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1.
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
2.
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
3.
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
4.
Steroids ; 186: 109089, 2022 10.
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
5.
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 de Imunodeficiência Adquirida , Ajuga , Fármacos Anti-HIV , Infecções por HIV , Síndrome de 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
6.
Curr Pharm Biotechnol ; 23(3): 318-336, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-33882804

RESUMO

BACKGROUND: Ajuga bracteosa is a traditional herb used against various diseases. OBJECTIVES: Current research aimed to investigate the anti-diabetic and hepato-protective effect of green synthesized silver nanoparticles (ABAgNPs) using Ajuga bracteosa aqueous extract (ABaqu). METHODS: In vitro anti-diabetic and cytotoxic effects were carried out via α- glucosidase inhibition, brine shrimp lethality, and protein kinase inhibition assays. For in vivo screening of 200 mg/kg and 400 mg/kg of both ABAgNPs and ABaqu in alloxan-induced and CCl4-induced Swiss albino mice were used. Liver and kidney functional markers, hematology, and histopathological studies were carried out after 14 days of administration. RESULTS: In vivo antidiabetic and anti-cancerous effects showed valuable anti-hyperglycemic and hepatoprotective potential when mice were treated with ABaqu and ABAgNPs. A significant reduction in the blood glucose level was recorded when ABaqu and ABAgNPs were administrated orally compared to Glibenclamide treated group. Significant reduction in ALT, AST, ALP, urea, uric acid, and creatinine was recorded in ABaqu and ABAgNPs treated diabetic mice. The hepato-protective findings indicated that ALT, ALP, AST were elevated in CCl4-induced mice while declined in both ABAgNPs and ABaqu treated CCl4-induced mice. Histopathological examination revealed that ABAgNPs have hepato-protective activity. CONCLUSION: It was concluded that ABAgNPs and ABaqu possessed strong anti-diabetic and hepatoprotective phytoconstituents, which could be used in the prevention of diseases.


Assuntos
Ajuga , Diabetes Mellitus Experimental , Nanopartículas Metálicas , Animais , Diabetes Mellitus Experimental/tratamento farmacológico , Fígado , Camundongos , Camundongos Endogâmicos BALB C , Extratos Vegetais/farmacologia , Prata
7.
Molecules ; 26(16)2021 08 11.
Artigo em Inglês | MEDLINE | ID: mdl-34443462

RESUMO

Ajuga bracteosa Wall. ex Benth. is an endangered medicinal herb traditionally used against different ailments. The present study aimed to create new insight into the fundamental mechanisms of genetic transformation and the biological activities of this plant. We transformed the A. bracteosa plant with rol genes of Agrobacterium rhizogenes and raised the regenerants from the hairy roots. These transgenic regenerants were screened for in vitro antioxidant activities, a range of in vivo assays, elemental analysis, polyphenol content, and different phytochemicals found through HPLC. Among 18 polyphenolic standards, kaempferol was most abundant in all transgenic lines. Furthermore, transgenic line 3 (ABRL3) showed maximum phenolics and flavonoids content among all tested plant extracts. ABRL3 also demonstrated the highest total antioxidant capacity (8.16 ± 1 µg AAE/mg), total reducing power, (6.60 ± 1.17 µg AAE/mg), DPPH activity (IC50 = 59.5 ± 0.8 µg/mL), hydroxyl ion scavenging (IC50 = 122.5 ± 0.90 µg/mL), and iron-chelating power (IC50 = 154.8 ± 2 µg/mL). Moreover, transformed plant extracts produced significant analgesic, anti-inflammatory, anticoagulant, and antidepressant activities in BALB/c mice models. In conclusion, transgenic regenerants of A. bracteosa pose better antioxidant and pharmacological properties under the effect of rol genes as compared to wild-type plants.


