Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 1.844
Filtrar
Más filtros

Medicinas Complementárias
Intervalo de año de publicación
1.
Parasit Vectors ; 17(1): 194, 2024 Apr 25.
Artículo en Inglés | MEDLINE | ID: mdl-38664829

RESUMEN

BACKGROUND: Sarcoptic mange is a serious animal welfare concern in bare-nosed wombats (Vombatus ursinus). Fluralaner (Bravecto®) is a novel acaricide that has recently been utilised for treating mange in wombats. The topical 'spot-on' formulation of fluralaner can limit treatment delivery options in situ, but dilution to a volume for 'pour-on' delivery is one practicable solution. This study investigated the in vitro acaricidal activity of Bravecto, a proposed essential oil-based diluent (Orange Power®), and two of its active constituents, limonene and citral, against Sarcoptes scabiei. METHODS: Sarcoptes scabiei were sourced from experimentally infested pigs. In vitro assays were performed to determine the lethal concentration (LC50) and survival time of the mites when exposed to varying concentrations of the test solutions. RESULTS: All compounds were highly effective at killing mites in vitro. The LC50 values of Bravecto, Orange Power, limonene and citral at 1 h were 14.61 mg/ml, 4.50%, 26.53% and 0.76%, respectively. The median survival times of mites exposed to undiluted Bravecto, Orange Power and their combination were 15, 5 and 10 min, respectively. A pilot survival assay of mites collected from a mange-affected wombat showed survival times of < 10 min when exposed to Bravecto and Orange Power and 20 min when exposed to moxidectin. CONCLUSIONS: These results confirm the acaricidal properties of Bravecto, demonstrate acaricidal properties of Orange Power and support the potential suitability of Orange Power and its active constituents as a diluent for Bravecto. As well as killing mites via direct exposure, Orange Power could potentially enhance the topical delivery of Bravecto to wombats by increasing drug penetration in hyperkeratotic crusts. Further research evaluating the physiochemical properties and modes of action of Orange Power and its constituents as a formulation vehicle would be of value.


Asunto(s)
Acaricidas , Isoxazoles , Aceites de Plantas , Sarcoptes scabiei , Escabiosis , Animales , Sarcoptes scabiei/efectos de los fármacos , Acaricidas/farmacología , Isoxazoles/farmacología , Escabiosis/tratamiento farmacológico , Escabiosis/parasitología , Aceites de Plantas/farmacología , Aceites de Plantas/química , Monoterpenos Acíclicos/farmacología , Porcinos , Limoneno/farmacología , Limoneno/química , Terpenos/farmacología , Terpenos/química , Ciclohexenos/farmacología , Ciclohexenos/química , Dosificación Letal Mediana
2.
J Med Food ; 27(4): 359-368, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38526569

RESUMEN

As the body's largest organ, the skin is located at the internal and external environment interface, serving as a line of defense against various harmful stressors. Recently, marine-derived physiologically active ingredients have attracted considerable attention in the cosmeceutical industry due to their beneficial effects on skin health. Sargassum, a genus of brown macroalgae, has traditionally been consumed as food and medicine in several countries and is rich in bioactive compounds such as meroterpenoids, sulfated polysaccharides, fucoidan, fucoxanthin, flavonoids, and terpenoids. Sargassum spp. have various beneficial effects on skin disorders. They help with atopic dermatitis by improving skin barrier protection and reducing inflammation. Several species show potential in treating acne by inhibiting bacterial growth and reducing inflammation. Some species, such as Sargassum horneri, demonstrate antiallergic effects by modulating mast cell activity. Certain Sargassum species exhibit anticancer activity by inhibiting tumor growth and promoting apoptosis, and some species help with wound healing by promoting angiogenesis and reducing oxidative stress. Overall, Sargassum spp. demonstrate potential for treating and managing various skin conditions. Therefore, the bioactive compounds of Sargassum spp. may be natural ingredients with a wide range of functional properties for preventing and treating skin disorders. The present review focused on the various biological effects of Sargassum extracts and derived compounds on skin disorders.


