growth factor and identified by flow cytometry. Cell proliferation was detected by CCK8 method, cell viability was detected by SRB assay, apoptosis was detected by flow cytometry and microstructure of ER was observed by transmission electron microscope. Western blot was used to detect the protein expression of CHOP and Grp78, and qPCR was used to detect the mRNA expression of CHOP and Grp78. RESULTS: The results of CCK8, SRB and flow cytometry showed that ICA could relieve ERS and reduce apoptosis of PC12 cells. The results of transmission microscope showed that ICA could reduce apoptosis of PC12 cells caused by ERS. The results of Western blot and q-PCR showed that ICA could inhibit ERS by down-regulating the expression of CHOP and Grp78. CONCLUSIONS: ICA can inhibit ERS and promote the repair of PC12 cells by down-regulating the expression of CHOP and Grp78. ICA has the potential to promote the recovery of spinal cord injury.


Asunto(s)
Estrés del Retículo Endoplásmico/efectos de los fármacos , Epimedium/química , Flavonoides/farmacología , Extractos Vegetales/farmacología , Traumatismos de la Médula Espinal/patología , Animales , Apoptosis , Proteínas Portadoras/metabolismo , Supervivencia Celular/efectos de los fármacos , Regulación hacia Abajo , Flavonoides/uso terapéutico , Células PC12 , Extractos Vegetales/uso terapéutico , Ratas , Traumatismos de la Médula Espinal/complicaciones , Traumatismos de la Médula Espinal/tratamiento farmacológico , Traumatismos de la Médula Espinal/metabolismo , Factor de Transcripción CHOP/metabolismo
7.
Arch Oral Biol ; 122: 105029, 2021 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-33387850

RESUMEN

OBJECTIVE: The flower of chrysanthemum, used worldwide as a medicinal and edible product, has shown various bioactivities, such as anti-inflammatory, antioxidant, anti-tumorigenic, and hepatoprotective activities, as well as cardiovascular protection. However, the effect of Chrysanthemum morifolium Ramat. on the regulation of osteoclast differentiation has not yet been reported. In this study, we aimed to investigate the inhibitory effect of Chrysanthemum morifolium Ramat. water extract (CME) on RANKL-induced osteoclast differentiation in mouse bone marrow-derived macrophages (BMMs). STUDY DESIGN: Bone marrow-derived macrophages (BMMs) isolated from the C57BL/6 J mice. The viability of BMMs was detected with MTT assays. Inhibitory effects of CME on osteoclast differentiation and bone resorption was measured by TRAP staining and Pit assay. Osteoclast differentiation-associated gene expression were assessed by Real-time quantitative polymerase chain reaction. Intracellular signaling molecules was assessed by western blot. RESULTS: CME significantly inhibited osteoclast differentiation in BMMs without cytotoxicity, besides inhibiting MAPK/c-fos and PLCγ2/CREB activation. The inhibitory effects of CME on differentiation-related signaling molecules resulted in significant repression of NFATc1 expression, which is a key transcription factor in osteoclast differentiation, fusion, and activation. CONCLUSION: Our results confirmed the inhibition of RANKL-induced PLCγ2/CREB/c-fos/NFATc1 activation by CME during osteoclast differentiation. The findings collectively suggested CME as a traditional therapeutic agent for osteoporosis, RA, and periodontitis.


