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1.
Int J Mol Sci ; 25(8)2024 Apr 20.
Artigo em Inglês | MEDLINE | ID: mdl-38674113

RESUMO

The diterpene 7α-acetoxy-6ß-hydroxyroyleanone isolated from Plectranthus grandidentatus demonstrates promising antibacterial, anti-inflammatory and anticancer properties. However, its bioactivity may be enhanced via strategic structural modifications of such natural products through semisynthesis. The anticancer potential of 7α-acetoxy-6ß-hydroxyroyleanone and five derivatives was analyzed in silico via the prediction of chemicals absorption, distribution, metabolism, excretion, and toxicity (ADMET), quantum mechanical calculations, molecular docking and molecular dynamic simulation. The protein targets included regulators of apoptosis and cell proliferation. Additionally, network pharmacology was used to identify potential targets and signaling pathways. Derivatives 7α-acetoxy-6ß-hydroxy-12-O-(2-fluoryl)royleanone and 7α-acetoxy-6ß-(4-fluoro)benzoxy-12-O-(4-fluoro)benzoylroyleanone achieved high predicted binding affinities towards their respective protein panels, with stable molecular dynamics trajectories. Both compounds demonstrated favorable ADMET parameters and toxicity profiles. Their stability and reactivity were confirmed via geometry optimization. Network analysis revealed their involvement in cancer-related pathways. Our findings justify the inclusion of 7α-acetoxy-6ß-hydroxy-12-O-(2-fluoryl)royleanone and 7α-acetoxy-6ß-(4-fluoro)benzoxy-12-O-(4-fluoro)benzoylroyleanone in in vitro analyses as prospective anticancer agents. Our binding mode analysis and stability simulations indicate their potential as selective inhibitors. The data will guide studies into their structure optimization, enhancing efficacy and drug-likeness.


Assuntos
Diterpenos , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Plectranthus , Humanos , Plectranthus/química , Diterpenos/química , Diterpenos/farmacologia , Diterpenos/síntese química , Antineoplásicos/farmacologia , Antineoplásicos/química , Antineoplásicos/síntese química , Simulação por Computador , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/química , Proliferação de Células/efeitos dos fármacos
2.
Molecules ; 29(8)2024 Apr 16.
Artigo em Inglês | MEDLINE | ID: mdl-38675627

RESUMO

The abietane diterpenoid 7α-acetoxy-6ß-hydroxyroyleanone (Roy) isolated from Plectranthus grandidentatus demonstrates cytotoxicity across numerous cancer cell lines. To potentiate anticancer attributes, a series of semi-synthetic Roy derivatives were generated and examined computationally. ADMET predictions were used to evaluate drug-likeness and toxicity risks. The antineoplastic potential was quantified by PASS. The DFT models were used to assess their reactivity and stability. Molecular docking determined cancer-related protein binding. MS simulations examined ligand-protein stability. Additionally, network pharmacology was used to identify potential targets and signaling pathways. Favorable ADME attributes and acceptable toxicity profiles were determined for all compounds. Strong anticancer potential was shown across derivatives (Pa 0.819-0.879). Strategic modifications altered HOMO-LUMO gaps (3.39-3.79 eV) and global reactivity indices. Favorable binding was revealed against cyclin-dependent kinases, BCL-2, caspases, receptor tyrosine kinases, and p53. The ligand exhibited a stable binding pose in MD simulations. Network analysis revealed involvement in cancer-related pathways. In silico evaluations predicted Roy and derivatives as effective molecules with anticancer properties. Experimental progress is warranted to realize their chemotherapeutic potential.


Assuntos
Abietanos , Diterpenos , Simulação de Acoplamento Molecular , Plectranthus , Humanos , Abietanos/química , Abietanos/farmacologia , Plectranthus/química , Simulação por Computador , Antineoplásicos/farmacologia , Antineoplásicos/química , Linhagem Celular Tumoral , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/química , Simulação de Dinâmica Molecular , Estrutura Molecular
3.
J Ethnopharmacol ; 330: 118202, 2024 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-38641078

