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1.
BMC Plant Biol ; 24(1): 401, 2024 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-38745126

RESUMO

BACKGROUND: Medicinal plants, such as Ajuga chamaecistus Ging. ex Benth. are a natural and available source of treatment for a wide range of diseases. The objective of the present study was to assess the morphological and biochemical variation of 70 accessions of this species collected from seven geographical areas of Markazi province in the center of Iran. RESULTS: The measured traits exhibited considerable variability across the populations. Positive correlations were observed between antioxidant activity and total phenolic content, as well as total flavonoid content. Principal component analysis showed six components explaining 72.15% of the total variance, and the PC1 explained 20.68% of the total variance. The Ward dendrogram based on morphological variables identified two main clusters. Morphological analysis of A. chamaecistus showed a high variation between qualitative and quantitative traits that help the breeders for selecting the desired genotypes. The accessions collected from the Robat-Mil area showed the highest values for the recorded morphological characteristics. Also, the populations of Robat-Mil, Hassanabad, and Khaneh-Miran were characterized by high values of total phenolic content, total flavonoid content, and antioxidant activity, which can be used in various industries, including pharmaceuticals, cosmetics, and food. CONCLUSIONS: Overall, the present results showed that the best place for the growth of A. chamaecistus with the production of significant contents of phenol and flavonoid is in Robat-Mil area.


Assuntos
Ajuga , Antioxidantes , Flavonoides , Irã (Geográfico) , Flavonoides/metabolismo , Antioxidantes/metabolismo , Ajuga/química , Ecossistema , Fenóis/metabolismo , Plantas Medicinais/anatomia & histologia
2.
Microsc Res Tech ; 87(8): 1984-1996, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38619301

RESUMO

In this study, gold nanoparticles (AuNPs) were bioreduced from Ajuga bracteosa, a medicinal herb known for its therapeutic properties against various diseases. Different fractions of the plant extract were used, including the methanolic fraction (ABMF), the n-hexane fraction (ABHF), the chloroform fraction (ABCF), and the aqueous extract for AuNPs synthesis. The characterization of AuNPs was performed using UV-Vis spectrophotometry, FT-IR, XRD, EDX, and TEM. UV-Vis spectroscopy confirmed the formation of AuNPs, with peaks observed at 555 nm. FT-IR analysis indicated strong capping of phytochemicals on the surface of AuNPs, which was supported by higher total phenolic contents (TPC) and total flavonoid contents (TFC) in AuNPs. XRD results showed high crystallinity and a smaller size distribution of AuNPs. TEM analysis revealed the spherical shape of AuNPs, with an average size of 29 ± 10 nm. The biologically synthesized AuNPs exhibited superior antibacterial, antioxidant, and cytotoxic activities compared to the plant extract fractions. The presence of active biomolecules in A. bracteosa, such as neoclerodan flavonol glycosides, diterpenoids, phytoecdysone, and iridoid glycosides, contributed to the enhanced biological activities of AuNPs. Overall, this research highlights the potential of A. bracteosa-derived AuNPs for various biomedical applications due to their remarkable therapeutic properties and effective capping by phytochemicals. RESEARCH HIGHLIGHTS: This research underscores the growing significance of herbal medicine in contemporary healthcare by exploring the therapeutic potential of Ajuga bracteosa and gold nanoparticles (AuNPs). The study highlights the notable efficacy of A. bracteosa leaf extracts and AuNPs in treating bacterial infections, demonstrating their bactericidal effects on a range of strains. The anti-inflammatory properties of plant extracts and nanoparticles are evidenced through paw edema method suggesting their applicability in managing inflammatory conditions. These findings position A. bracteosa and AuNPs as potential candidates for alternative and effective approaches to modern medication.


Assuntos
Ajuga , Antibacterianos , Antioxidantes , Ouro , Nanopartículas Metálicas , Extratos Vegetais , Ouro/química , Ouro/farmacologia , Nanopartículas Metálicas/química , Ajuga/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Antibacterianos/farmacologia , Antibacterianos/química , Antioxidantes/farmacologia , Antioxidantes/química , Espectroscopia de Infravermelho com Transformada de Fourier , Microscopia Eletrônica de Transmissão , Animais , Humanos , Flavonoides/química , Tamanho da Partícula
3.
Drug Dev Ind Pharm ; 50(4): 354-362, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38456836

