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1.
Nanoscale ; 13(32): 13681-13692, 2021 Aug 28.
Artigo em Inglês | MEDLINE | ID: mdl-34477643

RESUMO

A hypoxic environment in tumors hampers the therapeutic efficacy of radiotherapy. Moreover, radiotherapy, a localized treatment technique, can barely control tumor metastases. Herein, poly(lactic-co-glycolic acid) was used to encapsulate perfluorocarbon (PFC) for increasing the oxygen level and a lignan-derived compound (Q1) for enhancing IL-25 secretion from fibroblasts, thereby boosting the radiotherapeutic effect on local and distant tumors. The prepared co-delivery nanoplatform, PFC-Q1@PLGA, has a nano-scale size of around 160 nm and a negative zeta potential (about -13 mV). PFC-Q1@PLGA treatment leads to an arrest of the G2 phase (4n) in the cell cycle and reduces the mitochondria membrane potential. A high expression level of IL-25 in fibroblasts is detected after the cells are treated with PFC-Q1@PLGA, which increases the late apoptosis percentage of 4T1 cells after treatment with IL-25-containing conditional medium from fibroblasts. The oxygen level in tumors is significantly promoted to about 52.3% after injection of oxygen-saturated PFC-Q1@PLGA (O2), which is confirmed from the functional magnetic resonance images of the tumor site in mice. The in vivo study demonstrates that the injection of PFC-Q1@PLGA (O2) into local tumors significantly enhances the radiotherapeutic effect on local tumors and also inhibits the growth of remote tumors by an enhanced abscopal effect. This study presents a novel radiotherapy strategy to enable synergistic whole-body therapeutic responses after localized treatment with PFC-Q1@PLGA (O2).


Assuntos
Fluorcarbonetos , Lignanas , Nanopartículas , Neoplasias , Animais , Camundongos , Oxigênio , Microambiente Tumoral
2.
Zhongguo Zhong Yao Za Zhi ; 46(15): 3846-3852, 2021 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-34472258

RESUMO

The lignans in Urtica cannabina were isolated by preparative HPLC, silica, and ODS column chromatographies, and identified by NMR and HR-MS. The inhibitory activities on 5α-reductase were evaluated in vitro. As a result, ten secolignans,(2R,4S)-2,4-bis(3-methoxyl-4-hydroxyphenyl)-3-butoxypropanol(1), 3,4-trans-3-hydroxymethyl-4-[bis(3,4-dimethoxyphenyl)methyl] butyrolactone(2), 3,4-trans-3-hydroxymethyl-4-[(3,4-dimethoxyphenyl)(3-methoxyl-4-hydroxyphenyl)methyl] butyrolactone(3), 3,4-trans-3-hydroxymethyl-4-[bis(3-methoxyl-4-hydroxyphenyl)methyl] butyrolactone(trans urticol, 4), 3,4-trans-3-hydroxymethyl-4-[bis(3,4-dimethoxyphenyl)methyl] butyrolactone-3-O-ß-D-glucopyranoside(5), 3,4-trans-3-hydroxymethyl-4-[(3,4-dimethoxyphenyl)(3-methoxyl-4-hydroxyphenyl)methyl]butyrolactone-3-O-ß-D-glucopyranoside(6), 3,4-trans-3-hydroxymethyl-4-[bis(3-methoxyl-4-hydroxyphenyl)methyl]butyrolactone-3-O-ß-D-glucopyranoside(trans-urticol-7-O-ß-D-glucopyranoside, 7), cycloolivil-4-O-ß-D-glucopyranoside(8), isolariciresinol-4'-O-ß-D-glucopyranoside(9), and olivil-4'-O-ß-D-glucopyranoside(10), together with a polyphenol [α-viniferin(11)], were isolated from U. cannabina for the first time. Compound 1 was a new lignan. Compound 7 was potent in inhibiting 5α-reductase.


Assuntos
Colestenona 5 alfa-Redutase/farmacologia , Lignanas , Urticaceae , Inibidores de 5-alfa Redutase , Cromatografia Líquida de Alta Pressão , Lignanas/farmacologia , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Urticaceae/efeitos dos fármacos , Urticaceae/enzimologia
3.
Molecules ; 26(17)2021 Aug 26.
Artigo em Inglês | MEDLINE | ID: mdl-34500615