Asunto(s)
Sargassum , Algas Marinas , Humanos , Piel , Inflamación , Terpenos/farmacología
3.
Cutis ; 113(1): 22-24, 2024 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-38478934

RESUMEN

Azadirachta indica, commonly known as neem, has many uses as a natural remedy. We review and discuss the pharmacologic, biologic, and medicinal properties of neem in disease management. We also report a rare clinical case of a 77-year-old man who presented with a hypopigmented rash on the lower back, bilateral flanks, and buttocks after 6 months of repeated application of neem oil to treat persistent arthritis and lower back pain.


Asunto(s)
Azadirachta , Masculino , Humanos , Anciano , Glicéridos/farmacología , Terpenos/farmacología , Extractos Vegetales
4.
Biomolecules ; 14(2)2024 Feb 07.
Artículo en Inglés | MEDLINE | ID: mdl-38397437

RESUMEN

Cancer has become one of the most multifaceted and widespread illnesses affecting human health, causing substantial mortality at an alarming rate. After cardiovascular problems, the condition has a high occurrence rate and ranks second in terms of mortality. The development of new drugs has been facilitated by increased research and a deeper understanding of the mechanisms behind the emergence and advancement of the disease. Numerous preclinical and clinical studies have repeatedly demonstrated the protective effects of natural terpenoids against a range of malignancies. Numerous potential bioactive terpenoids have been investigated in natural sources for their chemopreventive and chemoprotective properties. In practically all body cells, the signaling molecule referred to as signal transducer and activator of transcription 3 (STAT3) is widely expressed. Numerous studies have demonstrated that STAT3 regulates its downstream target genes, including Bcl-2, Bcl-xL, cyclin D1, c-Myc, and survivin, to promote the growth of cells, differentiation, cell cycle progression, angiogenesis, and immune suppression in addition to chemotherapy resistance. Researchers viewed STAT3 as a primary target for cancer therapy because of its crucial involvement in cancer formation. This therapy primarily focuses on directly and indirectly preventing the expression of STAT3 in tumor cells. By explicitly targeting STAT3 in both in vitro and in vivo settings, it has been possible to explain the protective effect of terpenoids against malignant cells. In this study, we provide a complete overview of STAT3 signal transduction processes, the involvement of STAT3 in carcinogenesis, and mechanisms related to STAT3 persistent activation. The article also thoroughly summarizes the inhibition of STAT3 signaling by certain terpenoid phytochemicals, which have demonstrated strong efficacy in several preclinical cancer models.


Asunto(s)
Neoplasias , Factor de Transcripción STAT3 , Humanos , Apoptosis , Proliferación Celular , Neoplasias/tratamiento farmacológico , Extractos Vegetales/farmacología , Transducción de Señal , Factor de Transcripción STAT3/metabolismo , Terpenos/farmacología
5.
PLoS Pathog ; 20(1): e1011557, 2024 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-38277417

RESUMEN

A proposed treatment for malaria is a combination of fosmidomycin and clindamycin. Both compounds inhibit the methylerythritol 4-phosphate (MEP) pathway, the parasitic source of farnesyl and geranylgeranyl pyrophosphate (FPP and GGPP, respectively). Both FPP and GGPP are crucial for the biosynthesis of several essential metabolites such as ubiquinone and dolichol, as well as for protein prenylation. Dietary prenols, such as farnesol (FOH) and geranylgeraniol (GGOH), can rescue parasites from MEP inhibitors, suggesting the existence of a missing pathway for prenol salvage via phosphorylation. In this study, we identified a gene in the genome of P. falciparum, encoding a transmembrane prenol kinase (PolK) involved in the salvage of FOH and GGOH. The enzyme was expressed in Saccharomyces cerevisiae, and its FOH/GGOH kinase activities were experimentally validated. Furthermore, conditional knockout parasites (Δ-PolK) were created to investigate the biological importance of the FOH/GGOH salvage pathway. Δ-PolK parasites were viable but displayed increased susceptibility to fosmidomycin. Their sensitivity to MEP inhibitors could not be rescued by adding prenols. Additionally, Δ-PolK parasites lost their capability to utilize prenols for protein prenylation. Experiments using culture medium supplemented with whole/delipidated human plasma in transgenic parasites revealed that human plasma has components that can diminish the effectiveness of fosmidomycin. Mass spectrometry tests indicated that both bovine supplements used in culture and human plasma contain GGOH. These findings suggest that the FOH/GGOH salvage pathway might offer an alternate source of isoprenoids for malaria parasites when de novo biosynthesis is inhibited. This study also identifies a novel kind of enzyme related to isoprenoid metabolism.