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Members of Plectranthus genus such as Plectranthus amboinicus (Lour.) Spreng is a well-known folkloric medicine around the globe in treating several human ailments such as cardiovascular, respiratory, digestive, urinary tract, skin and infective diseases. Its therapeutic value is primarily attributed to its essential oil. Although several properties of Plectranthus amboinicus essential oil have been documented, its mechanism of action and safety has not been completely elucidated. AIM OF THE STUDY: To investigate the anti-infective potential of Plectranthus amboinicus essential oil against Klebsiella pneumoniae using in vitro and in vivo bioassays and identify its mode of action. The study was conducted to scientifically validate the traditional usage of Plectranthus amboinicus oil and propose it as a complementary and alternative medication to combat Klebsiella pneumoniae infections due to emerging antibiotic resistance problem. MATERIALS AND METHODS: Plectranthus amboinicus essential oil was extracted through steam distillation and was chemically characterized using Gas Chromatography Mass Spectrometry (GC-MS). The antibacterial activity was assessed using microbroth dilution assay, metabolic viability assay and growth curve analysis. The mode of action was elucidated by the proteomics approach using Nano-LC-MS/MS followed by in silico analysis. The results of proteomic analysis were further validated through several in vitro assays. The cytotoxic nature of the essential oil was also confirmed using adenocarcinomic human alveolar basal epithelial (A549) cells. Furthermore, the safety and in vivo anti-infective efficacy of Plectranthus amboinicus essential oil was evaluated through survival assay, CFU assay and histopathological analysis of vital organs using zebrafish as a model organism. RESULTS: The chemical characterization of Plectranthus amboinicus essential oil revealed that it is predominantly composed of thymol. Thymol rich P. amboinicus essential oil demonstrated potent inhibitory effects on Klebsiella pneumoniae growth, achieving a significant reduction at a concentration of 400 µg/mL within 4 h of treatment The nano-LC-MS/MS approach unveiled that the essential oil exerted its impact by disrupting the antioxidant defense system and efflux pump system of the bacterium, resulting in elevated cellular oxidative stress and affect the biosynthesis of biofilm. The same was validated through several in vitro assays. Furthermore, the toxicity of Plectranthus amboinicus essential oil determined using A549 cells and zebrafish survival assay established a non-toxic concentration of 400 µg/mL and 12.5 µg/mL respectively. The results of anti-infective potential of the essential oil using Zebrafish as a model organism demonstrated significantly improved survival rates, reduced bacterial load, alleviated visible signs of inflammation and mitigated the adverse effects of infection on various organs, as evidenced by histopathological analysis ensuring its safety for potential therapeutic application. CONCLUSION: The executed in vitro and in vivo assays established the effectiveness of essential oil in inhibiting bacterial growth by targeting key proteins associated with the bacterial antioxidant defense system and disrupted the integrity of the cell membrane, highlighting its critical role in addressing the challenge posed by antibiotic-resistant Klebsiella pneumoniae.


Assuntos
Klebsiella pneumoniae , Óleos Voláteis , Folhas de Planta , Plectranthus , Proteômica , Klebsiella pneumoniae/efeitos dos fármacos , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Animais , Plectranthus/química , Humanos , Folhas de Planta/química , Antibacterianos/farmacologia , Antibacterianos/isolamento & purificação , Testes de Sensibilidade Microbiana , Peixe-Zebra , Infecções por Klebsiella/tratamento farmacológico , Infecções por Klebsiella/microbiologia
4.
Biomed Pharmacother ; 174: 116516, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38583339

RESUMO

The Plectranthus genus is often cited for its medicinal properties. Plectranthus ornatus Codd. is traditionally used in Africa for the treatment of gastric and liver diseases and their leaves are used for their antibiotic action. The main constituent of P. ornatus is the halimane compound, 11 R∗-acetoxyhalima-5,13E-dien-15-oic acid (Hal), described for its antimicrobial and anticancer properties. The objective of this work was to improve the activity of the halimane lead molecule. Further physiochemical characterisation was performed on Hal. To the best of our knowledge, this work constitutes the first published data of the absolute configurations by SCXRD and thermal stability of Hal. Using Hal, reactions with different amines were carried out to afford novel semi-synthetic derivatives and their structural elucidation was completed. The cytotoxicity of the derivatives was assessed against three leukaemia cancer cell lines (CCRF-CEM, K562 and HL-60). The antioxidant activity was investigated using H2O2-induced HGF-1 cells and their anti-inflammatory activity was studied using RT-PCR and ELISA. Our data showed that amide derivatives of Hal presented moderate cytotoxicity and more potent activity when compared to the parent molecule, giving insight into the SAR of Hal. The derivatives also displayed protection against oxidative damage to DNA. Finally, the derivatives possessed anti-inflammatory properties at the level of gene and protein expression for the cytokines IL-1ß, TNF-α and IL-6, induced by LPS in normal HGF-1 cells. Overall, our study provides useful insight into the enhanced biological activities of semi-synthetic Hal derivatives, as a starting point for novel drug formulations in cancer therapy.


Assuntos
Plectranthus , Humanos , Plectranthus/química , Linhagem Celular Tumoral , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Diterpenos/farmacologia , Diterpenos/química , Diterpenos/isolamento & purificação , Antioxidantes/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Células K562 , Células HL-60 , Antineoplásicos/farmacologia , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Sobrevivência Celular/efeitos dos fármacos
5.
Sci Rep ; 14(1): 6693, 2024 03 20.
Artigo em Inglês | MEDLINE | ID: mdl-38509159

RESUMO

Coleus scutellarioides (L.) Benh. is a popular species in the world, known for its characteristic magnificent colourful leaves. The study has revealed that the contents of rosmarinic acid and caffeic acid are significantly higher in the plant tissues cultivated in vivo than when under in vitro conditions. The performed qualitative and quantitative analyses confirmed the presence (whose averaged content) of salvinorin A (6.65 µg/1 g of fresh plant) and salvinorin B (50.46 µg/1 g of fresh plant) in tissues of Coleus scutellarioides (L.) Benh. of 'Electric lime' variety. The greatest quantities of these compounds were recorded for plants cultivated in vitro on the MS medium enriched with NAA (naphthyl-1-acetic acid) at a concentration of 0.5 mg∙ dm-3. The research detected differences in the amounts of compounds between plants grown in vivo and those cultivated in vitro. Addition of plant growth regulators into the breeding medium under in vitro conditions was found affecting the amounts of compounds in plant tissues.


