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1.
Artigo em Inglês | MEDLINE | ID: mdl-36088746

RESUMO

Falcarinol is a polyacetylene which is found in carrots and known to have anti-neoplastic properties in rodents. Research in the bioactivity of falcarinol in humans require methods for quantification of falcarinol in human serum. Here we report the development of an LC-MS/MS method and its use to measure serum falcarinol concentrations in humans following intake of a carrot product. Falcarinol was measured by LC-MS/MS using the m/z 268 to m/z 182 mass transition. Six calibrator levels (0.2-20 ng/mL) and 3 control levels (0.4, 2 and 8 ng/mL) were prepared by addition of falcarinol to human serum pools. Linearity of the developed method was good with a mean R2 of 0.9942. Within-day, between-day and total coefficients of variation were 6.9-13.1%, 4.1-5.0% and 8.1-14.0%, respectively. The limits of detection and quantitation were 0.1 and 0.2 ng/mL, respectively, matrix effects 84.2%, recovery 101.4-105.4% and carry-over -0.24-0.07%. Serum falcarinol concentrations were measured in 18 healthy volunteers prior to and at 9 time-points following intake of a carrot product. Falcarinol concentrations peaked at the 1-hour time-point after intake in 15 out of 18 volunteers and declined according to a single exponential decay function with an aggregate t½ of 1.5 h. In conclusion, an LC-MS/MS method for quantification of falcarinol in human serum with acceptable performance was developed and used to measure falcarinol concentrations following intake of a carrot product.


Assuntos
Daucus carota , Cromatografia Líquida , Di-Inos , Álcoois Graxos , Humanos , Extratos Vegetais , Polímero Poliacetilênico , Poli-Inos , Espectrometria de Massas em Tandem
2.
Org Biomol Chem ; 20(37): 7391-7404, 2022 09 28.
Artigo em Inglês | MEDLINE | ID: mdl-36098263

RESUMO

In recent years, many methods for the facile synthesis of pyridines and their derivatives have been developed. The [2 + 2 + 2] cycloaddition reaction of alkynes and nitriles catalyzed by transition metals has emerged as the most straightforward and efficient method to obtain pyridine derivatives. Recently, Earth-abundant cobalt has been employed as a versatile and economical catalyst for the synthesis of functionalized molecules, as compared to other transition metals. This review mainly focuses on the recent research and development of the Co-catalyzed intramolecular [2 + 2 + 2] cycloaddition of diynes-nitriles or intermolecular [2 + 2 + 2] cycloaddition reaction of alkynes or diynes with nitriles for the construction of chiral or achiral multi-substituted pyridines. Meanwhile, brief mechanistic insights are also discussed here to explain the observed regioselectivity.


Assuntos
Nitrilas , Piridinas , Alcinos , Catálise , Cobalto , Reação de Cicloadição , Di-Inos
3.
Sci Total Environ ; 852: 158502, 2022 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-36058332