Assuntos
Ajuga/química , Polifenóis/farmacologia , Regeneração , Analgésicos/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Anticoagulantes/farmacologia , Antidepressivos/farmacologia , Antioxidantes/análise , Bioensaio , Compostos de Bifenilo/química , Cromatografia Líquida de Alta Pressão , Elementos Químicos , Flavonoides/análise , Sequestradores de Radicais Livres/química , Hidróxidos/química , Concentração Inibidora 50 , Quelantes de Ferro/farmacologia , Masculino , Camundongos Endogâmicos BALB C , Fenóis/análise , Picratos/química , Plantas Geneticamente Modificadas , Regeneração/efeitos dos fármacos
8.
BMC Complement Med Ther ; 21(1): 198, 2021 Jul 12.
Artigo em Inglês | MEDLINE | ID: mdl-34253216

RESUMO

BACKGROUND: Degenerative kidney diseases are mostly associated with oxidative stress. Natural products are considered as the antioxidants enrich food that can restrict the progress of oxidative stress induced disorders. Therefore, the present study was aimed to evaluate the renal protective effect of Ajuga parviflora leaf extract in carbon tetrachloride intoxicated rats. METHODS: The hydromethanolic extract of A. parviflora leaves was obtained by extracting twice in 60% methanol. The principal bioactive constituents were detected by LC/MS analysis. Toxicity of plant extract was assessed using brine shrimp lethal toxicity test and acute toxicity model on healthy Sprague-Dawley male rats. Nephroprotective effects of plant extract were also evaluated on rats by inducing CCl4 renal toxicity in comparison with positive control and naïve groups. The dose of A. parviflora administered to animal was 100, 200 and 300 mg/kg. All administrations were given orally on an alternate day basis for 30 days. Urine and serum biomarkers were analyzed, along with antioxidant enzymes. Finally, the DNA damages, lipid peroxides, hydrogen peroxides and nitrites were assessed in rat's renal tissue. The histopathology alterations in renal tissues were further studied for kidney damages. RESULTS: The LC/MS analysis confirmed the presence of different important pharmacological compounds in A. parviflora methanolic leaf extract. The key bioactive compounds include pyocyanin, zonisamide, D Saccharic acid, altretamine, carbocyclic thromboxane A2, Sinapyl alcohol, and vitamin C. The important polypeptides identified include Lys-Tyr-Lys, His-His-Lys, Met-Asp-Arg, Phe-Val-Arg, and PyroGlu-Val-Arg. The LD50 of A. parviflora was found to be > 1000 µg/mL. A. parviflora administration significantly subsides CCl4 toxicity in rats, reduced the elevated level of RBCs, pus and epithelial cells. The abnormal elevated level of specific gravity, creatinine, urobilinogen, urea and albumin were also reduced to normal physiological level. The reduced urinary protein and pH were also normalized. The serum urobilinogen, urea and total bilirubin levels were also reversed to normal levels while the diminished albumin and total protein levels also came to normal. The important phase I and II enzyme levels were also reversed in A. parviflora administered rats. The H2O2, thiobarbituric acid reactive substance (TBARS) and nitrite levels were significantly decreased. Furthermore, the damaged DNA and histopathological changes in CCl4 exposed rats were also highly significantly reversed after the administration of A. parviflora. All effects were significant (P < 0.05) and highly significant (P < 0.005) at 100 and 300 mg/kg respectively. CONCLUSION: The restored urine and serum profile of various parameters to normal physiological levels suggests that the A. parviflora has potential antioxidant and repairing potential in renal disorders.


Assuntos
Injúria Renal Aguda/induzido quimicamente , Injúria Renal Aguda/tratamento farmacológico , Ajuga/metabolismo , Ajuga/toxicidade , Antioxidantes/farmacologia , Tetracloreto de Carbono/toxicidade , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Animais , Ratos , Ratos Sprague-Dawley
9.
Bioorg Chem ; 115: 105177, 2021 10.
Artigo em Inglês | MEDLINE | ID: mdl-34303035

RESUMO

Ferroptosis is a new form of cell death, and inhibition of ferroptosis is a promising strategy to treat neurological diseases. In this work, sixteen compounds were isolated from Ajuga nipponensis and assayed for anti-ferroptosis activity in HT22 mouse hippocampal neuronal cells. Ajudecunoid C (1, ADC), a new neoclerodane diterpenoid, showed significant inhibitory activity against erastin and RSL3-induced ferroptosis with EC50 values of 4.1 ± 1.0 and 3.6 ± 0.3 µM, respectively. Experimental results demonstrated that ADC effectively prevented ferroptosis through scavenging free radical and activating NRF2-antioxidant response elements (AREs) pathway. This study reveals that ADC, as a new ferroptosis inhibitor, is a promising lead compound for the development of drugs against ferroptosis-related neurological diseases.