Assuntos
Ácidos Cafeicos , Coleus , Diterpenos Clerodânicos , Plectranthus , Ácido Rosmarínico , Melhoramento Vegetal , Reguladores de Crescimento de Plantas
6.
J Oleo Sci ; 73(3): 351-358, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38432999

RESUMO

Acute pancreatitis (AP) have been documented to have severe impact on pancreatic function. Frequent incidence of AP can result in chronic pancreatitis and thereby it can increase the probability of pancreatic cancers. This study intended to examine the effect of selenium nanoparticles (Se-NPs) synthesized from Coleus forskohlii leaf extract on pancreatic function and AP in rat. Primarily, Se-NPs was fabricated using the C. forskohlii leaf extract. The synthesized nanomaterial was characterized through UV-visible, XRD, and FTIR spectroscopies. Notably, the zeta potential of Se-NPs was found to be -32.8 mV with a polydispersity index (PDI) of 0.18. Morphological analysis on SEM unveiled the spherical shape of Se-NP with an average particle size of 12.69 nm. Strikingly, cytotoxicity analysis on pancreatic cancer and normal cells unveiled the concentration-dependent toxicity profile. However, IC 50 value is lower in normal pancreatic cell lines in comparison to pancreatic cancer cells lines. Assessment of Se-NPs on AP rats revealed the positive impact of Se-NPs. It effectively decreased the amount of lipase, amylase, IL-1ß, MDA, NO, and Bcl-2 while increased the glucose, insulin, HOMA-ß and antioxidant potential in AP rats. In addition, an evaluation of Se-NPs in the pancreatic functions revealed the non-harmful effect of Se-NPs.


Assuntos
Nanopartículas , Neoplasias Pancreáticas , Pancreatite , Plectranthus , Selênio , Animais , Ratos , Pancreatite/induzido quimicamente , Pancreatite/tratamento farmacológico , Doença Aguda , Extratos Vegetais
7.
Med Oncol ; 41(4): 81, 2024 Feb 24.
Artigo em Inglês | MEDLINE | ID: mdl-38400892

RESUMO

Plectranthus amboinicus leaves were subjected to hydrodistillation to obtain essential oil (EO). Phytochemical analysis using gas chromatography-mass spectrometry revealed a diverse range of compounds in the EO, with p-cymen-4-ol (18.57%) emerging as the most predominant, followed by isocaryophyllene (12.18%). The in vitro antiproliferative activity of EO against breast cancer was assessed in MCF-7 and MDA-MB-231 cell lines. The MTT assay results revealed that EO showed IC50 values of 42.25 µg/mL and 13.44 µg/mL in MCF-7 cells and 63.67 µg/mL and 26.58 µg/mL in MDA-MB-231 cells after 24 and 48 h, respectively. The in silico physicochemical and pharmacokinetic profiles of the EO constituents were within acceptable limits. Molecular docking was conducted to investigate the interactions between the constituents of the EO and protein Aromatase (PDB ID:3S79). Among the EO constituents, 4-tert-butyl-2-(5-tert-butyl-2-hydroxyphenyl)phenol (4BHP) exhibited the highest dock score of -6.580 kcal/mol when compared to the reference drug, Letrozole (-5.694 kcal/mol), but was slightly lesser than Anastrozole (-7.08 kcal/mol). Molecular dynamics simulation studies (100 ns) of the 4BHP complex were performed to study its stability patterns. The RMSD and RMSF values of the 4BHP protein complex were found to be 2.03 Å and 4.46 Å, respectively. The binding free energy calculations revealed that 4BHP displayed the highest negative binding energy of -43 kcal/mol with aromatase protein, compared to Anastrozole (-40.59 kcal/mol) and Letrozole (-44.54 kcal/mol). However, further research is required to determine the safety, efficacy, and mechanism of action of the volatile oil. Taking into consideration the key findings of the present work, the development of a formulation of essential oil remains a challenging task and novel drug delivery systems may lead to site-specific and targeted delivery for the effective treatment of breast cancer.


Assuntos
Neoplasias da Mama , Óleos Voláteis , Plectranthus , Humanos , Feminino , Óleos Voláteis/farmacologia , Óleos Voláteis/análise , Óleos Voláteis/química , Plectranthus/química , Plectranthus/metabolismo , Aromatase/metabolismo , Neoplasias da Mama/tratamento farmacológico , Anastrozol/metabolismo , Letrozol/metabolismo , Simulação de Acoplamento Molecular
8.
Drug Dev Ind Pharm ; 50(3): 248-261, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38317433