RESUMO

Mosquitoes' current insecticide resistance status in available public health insecticides is a serious threat to mosquito control initiatives. Microbe-based control agents provide an alternative to conventional pesticides and insecticides, as they can be more targeted than synthetic insecticides. The present study was focused on identifying and investigating the mosquitocidal potential of Cladophialophora bantiana, an endophytic fungus isolated from Opuntia ficus-indica. The Cladophialophora species was identified through phylogenetic analysis of the rDNA sequence. The isolated fungus was first evaluated for its potential to produce metabolites against Aedes aegpti and Culex quinquefasciatus larvae in the 1-4th instar. The secondary metabolites of mycelium extract were assessed at various test doses (100, 200, 300, 400, and 500 µg/mL) in independent bioassays for each instar of selected mosquito larvae. After 48 h of exposure, A. aegypti expressed LC50 values of 13.069, 18.085, 9.554, and 11.717 µg/mL and LC90 = 25.702, 30.860, 17.275, and 19.601 µg/mL; followed by C. quinquefasciatus LC50 = 14.467, 11.766, 5.934, and 7.589 µg/mL, and LC90 = 29.529, 20.767, 11.192, and 13.296 µg/mL. The mean % of ovicidal bioassay was recorded 120 h after exposure. The hatchability (%) was proportional to mycelia metabolite concentration. The enzymatic level of acetylcholinesterase in fungal mycelial metabolite treated 4th instar larvae indicated a dose-dependent pattern. The GC-MS profile of C. bantiana extracts identified five of the most abundant compounds, namely cyclobutane, trans-3-undecene-1,5-diyne, 1-bromo-2-chloro, propane, 1,2,3-trichloro-2-methyl-, 5,5,10,10-tetrachlorotricyclo, and phenol, which had the killing effect in mosquitoes. Furthermore, the C. bantiana fungus ethyl acetate extracts had a strong larvicidal action on A. aegypti and C. quinquefasciatus. Finally, the toxicity test on zebrafish embryos revealed the induction of malformations only at concentrations above 1 mg/mL. Therefore, our study pioneered evidence that C. bantiana fungal metabolites effectively control A. aegypti and C. qunquefasciastus and show less lethality in zebrafish embryos at concentrations up to 500 µg/mL.


Assuntos
Aedes , Anopheles , Culex , Ciclobutanos , Inseticidas , Animais , Peixe-Zebra , Inseticidas/toxicidade , Acetilcolinesterase , Propano/farmacologia , Filogenia , Ciclobutanos/farmacologia , Extratos Vegetais/farmacologia , Controle de Mosquitos , Larva , Fenóis , DNA Ribossômico , Di-Inos/farmacologia , Folhas de Planta
4.
J Org Chem ; 87(16): 10651-10663, 2022 08 19.
Artigo em Inglês | MEDLINE | ID: mdl-35917577

RESUMO

A straightforward, efficient, and selective method for the preparation of novel boryl-functionalized enynes or dienes via [Pt(PPh3)4]-catalyzed diboration of a broad spectrum of symmetrical and unsymmetrical 1,3-diynes was developed. The catalytic cycle of diboration was proposed on the basis of low-temperature 31P NMR studies. An alternative isolation method via product condensation on a cold finger was developed, which, in contrast to previous literature reports, eliminates the need for the additional transformation of rapidly decomposing enynyl pinacol boronates to more stable silica-based column chromatography derivatives during the separation step. To prove the efficiency of this simple catalytic protocol, bisboryl-functionalized enynes were synthesized in a gram scale and tested as useful building blocks in advanced organic transformations, such as hydrosilylation and Suzuki and sila-Sonogashira couplings. The presence of silyl, boryl, as well as other functions like halogen or alkoxy in their structures builds a new class of multifunctionalized enynes that might be modified in various chemical reactions.


Assuntos
Alcinos , Di-Inos , Alcinos/química , Catálise , Di-Inos/química
5.
J Integr Neurosci ; 21(4): 109, 2022 Jun 07.
Artigo em Inglês | MEDLINE | ID: mdl-35864761

RESUMO

BACKGROUND: Peripheral nerve regeneration is a coordinated process of Schwann cell (SC) reprogramming and intrinsic neuronal growth program activation. Panaxydol (PND) is a strong biologically active traditional Chinese medicine monomer extracted from Panax notoginseng rhizomes. In vitro, PND protects neurons and SCs from injury and stimulates the expression and secretion of neurotrophic factors (NTFs) by SCs. We hypothesized that PND may also promote peripheral nerve regeneration in adult animals. METHODS: PND (10 mg/kg body weight) was injected intraperitoneally into the Sprague-Dawley (SD) rats for two consecutive weeks after sciatic nerve transection. The morphology of the repaired sciatic nerve was evaluated after 16 weeks, and sensory and motor function recovery was evaluated using functional and behavioral techniques. RESULTS: PND was biologically safe at an injection dose of 10 mg/kg/day. After 14 days, it significantly increased the myelination of regenerated nerve fibers, and promoted sensory and motor function recovery. In the early stage of injury, PND significantly upregulated the mRNA expression of brain-derived neurotrophic factor (BDNF) and its receptors in distal injured nerves, which may represent a possible mechanism by which PND promotes nerve regeneration in vivo. CONCLUSIONS: Our study demonstrated that PND leads to sensory and motor recovery in a sciatic nerve transection model rat. Furthermore, we showed that BDNF mRNA level was significantly increased in the injured distal nerve, potentially contributing to the functional recovery. Further research is warrantied to examine whether direct injection is a more efficient method to increase BDNF expression compared to an exogenous BDNF administration.