RESUMO

OBJECTIVE: To develop a sensitive and fast detection method via ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) to assess the concentration of ajuforrestin A, ajuforrestin B, ajugamacrin and 8-O-Acetylharpagide primarily derived from Ajuga plants in mice blood and their pharmacokinetics. METHODS: Single protein precipitation with high-proportioned acetonitrile is chosen for sample clean-up. The UPLC HSS T3 (2.1 mm × 100 mm, 1.8 µm) column with a mobile phase in gradient elution mode at the flow rate of 0.4 mL/min was used for sample separation. Acetonitrile was selected as the organic phase solution and water containing 0.1% formic acid was chosen as the aqueous solution. A tandem mass spectrometer containing an electrospray ionization (ESI) source in the positive ionization mode was used to detect four compounds via multiple reaction monitoring (MRM). RESULTS: The calibration curves (5-1000 ng/mL) of four compounds were linear with correlation coefficients > 0.997. The matrix effects, accuracy, precision, and recovery were all within permissible scope. CONCLUSIONS: In this approach, the corresponding pharmacokinetic parameters were successfully clarified in mouse for the first time, which provided a theoretical basis for the improvement of the standard of Ajuga plants and the safety of clinical medication. Furthermore, this method may provide the UPLC-MS/MS evidence for the differentiation of the main close relative varieties of genus Ajuga according to these plants contain different mixtures of the four marker compounds.


Assuntos
Ajuga , Piranos , Espectrometria de Massas em Tandem , Camundongos , Animais , Espectrometria de Massas em Tandem/métodos , Cromatografia Líquida/métodos , Extratos Vegetais/química , Cromatografia Líquida de Alta Pressão/métodos , Ajuga/metabolismo , Espectrometria de Massa com Cromatografia Líquida , Acetonitrilas
4.
Chem Biodivers ; 21(4): e202400244, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38426640

RESUMO

Five new compounds (1, 2, 7, 12, and 16), along with fifteen known ones, were isolated from Ajuga lupulina Maxim. Their structures were revealed by analysing spectroscopic data (MS, NMR), and experimental and calculated ECD spectra was used to deduce the absolute configuration. Compound 16, with eight carbon atoms, was firstly isolated from the nature. All the isolates were evaluated for their inhibitory effect on RSL3-induced ferroptosis in HT22 mouse hippocampal neuronal cells. Among them, the abietane-type diterpenoids (7-11) significantly inhibited ferroptosis with EC50 values of 0.83 µM, 2.05 µM, 0.96 µM, 1.47 µM, and 1.19 µM, respectively.


Assuntos
Ajuga , Ferroptose , Animais , Camundongos , Estrutura Molecular , Ajuga/química , Abietanos/química , Espectroscopia de Ressonância Magnética
5.
Fitoterapia ; 172: 105742, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-37952764

RESUMO

Ten compounds (1-10) including one new neoclerodane diterpenoid (1) and nine known compounds were isolated from the whole plants of Ajuga nipponensis. Their structures were established by performing detailed analysis of NMR, the structure of 1 was determined using HRESIMS, 1D and 2D NMR, UV, and IR. Compounds 1 and 4-10 were isolated from Ajuga nipponensis for the first time. And it was the first time to report compounds 9 and 10 as natural products. Based on network pharmacology methods, 45 key targets were selected, which were compounds mapping to diseases. And compounds 2, 3, 7, and a (ajugacumbin B) exhibited excellent AKR1B10 inhibitory activities, with IC50 values of 53.05 ± 0.75, 87.22 ± 0.85, 61.85 ± 0.66, and 85.19±1.02 nM respectively, with Epalrestat used as the positive control (82.09 ± 1.62 nM). Additionally, the interaction between active compounds and AKR1B10 had been discussed according to the molecular docking results. Ultimately, the analysis of GO and KEGG enrichment indicated that the key signaling pathway of the active compounds may be related to prostate cancer. Our study results demonstrate the hypoglycemic and anti-tumor properties of A. nipponensis for the first time, and provide a comprehensive understanding of its application in traditional medicine. Furthermore, this article establishes a reference for further research on the optimized experimental design of novel AKR1B10 inhibitors.


Assuntos
Ajuga , Ajuga/química , Simulação de Acoplamento Molecular , Estrutura Molecular , Extratos Vegetais/química , Medicina Tradicional
6.
Microsc Res Tech ; 87(3): 434-445, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-37909218

RESUMO

The genus Ajuga is widely distributed in temperate to subtropical regions, and four species are currently recognized in Korea (A. decumbens, A. multiflora, A. nipponensis, and A. spectabilis), but epidermal anatomical differences across these species have never been described. A comparative study of the leaf micromorphological characteristics of Korean Ajuga species was performed using light microscopy (LM) and scanning electron microscopy (SEM) to elucidate their taxonomic usefulness and to assess leaf micromorphological diversity. Considerable diversity in epidermal and stomatal anatomy was observed across Korean Ajuga species. Species had both hypostomatic or amphistomatic leaves, with anomocytic, anisocytic, diactyic, or actinocytic stomatal complexes. Guard cell length across species ranged from 17.66 ± 0.57 µm to 32.50 ± 2.38 µm and correlated with genome size. Abnormal stomata were frequently observed in three species (A. decumbens, A. multiflora, and A. nipponensis) but not in A. spectabilis. Three types of glandular trichomes were found: peltate in all species, short-stalked in all species, and long-stalked glandular trichomes in A. multiflora. Among the investigated leaf micromophological characters, trichome type, epidermal cell shape, and stomatal morphology were all taxonomically informative traits at a species level. RESEARCH HIGHLIGHTS: A comprehensive micromorphological description of the leaf surface is provided for Korean Ajuga species using scanning electron microscopic (SEM) and light microscopic (LM) analyses. The diverse range of stomatal development and the occurrence of polymorphic stomatal types are documented for the first time in Korean Ajuga species. The great diversity in stomatal and trichome morphology in Korean Ajuga species are taxonomically useful traits for species identification.