RESUMO

OBJECTIVE: To develop Plectranthus amboinicus extract loaded Polyurethane foam dressing for burn wound healing. SIGNIFICANCE: Plectranthus amboinicus is traditionally used as an anti-inflammatory and wound-healing agent. Its incorporation in a PU foam dressing will offer the dual benefits of foam dressing as well as the healing potential of P. amboinicus. METHODS: PU foam dressings were prepared and loaded with P. ambionicus leaf extract (PAE). The dressings were prepared with varying concentrations (0.5-2%) of extract along with Toluene diisocyanate, polypropylene glycol (PPG), and liquid paraffin. The dressings were characterized by Scanning Electron Microscopy and evaluated for Moisture Vapor Transmission Rate, absorption rate, porosity, and mechanical strength followed by in vivo burn wound-healing studies in comparison to a marketed dressing. RESULTS: The MVTR was found to be optimum in formulations FD2-FD4 with values ranging from 2068.06 ± 0.99 to 2095.00 ± 0.25 g/m2/day. Absorption rate was found to be between 1.27 ± 0.01, 1.31 ± 0.00, and 1.30 ± 0.02 g/cm2 for formulations FD2-FD4. Formulations FD1, FD2, FD3, FD4 showed better porosity when compared to other formulations. Formulation FD4 was further characterized by micro-CT and a porosity of 46.32% was obtained. Tensile strength measurement indicated that the selected formulations were flexible enough to withstand regular handling during dressing changes. Acute dermal irritation performed on rabbits showed no irritation, erythema, eschar, and edema. In vivo wound-healing studies performed on albino wistar rats showed that the FD4 formulation has better wound healing property. CONCLUSION: Plectranthus ambionicus-loaded PU foam dressing demonstrated promising burn wound-healing potential.


Assuntos
Queimaduras , Plectranthus , Ratos , Animais , Coelhos , Cicatrização , Bandagens , Queimaduras/tratamento farmacológico , Infecção da Ferida Cirúrgica , Poliuretanos
9.
Inflammopharmacology ; 32(2): 1593-1606, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38308794

RESUMO

BACKGROUND: Inflammation is a key biological reaction that comprises a complex network of signals that both initiate and stop the inflammation process. PURPOSE: This study targets to evaluate the anti-inflammatory potential of the leaves of the Plectranthus rugosus (P. rugosus) plant involving both in vitro and in vivo measures. The current available drugs exhibit serious side effects. Traditional medicines impart an essential role in drug development. P. rugosus is a plant used in traditional medicine of Tropical Africa, China, and Australia to treat various diseases. METHODS: Lipopolysaccharide (LPS), an endotoxin, kindles macrophages to discharge huge quantities of pro-inflammatory cytokines like TNF-α and IL-6. So, clampdown of macrophage stimulation may have a beneficial potential to treat various inflammatory disorders. The leaves of the P. rugosus are used for swelling purpose by local population; however, its use as an anti-inflammatory agent and associated disorders has no scientific evidence. RESULTS: The extracts of the plant Plectranthus rugosus ethanolic extract (PREE), Plectranthus rugosus ethyl acetate extract (PREAF), and the compound isolated (oleanolic acid) suppress the pro-inflammatory cytokines (IL-6 and TNF-α) and nitric oxide (NO), confirming its importance in traditional medicine. CONCLUSION: The pro-inflammatory cytokines are inhibited by P. rugosus extracts, as well as an isolated compound oleanolic acid without compromising cell viability.


Assuntos
Antineoplásicos , Ácido Oleanólico , Plectranthus , Antioxidantes/uso terapêutico , Fator de Necrose Tumoral alfa , Interleucina-6 , Ácido Oleanólico/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Extratos Vegetais/uso terapêutico , Inflamação/tratamento farmacológico , Citocinas , Antineoplásicos/uso terapêutico , Óxido Nítrico , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Lipopolissacarídeos/farmacologia
10.
Int J Pharm ; 652: 123766, 2024 Mar 05.
Artigo em Inglês | MEDLINE | ID: mdl-38181991

RESUMO

Comparability stability studies of a live Newcastle Disease LaSota vaccine were conducted post freeze-drying and during storage at 5±2, 25±2 and 37±1 °C to demonstrate the equivalence/inequivalence of stability profiles of vaccines stabilized with peptone (reference), trehalose and starch derivatives (acetylated xerogel and carboxymethylated) from Plectranthus esculentus tubers. Variations in moisture content during storage at 5±2 °C; physical collapse/shrinkage, partial microcollapse, and hydrophilicity of lyophilisates were prominent in starch stabilized vaccines without additives. Using the mean embryo infective dose (EID50) test, the derivatives and peptone stabilized vaccines had < 0.5 logEID50 loss in titre during freeze-drying. At the storage temperatures of 5±2, 25±2 and 37±1 °C, using peptone, acetylated xerogel starch, carboxymethylated starch, and trehalose, the average shelf lives of the vaccines were 23-55, 21-26, and 2.6-4.9 months respectively. Acetylated xerogel and carboxymethylated derivatives of Plectranthus esculentus tuber starch with/without additives were able to keep the live ND LaSota vaccine stable during freeze-drying at 1-3 % w/v. The stability of all the vaccines declined as storage temperatures increased. The acetylated xerogel stabilized vaccines were more stable than all of the others at 25±2 and 37±1 °C temperatures.