Assuntos
Fator Neurotrófico Derivado do Encéfalo , Panax notoginseng , Animais , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Di-Inos , Álcoois Graxos , Regeneração Nervosa/fisiologia , Panax notoginseng/genética , Panax notoginseng/metabolismo , RNA Mensageiro/metabolismo , Ratos , Ratos Sprague-Dawley , Células de Schwann/metabolismo , Nervo Isquiático/lesões
6.
Chemistry ; 28(56): e202202015, 2022 Oct 07.
Artigo em Inglês | MEDLINE | ID: mdl-35771213

RESUMO

A new [4+2] cycloaddition of allenyne-alkyne is developed. The reaction is believed to proceed with forming an α,3-dehydrotoluene intermediate. This species behaves as a σπ-diradical to react with a hydrogen atom donor, whereas it displays a zwitterionic reactivity toward weak nucleophiles. The efficiency of trapping α,3-dehydrotoluene depends not only on its substituents but also the trapping agents. Notable features of the reaction are the activating role of the extra alkyne of the 1,3-diyne that reacts with the allenyne moiety and the opposite mode of trapping with oxygen and nitrogen nucleophiles. Oxygen nucleophiles result in the oxygen-end incorporation at the benzylic position of the α,3-dehydrotoluene, whereas with amine nucleophiles the nitrogen-end is incorporated into the aromatic core. Relying on the allenyne-alkyne cycloaddition as an enabling strategy, a concise total synthesis of phosphodiesterase-4 inhibitory selaginpulvilin A is realized.


Assuntos
Alcinos , Nucleotídeo Cíclico Fosfodiesterase do Tipo 4 , Aminas , Reação de Cicloadição , Di-Inos , Hidrogênio , Nitrogênio , Oxigênio
7.
Molecules ; 27(10)2022 May 17.
Artigo em Inglês | MEDLINE | ID: mdl-35630673

RESUMO

Cu-catalyzed 1,3-dipolar cycloaddition of ethyl 2-azidoacetate to iodobuta-1,3-diynes and subsequent Sonogashira cross-coupling were used to synthesize a large series of new triazole-based push-pull chromophores: 4,5-bis(arylethynyl)-1H-1,2,3-triazoles. The study of their optical properties revealed that all molecules have fluorescence properties, the Stokes shift values of which exceed 150 nm. The fluorescent properties of triazoles are easily adjustable depending on the nature of the substituents attached to aryl rings of the arylethynyl moieties at the C4 and C5 atoms of the triazole core. The possibility of 4,5-bis(arylethynyl)-1,2,3-triazoles' application for labeling was demonstrated using proteins and the HEK293 cell line. The results of an MTT test on two distinct cell lines, HEK293 and HeLa, revealed the low cytotoxicity of 4,5-bis(arylethynyl)triazoles, which makes them promising fluorescent tags for labeling and tracking biomolecules.