Asunto(s)
Diterpenos , Fosfomicina/análogos & derivados , Hemiterpenos , Parásitos , Pentanoles , Humanos , Animales , Bovinos , Parásitos/metabolismo , Fosfatos , Terpenos/farmacología , Terpenos/metabolismo
6.
J Agric Food Chem ; 72(2): 956-972, 2024 Jan 17.
Artículo en Inglés | MEDLINE | ID: mdl-38189231

RESUMEN

Petroselinum crispum (Mill.) Fuss (parsley) is a popular medicinal plant widely used in different traditional medicines all over the world. This paper provides an updated review on the traditional use, phytochemistry, and pharmacological activities of parsley. Parsley contains volatile compounds such as terpenes and terpenoids in the essential oil, as well as phenolic compounds in the plant extract. Parsley is traditionally used as a diuretic, liver and stomach tonic, and for urolithiasis and indigestion. Pharmacological investigations also confirm several biological activities of parsley including hepatoprotective, nephroprotective, antiurolithiatic, neuroprotective, cardioprotective, and antineoplastic effects in animal and cell-based studies. Parsley has currently demonstrated several pharmacological activities in preclinical studies; however, there is a big lack in clinical evidence. Considering parsley as a possible valuable medicinal food, future clinical trials are recommended to evaluate the clinical efficacy and safety of the plant in different health conditions.


Asunto(s)
Aceites Volátiles , Petroselinum , Animales , Petroselinum/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Aceites Volátiles/farmacología , Aceites Volátiles/química , Hígado , Terpenos/farmacología
7.
Molecules ; 29(2)2024 Jan 15.
Artículo en Inglés | MEDLINE | ID: mdl-38257323

RESUMEN

Cannabis, renowned for its historical medicinal use, harbours various bioactive compounds-cannabinoids, terpenes, and flavonoids. While major cannabinoids like delta-9-tetrahydrocannabinol (THC) and cannabidiol (CBD) have received extensive scrutiny for their pharmacological properties, emerging evidence underscores the collaborative interactions among these constituents, suggesting a collective therapeutic potential. This comprehensive review explores the intricate relationships and synergies between cannabinoids, terpenes, and flavonoids in cannabis. Cannabinoids, pivotal in cannabis's bioactivity, exhibit well-documented analgesic, anti-inflammatory, and neuroprotective effects. Terpenes, aromatic compounds imbuing distinct flavours, not only contribute to cannabis's sensory profile but also modulate cannabinoid effects through diverse molecular mechanisms. Flavonoids, another cannabis component, demonstrate anti-inflammatory, antioxidant, and neuroprotective properties, particularly relevant to neuroinflammation. The entourage hypothesis posits that combined cannabinoid, terpene, and flavonoid action yields synergistic or additive effects, surpassing individual compound efficacy. Recognizing the nuanced interactions is crucial for unravelling cannabis's complete therapeutic potential. Tailoring treatments based on the holistic composition of cannabis strains allows optimization of therapeutic outcomes while minimizing potential side effects. This review underscores the imperative to delve into the intricate roles of cannabinoids, terpenes, and flavonoids, offering promising prospects for innovative therapeutic interventions and advocating continued research to unlock cannabis's full therapeutic potential within the realm of natural plant-based medicine.