Assuntos
Ajuga/química , Ferroptose/efeitos dos fármacos , Fator 2 Relacionado a NF-E2/metabolismo , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/farmacologia , Animais , Elementos de Resposta Antioxidante/efeitos dos fármacos , Linhagem Celular , Camundongos , Neurônios/citologia , Neurônios/efeitos dos fármacos , Neurônios/metabolismo , Fármacos Neuroprotetores/isolamento & purificação , Transdução de Sinais/efeitos dos fármacos
10.
Nutrients ; 13(4)2021 Apr 02.
Artigo em Inglês | MEDLINE | ID: mdl-33918334

RESUMO

Dry extracts from the Eurasian plants, Ajuga turkestanica, Eurycoma longifolia, and Urtica dioica have been used as anabolic supplements, despite the limited scientific data on these effects. To assess their actions on early sarcopenia signs, male and female castrated mice were supplemented with lyophilized extracts of the three plants, isolated or in association (named TLU), and submitted to resistance exercise. Ovariectomy (OVX) led to body weight increase and non-high-density cholesterol (HDL) cholesterol elevation, which had been restored by exercise plus U. dioica extract, or by exercise and TLU, respectively. Orchiectomy (ORX) caused skeletal muscle weight loss, accompanied by increased adiposity, being the latter parameter reduced by exercise plus E. longifolia or U. dioica extracts. General physical activity was improved by exercise plus herbal extracts in either OVX or ORX animals. Exercise combined with TLU improved resistance to fatigue in OVX animals, though A. turkestanica enhanced the grip strength in ORX mice. E. longifolia or TLU also reduced the ladder climbing time in ORX mice. Resistance exercise plus herbal extracts partly altered gastrocnemius fiber size frequencies in OVX or ORX mice. We provide novel data that tested ergogenic extracts, when combined with resistance exercise, improved early sarcopenia alterations in castrated male and female mice.


Assuntos
Anabolizantes/farmacologia , Suplementos Nutricionais , Magnoliopsida/química , Condicionamento Físico Animal/fisiologia , Extratos Vegetais/farmacologia , Adiposidade/efeitos dos fármacos , Ajuga/química , Animais , Modelos Animais de Doenças , Eurycoma/química , Feminino , Masculino , Camundongos , Músculo Esquelético/efeitos dos fármacos , Orquiectomia , Ovariectomia , Sarcopenia/etiologia , Sarcopenia/prevenção & controle , Urtica dioica/química
11.
Phytochemistry ; 186: 112731, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-33721797

RESUMO

The Lamiaceae plant Ajuga forrestii Diels is a traditional Chinese herbal medicine with abundant glandular trichomes (GTs), but their chemistry and biological functions remain uninvestigated. Here, a panel of six highly functionalized neo-clerodane diterpenoids was localized to the peltate GTs of A. forrestii using laser microdissection coupled with HPLC analysis, indicating that the GTs of A. forrestii are an excellent material for the elucidation of the yet unclear biosynthetic pathway of natural neo-clerodane diterpenoids. In addition, four undescribed neo-clerodane diterpenoids with an acyclic C-9 side chain including two pairs of 1:1 mixture of inseparable diastereomers, ajuforrestins D-G, were isolated from the fresh leaves of A. forrestii together with six known compounds. The structures of the undescribed compounds were elucidated by spectroscopic (including 1D and 2D NMR and HR-ESI-MS) analyses. Biological assays indicated that the major GT compound ajugacumbin B and undescribed ajuforrestins D/E showed antifeedant activity against Helicoverpa armigera, suggesting that neo-clerodanes in A. forrestii should be involved in plant defence against insects. Moreover, the abietane diterpenoid ajuforrestin B exhibited significant anti-inflammatory activity on the secretion of interleukin-2 (IL-2) and cytotoxicity against three cancer cell lines, NCI-H1975, HepG2 and MCF-7, suggesting that ajuforrestin B could positively contribute to the therapeutic effects of this traditional Chinese medicine.