Asunto(s)
Resorción Ósea , Diferenciación Celular/efectos de los fármacos , Chrysanthemum/química , Osteoclastos/efectos de los fármacos , Extractos Vegetales/farmacología , Ligando RANK/metabolismo , Animales , Células de la Médula Ósea , Ratones , Ratones Endogámicos C57BL , Factores de Transcripción NFATC/metabolismo , Osteoclastos/citología , Proteínas Proto-Oncogénicas c-fos/metabolismo
8.
Sci Rep ; 11(1): 1462, 2021 01 14.
Artículo en Inglés | MEDLINE | ID: mdl-33446817

RESUMEN

Cannabis sativa is widely used for medical purposes and has anti-inflammatory activity. This study intended to examine the anti-inflammatory activity of cannabis on immune response markers associated with coronavirus disease 2019 (COVID-19) inflammation. An extract fraction from C. sativa Arbel strain (FCBD) substantially reduced (dose dependently) interleukin (IL)-6 and -8 levels in an alveolar epithelial (A549) cell line. FCBD contained cannabidiol (CBD), cannabigerol (CBG) and tetrahydrocannabivarin (THCV), and multiple terpenes. Treatments with FCBD and a FCBD formulation using phytocannabinoid standards (FCBD:std) reduced IL-6, IL-8, C-C Motif Chemokine Ligands (CCLs) 2 and 7, and angiotensin I converting enzyme 2 (ACE2) expression in the A549 cell line. Treatment with FCBD induced macrophage (differentiated KG1 cell line) polarization and phagocytosis in vitro, and increased CD36 and type II receptor for the Fc region of IgG (FcγRII) expression. FCBD treatment also substantially increased IL-6 and IL-8 expression in macrophages. FCBD:std, while maintaining anti-inflammatory activity in alveolar epithelial cells, led to reduced phagocytosis and pro-inflammatory IL secretion in macrophages in comparison to FCBD. The phytocannabinoid formulation may show superior activity versus the cannabis-derived fraction for reduction of lung inflammation, yet there is a need of caution proposing cannabis as treatment for COVID-19.


Asunto(s)
Antiinflamatorios/farmacología , Cannabinoides/farmacología , Cannabis/química , Células Epiteliales/inmunología , Macrófagos/inmunología , Extractos Vegetales/farmacología , /inmunología , Células A549 , Antiinflamatorios/química , /patología , Cannabinoides/química , Citocinas/inmunología , Células Epiteliales/patología , Células Epiteliales/virología , Regulación de la Expresión Génica/efectos de los fármacos , Regulación de la Expresión Génica/inmunología , Humanos , Macrófagos/patología , Macrófagos/virología , Extractos Vegetales/química , Receptores de IgG/inmunología
9.
Arch Oral Biol ; 122: 105032, 2021 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-33418435

RESUMEN

OBJECTIVES: This study aims to investigate the effects of tea extracts on biofilm formation by oral streptococci and the potential mechanisms behind the effects. DESIGN: We examined the effects of five types of tea extracts (green, oolong, black, pu-erh and chrysanthemum tea) on cell surface hydrophobicity and auto-aggregation of three different streptococcal species (Streptococcus mutans, Streptococcus salivarius and Streptococcus mitis) and evaluated their biofilm formation on four disparate hard surfaces (glass, stainless steel, hydroxyapatite and titanium). The correlation between biofilm formation and the cellular properties were investigated in order to study the mechanisms by which the tea extracts affect biofilm formation. RESULTS: Results show that the tea extracts reduced cell surface hydrophobicity (by up to 57.9 %) and, in some cases, altered cellular auto-aggregation (by up to 12 %) and biofilm formation (by up to 2.61 log CFU cm-2). Specifically, oolong tea extract was found to enhance biofilm formation by increasing cellular auto-aggregation and pu-erh tea extract retarded biofilm formation by increasing auto-aggregation. Biofilm formation correlated well to cell surface hydrophobicity and auto-aggregation in combination, but not to either one alone as determined by multiple linear regression analysis. CONCLUSIONS: Tea extracts have the ability to modulate streptococcal biofilm formation by altering cell surface hydrophobicity and cellular aggregation.