Assuntos
Ajuga , Estômatos de Plantas , Estômatos de Plantas/ultraestrutura , Epiderme Vegetal/ultraestrutura , Folhas de Planta/anatomia & histologia , Tricomas/ultraestrutura , Microscopia Eletrônica de Varredura , Células Epidérmicas , Epiderme , República da Coreia
7.
PLoS One ; 18(8): e0282485, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37549158

RESUMO

The current study is designed to synthesize gold nanoparticles using Ajuga bracteosa extract, which is a highly known medicinal herb found in the northern Himalayas. The synthesized gold nanoparticles were initially characterized by UV-Vis spectrophotometer, SEM, FTIR, pXRD, and, GC-MS. Antibacterial efficacy of A. bracteosa extract, AuNps, and AuNps-free supernatant activity was checked against highly pathogenic clinical isolates of Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa via agar well diffusion method, assuming that supernatant might have active compounds. The Nps-free supernatant showed the maximum antibacterial activity against E. coli (20.8±0.3 mm), Staphylococcus aureus (16.5±0.5), and Pseudomonas aeruginosa (13±0.6). While green synthesized AuNps showed effective antibacterial activity (Escherichia coli (16.4±0.3mm), Staphylococcus aureus (15.05±0.5mm), and Pseudomonas aeruginosa (11.07±0.6mm)) which was high compared to A. bracteosa extract. Anticancer activity was assessed by MTT assay on U87 and HEK293 cell lines. Aj-AuNps have an antigrowth effect on both the cell lines however Aj-AuNps-free supernatant which was also evaluated along with the Aj-AuNps, showed high toxicity toward HEK293 cell line compared to U87. Further, the GC-MS analysis of supernatant showed the presence of resultant toxic compounds after the reduction of gold salt, which include Trichloromethane, Propanoic acid, 2-methyl-, methyl ester, Methyl isovalerate, Pentanoic acid, 2-hydroxy-4-methyl-, Benzene-propanoic acid, and alpha-hydroxy. Based on the observation small molecular weight ligands of Ajuga bracteosa were analyzed in-silico for their binding efficacy towards selected membrane proteins of our target pathogens. RMSD is also calculated for the best docked protein ligand pose. The results revealed that among all listed ligands, Ergosterol and Decacetylajugrin IV have high virtuous binding affinities towards the membrane proteins of targeted pathogens. The current findings revealed that the Aj-AuNps are good antibacterial as well as anticancerous agents while the Nps-free supernatant is also exceedingly effective against resistant pathogens and cancer cell lines.


Assuntos
Ajuga , Nanopartículas Metálicas , Humanos , Ajuga/química , Propionatos , Ouro/química , Escherichia coli , Ligantes , Células HEK293 , Nanopartículas Metálicas/química , Antibacterianos/farmacologia , Antibacterianos/química , Staphylococcus aureus , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Testes de Sensibilidade Microbiana , Química Verde/métodos
8.
J Nat Prod ; 86(8): 2006-2021, 2023 08 25.
Artigo em Inglês | MEDLINE | ID: mdl-37566645

RESUMO

Twelve new neo-clerodane diterpenoids, eight undescribed methoxy/ethoxy acetal analogues, and one new nor-iridane monoterpenoid were isolated from Ajuga campylantha. Their structures were elucidated using a combination of spectroscopic data, quantum chemical calculations, and X-ray crystallography. This research reveals the distinctive structural features of A. campylantha diterpenes, including distinct C rings and 4,18-double bonds, distinguishing them from diterpenes of other plants in the Ajuga genus. Compound 2 represents the first example of a 19(5→6)-abeo-clerodane formed through a Wagner-Meerwein rearrangement. The isolated compounds were assessed for their neuroprotective effects against RSL3-induced ferroptosis in HT22 cells and LPS-induced neuroinflammation in BV-2 cells. Notably, compound 7 inhibits ferroptosis (EC50 = 10 µM) with a potentially new mechanism of action. The preliminary structure-activity relationship studies revealed that the furan-clerodane diterpenoids possess potential ferroptosis inhibitory activity, while the lactone-clerodanes do not. This study represents the first report of furan-containing clerodanes within the Ajuga genus, providing fresh insights into the phytochemistry and pharmacological potential of A. campylantha.