Assuntos
Ajuga , Diterpenos Clerodânicos , Anti-Inflamatórios/farmacologia , Diterpenos Clerodânicos/farmacologia , Estrutura Molecular , Folhas de Planta , Tricomas
12.
J Ethnopharmacol ; 270: 113791, 2021 Apr 24.
Artigo em Inglês | MEDLINE | ID: mdl-33444718

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Ajuga iva (L.) Schreb. (Labiatae) (AI) is used in folk medicine for a variety of ailments, including diabetes mellitus and hypertension. AIM OF THE STUDY: In this work, we aimed to investigate the antihypertensive and vasorelaxant effects of AI aqueous extract in stroke prone spontaneously hypertensive rats (SHR-SP). MATERIAL AND METHODS: Male SHR-SP rats were orally force-fed AI aqueous extract (500 mg/kg body weight) daily for one week. Systolic blood pressure and urine output were recorded in vivo by non-invasive methods. AI vasoactive effects on noradrenaline contractile response and acetylcholine-evoked relaxation were assessed ex vivo on aorta rings of treated and untreated SHR-SP rats. AI extract was then subjected to bio-guided fractionation using solvents of increasing polarity. For each fraction, in vitro vasorelaxation assay was performed on noradrenaline-precontracted aorta of Wistar rats, in the absence/presence of N-nitro-L-arginine (L-NNA). HPLC analysis of AI total extract, and the most in vitro active AI residual aqueous extract fraction (A1) was performed using naringin, naringenin, apigenin, apigenin 7-O-glucoside as marker compounds. RESULTS: AI aqueous extract (500 mg/kg) significantly (P < 0.05) decreased systolic blood pressure (SBP) in SHR-SP rats, while not affecting the urine output. In ex vivo experiments, the total extract decreased contractile response to noradrenaline of aortic rings isolated from AI-treated SHR-SP rats with or without addition of N-nitro-L-arginine, but endothelium dependent relaxation evoked by acetylcholine in noradrenaline-contracted aortic rings was not affected by the extract treatment. In vitro experiments on AI aqueous extract fractions showed that its polar fraction was the only one affecting in vitro noradrenaline induced contractions, but only in an endothelium dependent manner. This fraction was shown by HPLC-UV to contain flavonoid glycosides among other polar compounds whose activity and mode of action may be modified in vivo by metabolization. CONCLUSION: These results support the use of AI as antihypertensive treatment in folk medicine. The systolic blood pressure decrease may be attributed at least in part to vasorelaxant glycosylated/polar phenolic compounds as flavonoids and/or their metabolites.


Assuntos
Ajuga/química , Anti-Hipertensivos/farmacologia , Hipertensão/tratamento farmacológico , Extratos Vegetais/farmacologia , Vasodilatadores/farmacologia , Animais , Anti-Hipertensivos/química , Anti-Hipertensivos/uso terapêutico , Aorta/efeitos dos fármacos , Pressão Sanguínea/efeitos dos fármacos , Fracionamento Químico , Flavonoides/química , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Masculino , Medicina Tradicional , Marrocos , Contração Muscular/efeitos dos fármacos , Relaxamento Muscular/efeitos dos fármacos , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Ratos Endogâmicos SHR , Ratos Wistar , Solventes/química , Micção/efeitos dos fármacos , Vasodilatadores/química , Vasodilatadores/uso terapêutico , Água/química
13.
Chem Biodivers ; 18(1): e2000780, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-33205900

RESUMO

Two new diterpenoids, ajudecunoid A (1) and ajudecunoid B (14), along with thirteen known diterpenoids, were isolated from the whole plants of Ajuga nipponensis Makino. Their structures were elucidated by the extensive spectroscopic analysis (UV, IR, MS, and NMR). The absolute configurations of ajudecunoid A (1) and ajudecunoid B (14) were defined through analysis of X-ray crystallography. Fifteen compounds were evaluated for inhibition of the formation of osteoclasts in bone marrow-derived macrophages (BMM) cells. Two neo-clerodane diterpenoids ajuganipponin B (5) and (12S)-6α,19-diacetoxy-18-chloro-4α-hydroxy-12-tigloyloxy-neo-clerod-13-en-15,16-olide (12) showed significant inhibition of osteoclastogenesis with IC50 values of 0.88 and 0.79 µM, respectively. Here we firstly reported diterpenoids with anti-osteoclastogenesis activity from A. nipponensis.