RESUMO

Juniper representatives are natural sources of plenty of bioactive metabolites and have been used since ancient times as folk remedies against tapeworms, warts, cancer, etc. The antiproliferative activities of junipers are attributed to podophyllotoxin (PPT), which is a precursor for the synthesis of efficient anticancer drugs. However, the natural sources of PPT, Sinopodophyllum hexandrum (Royle) T. S. Ying and Podophyllum peltatum L., are already endangered species because of their intensive industrial exploitation. Therefore, identification of other sources of PPT is necessary. This study is a broad comparative investigation of junipers, for which original sources have been accessed from different continents of the world. The present research is aimed at the identification of species, producing PPT and other lignans at concentrations that are sufficient for the high antiproliferative activity of the corresponding extracts. Cytotoxic juniper leaf extracts demonstrated a broad spectrum of activity on a panel of cancer cell lines. The antiproliferative properties of junipers were attributed to the combined activity of great diversity of lignans (podophyllotoxin, deoxypodophyllotoxin, ß-peltatin, yatein, matairesinol, anhydropodorhizol, etc.), detected by UHPLC-HRMS and LC-ESI-MS/MS in the corresponding extracts. Several species of the genus Juniperus L. were outlined as perspective sources of drug precursors with potential pharmaceutical applications.


Assuntos
Antineoplásicos/farmacologia , Juniperus/química , Podofilotoxina/farmacologia , Antineoplásicos/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Medicamentos de Ervas Chinesas/farmacologia , Células HT29 , Humanos , Células K562 , Lignanas/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Pró-Fármacos/farmacologia
4.
J Biomed Nanotechnol ; 17(8): 1564-1573, 2021 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-34544534

RESUMO

Honokiol-loaded nanoparticles (HK-loaded NPs) exhibit potential antitumor activity; however, the factors affecting their antitumor efficacy are still unclear and need to be explored. This research was aimed to systematically estimate the influence of feed weight ratio (FWR) and nanocarrier structure on antitumor activity. Accordingly, three types of ethylene glycol derivatives, including linear poly(ethylene glycol) with molar mass of 2000 (PEG45), first and second generation oligo(ethylene glycol) dendrons (G1 and G2) were used as nanocarriers, and a series of HK-loaded NPs with different FWR were prepared successfully using the evaporation-ultrasonication method. These NPs showed similar stability but demonstrated differences with respect to particle size, morphology, cumulative profile, and antitumor efficacy. The influence of the FWR was studied using G1 dendrons as nanocarriers; the results indicated that the particle size and morphology of G1 NPs were significantly affected, and G1 NPs (8/1), with the FWR of 8/1 for HK versus G1 dendron, exhibited the highest antitumor activity among all G1 NPs. Furthermore, the influence of nanocarrier structure was investigated at the FWR of 4/1; the findings revealed reduction in the particle diameter from 280 nm to 109 nm and change in morphology from sphere to flower-like structure with an increase in the branch degree from linear to dendron. Moreover, G2 NPs (4/1), with the FWR of 4/1 for HK versus G2 dendron, carrying the highest branch degree exhibited the greatest antitumor efficacy among all. These results are suggestive of influence of particle size and morphology on antitumor efficacy of HK-loaded NPs. Conclusively, this study demonstrated nanocarrier structure and the FWR significantly affect the antitumor efficacy of NPs, which should be optimized for designing nanoscale delivery systems.


Assuntos
Portadores de Fármacos , Nanopartículas , Compostos de Bifenilo , Linhagem Celular Tumoral , Etilenoglicóis , Lignanas , Nanomedicina , Tamanho da Partícula , Poliésteres , Polietilenoglicóis
5.
Molecules ; 26(17)2021 Aug 27.
Artigo em Inglês | MEDLINE | ID: mdl-34500623

RESUMO

Lignans are the main secondary metabolites synthetized by Linum species as plant defense molecules. They are also valuable for human health, in particular, for their potent antiviral and antineoplastic properties. In this study, the adventitious root cultures of three Linum species (L. flavum, L. mucronatum and L. dolomiticum) were developed to produce aryltetralin lignans. The effect of two elicitors, methyl jasmonate and coronatine, on aryltetralin lignans production was also evaluated. The adventitious root cultures from L. dolomiticum were obtained and analyzed for the first time and resulted as the best producer for all the aryltetralins highlighted in this system: Podophyllotoxin, 6-methoxypodophyllotoxin and 6-methoxypodophyllotoxin-7-O-ß-glucoside, the last showing a productivity of 92.6 mg/g DW. The two elicitors differently affected the production of the 6-methoxypodophyllotoxin and 6-methoxypodophyllotoxin-7-O-ß-glucoside.