Assuntos
Ajuga , Diterpenos Clerodânicos , Ferroptose , Fármacos Neuroprotetores , Diterpenos Clerodânicos/farmacologia , Diterpenos Clerodânicos/química , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/química , Ajuga/química , Doenças Neuroinflamatórias , Estrutura Molecular
9.
Molecules ; 28(8)2023 Apr 12.
Artigo em Inglês | MEDLINE | ID: mdl-37110639

RESUMO

Iron oxide nanoparticles (NPs) have attracted substantial interest due to their superparamagnetic features, biocompatibility, and nontoxicity. The latest progress in the biological production of Fe3O4 NPs by green methods has improved their quality and biological applications significantly. In this study, the fabrication of iron oxide NPs from Spirogyra hyalina and Ajuga bracteosa was conducted via an easy, environmentally friendly, and cost-effective process. The fabricated Fe3O4 NPs were characterized using various analytical methods to study their unique properties. UV-Vis absorption peaks were observed in algal and plant-based Fe3O4 NPs at 289 nm and 306 nm, respectively. Fourier transform infrared (FTIR) spectroscopy analyzed diverse bioactive phytochemicals present in algal and plant extracts that functioned as stabilizing and capping agents in the fabrication of algal and plant-based Fe3O4 NPs. X-ray diffraction of NPs revealed the crystalline nature of both biofabricated Fe3O4 NPs and their small size. Scanning electron microscopy (SEM) revealed that algae and plant-based Fe3O4 NPs are spherical and rod-shaped, averaging 52 nm and 75 nm in size. Energy dispersive X-ray spectroscopy showed that the green-synthesized Fe3O4 NPs require a high mass percentage of iron and oxygen to ensure their synthesis. The fabricated plant-based Fe3O4 NPs exhibited stronger antioxidant properties than algal-based Fe3O4 NPs. The algal-based NPs showed efficient antibacterial potential against E. coli, while the plant-based Fe3O4 NPs displayed a higher zone of inhibition against S. aureus. Moreover, plant-based Fe3O4 NPs exhibited superior scavenging and antibacterial potential compared to the algal-based Fe3O4 NPs. This might be due to the greater number of phytochemicals in plants that surround the NPs during their green fabrication. Hence, the capping of bioactive agents over iron oxide NPs improves antibacterial applications.


Assuntos
Ajuga , Nanopartículas Metálicas , Spirogyra , Nanopartículas Metálicas/química , Escherichia coli , Staphylococcus aureus , Antibacterianos/farmacologia , Antibacterianos/química , Espectroscopia de Infravermelho com Transformada de Fourier , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Difração de Raios X , Testes de Sensibilidade Microbiana
10.
Nutrients ; 15(5)2023 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-36904246

RESUMO

The genus Ajuga (Lamiaceae) is rich in medicinally important species with biological activities ranging from anti-inflammatory, antitumor, neuroprotective, and antidiabetic to antibacterial, antiviral, cytotoxic, and insecticidal effects. Every species contains a unique and complex mixture of bioactive metabolites-phytoecdysteroids (PEs), iridoid glycosides, withanolides, neo-clerodane terpenoids, flavonoids, phenolics, and other chemicals with high therapeutic potential. Phytoecdysteroids, the main compounds of interest, are natural anabolic and adaptogenic agents that are widely used as components of dietary supplements. Wild plants remain the main source of Ajuga bioactive metabolites, particularly PEs, which leads to frequent overexploitation of their natural resources. Cell culture biotechnologies offer a sustainable approach to the production of vegetative biomass and individual phytochemicals specific for Ajuga genus. Cell cultures developed from eight Ajuga taxa were capable of producing PEs, a variety of phenolics and flavonoids, anthocyanins, volatile compounds, phenyletanoid glycosides, iridoids, and fatty acids, and demonstrated antioxidant, antimicrobial, and anti-inflammatory activities. The most abundant PEs in the cell cultures was 20-hydroxyecdysone, followed by turkesterone and cyasterone. The PE content in the cell cultures was comparable or higher than in wild or greenhouse plants, in vitro-grown shoots, and root cultures. Elicitation with methyl jasmonate (50-125 µM) or mevalonate and induced mutagenesis were the most effective strategies that stimulated cell culture biosynthetic capacity. This review summarizes the current progress in cell culture application for the production of pharmacologically important Ajuga metabolites, discusses various approaches to improve the compound yield, and highlights the potential directions for future interventions.