Assuntos
Ajuga/química , Diterpenos/química , Extratos Vegetais/química , Ajuga/metabolismo , Animais , Células da Medula Óssea/citologia , Diferenciação Celular/efeitos dos fármacos , Cristalografia por Raios X , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Macrófagos/citologia , Macrófagos/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Conformação Molecular , Osteoclastos/citologia , Osteoclastos/metabolismo , Osteogênese/efeitos dos fármacos , Ligante RANK/farmacologia
14.
Sci Rep ; 10(1): 19731, 2020 11 12.
Artigo em Inglês | MEDLINE | ID: mdl-33184359

RESUMO

Herbal medicines are attractive agents for human care. In this study, we found that the alcohol extract of Ajuga taiwanensis (ATE) screened from a chemical bank exhibited potent capacity for suppressing senescence associated biomarkers, including SA-ß-gal and up-regulated p53 in old human dermal fibroblasts (HDFs) without induction of significant cytotoxicity up to 100 µg/ml. Concomitantly, cells re-entered the cell cycle by reducing G1 phase arrest and increasing cell growth rate. The ATE was further partitioned to obtain the sub-fractions of n-butanol (BuOH), ethyl acetate (EA) and water. The BuOH and water sub-fractions exhibited less effects on prohibition of cell growth than the EA sub-fraction. All of these sub-fractions exhibited the ability on suppressing SA-ß-gal and p53 of old HDFs as low as 5-10 µg/ml. Under the activity guided fractionation and isolation, a major active constituent named AT-1 was isolated. The AT-1 was further identified as 8-O-acetylharpagide by structural analysis, and it could suppress SA-ß-gal and p53 of old HDFs below 10 µM. In addition, the intracellular reactive oxygen species (ROS) levels of old HDFs were suppressed by ATE, the sub-fractions of BuOH and water, and AT-1. However, the EA sub-fraction showed little ability on suppression of ROS. Furthermore, we performed an in vivo study using aging mice to be fed with ATE and the sub-fractions followed by immunohistochemical (IHC) staining. The expression of p53 and SA-ß-gal was significantly reduced in several tissue sections, including skin, liver, kidney, and spleen. Taken together, current data demonstrated that A. taiwanensis could suppress cellular senescence in HDFs, and might be used for health care.


Assuntos
Ajuga/química , Senescência Celular , Fibroblastos/efeitos dos fármacos , Piranos/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Pele/efeitos dos fármacos , Animais , Apoptose , Ciclo Celular , Movimento Celular , Proliferação de Células , Células Cultivadas , Fibroblastos/citologia , Fibroblastos/metabolismo , Humanos , Camundongos , Camundongos Endogâmicos BALB C , Fenótipo , Pele/citologia , Pele/metabolismo
15.
Food Chem Toxicol ; 144: 111589, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-32726593

RESUMO

In Turkish folk medicine, aerial parts of Ajuga chamaepitys (L.) Schreber subsp. chia (Schreber) are used for the treatment of diarrhea. The crude methanolic extract of aerial parts of A. chamaepitys subsp. chia was sequentially fractionated into five subextracts; n-hexane, dichloromethane, ethyl acetate, n-butanol and aqueous extracts. Effects of the methanol extract, subextracts and fractions were investigated in acetic acid-induced rat colitis model. The MeOH extract and n-BuOH subextract have regulated the caspase-3, myeloperoxidase, TNF-α, IL-6 levels and antioxidant parameters. After confirmation of the activity against ulcerative colitis, n-BuOH subextract was subjected to more chromatographic separation for the isolation of compounds ajugoside (1), asperulosidic acid (2) and deacetyl-asperulosidic acid (3). As a conclusion, A. chamaepitys subsp. chia can be used in cell, tissue, or individual-specific treatments that will be developed in the future treatment of IBD, or as a complementary therapeutic agent that contributes to these treatments.