Assuntos
Linho/metabolismo , Lignanas/biossíntese , Raízes de Plantas/metabolismo , Acetatos/metabolismo , Aminoácidos/biossíntese , Ciclopentanos/metabolismo , Indenos , Oxilipinas/metabolismo , Podofilotoxina/análogos & derivados , Podofilotoxina/biossíntese
6.
Poult Sci ; 100(10): 101371, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34481217

RESUMO

This study evaluated the therapeutic efficacy of Schisandrin A on systemic colibacillosis of chickens. One hundred and eighty, 1-day-old Hailan Brown chickens were divided into 6 groups of 30 chickens each and assigned to the following treatments: 1) uninfected/untreated control; 2) infected Escherichia coli; 3) infected-plus low dose of Schisandrin A therapy (50 mg/kg); 4) infected-plus medium dose of Schisandrin A therapy (100 mg/kg); 5) infected-plus high dose of Schisandrin A therapy (200 mg/kg) and 6) infected-plus antimicrobial therapy (florfenicol). Each group of chickens was placed in cages with a photoperiod of 12 h of light and 12 h of dark. Feed and water for all groups were provided ad libitum for the duration of the study. On d 14, all the chickens except the uninfected control group were intraperitoneally inoculated with a fresh culture of E. coli containing 1 × 108 CFU/mL. The parameters measured included: average daily weight gain (ADG), percent survivability, liver index, serum activity of enzymes (ALT and AST), hepatic and intestinal concentrations of TNF-α, IL-1ß, IL-6, IL-8, and LPS, expression of tight junction proteins (occludin, ZO-1, and claudin-1), relative abundance of bacterial species and histopathological changes in hepatic and intestinal tissue. The results showed that the medium and high doses of Schisandrin A ameliorated the detrimental effects of colibacillosis on weight gain. Regarding organ indexes, E. coli infection induced a significant increase in liver index, all the doses of Schisandrin A produced a significant reduction of liver index in comparison to the E. coli infected control. Serum activity of ALT and AST enzymes significantly increased due to E. coli infection, with the exception of the low dose of Schisandrin A for AST enzyme activity, all the Schisandrin A treatments significantly lowered enzyme activity in comparison to the E. coli infected control. Regarding concentrations of inflammatory markers in hepatic and intestinal, E. coli infection caused a significant increase in TNF-α, IL-1ß, IL-6, and IL-8, except the lowest dose of Schisandrin A for IL-1ß, the rest of the doses tested were able to significantly reduced the concentrations of inflammatory markers. Concentrations of LPS in hepatic and intestinal tissues were significantly increased by E. coli infection, all doses of Schisandrin A significantly reduced the concentration of LPS in hepatic and intestinal tissue. E. coli infection significantly reduced the expression of 2 tight junction proteins (ZO-1 and Claudin-1), the higher doses of Schisandrin A were effective in significantly increasing the expression of these tight junction proteins when compared with the E. coli infected control. Taken together, these results show that Schisandrin A has potential as an alternative therapy for the treatment of colibacillosis in chickens.


Assuntos
Galinhas , Infecções por Escherichia coli , Animais , Ciclo-Octanos , Escherichia coli , Infecções por Escherichia coli/tratamento farmacológico , Infecções por Escherichia coli/veterinária , Lignanas , Fígado , Compostos Policíclicos
7.
J Agric Food Chem ; 69(40): 11781-11793, 2021 Oct 13.
Artigo em Inglês | MEDLINE | ID: mdl-34582205

RESUMO

Plant pathogenic fungi seriously affect agricultural production and are difficult to control. The discovery of new leads based on natural products is an important way to innovate fungicides. In this study, 30 natural-product-based magnolol derivatives were synthesized and characterized on the basis of NMR and mass spectroscopy. Bioactivity tests on phytopathogenic fungi (Rhizoctonia solani, Fusarium graminearum, Botrytis cinerea, and Sclerotinia sclerotiorum) in vitro of these compounds were performed systematically. The results showed that 11 compounds were active against four kinds of phytopathogenic fungi with EC50 values in the range of 1.40-20.00 µg/mL, especially compound L5 that exhibited excellent antifungal properties against B. cinerea with an EC50 value of 2.86 µg/mL, approximately 2.8-fold more potent than magnolol (EC50 = 8.13 µg/mL). Moreover, compound L6 showed the highest antifungal activity against F. graminearum and Rhophitulus solani with EC50 values of 4.39 and 1.40 µg/mL, respectively, and compound L7 showed good antifungal activity against S. sclerotiorum. Then, an in vivo experiment of compound L5 against B. cinerea was further investigated in vivo using infected tomatoes (curative effect, 50/200 and 36%/100 µg/mL). The physiological and biochemical studies illustrated that the primary action mechanism of compound L5 on B. cinerea might change the mycelium morphology, increase cell membrane permeability, and destroy the function of mitochondria. Furthermore, structure-activity relationship (SAR) studies revealed that hydroxyl groups play a key role in antifungal activity. To sum up, this study provides a reference for understanding the application of magnolol-based antifungal agents in crop protection.