Assuntos
Ajuga , Ajuga/química , Antocianinas , Flavonoides , Fenóis , Glicosídeos Iridoides , Anti-Inflamatórios , Técnicas de Cultura de Células
11.
Molecules ; 28(3)2023 Jan 22.
Artigo em Inglês | MEDLINE | ID: mdl-36770779

RESUMO

Shigellosis is one of the major causes of death in children worldwide. Flavonoids and phenolic acids are expected to demonstrate anti-shigellosis activity and anti-diarrheal properties. The aerial part of A. integrifolia is commonly used against diarrhea. This study aimed to identify flavonoids and phenolic acids responsible for this therapeutic purpose. Antioxidant activity, total phenol content, and total flavonoid content were determined. The antibacterial activity of the aerial part against Shigella spp. was also tested using the agar well diffusion method. HPLC analysis was performed using UHPLC-DAD for different extracts of the aerial part. Autodock Vina in the PyRx platform was used to screen responsible components. Ciprofloxacin was used as a reference drug. An enzyme taking part in pyrimidine biosynthesis was used as a target protein. Molecular docking results were visualized using Discovery Studio and LigPlot1.4.5 software. Antioxidant activity, total phenol content, and total flavonoid content are more significant for the aerial part of A. integrifolia. From HPLC analysis, the presence of the flavonoids, quercetin, myricetin, and rutin and the phenolic acids gallic acid, chlorogenic acid, and syringic acid were identified from the aerial part of A. integrifolia. Regarding the antibacterial activity, the aerial part shows considerable activity against Shigella spp. Binding energies, RMSD and Ki values, interaction type, and distance are considered to identify the components most likely responsible for the therapeutic effects and observed activity. Antioxidant activity, total phenol content, and total flavonoid content of the aerial part are in line with anti-shigellosis activity. The top five components that are most likely potentially responsible for therapeutic purposes and anti-shigellosis activity are chlorogenic acid, rutin, dihydroquercetin, dihydromyricetin, and kaempferol.


Assuntos
Ajuga , Antioxidantes , Criança , Humanos , Antioxidantes/farmacologia , Antioxidantes/química , Ajuga/química , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Flavonoides/farmacologia , Flavonoides/análise , Fenóis/análise , Fenol , Componentes Aéreos da Planta/química , Rutina/farmacologia , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico
12.
Fitoterapia ; 166: 105461, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-36804655

RESUMO

Six new neoclerodane diterpenoids (1-6), along with ten known compounds (7-16), were isolated from Ajuga forrestii. Their structures were elucidated by HRESIMS, 1D and 2D NMR, ECD calculation, and single-crystal X-ray diffraction analysis. The structure of a known neoclerodane diterpene ajudecunoid C (6) was revised based on the reported NMR empirical rules. All the isolates were evaluated for their inhibitory effect on RSL3-induced ferroptosis in HT22 mouse hippocampal neuronal cells. Among them, compounds 8, 9, and 12 significantly inhibited RSL3-induced ferroptosis with EC50 values of 0.45 µM, 0.076 µM, and 0.14 µM.


Assuntos
Ajuga , Camundongos , Animais , Ajuga/química , Estrutura Molecular , Espectroscopia de Ressonância Magnética , Linhagem Celular Tumoral , Cristalografia por Raios X
13.
Anticancer Agents Med Chem ; 23(2): 237-244, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-35726426

RESUMO

AIMS: The aim of this study is to find the anticancer lead compounds or drug candidates from Chinese Traditional Plant Medicine of Ajuga decumbens Thunb. BACKGROUND: Ajuga decumbens Thunb. has been used in clinical for a long time in China and was selected in "Chinses Pharmacopoeia" (part I in 1977) for its wide spectrum biological activities: such as anticancer, antioxidant, antifeedant, antibacterial, anti-inflammatory, antihyperlipidemic, anti-cholinesterase and cytotoxicity activities. However, there are relatively fewer studies of Ajuga decumbens Thunb. that have been carried out till now. For some years, our research group focused on the discovery of new anticancer agents, so we studied the chemical compositions of Ajuga decumbens Thunb., planted in Pingtan island of Fujian Province, to discover new anticancer lead compounds or candidates from this Chinese Traditional Plant Medicine. METHODS: The dichloromethane (DCM) extract was obtained in this work, and then this extract was used for silica gel column chromatography to obtain different polar fractions. Several similar fractions were combined according to TLC or HPLC analysis. The combined fractions were isolated by preparative TLC or preparative HPLC to obtain the pure compounds and HPLC was used to detect the purity. All isolated compounds were determined by NMR (1HNMR, 13CNMR, DEPT, HMBC, HSQC, 1H-1H COSY and NOESY), HRESIMS and single crystal X-ray diffraction methods. The in vitro anticancer activity was evaluated using CCK8 method. RESULTS: Seven compounds [three new compounds 1-3; and four known compounds (Ajugacumbins A, Ajugacumbin B, Ajugamarin A2 and Ajugamarin A1)] were isolated from Ajuga decumbens Thunb. in this work, and their structures were confirmed. The biological evaluation showed that 3 and Ajugamarin A1 exhibited potent in vitro anticancer activity both against A549 cell lines with IC50s=71.4 µM and 76.7 µM; and against Hela cell lines with IC50s=71.6 mM and 5.39×10-7 µM, respectively. CONCLUSION: Compounds (3 and Ajugamarin A1) can be regarded as the lead compounds for the development of anticancer agents.