Assuntos
Ajuga/química , Colite/prevenção & controle , Iridoides/uso terapêutico , Extratos Vegetais/uso terapêutico , Animais , Colite/metabolismo , Colite/patologia , Masculino , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley
16.
Bioorg Chem ; 101: 103966, 2020 08.
Artigo em Inglês | MEDLINE | ID: mdl-32506016

RESUMO

A phytochemical survey to obtain bioactive natural products from Ajuga pantantha afforded five new neo-clerodane diterpenoids (1-5). The structures were established by analysis of their NMR spectroscopic data, and electronic circular dichroism calculations were applied to define their absolute configurations. Compounds 2 and 5 were found to have the property of inhibiting NO production (IC50 values < 40 µM). Molecular docking and Western blotting were used to study the mechanism of anti-inflammatory action. Furthermore, compound 5 with the highest activity was tested for its in vivo anti-inflammatory effects using a zebrafish model.


Assuntos
Ajuga/química , Anti-Inflamatórios/química , Diterpenos Clerodânicos/uso terapêutico , Simulação de Acoplamento Molecular/métodos , Animais , Modelos Animais de Doenças , Diterpenos Clerodânicos/farmacologia , Estrutura Molecular , Compostos Fitoquímicos , Peixe-Zebra
17.
J Ethnopharmacol ; 258: 112875, 2020 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-32387464

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Ajuga iva (L.,) Schreb (A. iva). is a medicinal plant commonly used in Africa to treat several diseases such as diabetes, rheumatism, allergy, cancer, renal, metabolic disorders, cardiovascular disorders, digestive, and respiratory disorders. AIM OF THE REVIEW: We highlighted previous reports on A. iva including its ethnopharmacological uses, the chemistry of its secondary metabolites, in vitro and in vivo pharmacological properties, and toxicological evidence. MATERIALS AND METHODS: The data on A. iva were gathered using scientific research databases such as ScienceDirect, PubMed, SpringerLink, Web of Science, Scopus Wiley Online, and Google Scholar. In this review, studies focused on A. iva and its phytopharmacological activities were explored. RESULTS: A. iva is used by many North African folk medicine practitioners especially against diabetes and immunological diseases. Our analysis of the previous reports confirmed the scientific evidence of A. iva ethnomedicinal uses, especially the antidiabetic and anti-hypercholesterolemia activity. However, there was no clear correlation between previous pharmacological reports on A. iva and its other ethnomedicinal uses in the treatment of rheumatism, allergy, metabolic, digestive, and respiratory disorders. The extracts and isolated compounds from A. iva exhibited numerous in vitro and in vivo pharmacological activities such as antidiabetic, antioxidant, antimicrobial, anti-hypercholesterolemia, insecticide, and litholitic effects. Chemical characterization using GC-MS, HPLC, and NMR revealed the presence of many chemical compounds such as 20-hydroxyecdysone, cyasterone, ajugasterone, apigenin dihexoside, apigenin, carvacrol, ecdysterone, palmitic acid in different parts of A. iva. These compounds belong to different classes of chemical compounds such as steroids, flavonoids, fatty acids, and terpenoids. CONCLUSIONS: A. iva extracts especially from the leaves showed significant antidiabetic, antioxidant, anti-hypercholesterolemia, and analgesic effects. Future studies are required to validate the results of clinical trials on A. iva antidiabetic, anti-hypercholesterolemia, antioxidant/anti-inflammatory, antimicrobial, and analgesic properties. Toxicological validation and pharmacokinetics investigation are necessary to validate the efficacy and safety A. iva extracts and its secondary metabolites. An in-depth investigation is needed to reveal the biological activity of A. iva active compounds in preventing the development of cancer and neurodegenerative disorders such as Alzheimer's and Parkinson's diseases.


Assuntos
Ajuga/química , Medicina Tradicional Africana , Extratos Vegetais/farmacologia , Animais , Etnofarmacologia , Humanos , Masculino , Fitoterapia , Extratos Vegetais/efeitos adversos , Metabolismo Secundário
18.
Pak J Pharm Sci ; 33(1(Supplementary)): 325-331, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-32122865