Asunto(s)
Cannabidiol , Cannabis , Alucinógenos , Enfermedades Neuroinflamatorias , Terpenos/farmacología , Agonistas de Receptores de Cannabinoides , Cannabidiol/farmacología , Cannabidiol/uso terapéutico , Flavonoides/farmacología , Flavonoides/uso terapéutico , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico
8.
Phytother Res ; 38(2): 636-645, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-37963759

RESUMEN

Hyperforin is a phloroglucinol derivative isolated from the medicinal plant Hypericum perforatum (St John's wort, SJW). This lipophilic biomolecule displays antibacterial, pro-apoptotic, antiproliferative, and anti-inflammatory activities. In addition, in vitro and in vivo data showed that hyperforin is a promising molecule with potential applications in neurology and psychiatry. For instance, hyperforin possesses antidepressant properties, impairs the uptake of neurotransmitters, and stimulates the brain derived neurotrophic factor (BDNF)/TrkB neurotrophic signaling pathway, the adult hippocampal neurogenesis, and the brain homeostasis of zinc. In fact, hyperforin is a multi-target biomolecule with a complex neuropharmacological profile. However, one prominent pharmacological feature of hyperforin is its ability to influence the homeostasis of cations such as Ca2+ , Na+ , Zn2+ , and H+ . So far, the pathophysiological relevance of these actions is currently unknown. The main objective of the present work is to provide an overview of the cellular neurobiology of hyperforin, with a special focus on its effects on neuronal membranes and the movement of cations.


Asunto(s)
Hypericum , Neurobiología , Floroglucinol/análogos & derivados , Antidepresivos/farmacología , Terpenos/farmacología , Floroglucinol/farmacología , Extractos Vegetales/farmacología , Cationes , Compuestos Bicíclicos con Puentes/farmacología
9.
Mol Cancer Ther ; 23(1): 14-23, 2024 Jan 03.
Artículo en Inglés | MEDLINE | ID: mdl-37756579

RESUMEN

Geranylgeranyl diphosphate synthase (GGDPS), the source of the isoprenoid donor in protein geranylgeranylation reactions, has become an attractive target for anticancer therapy due to the reliance of cancers on geranylgeranylated proteins. Current GGDPS inhibitor development focuses on optimizing the drug-target enzyme interactions of nitrogen-containing bisphosphonate-based drugs. To advance GGDPS inhibitor development, understanding the enzyme structure, active site, and ligand/product interactions is essential. Here we provide a comprehensive structure-focused review of GGDPS. We reviewed available yeast and human GGDPS structures and then used AlphaFold modeling to complete unsolved structural aspects of these models. We delineate the elements of higher-order structure formation, product-substrate binding, the electrostatic surface, and small-molecule inhibitor binding. With the rise of structure-based drug design, the information provided here will serve as a valuable tool for rationally optimizing inhibitor selectivity and effectiveness.


Asunto(s)
Inhibidores Enzimáticos , Neoplasias , Humanos , Farnesiltransferasa/química , Farnesiltransferasa/metabolismo , Inhibidores Enzimáticos/farmacología , Inhibidores Enzimáticos/uso terapéutico , Inhibidores Enzimáticos/química , Terpenos/química , Terpenos/farmacología , Prenilación de Proteína , Neoplasias/tratamiento farmacológico
10.
Phytochemistry ; 217: 113923, 2024 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-37963510

RESUMEN

Terpenoids are the largest class of all known natural products, possessing structural diversity and numerous biological activities. Ten previously undescribed terpenoid glycosides, glechlongsides A-J (1-10), were isolated from the ethanol extract of the whole plant of Glechoma longituba, including diterpenoid glycoside and pentacyclic triterpenoid saponin. The structures of these compounds were characterized by extensive analysis of 1D and 2D NMR as well as HRESIMS spectra. In addition, glechlongsides F-I (6-9) exhibited weak cytotoxicity against human cancer cell lines BGC-823, Be1, HCT-8, A2780, and A549 with IC50 values ranging from 3.77 to 30.95 µM, respectively.


Asunto(s)
Lamiaceae , Neoplasias Ováricas , Humanos , Femenino , Terpenos/farmacología , Glicósidos/farmacología , Glicósidos/química , Línea Celular Tumoral , Extractos Vegetales , Lamiaceae/química , Estructura Molecular
11.
J Agric Food Chem ; 72(1): 424-436, 2024 Jan 10.
Artículo en Inglés | MEDLINE | ID: mdl-38126326