Assuntos
Antifúngicos , Fungicidas Industriais , Animais , Antifúngicos/farmacologia , Ascomicetos , Compostos de Bifenilo , Botrytis , Fungicidas Industriais/farmacologia , Fusarium , Lignanas , Estrutura Molecular , Rhizoctonia , Relação Estrutura-Atividade
8.
J Agric Food Chem ; 69(32): 9229-9237, 2021 Aug 18.
Artigo em Inglês | MEDLINE | ID: mdl-34357758

RESUMO

The dried leaves and rhizomes of Alpinia zerumbet have been traditionally used as food and medicine. Anti-inflammatory activity-guided phytochemical investigation into the rhizomes of A. zerumbet led to the isolation of 17 compounds including 10 neolignans (1-10, 1a, 1b, 2a, 2b, 3a, 3b, 4, and 5 are new compounds) and seven diarylheptanoids (11-17) in which 1-3 were three pairs of enantiomers. 4 was only one enantiomer and 5 was a racemic mixture. Compounds 1a, 1b, 2a, and 2b incorporated an 8',9'-dinorneolignan skeleton, which was rare in the lignan family. The planar structures of these compounds were elucidated by extensive analyses of spectroscopic data. The relative and absolute configurations were determined by the time-dependent density functional theory (TDDFT)-based electronic circular dichroism (ECD) calculation method. The 95% ethanol extract and ethyl acetate extract of A. zerumbet were found to show anti-inflammatory activity against croton oil-induced ear edema in mice with inhibition rates of 20.0 and 47.6% at a dose of 80 mg/kg, respectively. Bioassays showed that compounds 1a, 1b, 2a, 2b, and 12 moderately inhibited nitric oxide (NO) production in lipopolysaccharide (LPS)-induced RAW264.7 cells with IC50 values of 3.62, 7.63, 6.51, 5.60, and 8.33 µM, respectively.


Assuntos
Alpinia , Lignanas , Animais , Anti-Inflamatórios/farmacologia , Diarileptanoides , Lignanas/farmacologia , Camundongos , Estrutura Molecular , Extratos Vegetais/farmacologia , Rizoma
9.
Pestic Biochem Physiol ; 178: 104942, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34446208

RESUMO

Rice sheath blight is a destructive fungal disease caused by Rhizoctonia solani. To find a safe and green measure, the biological activity of six plant extracts against R. solani was determined by mycelial growth rate method. The results showed that magnolol possessed better antifungal activities against R. solani, with an EC50 value of 7.47 mg/L. further action mechanism of magnolol against R. solani was carried out. Studies by scanning electron microscopy (SEM) showed that the morphology of R. solani mycelia was deformation and surface folds. Transmission electron microscope (TEM) observation on treated R. solani showed that magnolol could induce cytoplasmic membrane rupture and cytoplasmic membrane even disappeared completely accompanied with cellular debris was covered around this fungal, and the mycelia treated with magnolol showed fluorescence after PI staining. Further study showed that the content of malondialdehyde (MDA) and activity of chitinase, ß-1,3-glucanase and relative conductivity of mycelia were increased, while the content of soluble protein and activities of catalase (CAT), polyphenol oxidase (PPO), superoxide dismutase (SOD), succinate dehydrogenase (SDH) and NAD-malate dehydrogenase (NAD-MDH) were significantly decreased. These results indicated that magnolol could significantly damage the plasma membrane of R. solani, and interfere with cell respiratory metabolism, thus inhibiting the growth of mycelium.


Assuntos
Doenças das Plantas , Rhizoctonia , Compostos de Bifenilo , Membrana Celular , Lignanas
10.
J Med Food ; 24(8): 825-832, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34406878

RESUMO

Schisandra chinensis (S. chinensis) is one of the core drugs used for relieving cough and asthma in traditional Chinese medicine. However, there are few basic studies on the treatment of respiratory diseases with S. chinensis in modern pharmacology, and the material basis and mechanism of its antiasthmatic effect are still unclear. Lignans are the main active components of S. chinensis. The aim of this study was to observe the relaxation effect of S. chinensis lignans (SCL) on the tracheal smooth muscle of rats by in vitro tracheal perfusion experiments, and to explore the mechanism by preincubation with L-type calcium channel blocker verapamil, four potassium channel blockers glibenclamide, tetraethylamine, 4-aminopyridine and barium chloride (BaCl2), ß-adrenoceptor blocker propranolol, nitric oxide synthase inhibitor Nω-nitro-L-arginine methyl ester (L-NAME), and the cyclooxygenase inhibitor indomethacin, respectively. The results showed that SCL (0.25-1.75 mg/mL) reduced the contraction of isolated tracheal smooth muscle induced by acetylcholine, the preincubation with verapamil and glibenclamide could attenuate the relaxation effect, whereas propranolol, 4-aminopyridine, BaCl2, tetraethylamine, L-NAME, and indomethacin had no such effect. These results suggest that SCL has a significant relaxation effect on the isolated tracheal smooth muscle of rats, and the mechanism may be related to the inhibition of extracellular calcium influx and intracellular calcium release from the sarcoplasmic reticulum, as well as the activation of ATP-sensitive potassium channels. These findings may provide a pharmacological basis for the traditional use of S. chinensis to treat asthma.