RESUMO

Owing to its traditional applications, the current study focuses on Ajuga parviflora (A. parviflora) leaves extract for phytochemical and pharmacological analysis. The principle constituents were identified through gas chromatography (GC), and gas chromatography/mass spectroscopy (GC/MS), these includes phthalic acid, squalene, α-tocopherol, vitamin E, phytol, 2-methylenecholestan-3-ol, stigmasterol, cholest-22-ene-21-ol and 3,5-dehydro-6-methoxy. Hepatoprotective effect of A. parviflora was evaluated through isoniazid and rifampicin (INH and RFP) induced hepatotoxicity in rat. Animals in group A were treated with INH and RFP 50 mg/kg. Animals in group B, C, and D were pre-treated with A. parviflora extract at 100, 200 and 300 mg/kg dose prior drug administration. A. parviflora extract at 200 and 300 mg/kg in group C and D significantly reduced aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), and bilirubin (p<0.001) as compare to group B (100mg/kg). Total protein (TP) was also significantly (p<0.01) reduced in group C and D at dose of 200 and 300 mg/kg, respectively. The extract pre-treated animals with (A. parviflora, 200, and 300 mg/kg) showed that the epithelium of the central portal vein is intact with replete glucagon. The pre-treatment with A. parviflora protected the liver from INH and RFP induced hepatotoxicity. The results of pre-treated animals with A. parviflora 200, and 300 mg/kg dose prettily revert the severely disturb parameters like, cytolysis, lymphocytic infiltration, and lymphoid aggregate in portal vein and hydropic degeneration. The decrease peroxisome proliferator-receptor activator-δ (PPAR-δ) gene expression by INH, and RFP was significantly up regulated by A. parviflora extract in pre-treated animals at 200 and 300 mg/kg dose. These findings provide baseline pharmacological uses of A. parviflora in liver disorders. Further investigations are required for identification and isolation of biologically active components responsible for pharmacological activity.


Assuntos
Ajuga , Antituberculosos/toxicidade , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/uso terapêutico , Folhas de Planta , Animais , Doença Hepática Induzida por Substâncias e Drogas/patologia , Cromatografia Gasosa/métodos , Masculino , Espectrometria de Massas/métodos , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/uso terapêutico , Ratos , Ratos Wistar
19.
J Nat Prod ; 83(4): 894-904, 2020 04 24.
Artigo em Inglês | MEDLINE | ID: mdl-32216313

RESUMO

Eight new neo-clerodane diterpenoids (1-8) were acquired from the aerial parts of Ajuga pantantha. Spectroscopic data analysis permitted the definition of their structures, and experimental and calculated electronic circular dichroism data were used to define their absolute configurations. Compounds 2 and 4-8 were found to have NO inhibitory effects with IC50 values of 20.2, 45.5, 34.0, 27.0, 45.0, and 25.8 µM, respectively. The more potent compounds 2, 6, and 8 were analyzed to establish their anti-inflammatory mechanism, including regulation of the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) proteins as well as their binding interactions with the two proteins.


Assuntos
Ajuga/química , Anti-Inflamatórios não Esteroides/farmacologia , Diterpenos Clerodânicos/química , Diterpenos Clerodânicos/farmacologia , Diterpenos/química , Diterpenos/farmacologia , Inibidores de Ciclo-Oxigenase 2/química , Inibidores de Ciclo-Oxigenase 2/farmacologia , Espectroscopia de Ressonância Magnética , Modelos Moleculares , Simulação de Acoplamento Molecular , Estrutura Molecular , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico Sintase Tipo II/antagonistas & inibidores , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Ligação Proteica/efeitos dos fármacos
20.
Microsc Res Tech ; 83(4): 345-353, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31789485

RESUMO

Recent field exploration and collections has led to the findings of several new species in Pakistan. Here we reported two new species Ajuga reptance L and Sphagneticola trilobata (L.) Prusk for the first time in Pakistan flora as these species were neither listed in any other literature nor identified before in Pakistan. These species were found as a result of taxonomic studies performed in the year 2019 in District Rawalpindi and Islamabad, Pakistan. Microscopic techniques were used for the confirmation of foliar epidermal and pollen micromorphological features. Detailed study (morphological, palynological, and foliar epidermal) was provided for the correct identification and delimitation of the species using both light and scanning electron microscopy. Morphological results were compared with the flora of Taiwan and China.


Assuntos
Ajuga/anatomia & histologia , Microscopia/métodos , Estômatos de Plantas/ultraestrutura , Plantas/anatomia & histologia , Pólen/ultraestrutura , Tricomas/ultraestrutura , China , Microscopia Eletrônica de Varredura , Paquistão , Plantas/classificação , Taiwan
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