RESUMEN

Shell ginger (Alpinia zerumbet) is a perennial ornamental plant of ginger native to East Asia, which can be used as a flavoring agent in food or beverage, as well as a traditional Chinese medicine. In this study, a total of 37 terpenoids, including 7 new compounds, zerumin D1 to zerumin D7 (2, 3, 28-30, 36, and 37), and 5 new naturally occurring compounds, zerumin D10 to zerumin D14 (9, 12, 15, 20, and 24), were isolated and identified from the rhizomes of shell ginger. Compound 3 was an unprecedented variant labdane diterpenoid featuring a unique 6/7/6/3 tetracyclic cyclic ether system in its side chain. The anti-inflammatory activities of the isolated terpenoids were assessed in RAW 264.7 macrophages stimulated by lipopolysaccharide (LPS). Compound 4 significantly inhibited the production of nitric oxide with an IC50 value of 5.4 µM. Further investigation revealed that compounds 2 and 3 may inhibit the nuclear translocation of NF-κB, thus suppressing the expression of IL-6, IL-1ß, iNOS, and COX-2 to exert the anti-inflammatory effects.


Asunto(s)
Alpinia , Zingiber officinale , Rizoma , Terpenos/farmacología , Antiinflamatorios/farmacología , FN-kappa B/metabolismo , Lipopolisacáridos/farmacología , Óxido Nítrico/metabolismo , Óxido Nítrico Sintasa de Tipo II/genética , Óxido Nítrico Sintasa de Tipo II/metabolismo , Ciclooxigenasa 2/genética , Ciclooxigenasa 2/metabolismo
12.
Acta Chim Slov ; 70(4): 651-660, 2023 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-38124642

RESUMEN

In 2020, around 19.3 million new cancer cases resulted in 3.5 million deaths. It is estimated that there will be 28.4 million cases by 2040. Plant-derived natural products, such as alkaloids, flavonoids, terpenoids, and phenolic compounds, offer a wide range of chemical structures and biological activities that can be explored for their potential in cancer research. In a particular study, researchers investigated the potential anticancer effects of Fallopia flower extracts on cancer induced by TAA (a carcinogen). They examined the extracts to identify specific amino acids with antioxidant properties and assessed their impact on liver function and tissue structure. The results showed that the plant extracts had positive effects on the histological section of the TAA-treated group. Additionally, the group of male rats treated with TAA and a chemotherapy drug called MMC displayed positive effects. Similarly, the group of male rats treated with TAA, flower plant extract, and MMC also showed positive effects. These findings suggest that the extract from Fallopia flowers could be considered as a traditional therapy with potential anticancer properties.


Asunto(s)
Carcinoma Hepatocelular , Neoplasias Hepáticas , Animales , Ratas , Antioxidantes/farmacología , Carcinoma Hepatocelular/tratamiento farmacológico , Flavonoides , Neoplasias Hepáticas/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Extractos Vegetales/química , Terpenos/química , Terpenos/farmacología , Polifenoles/química , Polifenoles/farmacología , Alcaloides/química , Alcaloides/farmacología
13.
Int J Med Mushrooms ; 25(12): 15-31, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37947061

RESUMEN

Mycochemical properties and bioactivities of Ganoderma resinaceum and Serpula similis remain unexplored. The present study assessed antioxidant, cytotoxicity, and cell migration abilities of Ganoderma and Serpula extracts, followed by their phytochemical analyses. The MTT assay was conducted to determine the cytotoxicity along with the cell migration studies in human cancer cell lines. The antioxidant profiles were evaluated through DPPH and FRAP assays. Furthermore, LC-MS/MS analysis was performed to elucidate the phytochemicals responsible for anticancer and antioxidant activities. Significant concentration-dependent cytotoxicities of 12.7% and 13.7% were observed against HCT 116 cell lines at 1% and 5% concentrations of the G. resinaceum extract, respectively. Similarly, significant concentration-dependent cytotoxicities of 6.7% and 25.5% were observed at 1% and 5% concentrations of the S. similis extract, respectively. The extracts of G. resinaceum and S. similis both shows better anti-migration potential in lung cancer cells. Both extracts demonstrated good scavenging activity on DPPH and ferric ion free radicals. LC-MS analysis revealed 11 compounds from S. similis and 15 compounds from G. resinaceum fruiting bodies. Compounds such as terpenoids, alkaloids, cytotoxic peptides, and other metabolites were identified as major components in both extracts. These extracts exhibited cytotoxic activity against HCT 116 cancer cells, along with moderate antioxidant activity. This implies that the extracts might be used as bioactive natural sources in the pharmaceutical and food industries.