Assuntos
Lignanas , Schisandra , Animais , Bloqueadores dos Canais de Cálcio/farmacologia , Lignanas/farmacologia , Relaxamento Muscular , Músculo Liso , Óxido Nítrico , Bloqueadores dos Canais de Potássio/farmacologia , Ratos
11.
Molecules ; 26(16)2021 Aug 08.
Artigo em Inglês | MEDLINE | ID: mdl-34443392

RESUMO

Thymic stromal lymphopoietin (TSLP) plays an important role in the pathophysiology of various allergic diseases that are mediated by T helper cell type-2 (Th2) responses, including asthma and atopic dermatitis. The primary focus of this study was the identification of potent inhibitors of the TSLP signaling pathway for potential therapeutic use. The 80% methanol extract of Machilus thunbergii bark significantly inhibited the signal transducer and activator of transcription 5 (STAT5) phosphorylation in human mast cell (HMC)-1 cells. Through activity-guided isolation, three lignans (1-3) were obtained and identified as (+)-galbelgin (1), meso-dihydroguaiaretic acid (2), and machilin A (3). Among them, two lignans (1 and 2) significantly inhibited STAT5 phosphorylation and TSLP/TSLPR interaction, as determined by ELISA. Our results indicated that lignans isolated from M. thunbergii are a promising resource for the treatment of allergic diseases.


Assuntos
Citocinas/antagonistas & inibidores , Lauraceae/química , Lignanas/farmacologia , Linhagem Celular , Fosforilação/efeitos dos fármacos , Casca de Planta/química , Fator de Transcrição STAT5/metabolismo , Células Th2/efeitos dos fármacos
12.
Food Res Int ; 147: 110488, 2021 09.
Artigo em Inglês | MEDLINE | ID: mdl-34399484

RESUMO

Flaxseed (Linum usitatissimum L.) is of interest as functional food because of the presence of compounds in its composition with potential health benefits, such as fatty acid omega-3, fiber, lignans and flavonoids. The bioactivity of lignans and flavonoids depends greatly on bacterial metabolism. Previously, lactobacilli and bifidobacteria strains were described to produce enterolignans and bioactive flavonoids (herbacetin, quercetin, quercetagetin, kaempferol, naringenin and eriodictyol) from flaxseed extracts and/or from secoisolariciresinol (SECO) in culture medium. In this work, cow's milk and soy beverage were supplemented with flaxseed extracts and fermented with selected lactobacilli and bifidobacteria strains. Lacticaseibacillus rhamnosus INIA P224, Limosilactobacillus mucosae INIA P508 and Lactiplantibacillus plantarum ESI 144 were capable of producing enterolactone (ENL) in both beverages supplemented with flaxseed, in addition to matairesinol and the flavonoids daidzein, genistein, glycitein, quercetin, naringenin, kaempferol and eriodictyol. On the other hand, Bifidobacterium breve INIA P367, Bifidobacterium pseudocatenulatum INIA P815 and Bifidobacterium pseudocatenulatum INIA P946 were able to produce quercetin, quercetagetin and high concentrations of herbacetin and SECO, in addition to pinoresinol, matairesinol, daidzein, genistein, naringenin, kaempferol and eriodictyol. The co-incubation of Lacticaseibacillus paracasei INIA P74 and Ligilactobacillus salivarius INIA P183 with Lactococcus lactis MG1363 harboring the food grade vector pLEB590.gly913, facilitated the production of ENL in soy beverage enriched with flaxseed. In this work, it is demonstrated how lactobacilli and bifidobacteria strains can improve the nutritional properties of flaxseed-enriched beverages, providing metabolites of great interest for human health.


Assuntos
Linho , Lignanas , Animais , Bebidas , Bifidobacterium , Bovinos , Flavonoides , Humanos , Lactobacillus , Lignanas/análise
13.
Theriogenology ; 174: 124-130, 2021 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-34428678

RESUMO

The aim of this study was to evaluate the effect of 1 µmol/L zearalenone (ZEN) and 1 µmol/L enterolactone (ENL), alone or in combination, on the survival and morphology of in vitro cultured ovarian preantral follicles. Ovaries from 10 sheep were collected at a local abattoir and fragmented, and the ovarian pieces were submitted to in vitro culture for 3 days in the presence or absence of the test compounds. The morphology of primordial and primary follicles was impaired by ZEN, whereas that of cultured secondary follicles was improved by ENL. However, the combination of ENL with ZEN impaired the quality of primary and secondary follicles. Both ZEN and ENL induced apoptosis, but only ZEN was responsible for oocyte autophagy. None of these xenoestrogens affected endoplasmic reticulum stress as observed by the unaltered expression of ERP29. Differently from ZEN, ENL increased the expression of the efflux transporter ABCG2. In conclusion, although ENL can counteract the negative effects of ZEN on primordial and primary follicles, this positive effect is not similar to that observed in ovarian tissue cultures in the presence of ENL alone.