Assuntos
Di-Inos , Triazóis , Reação de Cicloadição , Células HEK293 , Células HeLa , Humanos , Triazóis/farmacologia
8.
ACS Macro Lett ; 11(5): 630-635, 2022 05 17.
Artigo em Inglês | MEDLINE | ID: mdl-35570817

RESUMO

Ruthenium alkoxymethylidene complexes have recently come into view as competent species for metathesis copolymerization reactions when coupled with appropriate comonomer targets. Here, we explore the ability of Fischer-type carbenes to participate in cascade alternating metathesis cyclopolymerization (CAMC) through facile terminal alkyne addition. The combination of diyne monomers and an equal feed ratio of low-strain dihydrofuran leads to a controlled chain-growth copolymerization with high degrees of alternation (>97% alternating diads) and produces degradable polymer materials with low dispersities and targetable molecular weights. When combined with enyne monomers, this method is amenable to the synthesis of alternating diblock copolymers that can be fully degraded to short oligomer fragments under aqueous acidic conditions. This work furthers the potential for the generation of functional metathesis materials via Fischer-type ruthenium alkylidenes.


Assuntos
Rutênio , Alcinos , Di-Inos , Polimerização , Polímeros
9.
Org Lett ; 24(15): 2899-2904, 2022 04 22.
Artigo em Inglês | MEDLINE | ID: mdl-35404065

RESUMO

An efficient synthetic organic transformation was developed to access isoquinoline-substituted isobenzofurans by reaction of substituted 1,5-diynes with isoquinoline N-oxides. Moderate to excellent yields of isoquinoline-derived isobenzofurans were achieved by formation of a new C-C and two C-O bonds in the presence of copper catalyst in one pot. whereas quinoline-substituted isobenzofurans were obtained when the reaction was conducted using quinoline N-oxides and 1,5-diynes in the presence copper catalyst.


Assuntos
Cobre , Di-Inos , Catálise , Cobre/química , Di-Inos/química , Isoquinolinas , Óxidos/química , Quinolinas
10.
J Am Chem Soc ; 144(17): 7750-7757, 2022 05 04.
Artigo em Inglês | MEDLINE | ID: mdl-35442671

RESUMO

The hexadehydro-Diels-Alder (HDDA) reaction converts a 1,3-diyne bearing a tethered alkyne (the diynophile) into bicyclic benzyne intermediates upon thermal activation. With only a few exceptions, this unimolecular cycloisomerization requires, depending on the nature of the atoms connecting the diyne and diynophile, reaction temperatures of ca. 80-130 °C to achieve a convenient half-life (e.g., 1-10 h) for the reaction. In this report, we divulge a new variant of the HDDA process in which the tether contains a central, quaternized nitrogen atom. This construct significantly lowers the activation barrier for the HDDA cycloisomerization to the benzyne. Moreover, many of the ammonium ion-based, alkyne-containing substrates can be spontaneously assembled, cyclized to benzyne, and trapped in a single-vessel, ambient-temperature operation. DFT calculations provide insights into the origin of the enhanced rate of benzyne formation.


Assuntos
Alcinos , Compostos de Amônio , Alcinos/química , Reação de Cicloadição , Di-Inos , Temperatura
11.
Org Biomol Chem ; 20(18): 3755-3762, 2022 05 11.
Artigo em Inglês | MEDLINE | ID: mdl-35420116

RESUMO

A highly regio- and chemoselective synthesis of 1H-isoindoliums through a facile and novel cascade cyclization reaction of propargylamine-based 1,6-diynes under mild conditions has been developed. Different functional groups were compatible under the optimized reaction conditions, giving the corresponding products in up to 94% yields. Upon treatment with a base, the alkyne moiety of 1H-isoindoliums could be further transformed to allenes in excellent yields.


Assuntos
Di-Inos , Halogenação , Catálise , Ciclização , Estrutura Molecular , Pargilina/análogos & derivados , Propilaminas
12.
J Org Chem ; 87(9): 5577-5591, 2022 05 06.
Artigo em Inglês | MEDLINE | ID: mdl-35389223

RESUMO

An efficacious synthetic solution to offer functionalized bisindoles and indoles has been developed based on catalyst-controlled C-H functionalization of pyrazolidinones and 1,3-diynes with highly selective control of both chemoselectivity and regioselectivity. This straightforward pathway conquers chemo- and regioselectivity challenges concerning the use of 1,3-diynes.