Asunto(s)
Antineoplásicos , Ganoderma , Humanos , Antioxidantes/química , Cromatografía Liquida , Terpenos/farmacología , Terpenos/metabolismo , Extractos Vegetales/química , Espectrometría de Masas en Tándem , Ganoderma/química , Antineoplásicos/farmacología , Antineoplásicos/metabolismo
14.
Molecules ; 28(22)2023 Nov 14.
Artículo en Inglés | MEDLINE | ID: mdl-38005310

RESUMEN

Neurological ailments, including stroke, Alzheimer's disease (AD), epilepsy, Parkinson's disease (PD), and other related diseases, have affected around 1 billion people globally to date. PD stands second among the common neurodegenerative diseases caused as a result of dopaminergic neuron loss in the midbrain's substantia nigra regions. It affects cognitive and motor activities, resulting in tremors during rest, slow movement, and muscle stiffness. There are various traditional approaches for the management of PD, but they provide only symptomatic relief. Thus, a survey for finding new biomolecules or substances exhibiting the therapeutic potential to patients with PD is the main focus of present-day research. Medicinal plants, herbal formulations, and natural bioactive molecules have been gaining much more attention in recent years as synthetic molecules orchestrate a number of undesired effects. Several in vitro, in vivo, and in silico studies in the recent past have demonstrated the therapeutic potential of medicinal plants, herbal formulations, and plant-based bioactives. Among the plant-based bioactives, polyphenols, terpenes, and alkaloids are of particular interest due to their potent anti-inflammatory, antioxidant, and brain-health-promoting properties. Further, there are no concise, elaborated articles comprising updated mechanism-of-action-based reviews of the published literature on potent, recently investigated (2019-2023) medicinal plants, herbal formulations, and plant based-bioactive molecules, including polyphenols, terpenes, and alkaloids, as a method for the management of PD. Therefore, we designed the current review to provide an illustration of the efficacious role of various medicinal plants, herbal formulations, and bioactives (polyphenols, terpenes, and alkaloids) that can become potential therapeutics against PD with greater specificity, target approachability, bioavailability, and safety to the host. This information can be further utilized in the future to develop several value-added formulations and nutraceutical products to achieve the desired safety and efficacy for the management of PD.


Asunto(s)
Alcaloides , Enfermedades Neurodegenerativas , Enfermedad de Parkinson , Plantas Medicinales , Humanos , Enfermedad de Parkinson/tratamiento farmacológico , Alcaloides/farmacología , Alcaloides/uso terapéutico , Terpenos/farmacología , Terpenos/uso terapéutico
15.
Fitoterapia ; 171: 105711, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37866425

RESUMEN

Motivated by the potential anti-inflammatory effect of the crude extract of endophytic fungus Microdiplodia sp. CJ01 derived from Camellia sinensis, chemical investigation of the extract of Microdiplodia sp. CJ01 led to the isolation and identification of sixteen terpenoids, including five undescribed eremophilane sesquiterpenoids named microdiplodins A-E (1-5), one undescribed meroterpenoid 13-carboxymacrophorin A (13), seven known eremophilane sesquiterpenoids (6-12), and three known meroterpenoids (14-16). The structures of these compounds were elucidated based on extensive spectroscopic analysis, including nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS) data. Their absolute configurations were determined by calculational and experimental electronic circular dichroism (ECD) data. Anti-inflammatory activity assays revealed that compounds 3, 4, 14-16 exhibited moderate inhibitory effects on the production of nitric oxide (NO) in the lipopolysaccharide (LPS)-induced RAW 264.7 macrophage cells.