Asunto(s)
Biopelículas/efectos de los fármacos , Extractos Vegetales/farmacología , Streptococcus mutans/efectos de los fármacos , Té/química , Durapatita , Vidrio , Interacciones Hidrofóbicas e Hidrofílicas , Acero Inoxidable , Titanio
10.
Life Sci ; 267: 118981, 2021 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-33385409

RESUMEN

AIM: 15-Hydroxy-8(17),13(E)-labdadiene-19-carboxylic acid (HLCA) isolated from Juniperus foetidissima, has been recently identified as an antiproliferative agent; however, the molecular basis of antiproliferative effects of HLCA remains unknown. To investigate it, the current study has emphasized the hypothesis that HLCA induced cell death is a consequence of intracellular reactive oxygen species (ROS) production followed by cell cycle arrest and apoptosis. MAIN METHODS: Human ovarian OVCAR-3 and Caov-4 cells were treated with various concentrations of HLCA (48 h) and the measurement of intracellular ROS was considered. Then, the potential of HLCA in promoting apoptosis was investigated via flow cytometry, western blot, and caspase activity assay. Also, the inhibitory effect of HLCA on the cell cycle was evaluated using flow cytometry and western blot analysis. KEY FINDINGS: We found intracellular (ROS) accumulation in HLCA-treated cells. Subsequent observation of the increment in pro-apoptotic Bax as well as the decrement in antiapoptotic Bcl2 revealed that the HLCA-induced cytotoxicity may be triggered by the intrinsic pathway of apoptosis. Our subsequent experiments suggested that caspase-9 and -3 were activated and led the cells to apoptosis during the process. Cell cycle disruption at the G1 phase via down-regulation of cyclin D1 and Cyclin-dependent kinase 4 (CDK4) was another proved mechanism by which HLCA exerts its antiproliferative effects on the ovarian cell lines, OVCAR-3 and Caov-4, especially at relatively lower concentrations. SIGNIFICANCE: This is the first study that reveals the apoptotic effects of HLCA, suggesting its therapeutic potential as an effective anti-tumor agent. However, further in vivo studies are required to confirm these effects.


Asunto(s)
Diterpenos/farmacología , Neoplasias Ováricas/tratamiento farmacológico , Antineoplásicos Fitogénicos/aislamiento & purificación , Antineoplásicos Fitogénicos/farmacología , Apoptosis/efectos de los fármacos , Carcinoma Epitelial de Ovario , Caspasa 9/metabolismo , Ciclo Celular/efectos de los fármacos , Puntos de Control del Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Ciclina D1/metabolismo , Quinasa 4 Dependiente de la Ciclina/metabolismo , Diterpenos/aislamiento & purificación , Femenino , Humanos , Juniperus/química , Neoplasias Ováricas/metabolismo , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Proteínas Proto-Oncogénicas c-bcl-2/metabolismo , Especies Reactivas de Oxígeno/metabolismo
11.
ACS Appl Mater Interfaces ; 13(4): 4874-4885, 2021 Feb 03.
Artículo en Inglés | MEDLINE | ID: mdl-33464809

RESUMEN

This work is strategically premeditated to study the potential of a herbal medicinal product as a natural bioactive ingredient to generate nanocellulose-based antibacterial architectures. In situ fibrillation of purified cellulose was done in cinnamon extract (ciE) to obtain microfibrillated cellulose (MFC). To this MFC suspension, carboxylated cellulose nanocrystals (cCNCs) were homogeneously mixed and the viscous gel thus obtained was freeze-dried to obtain lightweight and flexible composite aerogel architectures impregnated with ciE, namely, ciMFC/cCNCs. At an optimal concentration of 0.3 wt % cCNCs (i.e., for ciMFC/cCNCs_0.3), an improvement of around 106% in compressive strength and 175% increment in modulus were achieved as compared to pristine MFC architecture. The efficient loading and interaction of ciE components, specifically cinnamaldehyde, with MFC and cCNCs resulted in developing competent antibacterial surfaces with dense and uniform microstructures. Excellent and long-term antimicrobial activity of the optimized architectures (ciMFC/cCNCs_0.3) was confirmed through various antibacterial assays like the zone inhibition method, bacterial growth observation at OD600, minimum inhibitory concentration (MIC, here 1 mg/mL), minimum bactericidal concentration (MBC, here 3-5 mg/mL), and Live/Dead BacLight viability tests. The changes in the bacterial morphology with a disrupted membrane were further confirmed through various imaging techniques like confocal laser scanning microscopy, FESEM, AFM, and 3D digital microscopy. The dry composite architecture showed the persuasive capability of suppressing the growth of airborne bacteria, which in combination with antibacterial efficiency in the wet state is considered as an imperative aspect for a material to act as the novel biomaterial. Furthermore, these architectures demonstrated excellent antibacterial performance under real "in use" contamination prone conditions. Hence, this work provides avenues for the application of crude natural extracts in developing novel forms of advanced functional biomaterials that can be used for assorted biological/healthcare applications such as wound care and antimicrobial filtering units.