Assuntos
Di-Inos , Indóis , Catálise
13.
Chem Asian J ; 17(8): e202101408, 2022 Apr 14.
Artigo em Inglês | MEDLINE | ID: mdl-35243791

RESUMO

An efficient intramolecular cyclization reaction was developed to achieve indenone derivatives. The substituted 1,5-diyenes were converted to the corresponding indenones via a gold-catalyzed organic transformation, and moderate to excellent yields of the title molecules were obtained via formation of two C=O and one C-C bonds under mild reaction conditions in one pot.


Assuntos
Di-Inos , Ouro , Catálise , Cátions , Ciclização , Di-Inos/química , Ouro/química , Estrutura Molecular
14.
J Org Chem ; 87(6): 4134-4153, 2022 03 18.
Artigo em Inglês | MEDLINE | ID: mdl-35245072

RESUMO

Air-stable, highly abundant, and cost-effective Co(III)-catalyzed redox-neutral [4 + 2]-annulation of aromatic sulfoxonium ylides with 1,3-diynes providing useful substituted 1-naphthol derivatives in a regioselective manner is described. Further, the prepared 1-naphthols having internal alkyne were converted into useful polycarbocyclic molecules and spiro-dienone derivatives in good-to-excellent yields. A possible reaction mechanism involving ortho C-H activation as a key step was proposed and supported by deuterium labeling and kinetic isotope labeling studies.


Assuntos
Cobalto , Di-Inos , Alcinos , Catálise , Naftóis
15.
Chem Soc Rev ; 51(3): 869-994, 2022 Feb 07.
Artigo em Inglês | MEDLINE | ID: mdl-35005762

RESUMO

This review highlights the hydroelementation reactions of conjugated and separated diynes, which depending on the process conditions, catalytic system, as well as the type of reagents, leads to the formation of various products: enynes, dienes, allenes, polymers, or cyclic compounds. The presence of two triple bonds in the diyne structure makes these compounds important reagents but selective product formation is often difficult owing to problems associated with maintaining appropriate reaction regio- and stereoselectivity. Herein we review this topic to gain knowledge on the reactivity of diynes and to systematise the range of information relating to their use in hydroelementation reactions. The review is divided according to the addition of the E-H (E = Mg, B, Al, Si, Ge, Sn, N, P, O, S, Se, Te) bond to the triple bond(s) in the diyne, as well as to the type of the reagent used, and the product formed. Not only are the hydroelementation reactions comprehensively discussed, but the synthetic potential of the obtained products is also presented. The majority of published research is included within this review, illustrating the potential as well as limitations of these processes, with the intent to showcase the power of these transformations and the obtained products in synthesis and materials chemistry.


Assuntos
Di-Inos , Catálise
16.
Cell Biochem Biophys ; 80(1): 229-243, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34709575

RESUMO

Acne is one of the most common dermatological skin problem caused due to inflammation of the skin, leading to unfavorable growth of Propionibacterium acnes. It is a slow growing anaerobic, gram-positive bacterium that releases chemotactic factors and leads to the complex pathogenicity of acne. There are several acne treatments/therapies available, but topical therapy is usually the first choice for mild to moderate acne, and as the severity of the acne increases, the treatment modalities fail. There are many acne treatment options available, but topical therapy is best suited for mild - to - moderate skin problems, and then as the seriousness of the acne grows, the therapeutic approaches fall short. Biosurfactants are surfactants produced from plants or animals; Saponins are plant derived non-ionic biosurfactants which have steroidal and triterpenic glycosides distributed largely in plant kingdom. Numerous studies conducted by scientists have established the antimicrobial activity of and are considered more advantageous over synthetic precursors as they are eco-friendly, cheap and non-toxic. The present study was undertaken to investigate the antibacterial activity of saponins (bio-surfactants) characterized using mass spectroscopy against acne-causing bacteria. The discharge of cellular components including protein and UV-sensitive materials in the cell-free supernatant was provoked by saponin, confirming the cellular and membrane disturbances.. Furthermore, various morphological changes on the bacterial cell surface structure by Transmission electron microscopy and scanning electron microscopy revealed the disruption of the cell integrity leading to death. Results confirmed presence of non-ionic surfactants primarily affecting the disruption and destruction to the bacteria which indicates that saponins are efficient components with great potential applications in various pharmaceutical preparations. Effects of Prednisolone derivative and Panaxydol: Biosurfactants on cell wall integrity of Acne-Causing Resistant Bacteria.