Assuntos
Zearalenona , 4-Butirolactona/análogos & derivados , Animais , Feminino , Lignanas , Oócitos , Folículo Ovariano , Ovário , Ovinos , Zearalenona/toxicidade
14.
Phytochemistry ; 191: 112905, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34392008

RESUMO

(+)-(2S,3S)- and (-)-(2R,3R)-Oxybaphuslactam A glucosides are two undescribed benzofuran ε-caprolactams featuring a unique 7/6/5 fused tricyclic framework with p-glucosyl-O-phenyl unit. They were isolated from the root of Tibetan medicinal plant Oxybaphus himalaicus along with an undescribed sucrose ester, 3-O-feruloyl sucrose, an undescribed lignan glucoside, (7'R,8R,8'S)-3,3',5,5'-tetramethoxy-7',9-epoxylignan-9'-ol-7-one 4,4'-di-O-ß-D-glucopyranoside and ten known amides and phenylpropanoid derivatives. Based on the spectral analyses, X-ray crystallography and comparison of experimental and TD-DFT calculated ECD spectra, the structures of these compounds were determined. The anti-inflammatory assay showed the undescribed compounds had significant inhibitory effects on the formation of NO, TNF-α and IL-6, which were evaluated by LPS induced RAW 264.7 cell model.


Assuntos
Benzofuranos , Caprolactama , Lignanas , Amidas , Anti-Inflamatórios/farmacologia , Benzofuranos/farmacologia , Glucosídeos/farmacologia , Lignanas/farmacologia , Estrutura Molecular
15.
Adv Exp Med Biol ; 1330: 55-73, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34339030

RESUMO

Ovarian cancer, one of the three leading malignancies in women, has high incidence and mortality worldwide. It is hard to diagnose until very late stages and the 5-year survival rate is very low, due mostly to its distant metastasis. Chemotherapy is currently the most common treatment to inhibit cancer growth, but long-term use could result in resistance and tumor recurrence in addition to damages to normal tissues and functions of the patients. In order to achieve safe and curative effects against cancers, many investigators have focused their attention on traditional Chinese herbal medicines. Paclitaxel, a natural antitumor agent, has significant effects on advanced malignancies including ovarian cancer and is in the standard front-line treatment. Additional natural anticancer substances have continually been discovered for their high effectiveness and low side-effects in ovarian cancer prevention and therapy. In this chapter, we summarize recent work on a selected group of natural components, including lignans, ellagic acid, luteolin, mangiferin, and Acanthopanax senticosus, which have all been demonstrated to reduce the progress of epithelial ovarian cancer in a dose-depend manner, by both in vitro and in vivo experiments. The mechanisms of the anticancer activities by these natural components involve expression suppression of MMP2 and MMP9.


Assuntos
Antineoplásicos , Lignanas , Neoplasias Ovarianas , Antineoplásicos/uso terapêutico , Carcinoma Epitelial do Ovário , Feminino , Humanos , Lignanas/farmacologia , Lignanas/uso terapêutico , Recidiva Local de Neoplasia , Neoplasias Ovarianas/tratamento farmacológico
16.
Int J Mol Sci ; 22(15)2021 Jul 21.
Artigo em Inglês | MEDLINE | ID: mdl-34360535

RESUMO

The aims of this study were to develop the magnolol-chitosan films and study the positive effect of the combination of magnolol and chitosan. The addition of magnolol made the magnolol-chitosan films exhibit higher density (1.06-1.87 g/cm3), but the relatively lower water vapor permeability (12.06-7.36 × 10-11·g·m-1·s-1·Pa-1) and water content (16.10-10.64%). The dense and smooth surface and cross-section of magnolol-chitosan films were observed by environmental scanning electron microscopy (ESEM) images. The interaction of magnolol and chitosan was observed by X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy and thermogravimetric analysis (TGA). After the addition of magnolol, the antioxidant capacity of magnolol-chitosan films was increased from 18.99 to 82.00%, the growth of P. aeruginosa was inhibited and the inhibition percentage of biofilm formation was increased from 30.89 to 86.04%. We further verified that the application of magnolol-chitosan films on chilled pork significantly reduced the increases in pH value, inhibited the growth of microorganisms and extended the shelf life. Results suggest that magnolol had a positive effect on magnolol-chitosan films and could be effectively applied to pork preservation.