Assuntos
Plectranthus , Amido , Animais , Trealose , Peptonas , Liofilização , Vacinas Atenuadas , Estabilidade de Medicamentos
11.
Int J Mol Sci ; 25(2)2024 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-38256118

RESUMO

Plectranthus scutellarioides (L.) R.Br. is a medicinal plant that has long been used in traditional medicine to treat conditions such as abscesses, ulcers, and ear and eye infections. It is known to have a wide range of biological properties, such as antibacterial, antioxidant, antifungal, anti-inflammatory, anti-diabetic and anti-cancer effects. In this study, we established in vitro cultures from both the aerial parts and roots of Plectranthus scutellarioides. Subsequently, we compared the basic phytochemical profile of the obtained extracts and conducted a biological analysis to assess their potential for inducing apoptosis in breast (MCF-7) and lung (A549) cancer cells. Phytochemical analysis by HPLC-MS revealed the presence of compounds belonging to phenolic acids (ferulic, syringic, vanillic, rosmarinic, chlorogenic, caffeic, coumaric, dihydroxybenzoic acids), flavonoids (eriodyctiol and cirsimaritin), and terpenes such as 6,11,12,14,16-Pentahydroxy-3,17diacetyl-8,11,13-abietatrien-7-one, 6,11,12,14,16-Pentahydroxy-3,17-diacetyl5,8,11,13-abietatetraen-7-one, and 3,6,12-Trihydroxy-2-acetyl-8,12-abietadien7,11,14-trione. The results show that both extracts have a cytotoxic and genotoxic effect against MCF-7 and A549 cancer cells, with a different degree of sensitivity. It was also shown that both extracts can induce apoptosis by altering the expression of apoptotic genes (Bax, Bcl-2, TP53, Fas, and TNFSF10), reducing mitochondrial membrane potential, increasing ROS levels, and increasing DNA damage. In addition, it has been shown that the tested extracts can alter blood coagulation parameters. Our results indicate that extracts from in vitro cultures of Plectranthus scutellarioides aerial parts and roots have promising therapeutic application, but further research is needed to better understand the mechanisms of their action in the in vitro model.


Assuntos
Ácidos Cumáricos , Plectranthus , Humanos , Células A549 , Antibacterianos , Compostos Fitoquímicos
12.
Microsc Res Tech ; 87(3): 616-627, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38031715

RESUMO

Recent developments in the green synthesis of metallic nanoparticles (NPs) using phytoconstituents have attracted the attention of the global scientific community. The present study was designed to synthesize silver NPs (AgNPs) using Punica granatum and Plectranthus rugosus plant extracts. The fabricated AgNPs were characterized using UV-visible spectrophotometry (UV-Vis), Fourier-transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), and energy-dispersive x-ray spectroscopy (EDS). The shift in the color of the silver nitrate (AgNO3 ) solution after the addition of P. granatum and P. rugosus extracts indicated the synthesis of AgNPs. The effect of AgNO3 concentrations and pH on the synthesis of AgNPs was also evaluated. The findings of this study suggest that AgNO3 concentration of 1 mM, reaction time of 1 h, and pH of 7 at room temperature were the best suited conditions for the synthesis of AgNPs. According to the FTIR analysis, amidic and carbonyl compounds were primarily responsible for the encapsulation of AgNPs. SEM investigations have shown irregularly shaped geometry with sizes of 35 nm (P. granatum) and 33 nm (P. rugosus) with low agglomeration. The prepared AgNPs exhibited good potential for 2,2-diphenyl-1-picrylhydrazyl radical scavenging, with values of 70% (P. granatum) and 68% (P. rugosus). Hence, we conclude that the leaves of P. granatum and P. rugosus are excellent material for designing of different plant-extracted-conjugated AgNPs for biomedical applications. RESEARCH HIGHLIGHTS: Preparation of the AgNPs using novel plants extracts. P. granatum and P. rugosus extract as reducing, capping, stabilizing, and optimizing agents. Thorough comparative characterization using UV-Vis spectrophotometer, FTIR, SEM, and EDS which is a first of its kind. Comparative antioxidant activity.


Assuntos
Nanopartículas Metálicas , Plectranthus , Punica granatum , Microscopia Eletrônica de Varredura , Nanopartículas Metálicas/química , Espectroscopia de Infravermelho com Transformada de Fourier , Prata , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Antibacterianos/química
13.
Cardiovasc Ther ; 2023: 9948707, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38024105

RESUMO

Plectranthus barbatus, popularly known as Brazilian boldo, is used in Brazilian folk medicine to treat cardiovascular disorders including hypertension. This study investigated the chemical profile by UFLC-DAD-MS and the relaxant effect by using an isolated organ bath of the hydroethanolic extract of P. barbatus (HEPB) leaves on the aorta of spontaneously hypertensive rats (SHR). A total of nineteen compounds were annotated from HEPB, and the main metabolite classes found were flavonoids, diterpenoids, cinnamic acid derivatives, and organic acids. The HEPB promoted an endothelium-dependent vasodilator effect (~100%; EC50 ~347.10 µg/mL). Incubation of L-NAME (a nonselective nitric oxide synthase inhibitor; EC50 ~417.20 µg/mL), ODQ (a selective inhibitor of the soluble guanylate cyclase enzyme; EC50 ~426.00 µg/mL), propranolol (a nonselective α-adrenergic receptor antagonist; EC50 ~448.90 µg/mL), or indomethacin (a nonselective cyclooxygenase enzyme inhibitor; EC50 ~398.70 µg/mL) could not significantly affect the relaxation evoked by HEPB. However, in the presence of atropine (a nonselective muscarinic receptor antagonist), there was a slight reduction in its vasorelaxant effect (EC50 ~476.40 µg/mL). The addition of tetraethylammonium (a blocker of Ca2+-activated K+ channels; EC50 ~611.60 µg/mL) or 4-aminopyridine (a voltage-dependent K+ channel blocker; EC50 ~380.50 µg/mL) significantly reduced the relaxation effect of the extract without the interference of glibenclamide (an ATP-sensitive K+ channel blocker; EC50 ~344.60 µg/mL) or barium chloride (an influx rectifying K+ channel blocker; EC50 ~360.80 µg/mL). The extract inhibited the contractile response against phenylephrine, CaCl2, KCl, or caffeine, similar to the results obtained with nifedipine (voltage-dependent calcium channel blocker). Together, the HEPB showed a vasorelaxant effect on the thoracic aorta of SHR, exclusively dependent on the endothelium with the participation of muscarinic receptors and K+ and Ca2+ channels.