Asunto(s)
Ascomicetos , Sesquiterpenos , Terpenos/farmacología , Terpenos/química , Estructura Molecular , Ascomicetos/química , Sesquiterpenos Policíclicos , Dicroismo Circular , Antiinflamatorios
16.
Phytochemistry ; 216: 113863, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37751824

RESUMEN

Seven undescribed terpenoids, comprising two guaiane-type sesquiterpene lactones (1-2), one eucalyptol-type sesquiterpene (3), one monolactone (4), and three triterpenoids (5-7), along with 35 known analogues, were isolated from the leaves of Artemisia vulgaris L. Their structures and configurations were analysed by extensive spectroscopy. Compounds 1, 2, 8-10, 13, 17, 19, and 28 showed antineuroinflammatory activity, and compounds 1 and 2 revealed remarkable antineuroinflammatory effects, with an IC50 value of 2.2 ± 0.1 and 1.6 ± 0.1 µM, more potent than the positive control drug dexamethasone. Furthermore, compounds 1 and 2 could inhibit the expression of BV-2 inflammatory genes (IL-6, TNF-α, IL-1ß) induced by LPS, downregulate the critical inflammatory protein production of iNOS and COX-2. The anti-HSV-1 activity screening revealed that compounds 28, 29 and 38 exhibited inhibitory activity against HSV-1 proliferation. Particularly, compound 28 exhibited a significant anti-HSV-1 effect, inhibiting the proliferation of HSV-1 and acyclovir-resistant strains of HSV-1/153 and HSV-1/Blue. Our research identified compounds 1, 2, and 28 from A. vulgaris., which could potentially serve as lead compounds for antineuroinflammatory and anti-HSV-1 activities.


Asunto(s)
Artemisia , Sesquiterpenos , Artemisia/química , Terpenos/farmacología , Cromatografía Liquida , Espectrometría de Masas en Tándem , Sesquiterpenos/química , Estructura Molecular
17.
Z Naturforsch C J Biosci ; 78(11-12): 415-420, 2023 Nov 27.
Artículo en Inglés | MEDLINE | ID: mdl-37748096

RESUMEN

Eleven compounds were isolated and identified from ethanolic extracts of Solanum virginianum fruits, including two new compounds (1-2) and nine known compounds (3-11). Their structures were determined to be melongenaterpene C15-O-ß-D-glucopyranoside (1), (9Z)-3,7,11,15-tetramethyl -hexadeca-1,6,10-triene-3,5,14,15-tetraol-5-O-ß-D-glucopyranoside (2), actini-dioionoside A (3), byzantionoside B (4), citroside A (5), 7Z-roseoside (6), matenoside A (7), megastigmane (8), dihydrophaseic acid 3'-O-ß-D-glucopyranoside (9), taraxerol (10), and huzhangoside C (11). In this paper, NMR spectroscopy was used to study the structures of the compounds, comparing their data with those in the literature. In addition, the potential anti-inflammatory activity of the compounds was also evaluated using the RAW264.7 cell inflammation model induced by lipopolysaccharide (LPS). The terpenoids showed no significant anti-inflammatory activity.


Asunto(s)
Frutas , Solanum , Frutas/química , Terpenos/farmacología , Extractos Vegetales/química , Antiinflamatorios/farmacología
18.
Molecules ; 28(18)2023 Sep 14.
Artículo en Inglés | MEDLINE | ID: mdl-37764389

RESUMEN

Four previously undescribed terpenoid glucosides, including one sesquiterpenoid di-glucoside (1), two new iridoid glucosides (2, 3), and a new triterpenoid tri-glucoside (4), were isolated from a 70% ethanol extract of the root of Gentiana macrophylla (Gentianaceae), along with eight known terpenoids. Their structures were determined by spectroscopic techniques, including 1D, 2D NMR, and HRMS (ESI), as well as chemical methods. The absolute configuration of compound 1 was determined by quantum chemical calculation of its theoretical electronic circular dichroism (ECD) spectrum. The sugar moieties of all the new compounds were confirmed to be D-glucose by GC analysis after acid hydrolysis and acetylation. Anti-pulmonary inflammation activity of the iridoids were evaluated on a TNF-α induced inflammation model in A549 cells. Compound 2 could significantly alleviate the release of proinflammatory cytokines IL-1ß and IL-8 and increase the expression of anti-inflammatory cytokine IL-10.