Assuntos
Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Compostos de Bifenilo/farmacologia , Quitosana/química , Conservação de Alimentos/métodos , Lignanas/farmacologia , Infecções por Pseudomonas/tratamento farmacológico , Pseudomonas aeruginosa/efeitos dos fármacos , Animais , Anti-Inflamatórios não Esteroides/farmacologia , Embalagem de Alimentos/métodos , Carne de Porco/análise , Infecções por Pseudomonas/microbiologia , Suínos
17.
Biomed Res Int ; 2021: 9919789, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34350295

RESUMO

This paper presents a new high-performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS) method with a rapid analysis of 6 min to determine the concentration of galgravin in rat plasma so as to study its pharmacokinetic features and bioavailability in vivo. Schisandrin was selected as the internal standard (IS). After extracting the analyte from plasma samples with ethyl acetate, methanol-H2O (0.1% formic acid) (85 : 15, v/v) was used as mobile phase to achieve chromatographic separation on a C18 reversed phase column. The MS detection was performed in positive ion mode using electrospray ionization (ESI) source. This method showed good linearity over the range of 1~500 ng/mL (R 2 > 0.999), and the lower limit of quantitation (LLOQ) was 1.0 ng/mL. The intraday precision and interday precision were both within 8.5%, whereas the accuracies were in the range of -2.6%-6.0%. The average recoveries of galgravin in rat plasma were between 92.3% and 99.3%. Moreover, galgravin was stable throughout storage and processing with all RSDs below 12.1%. After the successful application of this optimized method, the oral bioavailability of galgravin was determined to be 8.5%. This study will be helpful to the future research and development of galgravin.


Assuntos
Furanos/administração & dosagem , Furanos/farmacocinética , Lignanas/administração & dosagem , Lignanas/farmacocinética , Espectrometria de Massas em Tandem , Administração Intravenosa , Administração Oral , Animais , Disponibilidade Biológica , Cromatografia Líquida de Alta Pressão , Estabilidade de Medicamentos , Furanos/sangue , Furanos/química , Lignanas/sangue , Lignanas/química , Masculino , Ratos Sprague-Dawley , Padrões de Referência , Reprodutibilidade dos Testes , Fatores de Tempo
18.
Phytomedicine ; 90: 153647, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34362632

RESUMO

BACKGROUND: Honokiol is a pleiotropic compound which been isolated from Magnolia species such as Magnolia grandiflora and Magnolia dealbata. Magnolia species Magnolia grandiflora is used in traditional medicine for the treatment of various diseases. PURPOSE: The objective of this review is to summarize the pharmacological potential and therapeutic insights of honokiol. STUDY DESIGN: Honokiol has been specified as a novel alternative to treat various disorders such as liver cancer, neuroprotective, anti-spasmodic, antidepressant, anti-tumorigenic, antithrombotic, antimicrobial, analgesic properties and others. Therefore, this study designed to represent the in-depth therapeutic potential of honokiol. METHODS: Literature searches in electronic databases, such as Web of Science, Science Direct, PubMed, Google Scholar, and Scopus, were performed using the keywords 'Honokiol', 'Health Benefits' and 'Therapeutic Insights' as the keywords for primary searches and secondary search terms were used as follows: 'Anticancer', 'Oxidative Stress', 'Neuroprotective', 'Antimicrobial', 'Cardioprotection', 'Hepatoprotective', 'Anti-inflammatory', 'Arthritis', 'Reproductive Disorders'. RESULTS: This promising bioactive compound presented an wide range of therapeutic and biological activities which include liver cancer, neuroprotective, anti-spasmodic, antidepressant, anti-tumorigenic, antithrombotic, antimicrobial, analgesic properties, and others. Its pharmacokinetics has been established in experimental animals, while in humans, this is still speculative. Some of its mechanism for exhibiting its pharmacological effects includes apoptosis of diseased cells, reduction in the expression of defective proteins like P-glycoproteins, inhibition of oxidative stress, suppression of pro-inflammatory cytokines (TNF-α, IL-10 and IL-6), amelioration of impaired hepatic enzymes and reversal of morphological alterations, among others. CONCLUSION: All these actions displayed by this novel compound could make it serve as a lead in the formulation of drugs with higher efficacy and negligible side effects utilized in the treatment of several human diseases.