Asunto(s)
Acroleína/análogos & derivados , Antibacterianos/química , Celulosa/química , Cinnamomum aromaticum/química , Nanogeles/química , Extractos Vegetales/química , Acroleína/química , Acroleína/farmacología , Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Adhesión Bacteriana/efectos de los fármacos , Infecciones Bacterianas/prevención & control , Humanos , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/farmacología
12.
Biol Res ; 54(1): 2, 2021 Jan 06.
Artículo en Inglés | MEDLINE | ID: mdl-33407904

RESUMEN

BACKGROUND: The preventive and therapeutic medical utilization of this plant is an age-long practice across the globe. This study aimed to validate the impact of dark purple blossoms of basil (Ocimum basilicum L.) aqueous extract at low temperature (0 °C) mediated mitochondrial fission contributed to induced apoptosis in human breast cancer cells. METHODS: Fresh blossoms were extracted at low temperature (0 °C) using a watery solvent. Human MCF7 breast cancer cells were then treated with 3 separate fluctuated concentrations of 0, 50, 150 and 250 µg/mL for 24 and 48 h. RESULTS: The outcomes demonstrated the presence of anthocyanins, anthraquinones, tannins, reducing sugars, glycosides, proteins, amino acids, flavonoids and volatile oils and nonappearance of Terpinoids and alkaloids. Contrastingly, frail presence of steroids in basil blossoms aqueous concentrate was noted. In addition, the results from a phytochemical subjective examination of basil (Ocimum basilicum L.) blossoms aqueous extract demonstrated that most of the credited natural impacts containing more remarkable contents of antioxidants and anticancer compounds in basil blossoms aqueous extract. Moreover, the restraint of glucose take-up was alleviated mediated by a dose-dependent manner in MCF7 cells with basil (Ocimum basilicum L.) blossoms aqueous extract inducted for 24 h, resulting in mitochondrial fission. CONCLUSION: This is the first study that shows the impact of the aqueous extract of basil (Ocimum basilicum L.) blossoms was extracted at low temperature (0℃/6 h) underlined high amounts of flavonoids and phenolic compounds bearing more anticancer and antioxidant activities compared to another aqueous extract (using boiled water solvent) and alcoholic extracts.


Asunto(s)
Apoptosis , Flores/química , Dinámicas Mitocondriales , Ocimum basilicum/química , Extractos Vegetales/farmacología , Neoplasias de la Mama , Frío , Humanos , Células MCF-7
13.
J Enzyme Inhib Med Chem ; 36(1): 497-503, 2021 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-33491508

RESUMEN

COVID-19 has become a global pandemic and there is an urgent call for developing drugs against the virus (SARS-CoV-2). The 3C-like protease (3CLpro) of SARS-CoV-2 is a preferred target for broad spectrum anti-coronavirus drug discovery. We studied the anti-SARS-CoV-2 activity of S. baicalensis and its ingredients. We found that the ethanol extract of S. baicalensis and its major component, baicalein, inhibit SARS-CoV-2 3CLpro activity in vitro with IC50's of 8.52 µg/ml and 0.39 µM, respectively. Both of them inhibit the replication of SARS-CoV-2 in Vero cells with EC50's of 0.74 µg/ml and 2.9 µM, respectively. While baicalein is mainly active at the viral post-entry stage, the ethanol extract also inhibits viral entry. We further identified four baicalein analogues from other herbs that inhibit SARS-CoV-2 3CLpro activity at µM concentration. All the active compounds and the S. baicalensis extract also inhibit the SARS-CoV 3CLpro, demonstrating their potential as broad-spectrum anti-coronavirus drugs.