Assuntos
Hipertensão , Peumus , Plectranthus , Ratos , Animais , Vasodilatadores/farmacologia , Vasodilatação , Brasil , Ratos Endogâmicos SHR , Inibidores Enzimáticos/farmacologia , Endotélio Vascular
14.
Molecules ; 28(21)2023 Oct 25.
Artigo em Inglês | MEDLINE | ID: mdl-37959680

RESUMO

The Ethiopian potato (Plectranthus edulis) is an annual tuber crop indigenous to Ethiopia. The crop is underutilized and not much studied despite its high yield of starch, which has a good potential to contribute to the effort in meeting the quickly growing demand for starch. In this study, the effects of the ecotype and isolation methods on the physicochemical, functional, structural, and crystalline properties of starches were evaluated. Starches were isolated from two Ethiopian potato ecotypes (Loffo and Chanqua) using distilled water (DW), 0.01% sodium metabisulphite (SMS), and 1M sodium chloride (NaCl) in the isolation media. The results showed that the lowest starch yield was obtained from Chanqua using DW (97.4%), while the maximum was from Loffo using SMS (99.3%). The L* (lightness) and whiteness values of the starches obtained from Loffo were higher than those of Chanqua starches, with NaCl and SMS extractants yielding the highest values. The bulk density, water activity (aw), pH, proximate composition (moisture content, protein, ash, fat, crude fiber, and carbohydrate contents), and techno-functional properties were established. The majority of these parameters varied depending on both the isolation method and the ecotype. The crystallinity pattern of all starches showed B-type diffraction, with differences in diffraction peak intensities between all starches. FTIR tests showed structural changes as a function of the ecotype and isolation procedure used. The Loffo ecotype exhibited considerably better results, and the SMS isolation method was found to be the most effective way to acquire the highest starch quality in most of the characteristics evaluated.


Assuntos
Plectranthus , Solanum tuberosum , Amido/química , Solanum tuberosum/química , Ecótipo , Cloreto de Sódio , Água , Amilose/química
15.
Int J Biol Macromol ; 252: 126423, 2023 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-37604418

RESUMO

The innovation of this study was to develop a novel biodegradable intelligent packaging based on chitosan/fucoidan combined with different amounts (1, 3 and 5 wt% on chitosan basis) of coleus grass (Plectranthus scutellarioides) leaves anthocyanins (CGL) to monitor the spoilage of salmon (Salmo salar L.). The addition of fucoidan improved the barrier and mechanical properties of the chitosan films (CS) due to hydrogen bonds and intermolecular electrostatic interactions. Moreover, the addition of CGL not only improved the physical properties but also improved the biological activity of chitosan/fucoidan film (CF). The DPPH and ABTS radical scavenging activity of CF contained 5 wt% CGL was 1.83 and 1.75 times than CF, respectively. The inhibition zone size of CF films containing 5 wt% CGL (CF-5%CGL) was approximately 2.04 (Escherichia coli) and 2.16 (Staphylococcus aureus) times higher than that of CF. Moreover, CF-CGL displayed obvious color changes in different pH environments and is highly sensitive to ammonia gas. The CF-CGL has visible color changes during the monitoring of salmon spoilage and extended the shelf life of salmon. According to our findings, CF-CGL film might be employed as a possible intelligent packaging material for monitoring and preserving salmon in the future.


Assuntos
Quitosana , Coleus , Plectranthus , Salmo salar , Animais , Quitosana/química , Antocianinas/química , Embalagem de Alimentos , Poaceae , Concentração de Íons de Hidrogênio
16.
Molecules ; 28(15)2023 Jul 26.
Artigo em Inglês | MEDLINE | ID: mdl-37570622