Assuntos
Compostos de Bifenilo , Lignanas , Magnolia , Animais , Compostos de Bifenilo/farmacologia , Humanos , Lignanas/farmacologia , Magnolia/química , Extratos Vegetais/farmacologia
19.
Molecules ; 26(15)2021 Jul 27.
Artigo em Inglês | MEDLINE | ID: mdl-34361665

RESUMO

In vitro cultures of scarlet flax (Linum grandiflorum L.), an important ornamental flax, have been established as a new possible valuable resource of lignans and neolignans for antioxidant and anti-inflammatory applications. The callogenic potential at different concentrations of α-naphthalene acetic acid (NAA) and thidiazuron (TDZ), alone or in combinations, was evaluated using both L. grandiflorum hypocotyl and cotyledon explants. A higher callus induction frequency was observed on NAA than TDZ, especially for hypocotyl explants, with a maximum frequency (i.e., 95.2%) on 1.0 mg/L of NAA. The presence of NAA (1.0 mg/L) in conjunction with TDZ tended to increase the frequency of callogenesis relative to TDZ alone, but never reached the values observed with NAA alone, thereby indicating the lack of synergy between these two plant growth regulators (PGRs). Similarly, in terms of biomass, NAA was more effective than TDZ, with a maximum accumulation of biomass registered for medium supplemented with 1.0 mg/L of NAA using hypocotyls as initial explants (DW: 13.1 g). However, for biomass, a synergy between the two PGRs was observed, particularly for cotyledon-derived explants and for the lowest concentrations of TDZ. The influence of these two PGRs on callogenesis and biomass is discussed. The HPLC analysis confirmed the presence of lignans (secoisolariciresinol (SECO) and lariciresinol (LARI) and neolignan (dehydrodiconiferyl alcohol [DCA]) naturally accumulated in their glycoside forms. Furthermore, the antioxidant activities performed for both hypocotyl- and cotyledon-derived cultures were also found maximal (DPPH: 89.5%, FRAP 866: µM TEAC, ABTS: 456 µM TEAC) in hypocotyl-derived callus cultures as compared with callus obtained from cotyledon explants. Moreover, the anti-inflammatory activities revealed high inhibition (COX-1: 47.4% and COX-2: 51.1%) for extract of hypocotyl-derived callus cultures at 2.5 mg/L TDZ. The anti-inflammatory action against COX-1 and COX-2 was supported by the IC50 values. This report provides a viable approach for enhanced biomass accumulation and efficient production of (neo)lignans in L. grandiflorum callus cultures.


Assuntos
Anti-Inflamatórios/análise , Antioxidantes/análise , Butileno Glicóis/análise , Cotilédone/química , Linho/química , Furanos/análise , Hipocótilo/química , Lignanas/análise , Extratos Vegetais/análise , Biomassa , Cromatografia Líquida de Alta Pressão/métodos , Cotilédone/metabolismo , Meios de Cultura/química , Técnicas de Cultura/métodos , Linho/metabolismo , Hipocótilo/metabolismo , Ácidos Naftalenoacéticos/farmacologia , Fenóis/análise , Compostos de Fenilureia/farmacologia , Reguladores de Crescimento de Plantas/farmacologia , Tiadiazóis/farmacologia
20.
Molecules ; 26(15)2021 Jul 27.
Artigo em Inglês | MEDLINE | ID: mdl-34361683

RESUMO

Six lignols (1-6), including two new compounds (+)-(7R,8R)-palmitoyl alatusol D (1) and (+)-(7R,8R)-linoleyl alatusol D (2), along with four phenolics (7-10), a neolignan (11), three alkyl aryl ether-type lignans (12-14), two furofuran-type lignans (15-16), three benzofuran-type lignans (17-19), a tetrahydrofuran-type lignan (20), and a dibenzylbutane-type lignan (21) were isolated from the ethyl acetate-soluble fraction of the methanol extract of Platycodon grandiflorum (Jacq.) A. DC. root. The chemical structures of the obtained compounds were elucidated via high-resolution mass spectrometry and nuclear magnetic resonance (NMR) spectroscopy analyses. The obtained spectroscopic data agreed well with literature. Among the isolated compounds, eighteen (1-7 and 11-21) were isolated from P. grandiflorum and the Campanulaceae family for the first time. This is the first report on lignol and lignan components of P. grandiflorum. The anti-inflammatory effects of the isolated compounds were examined in terms of their ability to inhibit the production of pro-inflammatory cytokines IL-6, IL-12 p40, and TNF-α in lipopolysaccharide-stimulated murine RAW264.7 macrophage cells. Nine compounds (4-6, 12, and 15-19) exhibited inhibitory effects on IL-12 p40 production, eleven compounds (1-6, 12, 15-17, and 19) exhibited inhibitory activity on IL-6 production, and eleven compounds (1-6 and 15-19) exhibited inhibitory effects against TNF-α. These results warrant further investigation into the potential anti-inflammatory activity and general benefits of the phenolic constituents of P. grandiflorum root.


Assuntos
Anti-Inflamatórios/farmacologia , Citocinas/metabolismo , Lignanas/farmacologia , Macrófagos/imunologia , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Platycodon/química , Transdução de Sinais/efeitos dos fármacos , Animais , Anti-Inflamatórios/química , Citocinas/antagonistas & inibidores , Lignanas/química , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Camundongos , Estrutura Molecular , Fenóis/química , Extratos Vegetais/química , Células RAW 264.7
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