Asunto(s)
Antivirales/farmacología , /antagonistas & inhibidores , Flavanonas/farmacología , Extractos Vegetales/farmacología , Inhibidores de Proteasas/farmacología , Replicación Viral/efectos de los fármacos , Animales , /virología , Chlorocebus aethiops , Descubrimiento de Drogas , Inhibidores Enzimáticos/farmacología , Humanos , Técnicas In Vitro , Modelos Moleculares , Células Vero
14.
Ecotoxicol Environ Saf ; 211: 111902, 2021 Mar 15.
Artículo en Inglés | MEDLINE | ID: mdl-33493717

RESUMEN

Application of activating agents can significantly improve efficiency of plants for remediation of soils contaminated by heavy metals, however, damage to soil and plants limits application of traditional activating agents. The aim of our experiments is to select an efficient,green and low-cost activating agent to improve efficiency of plant extraction technology. In this study, contaminated soil was remediated by Sedum alfredii. The effects of two plant extracts (i.e., Oxalis corniculata,OX and Medicago sativaextract, ME) in addition to citric acid (CA) were studied in oscillatory activation experiment and pot experiment. The oscillation activation experiment revealed that extraction quantity of heavy metals in the soil was enhanced significantly with concentration of plant extract. The extraction quantity of Zn from 100% OX extract and ME extract were significantly higher than 10 mmol/L CA (54.04% and 33.09%, respectively). The 10 mmol/L CA has best extraction efficiency for Cd, up to 41.36 µg/kg, which is significantly higher than CK (control) (p < 0.05). The pot experiment exhibited that application of CA has significantly reduced soil pH and organic matter content by 8.63% and 28.21%, respectively, however the two extracts have no significant effect on soil properties. The study indicated that application of CA has negative effects on root morphological parameters and chlorophyll fluorescence parameters of Sedum alfredii.The addition of extracts of two plants have not caused any harm to Sedum alfredii. The application of three activating agents was beneficial for purification of Cd and Zn in soils, and its repairing efficiency was improved by 3.92, 3.37, 3.33 times and 0.44, 0.20, 0.86 times, respectively. The combination of plant extracts and hyperaccumulators can effectively remove heavy metals from contaminated soils, which provided a theoretical basis for mitigation of pollution in soils.


Asunto(s)
Biodegradación Ambiental , Ácido Cítrico , Extractos Vegetales , Contaminantes del Suelo , Cadmio/análisis , Ácido Cítrico/farmacología , Metales Pesados/análisis , Extractos Vegetales/farmacología , Raíces de Plantas/química , Sedum/efectos de los fármacos , Suelo/química , Contaminantes del Suelo/análisis
15.
J Chromatogr A ; 1637: 461836, 2021 Jan 25.
Artículo en Inglés | MEDLINE | ID: mdl-33422795