Assuntos
Ajuga , Diterpenos Clerodânicos , Humanos , Diterpenos Clerodânicos/química , Ajuga/química , Células HeLa , Estrutura Molecular , Extratos Vegetais/química
14.
Nat Prod Res ; 37(12): 1978-1985, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-36000191

RESUMO

Ajuga multiflora Bunge is a perennial ornamental herb and has been used for the treatment of fever in Korean folk medicine. In the course of searching for protective agents associated with the potential of A. multiflora against dexamethsone (DEX)-induced muscle atrophy, a new phytoecdysteroid, 29-hydroxyprecyasterone (1), together with four known compounds (2-5), were isolated from A. multiflora. The structures of the compounds were determined by spectroscopic analyses, including 1D-, 2D-NMR and HR-MS interpretation. To elucidate the effects of obtained compounds on DEX-induced muscle atrophy, the myotubes diameter, myosin heavy chain (MyHC) positive area, and fusion index were evaluated by immunofluorescence staining. Overall, each compound treatment effectively prevented the atrophic myotubes through an increase of MyHC-positive myotubes and the number of nuclei. Particularly, the measurement of myotube diameter showed that compounds 1 and 5 treatment significantly alleviated the myotube thickness.


Assuntos
Ajuga , Dexametasona , Dexametasona/farmacologia , Atrofia Muscular/induzido quimicamente , Atrofia Muscular/tratamento farmacológico , Atrofia Muscular/patologia , Fibras Musculares Esqueléticas
15.
Braz. j. biol ; 83: 1-11, 2023. graf, ilus, tab
Artigo em Inglês | LILACS, VETINDEX | ID: biblio-1468840

RESUMO

Oral diseases caused by various microorganisms are common around the world. Scientific research has now been focusing on novel medicines to overcome bacterial resistance and antibiotics side effects; therefore, the current study was designed to assess the efficacy of certain antibiotics, toothpaste, and medicinal plant extracts (Ajuga bracteosa and Curcuma longa) versus the bacterial pathogens isolated from the human oral cavity. A total of 130 samples were collected from Khyber Teaching Hospital Peshawar, Pakistan, among those 27 species isolated, and eight bacterial species were identified from the samples. Among all the bacterial species, Staphylococcus aureus (29.62%) and Proteus mirabilis (22.2%) were found to be more prevalent oral pathogens. In comparison, the least pervasive microbes were Proteus vulgaris, Shigella sonnei, Escherichia coli and Aeromonas hydrophila. The study also suggested that dental problems were more prevalent in males (41-50 years of age) than females. Among the eight antibiotics used in the study, the most promising results were shown by Foxicillin against A. hydrophila. The survey of TP1 revealed that it showed more potent antagonist activity against Proteus vulgaris as compared TP2 and TP3 that might be due to the high content of fluoride. The Curcuma longa showed more significant activity than Ajuga bracteosa (Stem, leaves and root) extracts. The data obtained through this study revealed that antibiotics were more effective for oral bacterial pathogens than toothpaste and plant extracts which showed moderate and low activity, respectively. Therefore, it is suggested that the active compounds in individual medicinal plants like Curcuma longa and Ajuga bracteosa could replace the antibiotics when used in daily routine as tooth cleansers or mouth rinses.


As doenças bucais causadas por vários microrganismos são comuns em todo o mundo. A pesquisa científica agora tem se concentrado em novos medicamentos para superar a resistência bacteriana e os efeitos colaterais dos antibióticos; portanto, o presente estudo foi desenhado para avaliar a eficácia de certos antibióticos, pasta de dente e extratos de plantas medicinais (Ajuga bracteosa e Curcuma longa) contra os patógenos bacterianos isolados da cavidade oral humana. No total, 130 amostras foram coletadas do Khyber Teaching Hospital Peshawar, Paquistão, entre essas, 27 espécies foram isoladas e oito espécies bacterianas foram identificadas a partir das amostras. Entre todas as espécies bacterianas, Staphylococcus aureus (29.62%) e Proteus mirabilis (22.2%) foram os patógenos orais mais prevalentes. Em comparação, os micróbios menos difundidos foram Proteus vulgaris, Shigella sonnei, Escherichia coli e Aeromonas hydrophila. O estudo também sugeriu que os problemas dentários eram mais prevalentes em homens (41-50 anos de idade) do que em mulheres. Entre os oito antibióticos usados no estudo, os resultados mais promissores foram mostrados pelo Foxicillin contra A. hydrophila. A pesquisa de TP1 revelou que ele mostrou atividade antagonista mais potente contra Proteus vulgaris em comparação a TP2 e TP3, o que pode ser devido ao alto teor de flúor. A Curcuma longa apresentou atividade mais significativa em relação aos extratos de Ajuga bracteosa (caule, folhas e raiz). Os dados obtidos neste estudo revelaram que os antibióticos foram mais eficazes para os patógenos bacterianos orais do que os dentifrícios e os extratos vegetais que apresentaram atividade moderada e baixa, respectivamente. Portanto, sugere-se que os compostos ativos em plantas medicinais individuais como Curcuma longa e Ajuga bracteosa possam substituir os antibióticos quando usados na rotina diária como limpadores de dentes ou enxaguatórios bucais.