Assuntos
Acne Vulgar , Prednisolona , Acne Vulgar/tratamento farmacológico , Animais , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Parede Celular , Di-Inos , Álcoois Graxos , Prednisolona/farmacologia , Prednisolona/uso terapêutico , Propionibacterium acnes
17.
Chem Commun (Camb) ; 58(27): 4376-4379, 2022 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-35297437

RESUMO

A novel metal-free nitrative bicyclization of 1,7-diynes with tBuONO in the presence of H2O is reported, producing three types of skeletally diverse tricyclic pyrroles, namely pyrrolo[3,4-c]quinolines, chromeno[3,4-c]pyrroles and benzo[e]isoindoles, with moderate to good yields by simply tuning the linkers of the 1,7-diynes. This domino protocol demonstrates remarkable compatibility regarding 1,7-diynes with different linkers, such as nitrogen and oxygen atoms and a hydroxymethyl group, and tBuONO plays dual roles as a nitro precursor as well as a nitrogen atom source.


Assuntos
Di-Inos , Quinolinas , Catálise , Pirróis
18.
Am J Chin Med ; 50(1): 295-311, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-34931585

RESUMO

Human oral squamous cell carcinomas (OSCCs) have high cancer mortality and a 5-year survival rate lower than that of most other carcinomas. New therapeutic strategies are required for the treatment and prevention against OSCCs. An approach to cancer therapy using plant-derived natural compounds has been actively in progress as a trend. Falcarindiol (FALC), or its isolated form Ostericum koreanum Kitagawa (O. koreanum), is present in many food and dietary plants, especially in carrots, and this compound has a variety of beneficial effects. However, biological activity of FALC has not been reported in OSCCs yet. This study aimed to demonstrate the antitumor effects of FALC against OSCCs, YD-10B cells. In this study, FALC was selected as a result of screening for compounds isolated from various natural products in YD-10B cells. FALC suppressed cell growth, and FALC-induced apoptotic cell death was mainly accompanied by the dephosphorylation of PI3K, AKT, mTOR, and p70S6K. The apoptotic cell death was also associated with autophagy as evidenced by the expression of Beclin-1, the conversion of LC3-II, and the formation of autophagosome. FALC-induced autophagy was accompanied by MAPKs including ERK1/2 and p38. Furthermore, FALC caused the antimetastatic effects by inhibiting the migration and invasion of YD-10B cells. Taken together, the findings suggest the potential value of FALC as a novel candidate for therapeutic strategy against OSCCs.


Assuntos
Morte Celular Autofágica , Neoplasias Bucais , Carcinoma de Células Escamosas de Cabeça e Pescoço , Apoptose , Autofagia , Linhagem Celular Tumoral , Proliferação de Células , Di-Inos , Álcoois Graxos , Humanos , Neoplasias Bucais/tratamento farmacológico , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Proteínas Quinases S6 Ribossômicas 70-kDa , Serina-Treonina Quinases TOR/metabolismo
19.
J Appl Biomed ; 19(2): 113-124, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34754259