RESUMEN

The interest in the therapeutic values of natural compounds from plants is growing worldwide because the development of modern synthetic drugs has not lived up to expectations. The tree Ficus religiosa native to India, China and Southeast Asia is traditionally used for curing almost 50 ailments, although the majority of the individual active compounds are not known. Hence, a hyphenated high-performance thin-layer chromatography (HPTLC) method was newly developed. It allowed a physicochemical, but especially effect-directed profiling of individual compounds present in Ficus religiosa leaves obtained from four locations (in India and Germany). Extracts of different polarities were screened for bioactivity responses and most bioactivities were found in the ethyl acetate extracts. A multi-imaging via 26 different detection modes was performed, i. e. UV/Vis/FLD, 11 microchemical derivatizations and 12 effect-directed assays (EDA). By HPTLC-UV/Vis/FLD-EDA, antibiotics against Gram-positive and Gram-negative bacteria as well as acetylcholinesterase, butyrylcholinesterase, tyrosinase, α-amylase, α-glucosidase and ß-glucosidase inhibitors and radical scavenging compounds were detected. Estrogen-like or gentotoxic compounds were not detected at higher extract amounts of even 5 mg/band applied. For further characterization of three most important, multipotent, bioactive compound zones, HPTLC was hyphenated with heated electrospray ionization high-resolution mass spectrometry including fragmentation (HPTLC-HESI-HRMS/MS). Multipotent bioactive compounds discovered in the extracts were equivalently calculated in reference to well-known reference inhibitors.


Asunto(s)
Antibacterianos/aislamiento & purificación , Ficus/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , Antibacterianos/farmacología , Cromatografía en Capa Delgada/métodos , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Espectrometría de Masa por Ionización de Electrospray/métodos , Espectrometría de Masas en Tándem/métodos
16.
Anticancer Res ; 41(2): 619-633, 2021 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-33517266

RESUMEN

BACKGROUND/AIM: The outlook for patients with high grade glioma (HGG) remains dismal. Hence, attention has focused on numerous innovative treatments. Our group has proposed a strategy on the use of a combination of polyphenols, as anti-invasive agents for the management of these neoplasms. MATERIALS AND METHODS: The aim of this study was to evaluate the in vitro effects of citrus flavonoids (tangeretin, nobiletin, naringin and limonin) and berry extracts (chokeberry, elderberry and bilberry) on selected mediators of invasion in 2 HGG cell cultures. RESULTS: The IC50 values could only be determined for tangeretin and chokeberry extract. The rest were non-functional in this context. Immunocytochemistry and flow cytometry results showed that chokeberry extract was most effective in down-regulating the expression of CD44. Similarly, RT-PCR data supported its ability to reduce gene expression of MMP-14 and EGFR. 2D invasion assays confirmed that inhibition is greater with chokeberry extract. CONCLUSION: Both polyphenols have anti-invasive potential but chokeberry extract is a stronger agent for glioma management.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Neoplasias Encefálicas/tratamiento farmacológico , Movimiento Celular/efectos de los fármacos , Frutas , Glioma/tratamiento farmacológico , Extractos Vegetales/farmacología , Polifenoles/farmacología , Antineoplásicos Fitogénicos/aislamiento & purificación , Neoplasias Encefálicas/genética , Neoplasias Encefálicas/metabolismo , Neoplasias Encefálicas/patología , Línea Celular Tumoral , Citrus , Receptores ErbB/genética , Receptores ErbB/metabolismo , Frutas/química , Glioma/genética , Glioma/metabolismo , Glioma/patología , Humanos , Metaloproteinasa 14 de la Matriz/genética , Metaloproteinasa 14 de la Matriz/metabolismo , Invasividad Neoplásica , Extractos Vegetales/aislamiento & purificación , Polifenoles/aislamiento & purificación , Prunus , Inhibidores Tisulares de Metaloproteinasas/genética , Inhibidores Tisulares de Metaloproteinasas/metabolismo , Vaccinium myrtillus
17.
Proc Natl Acad Sci U S A ; 118(5)2021 02 02.
Artículo en Inglés | MEDLINE | ID: mdl-33452205