Assuntos
Masculino , Feminino , Humanos , Adulto , Ajuga , Antibacterianos/análise , Curcuma , Doenças da Gengiva/patologia , Doenças da Gengiva/tratamento farmacológico
16.
Molecules ; 27(20)2022 Oct 20.
Artigo em Inglês | MEDLINE | ID: mdl-36296695

RESUMO

The main objective of this research was to study the biological characteristics in terms of antioxidant and antimicrobial activities of Ajuga iva and determine the best analytical and extraction methods applicable to this specie and studied compounds. A short screening of its nutritional value in terms of chemical composition is also included. A. iva leaves were analyzed for crude protein (CP), cell wall [neutral detergent fiber (NDF), acid detergent fiber (ADF), and acid detergent lignin (ADL)], minerals, fatty acids, essential oils, and phenolic compounds. Mature aerial parts of A. iva were randomly collected during the Spring season from Mograne-Zaghouan, Tunisia. Leaves of A. iva contained 13.4 ± 0.4% CP, 26.3 ± 0.35% NDF, 20.2 ± 0.42% ADF, and 5.13 ± 0.21% ADL. Mineral content (13.0 ± 0.45%) was mainly composed of potassium (4.5% g DM) and magnesium (4.25% DM). Leaves of A. iva had linolenic (26.29 ± 0.760%) and linoleic (37.66 ± 2.35%) acids as the main components of the acid profile. Thymol was found to be the most dominant (23.43%) essential oil, followed by 4-vinylguaiacol (14.27%) and linalool (13.66%). HPLC-PDA-ESI-MS/MS analysis pointed out the presence of phytoecdysteroids. Phenolic acids and flavonoids, such as glycosylated derivatives of naringenin, eriodyctiol, and apigenin, were detected in the methanol extract of A. iva leaves. Our results underline the importance of choosing proper extraction methods and solvents to extract and characterize the described compounds profile of A. iva leaves. Results also show A. iva leaves as a potential source of functional ingredients with beneficial health-promoting properties. Overall, leaves of A. iva have low biological activities (antioxidant and antimicrobial activities) with a chemical composition suitable as a feed for ruminants in rangeland pasture. It also has low-grade antibacterial or medicinal characteristics when fed to ruminants.


Assuntos
Ajuga , Óleos Voláteis , Ajuga/química , Antioxidantes/química , Metanol/química , Lignina/análise , Apigenina/análise , Timol/análise , Magnésio/análise , Detergentes , Espectrometria de Massas em Tandem , Extratos Vegetais/química , Folhas de Planta/química , Óleos Voláteis/química , Flavonoides/química , Antibacterianos/química , Solventes/química , Potássio/análise , Ácidos Graxos Essenciais/análise
17.
Molecules ; 27(17)2022 Aug 25.
Artigo em Inglês | MEDLINE | ID: mdl-36080236

RESUMO

The Src-homology 2 domain-containing phosphatase 2 (SHP2), which is encoded by PTPN11, participates in many cellular signaling pathways and is closely related to various tumorigenesis. Inhibition of the abnormal activity of SHP2 by small molecules is an important part of cancer treatment. Here, three abietane diterpenoids, named compounds 1-3, were isolated from Ajuga ovalifolia var. calantha. Spectroscopic analysis was used to identify the exact structure of the compounds. The enzymatic kinetic experiment and the cellular thermal shift assay showed compound 2 selectively inhibited SHP2 activity in vitro. Molecular docking indicated compound 2 targeted the SHP2 catalytic domain. The predicted pharmacokinetic properties by SwissADME revealed that compound 2 passed the majority of the parameters of common drug discovery rules. Compound 2 restrained A549 proliferation (IC50 = 8.68 ± 0.96 µM), invasion and caused A549 cell apoptosis by inhibiting the SHP2-ERK/AKT signaling pathway. Finally, compound 2 (Ajuforrestin A) is a potent and efficacious SHP2 inhibitor and may be a promising compound for human lung epithelial cancer treatment.