RESUMO

The use of medicinal plants to treat inflammatory conditions and painful processes has attracted the attention of scientists and health professionals due to the evidence that natural products can promote significant therapeutic benefits associated with fewer adverse effects compared to conventional anti-inflammatory drugs. The genus Plectranthus is composed of various plants with pharmacological potential, which are used to treat various diseases in traditional communities worldwide. The present study systematically reviewed Plectranthus species with anti-inflammatory and analgesic potential. To this end, a systematic review was conducted following the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) protocol. The search was conducted on the following databases: PubMed, ScienceDirect, SciVerse Scopus, and Web of Science. Different combinations of search terms were used to ensure more excellent article coverage. After the selection, a total of 45 articles were included in this review. This study identified twelve Plectranthus species indicated for the treatment of different inflammatory conditions, such as wounds, fever, bronchitis, abscess, asthma, hepatitis, labyrinthitis, tonsillitis, and uterine inflammation. The indications for pain conditions included headache, sore throat, heartburn, menstrual cramp, colic, toothache, stomachache, migraine, chest pain, abdominal pain, local pain, labor pain, and recurring pain. Among the listed species, ten plants were found to be used according to traditional knowledge, although only four of them have been experimentally studied. When assessing the methodological quality of preclinical in vivo assays, most items presented a risk of bias. The SR results revealed the existence of different Plectranthus species used to treat inflammation and pain. The results of this systematic review indicate that Plectranthus species have the potential to be used in the treatment of diseases with an inflammatory component, as well as in the management of pain. However, given the risk of biases, the experimental analysis of these species through preclinical testing is crucial for their safe and effective use.


Assuntos
Fitoterapia , Plectranthus , Feminino , Gravidez , Humanos , Etnofarmacologia , Dor Abdominal , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Inflamação , Compostos Fitoquímicos
17.
Toxicon ; 232: 107212, 2023 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-37419284

RESUMO

The hepatoprotective activity of ethanolic of Plectranthus amboinicus Lour Spreng leaf extract (PEE) on blood biochemical profiles, non-specific immune system, liver histology were evaluated in rats induced DMBA. Twenty five female rats were divided into five groups, each with 5 rats. The negative control group (NC) received only food and water. The positive control group (PC) administered orally DMBA 20 mg/kg body weight (bw) once every four days for 32 days. The treatment groups received the PEE with three different doses of 175 (T1), 350 (T2), 700 (T3) mg/kg bw, respectively for 27 days after DMBA induction. At the end of the treatment, blood samples were collected to investigate the levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), bilirubin, total protein, albumin and globulin as well as the hematological parameter, such as neutrophils, monocyte, mean corpuscular hemoglobin (MCH), mean corpuscular volume (MCV), mean corpuscular hemoglobin concentration (MCHC), and red cell distribution width (RDW) were monitored. The results showed an increased level in ALT, AST, ALP, and bilirubin in the PC group. However, the T3 group (PEE 700 mg/kg) showed a significant decrease value (p < 0.05) in ALT, ALP, and bilirubin compared to the PC group. Our finding revealed that all PEE treatments had a significant increase (p < 0.05) in the total protein, albumin and globulin compared to the PC group. The neutrophils (18.60 ± 4.64) and monocytes (61.40 ± 4.99) are lowest in the T2 groups as well as the value of MCH, RDW and MCV were significantly alleviated compared to all other groups. Histopathological observation demonstrated that the administration of PEE improved hepatocyte architecture and reduced the number of necrosis and hydrophilic degeneration. In conclusion, PEE has hepatoprotective activity by improving liver function, enhancing the non-specific immune system and recovering histopathological hepatocytes in rats exposed to DMBA.


Assuntos
Extratos Vegetais , Plectranthus , Ratos , Feminino , Animais , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Alanina Transaminase , Aspartato Aminotransferases , Bilirrubina
18.
Asian Pac J Cancer Prev ; 24(3): 881-887, 2023 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-36974541

RESUMO

BACKGROUND AND OBJECTIVE: Oral cancer is a commonly encountered type of cancer with multifactorial etiology. The number of oral cancer cases are increasing in the recent past. Advancements in cancer therapy are continuously evolving. In spite of that, the survival rate is very low along with adverse effects associated with each treatment modality. This poses a need for a constant search for newer or alternative treatment options. Herbal medicines or plant-based medicines are derived from plant sources. Evidence supports that incorporating herbal medicines in cancer therapy offers many advantages. Hence, exploring plant species for anticarcinogenic properties can potentially benefit cancer therapy. Studies show that the two medicinal herbs Plectranthus amboinicus (Indian borage, Karpooravalli) and Glycyrrhiza glabra (Liquorice, Athimathuram) have shown excellent anticancer activity on various cancers. The present study aimed to evaluate and assess the anticancer property of two medicinal plants Plectranthus amboinicus (Indian borage, Karpooravalli) and Glycyrrhiza glabra (Liquorice, Athimathuram) on oral cancer (KB) cell line. MATERIALS AND METHODS: Ethanolic extracts of leaves of Plectranthus amboinicus and roots of Glycyrrhiza glabra were prepared. The oral cancer (KB) cell line was procured and cultured. Cell viability (MTT) assay was performed using various concentrations of both the plant extracts on oral cancer cells. The percentage of cell viability for each concentration was calculated and the IC50 value was derived for the two plant extracts. RESULTS: The results revealed a significant decrease in the percentage of viable cells with increasing concentration of the extracts. The IC50 values of Plectranthus amboinicus and Glycyrrhiza glabra were 53.0 µg/ml and 43.6 µg/ml respectively. On comparing the anticancer effect of the two extracts, Glycyrrhiza glabra was more cytotoxic than Plectranthus amboinicus on oral cancer (KB) cells. CONCLUSION: The two medicinal plants Plectranthus amboinicus and Glycyrrhiza glabra exhibited potent anticancer activity against oral cancer (KB) cells.