RESUMEN

The outbreak of COVID-19 caused by SARS-CoV-2 has resulted in more than 50 million confirmed cases and over 1 million deaths worldwide as of November 2020. Currently, there are no effective antivirals approved by the Food and Drug Administration to contain this pandemic except the antiviral agent remdesivir. In addition, the trimeric spike protein on the viral surface is highly glycosylated and almost 200,000 variants with mutations at more than 1,000 positions in its 1,273 amino acid sequence were reported, posing a major challenge in the development of antibodies and vaccines. It is therefore urgently needed to have alternative and timely treatments for the disease. In this study, we used a cell-based infection assay to screen more than 3,000 agents used in humans and animals, including 2,855 small molecules and 190 traditional herbal medicines, and identified 15 active small molecules in concentrations ranging from 0.1 nM to 50 µM. Two enzymatic assays, along with molecular modeling, were then developed to confirm those targeting the virus 3CL protease and the RNA-dependent RNA polymerase. Several water extracts of herbal medicines were active in the cell-based assay and could be further developed as plant-derived anti-SARS-CoV-2 agents. Some of the active compounds identified in the screen were further tested in vivo, and it was found that mefloquine, nelfinavir, and extracts of Ganoderma lucidum (RF3), Perilla frutescens, and Mentha haplocalyx were effective in a challenge study using hamsters as disease model.


Asunto(s)
Antivirales/farmacología , /efectos de los fármacos , Adulto , Animales , Antivirales/química , Antivirales/uso terapéutico , /virología , Chlorocebus aethiops , Cricetinae , Modelos Animales de Enfermedad , Reposicionamiento de Medicamentos/métodos , Femenino , Humanos , Masculino , Pandemias , Extractos Vegetales/farmacología , Células Vero
18.
Aging (Albany NY) ; 13(2): 1571-1590, 2021 01 19.
Artículo en Inglés | MEDLINE | ID: mdl-33465050

RESUMEN

The main aspects of severe COVID-19 disease pathogenesis include hyper-induction of proinflammatory cytokines, also known as 'cytokine storm', that precedes acute respiratory distress syndrome (ARDS) and often leads to death. COVID-19 patients often suffer from lung fibrosis, a serious and untreatable condition. There remains no effective treatment for these complications. Out of all cytokines, TNFα and IL-6 play crucial roles in cytokine storm pathogenesis and are likely responsible for the escalation in disease severity. These cytokines also partake in the molecular pathogenesis of fibrosis. Therefore, new approaches are urgently needed, that can efficiently and swiftly downregulate TNFα, IL-6, and the inflammatory cytokine cascade, in order to curb inflammation and prevent fibrosis, and lead to disease remission. Cannabis sativa has been proposed to modulate gene expression and inflammation and is under investigation for several potential therapeutic applications against autoinflammatory diseases and cancer. Here, we hypothesized that the extracts of novel C. sativa cultivars may be used to downregulate the expression of pro-inflammatory cytokines and pathways involved in inflammation and fibrosis. Initially, to analyze the anti-inflammatory effects of novel C. sativa cultivars, we used a well-established full thickness human 3D skin artificial EpiDermFTTM tissue model, whereby tissues were exposed to UV to induce inflammation and then treated with extracts of seven new cannabis cultivars. We noted that out of seven studied extracts of novel C. sativa cultivars, three (#4, #8 and #14) were the most effective, causing profound and concerted down-regulation of COX2, TNFα, IL-6, CCL2, and other cytokines and pathways related to inflammation and fibrosis. These data were further confirmed in the WI-38 lung fibroblast cell line model. Most importantly, one of the tested extracts had no effect at all, and one exerted effect that may be deleterious, signifying that careful cannabis cultivar selection must be based on thorough pre-clinical studies. The observed pronounced inhibition of TNFα and IL-6 is the most important finding, because these molecules are currently considered to be the main targets in COVID-19 cytokine storm and ARDS pathogenesis. Novel anti-TNFα and anti-IL-6 cannabis extracts can be useful additions to the current anti-inflammatory regimens to treat COVID-19, as well as various rheumatological diseases and conditions, and 'inflammaging' - the inflammatory underpinning of aging and frailty.