RESUMO

Oplopanax elatus (Nakai) Nakai has a long history of use as an ethnomedicine by the people living in eastern Asia. However, its bioactive constituents and cancer chemopreventive mechanisms are largely unknown. The aim of this study was to prepare O. elatus extracts, fractions, and single compounds and to investigate the herb's antiproliferative effects on colon cancer cells and the involved mechanisms of action. Two polyyne compounds were isolated from O. elatus, falcarindiol and oplopandiol. Based on our HPLC analysis, falcarindiol and oplopandiol are major constituents in the dichloromethane (CH2Cl2) fraction. For the HCT-116 cell line, the dichloromethane fraction showed significant effects. Furthermore, the IC50 for falcarindiol and oplopandiol was 1.7 µM and 15.5 µM, respectively. In the mechanistic study, after treatment with 5 µg/ml for 48 h, dichloromethane fraction induced cancer cell apoptosis by 36.5% (p < 0.01% vs. control of 3.9%). Under the same treatment condition, dichloromethane fraction caused cell cycle arrest at the G2/M phase by 32.6% (p < 0.01% vs. control of 23.4%), supported by upregulation of key cell cycle regulator cyclin A to 21.6% (p < 0.01% vs. control of 8.6%). Similar trends were observed by using cell line HT-29. Data from this study filled the gap between phytochemical components and the cancer chemoprevention of O. elatus. The dichloromethane fraction is a bioactive fraction, and falcarindiol is identified as an active constituent. The mechanisms involved in cancer chemoprevention by O. elatus were apoptosis induction and G2/M cell cycle arrest mediated by a key cell cycle regulator cyclin A.


Assuntos
Neoplasias do Colo , Oplopanax , Apoptose , Pontos de Checagem do Ciclo Celular , Quimioprevenção , Ciclina A/farmacologia , Ciclinas/farmacologia , Di-Inos , Álcoois Graxos , Humanos , Cloreto de Metileno/farmacologia , Oplopanax/química , Regulação para Cima
20.
Int Immunopharmacol ; 101(Pt A): 108321, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34741869

RESUMO

BACKGROUND AND PURPOSE: Panaxynol (PAL, PubChem CID: 5281149) is a common natural minor component in Umbelliferae plants, such as Radix Saposhnikoviae Divaricatae. Modern pharmacology studies show that PAL has nutritional value and anti-inflammatory and other pharmaceutical activities. Therefore, the scientific hypothesis of PAL in the treatment of rheumatoid arthritis was put forward, and the hypothesis was further verified by Fibroblast-like synovial cells (RA-FLS) and Collagen Induced Arthritis (CIA) rats models. EXPERIMENTAL METHOD: CIA method was used to establish a rat arthritis model. After extracting RA-FLS, flow cytometry and immunofluorescence were used to explore the effect of PAL on the apoptosis and proliferation of RA-FLS. Wound healing and transwell experiment explored the effect of PAL on the migration and invasion of RA-FLS. Western blot analysis explored the inner mechanism of the effect of PAL on RA-FLS. At the same time, it also explored the role of PAL in CIA rats, including pathological section detection and western blot analysis. MAIN RESULTS: PAL can promote the apoptosis and inhibit the proliferation, migration and invasion of RA-FLS. PAL can also reduce joint swelling in CIA rats, reduce pannus formation and inflammatory infiltration in the joints. Western blot analysis showed that PAL mainly played a role through the TLR4/NF-κB signaling pathway. CONCLUSION: The results of in vivo and in vitro experiments show that PAL can effectively alleviate the condition of RA, and may be a potential drug for the treatment of RA.


Assuntos
Antirreumáticos/uso terapêutico , Apoptose/efeitos dos fármacos , Artrite Reumatoide/tratamento farmacológico , Proliferação de Células/efeitos dos fármacos , Di-Inos/uso terapêutico , Álcoois Graxos/uso terapêutico , NF-kappa B/metabolismo , Transdução de Sinais/efeitos dos fármacos , Membrana Sinovial/citologia , Receptor 4 Toll-Like/metabolismo , Animais , Western Blotting , Movimento Celular/efeitos dos fármacos , Feminino , Ratos , Ratos Wistar , Membrana Sinovial/efeitos dos fármacos , Membrana Sinovial/metabolismo
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