Assuntos
Glycyrrhiza , Neoplasias Bucais , Plantas Medicinais , Plectranthus , Humanos , Extratos Vegetais/farmacologia , Linhagem Celular , Neoplasias Bucais/tratamento farmacológico
19.
Front Endocrinol (Lausanne) ; 14: 1130003, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36926021

RESUMO

Introduction: In obese humans, Coleus forskohlii root extract (CF) protects against weight gain owing to the presence of forskolin, an adenylate cyclase (AC) activator. As AC increases intracellular cyclic adenosine monophosphate (cAMP) levels in osteoblasts that has an osteogenic effect, we thus tested the skeletal effects of a standardized CF (CFE) in rats. Methods: Concentrations of forskolin and isoforskolin were measured in CFE by HPLC. CFE and forskolin (the most abundant compound present in CFE) were studied for their osteogenic efficacy in vitro by alkaline phosphatase (ALP), cAMP and cyclic guanosine monophosphate (cGMP) assays. Femur osteotomy model was used to determine the osteogenic dose of CFE. In growing rats, CFE was tested for its osteogenic effect in intact bone. In adult ovariectomized (OVX) rats, we assessed the effect of CFE on bone mass, strength and material. The effect of forskolin was assessed in vivo by measuring the expression of osteogenic genes in the calvarium of rat pups. Results: Forskolin content in CFE was 20.969%. CFE increased osteoblast differentiation and intracellular cAMP and cGMP levels in rat calvarial osteoblasts. At 25 mg/kg (half of human equivalent dose), CFE significantly enhanced calcein deposition at the osteotomy site. In growing rats, CFE promoted modeling-directed bone formation. In OVX rats, CFE maintained bone mass and microarchitecture to the level of sham-operated rats. Moreover, surface-referent bone formation in CFE treated rats was significantly increased over the OVX group and was comparable with the sham group. CFE also increased the pro-collagen type-I N-terminal propeptide: cross-linked C-telopeptide of type-I collagen (PINP : CTX-1) ratio over the OVX rats, and maintained it to the sham level. CFE treatment decreased the OVX-induced increases in the carbonate-to-phosphate, and carbonate-to-amide-I ratios. CFE also prevented the OVX-mediated decrease in mineral crystallinity. Nanoindentation parameters, including modulus and hardness, were decreased by OVX but CFE maintained these to the sham levels. Forskolin stimulated ALP, cAMP and cGMP in vitro and upregulated osteogenic genes in vivo. Conclusion: CFE, likely due to the presence of forskolin displayed a bone-conserving effect via osteogenic and anti-resorptive mechanisms resulting in the maintenance of bone mass, microarchitecture, material, and strength.


Assuntos
Osteogênese , Plectranthus , Feminino , Ratos , Humanos , Animais , Colforsina/farmacologia , Fosfatase Alcalina , Ovariectomia/efeitos adversos , Colágeno
20.
Chem Biodivers ; 20(3): e202200691, 2023 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-36692091

RESUMO

Plectranthus amboinicus (Lour.) Spreng, known as the Indian borage or Mexican mint, is one of the most documented species in the family Lamiaceae for its therapeutic and pharmaceutical values. It is found in the tropical and subtropical regions of the world. The leaf essential oil has immense medicinal benefits like treating illnesses of the skin and disorders like colds, asthma, constipation, headaches, coughs, and fevers. After analyzing earlier reports with regard to the quantity and quality of leaf oil yield, we discovered that the germplasm taken from Odisha is preferable to other germplasms. The objective of the present work is to evaluate the free radical scavenging activity and bactericidal effect of leaf essential oil (EO) of Plectranthus amboinicus (Lour.) Spreng collected from the state of Odisha, India. The hydro distillation technique has been used for essential oil extraction. Upon GC/MS analysis, approximately 57 compounds were identified with Carvacrol as the major compound (peak area=20.25 %), followed by p-thymol (peak area=20.17 %), o-cymene (peak area=19.41 %) and carene (peak area=15.89 %). On evaluation of free radical scavenging activity, it was recorded that the best value of inhibitory concentration, was for DPPH with IC50 =18.64 ppm and for H2 O2 with IC50 =9.35 ppm. The EO showed efficient bactericidal effect against both gram positive (Mycobacterium smegmatis, Staphylococcus aureus, Enterococcus faecium) and gram negative (Escherichia coli, Vibrio cholerae, Klebsiella pneumoniae) bacteria studied through well diffusion method. Fumigatory action of the essential oil was found against M. smegmatis, the model organism for tuberculosis study. Alamar Blue assay, gave a result with MIC value for M. smegmatis i. e., 0.12 µg/ml and the MBC value of 0.12 µg/ml. Hence, P. amboinicus found in Odisha can be suggested as an elite variety and should be further investigated for efficient administration in drug formulation.


Assuntos
Óleos Voláteis , Plectranthus , Antibacterianos/farmacologia , Antibacterianos/análise , Radicais Livres , Testes de Sensibilidade Microbiana , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Folhas de Planta/química , Plectranthus/química , Mycobacterium smegmatis/efeitos dos fármacos
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