Asunto(s)
Cannabis , Síndrome de Liberación de Citoquinas , Interleucina-6/antagonistas & inhibidores , Extractos Vegetales/farmacología , Factor de Necrosis Tumoral alfa/antagonistas & inhibidores , Antiinflamatorios/farmacología , Cannabinoides/farmacología , Línea Celular , Fibroblastos/efectos de los fármacos , Humanos , Inflamación/virología , Piel/efectos de los fármacos , Técnicas de Cultivo de Tejidos
19.
Med Hypotheses ; 147: 110480, 2021 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-33421690

RESUMEN

The ongoing coronavirus disease 2019 (COVID-19) pandemic caused by the SARS-CoV-2 virus is now considered a global public health threat. The primary focus has been on reducing the viral spread and treating respiratory symptoms; as time goes on, the impact of COVID-19 on neurological and haemostatic systems becomes more evident. The clinical data suggest that platelet hyperactivity plays a role in the pathology of COVID-19 from its onset and that platelets may serve critical functions during COVID-19 progression. Hyperactivation of blood platelets and the coagulation system are emerging as important drivers of inflammation and may be linked to the severity of the 'cytokine storm' induced in severe cases of COVID-19, in which disseminated intravascular coagulation, and platelet hyperactivity are associated with poor prognosis and increased risk of mortality. We propose that targeting platelet hyperactivity in the early stages of COVID-19 infection may reduce the immunothrombotic complications of COVID-19 and subdue the systemic inflammatory response. Lowering baseline platelet activity may be of particular importance for higher-risk groups. As an alternative to antiplatelet drugs, an inappropriate intervention in public health, we propose that the dietary antiplatelet agent Fruitflow®, derived from tomatoes, may be considered a suitable therapy. Fruitflow® contains antiplatelet and anti-inflammatory compounds that target the mechanisms of platelet activation specific to COVID-19 and can be considered a safe and natural antiplatelet regime.


Asunto(s)
Plaquetas/citología , Lycopersicon esculentum , Extractos Vegetales/farmacología , Inhibidores de Agregación Plaquetaria/farmacología , Antiinflamatorios , Coagulación Sanguínea , Presión Sanguínea , Progresión de la Enfermedad , Humanos , Inmunoglobulina G , Inflamación/patología , Modelos Teóricos , Activación Plaquetaria , Pronóstico , Trombosis
20.
Food Chem ; 346: 128933, 2021 Jun 01.
Artículo en Inglés | MEDLINE | ID: mdl-33418408

RESUMEN

Immensely aggravated situation of COVID-19 has pushed the scientific community towards developing novel therapeutics to fight the pandemic. Small molecules can possibly prevent the spreading infection by targeting specific vital components of the viral genome. Non-structural protein 15 (Nsp15) has emerged as a promising target for such inhibitor molecules. In this investigation, we docked bioactive molecules of tea onto the active site of Nsp15. Based on their docking scores, top three molecules (Barrigenol, Kaempferol, and Myricetin) were selected and their conformational behavior was analyzed via molecular dynamics simulations and MMPBSA calculations. The results indicated that the protein had well adapted the ligands in the binding pocket thereby forming stable complexes. These molecules displayed low binding energy during MMPBSA calculations, substantiating their strong association with Nsp15. The inhibitory potential of these molecules could further be examined by in-vivo and in-vitro investigations to validate their use as inhibitors against Nsp15 of SARS-CoV2.


Asunto(s)
Antivirales/farmacología , Simulación por Computador , Endorribonucleasas/antagonistas & inhibidores , Extractos Vegetales/farmacología , Té/química , Proteínas no Estructurales Virales/antagonistas & inhibidores , Dominio Catalítico , Endorribonucleasas/química , Endorribonucleasas/metabolismo , Humanos , Ligandos , Simulación de Dinámica Molecular , Proteínas no Estructurales Virales/química , Proteínas no Estructurales Virales/metabolismo
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