Assuntos
Abietanos , Ajuga , Células A549 , Abietanos/química , Abietanos/farmacologia , Apoptose , Humanos , Simulação de Acoplamento Molecular
18.
J Nat Prod ; 85(7): 1808-1815, 2022 07 22.
Artigo em Inglês | MEDLINE | ID: mdl-35796002

RESUMO

Two new 3,4-epoxy group-containing abietane diterpenoids (1 and 2), together with five known diterpenoids (3-7), were isolated from Ajuga decumbens. Their structures were elucidated by spectroscopic data analysis, NMR calculations, and X-ray diffraction experiments. The structures of two known abietane diterpenoids were revised based on NMR calculations and X-ray diffraction data. Notably, compound 4 specifically inhibited RSL3-induced ferroptosis with an EC50 of 56 nM by antioxidation. Moreover, 4 significantly decreased RSL3-induced lipid and cytosolic ROS accumulation and ferroptosis marker gene PTGS2 mRNA expression. This work reports the most potent natural inhibitor against ferroptosis found so far.


Assuntos
Ajuga , Diterpenos , Ferroptose , Abietanos/química , Abietanos/farmacologia , Diterpenos/química , Diterpenos/farmacologia , Espectroscopia de Ressonância Magnética , Estrutura Molecular
19.
Steroids ; 186: 109089, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-35843360

RESUMO

Five new phytoecdysteroids (1, 2, 3, 4, and 5) were isolated from Ajuga decumbens Thunb. planted at Pingtan island of Fujian Province. Their structures were elucidated by NMR(1H NMR, 13C NMR, DEPT, HMBC, HSQC, 1H-1H COSY, ROESY), and HRESIMS. Especially, compound 2 is the epimer of Cyasterone, which was directly confirmed using single crystal X-ray diffraction analysis.


Assuntos
Ajuga , Ajuga/química , Cristalografia por Raios X , Espectroscopia de Ressonância Magnética
20.
PLoS One ; 17(6): e0270044, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35709223

RESUMO

INTRODUCTION: Panama's HIV epidemic is far from under control. One of the populations with the fastest-growing epidemic among the Indigenous peoples of the Comarca Ngäbe-Buglé (CNB). The CNB is an administratively autonomous Indigenous region in Western Panama that is home to over 200,000 individuals of Ngäbe and Buglé ethnicities. This population is unique and, in several ways, represents the early stages of the AIDS epidemics in high-income countries. The CNB is the most impoverished region in Panama and is relatively isolated from outside influences, with limited roads, electricity, and an internet connection, including medical assistance. Around 1.5% of all rapid HIV tests are positive, compared to a national prevalence of 0.9%; in CNB, diagnosis tends to be late. In CNB, 56.3% of individuals had an initial CD4 count of <350 cells/mm3. Antiretroviral treatment (ART) dropout in this region is five times higher than the national average; there is high early mortality due to opportunistic infections. Using the Social-Ecological Theory for Health as a framework, this study aims to describe the facilitators and barriers associated with ART adherence and retention in HIV care among people living with HIV (PLHIV) in the CNB. A better understanding of factors that obstruct adherence could lead to more effective HIV care and prevention in CNB. METHODS: We conducted 21 semi-structured interviews with PLHIV who reside across all three regions of the CNB and have attended an antiretroviral (ART) clinic at least once. Deductive thematic analysis was used to uncover themes related ART adherence and retention in HIV care at the individual, social and structural levels. DISCUSSION: This unique, isolated population of rural Indigenous peoples has high infection rates, late diagnosis, poor ART adherence, and high AIDS-related death rates. The CNB is an important region to examen ART adherence and retention in care. We determined that psychological health, social support, and discrimination acted as individual-level facilitators and barriers to adherence and retention. Notably, structural barriers included difficult access to ART care due to travel costs, ART shortages, and uncooperative Western/Traditional medical systems. Recommended interventions used in other Low- and Middle-Income settings include increasing peer and family-level support and community knowledge and understanding of HIV infection. Additionally, our study suggests structural interventions, including decreasing the cost and distance of traveling to the ART clinic, by decentralizing services, decreasing food scarcity, and increasing collaboration between Western and Traditional providers.


Assuntos
Síndrome da Imunodeficiência Adquirida , Ajuga , Fármacos Anti-HIV , Infecções por HIV , Síndrome da Imunodeficiência Adquirida/tratamento farmacológico , Fármacos Anti-HIV/uso terapêutico , Antirretrovirais/uso terapêutico , Infecções por HIV/tratamento farmacológico , Infecções por HIV/epidemiologia , Infecções por HIV/psicologia , Humanos , Adesão à Medicação
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