Asunto(s)
Gentiana , Neumonía , Humanos , Terpenos/farmacología , Factor de Necrosis Tumoral alfa , Glucósidos/farmacología , Células A549 , Citocinas , Extractos Vegetales/farmacología
19.
Acta Parasitol ; 68(4): 793-806, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37603126

RESUMEN

PURPOSE: The resistance of parasite to readily affordable antimalarial drugs, the high cost of currently potent drugs, and the resistance of vector mosquitoes to insecticides threaten the possibility of malaria eradication in malaria endemic areas. Due to the fact that quinine and artemisinin were isolated from plants sources, researchers have been encouraged to search for new antimalarials from medicinal plants. This is especially the case in Africa where a large percentage of the population depends on medicinal plant to treat malaria and other ailments. METHOD: In this study, we evaluated previously characterized Plasmodium-cidal compounds obtained from the African flora to identify their likely biochemical targets, for an insight into their possible antimalarial chemotherapy. Molecular docking study was first conducted, after which remarkable compounds were submitted for molecular dynamic (MD) simulations studies. RESULTS: From a total of 38 Plasmodium-cidal compounds docked with confirmed Plasmodium falciparum protein drug targets [plasmepsin II (PMII), histo-aspartic protein (HAP) and falcipain-2 (FP)], two pentacyclic triterpene, cucurbitacin B and 3 beta-O-acetyl oleanolic acid showed high binding affinity relative to artesunate. This implies their capacity to inhibit the three selected P. falciparum target proteins, and consequently, antimalarial potential. From the MD simulations studies and binding free energy outcomes, results confirmed that the two compounds are stable in complex with the selected antimalarial targets; they also showed excellent binding affinities during the 100 ns simulation. CONCLUSION: These results showed that cucurbitacin B and 3 beta-O-acetyl oleanolic acid are potent antimalarials and should be considered for further studies.


Asunto(s)
Antimaláricos , Malaria Falciparum , Malaria , Ácido Oleanólico , Plasmodium , Animales , Antimaláricos/farmacología , Antimaláricos/uso terapéutico , Plasmodium falciparum , Terpenos/farmacología , Terpenos/uso terapéutico , Simulación del Acoplamiento Molecular , Ácido Oleanólico/uso terapéutico , Malaria/parasitología , Malaria Falciparum/tratamiento farmacológico
20.
Int J Biol Macromol ; 247: 125817, 2023 Aug 30.
Artículo en Inglés | MEDLINE | ID: mdl-37455002

RESUMEN

The present study focused to determine the neuroprotective effects of terpenoids in streptozotocin & nicotinamide-induced type-2 diabetes in rats. The in silico studies were carried out for 68 terpenoids using AutoDock 4.2. The in vitro cholinestrerase, α-amylase enzyme inhibitory assays were perfomed using standard procedures. For in vivo neuroprotective studies, male wistar rats were separated into five groups and each group comprised of six animals. Treatment groups were received low dose and high dose α-Bisabolol 100 and 200 mg/kg respectively, and the standard groups received rivastigmine 2 mg/kg, p.o. and metformin group 100 mg/kg, p.o. for 30 consecutive days. Administration of streptozotocin (45 mg/kg, i.p.) and nicotinamide (110 mg/kg, i.p.)-induced the type 2 diabetes in all groups except the control. The behavioural assessments such as Morris water maze, and open field test were performed and biochemical parameters such as acetylcholinesterase levels and enzymatic antioxidants and reduced glutathione level were estimated from brain homogenates. Treatment of diabetic rats with α-Bisabolol was lowered blood glucose level, improved spatial recognition memory in behavioural assessments in a concentration dependent manner. It can be concluded that α-Bisabolol could act as a potential drug candidate in the management of diabetic Alzheimer's disease.


Asunto(s)
Diabetes Mellitus Experimental , Diabetes Mellitus Tipo 2 , Fármacos Neuroprotectores , Ratas , Masculino , Animales , Acetilcolinesterasa/metabolismo , Fármacos Neuroprotectores/farmacología , Fármacos Neuroprotectores/uso terapéutico , Estreptozocina/farmacología , Diabetes Mellitus Experimental/inducido químicamente , Diabetes Mellitus Experimental/tratamiento farmacológico , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Niacinamida/farmacología , Estrés Oxidativo , Terpenos/farmacología , Antioxidantes/metabolismo , Ratas Wistar , Aprendizaje por Laberinto
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA