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1.
J Ethnopharmacol ; 330: 118200, 2024 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-38621467

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Malaria eradication has been a major goal of the Indonesian government since 2020. Medicinal plants, such as Strychnos lucida R. Br., are empirically used to treat malaria through traditional preparation methods. However, the safety and efficacy of these plants have not yet been confirmed. Therefore, further investigations are necessary to confirm the safety and efficacy of S. lucida as an antimalarial agent. AIMS OF THE STUDY: To quantify the concentration of brucine in the S. lucida extract, determine the acute oral toxicity of the standardized extract, and evaluate the in vivo antimalarial potency of S. lucida tablet (SLT). MATERIALS AND METHODS: Acute oral toxicity of S.lucida extract was determined using the Organization for Economic Co-operation and Development 420 procedure, and the analytical method for brucine quantification was validated using high-performance liquid chromatography. In addition, antimalarial activity was determined using the Peter's four-day suppressive method. RESULTS: Acute toxicity analysis revealed S. lucida as a low-toxicity compound with a cut-off median lethal dose of 2000-5000 mg/kg body weight [BW], which was supported by the hematological and biochemical profiles of the kidneys, liver, and pancreas (p > 0.05). Extract standardization revealed that S. lucida contained 3.91 ± 0.074% w/w brucine, adhering to the limit specified in the Indonesian Herbal Pharmacopeia. Antimalarial test revealed that SLT inhibited the growth of Plasmodium berghei by 27.74-45.27%. Moreover, SLT improved the hemoglobin and hematocrit levels. White blood cell and lymphocyte counts were lower in the SLT-treated group than in the K (+) group (p < 0.05). CONCLUSION: Histopathological and biochemical evaluations revealed that S. lucida extract was safe at a dose of 2000 mg/kg BW with low toxicity. SLT inhibited Plasmodium growth and improved the hemoglobin, hematocrit, and red blood cell profiles. Additionally, SLT reduced the lymphocyte and WBC counts and increased the monocyte and thrombocyte counts as part of the immune system response against Plasmodium infection.


Assuntos
Antimaláricos , Extratos Vegetais , Plasmodium berghei , Strychnos , Comprimidos , Antimaláricos/toxicidade , Antimaláricos/farmacologia , Animais , Extratos Vegetais/farmacologia , Extratos Vegetais/toxicidade , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Camundongos , Masculino , Strychnos/química , Plasmodium berghei/efeitos dos fármacos , Administração Oral , Estricnina/análogos & derivados , Estricnina/toxicidade , Estricnina/farmacologia , Feminino , Malária/tratamento farmacológico , Testes de Toxicidade Aguda , Dose Letal Mediana
2.
J Ethnopharmacol ; 283: 114704, 2022 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-34601082

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Spiny monkey orange (Strychnos spinosa Lam.) is an African endemic fruit tree that is widely consumed by humans and animals for its nutritional value. In folk medicine, different parts of S. spinosa are widely used for the management of the health and well-being of humans and livestock. AIM: We provide a critical appraisal on the ethnobotanical uses, nutritional and pytochemical as well as the biological activities of S. spinosa. METHODS: Articles were mined from online databases such as Google Scholar, PubMed, Science Direct, SciELO and SpringerLink. We captured research outputs that aligned with the scope of the review. RESULTS: Strychnos spinosa remains a commonly consumed fruit due to its high nutritional (e.g. carbohydrates, crude protein and fats) content and energy. In folk medicine, different parts of S. spinosa are prescribed as remedy for diverse medical conditions especially for treating malaria, diabetes, snakebites, skin-related conditions and sexually transmitted infections in humans as well as sleeping sickness in livestock. Together with essential oils, more than 25 compounds have been profiled using Gas chromatography-mass spectrometry (GC-MS), and approximately 45 compounds have been isolated and structurally elucidated using diverse spectroscopic techniques such as UV-visible, Infrared (IR), Nuclear Magnetic Resonance (NMR) and mass spectroscopy (MS). Strychnos spinosa exerts varying degrees of biological activities against different microorganisms (bacteria and fungi) and parasites (plasmodia, trypanosomes and ticks) responsible for many diseases in humans and livestock. Furthermore, low to moderate enzyme-inhibitory effects of S. spinosa extracts suggest its ability to mitigate pains, inflammations and diabetics as well as snakebite venom. Increasing evidence from the in vivo studies support the use of the plant as a popular remedy for managing diabetics in folk medicine. The low cytotoxic effect of the plant extracts against different cell lines could be an indication of its relative safety. CONCLUSION: Strychnos spinosa exhibits various health-promoting benefits due to its diverse nutritional and phytochemical constituents. Given that the majority of the existing evidence on these aforementioned therapeutic properties and safety are in vitro-based, the clinical significance of these results remain limited.


Assuntos
Medicinas Tradicionais Africanas/métodos , Extratos Vegetais/farmacologia , Strychnos/química , Animais , Etnobotânica , Etnofarmacologia , Frutas , Humanos , Extratos Vegetais/efeitos adversos
3.
Rapid Commun Mass Spectrom ; 34 Suppl 3: e8683, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31783430

RESUMO

RATIONALE: Monoterpene indole alkaloids (MIAs) are a large group of biologically active compounds produced by hundreds of plant species in numerous plant families, such as Apocynaceae, Loganiaceae and Rubiaceae. Although this diversity is biosynthetically intermediated by strictosidine, there are no works focused on the fragmentation patterns under collision-induced dissociation of strictosidine-derived alkaloids. METHODS: Initially, the alkaloid fingerprint of Strychnos peckii was established using leaf spray with tandem mass spectrometry (LS-MS/MS). Then, high-performance liquid chromatography coupled to tandem mass spectrometry (HPLC/MS/MS) analyses were carried out to focus on the patterns of neutral losses in product ion scan experiments with the leaf aqueous extract. Finally, the product ion spectra from a set of presumable strictosidine-type derivatives were analyzed and organized via molecular networking (MN), and dereplicated by manual interpretation of MS/MS spectra. RESULTS: LS-MS/MS allowed the tentative identification of strictosidine-derived alkaloids in the leaves of S. peckii, showing useful neutral losses for the dereplication of strictosidine analogues by HPLC/MS/MS experiments. The use of MN combined with manual interpretation of the fragmentation patterns highlighted characteristic fragmentation pathways, and allowed the tentative identification of strictosidine, desoxycordifoline, strictosidinic acid, 10-hydroxystrictosidine, 5-carboxystrictosidine, lyaloside, 3,4-dehydrostrictosidine and strictosidine lactam. CONCLUSIONS: The use of MN combined with the analysis of the fragmentation patterns proved to be a useful strategy for the dereplication of strictosidine-derived MIAs from S. peckii, highlighting known and unprecedented structures, as well as useful diagnostic product ions. Therefore, this workflow is an effective approach for the characterization of strictosidine-type alkaloids in future dereplication works.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Alcaloides de Triptamina e Secologanina/análise , Strychnos/química , Espectrometria de Massas em Tandem/métodos , Curare/química , Folhas de Planta/química , Alcaloides de Triptamina e Secologanina/química , Alcaloides de Triptamina e Secologanina/metabolismo , Processamento de Sinais Assistido por Computador
4.
Drug Chem Toxicol ; 43(5): 539-545, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30212238

RESUMO

Strychnos pseudoquina is a plant species whose stem bark is used as bitter tonic beverage. The phytochemical analysis, as well as quantification of phenolic constituents and antioxidant activity of ethanolic extracts from S. pseudoquina stem bark, and leaves were conducted. The extracts were tested for mutagenicity (Ames test) and DNA-damaging activity (Plasmid Cleavage test). Leaves recorded the largest amount of flavonoids. The performed high-performance liquid chromatography (HPLC) showed flavonoids such as isorhamnetin and strychnobiflavone (phytochemical markers of the investigated species) in stem barks, but not in leaves. The proanthocyanidin content and antioxidant activity were significantly higher in stem barks than in leaves. Stem bark and leaf extracts presented mutagenic activity against TA98 and TA100 strains with, and without, metabolic activation (S9). The Plasmid Cleavage test did not indicate DNA-damaging activity. Our results suggest that extracts deriving from S. pseudoquina should be used with extreme caution, mainly the stem bark extract, which is widely used in folk medicine.


Assuntos
Dano ao DNA , Fenóis/análise , Casca de Planta/química , Extratos Vegetais/química , Extratos Vegetais/toxicidade , Strychnos/química , Antioxidantes/análise , Antioxidantes/farmacologia , Etanol/química , Flavonoides/análise , Testes de Mutagenicidade , Compostos Fitoquímicos/análise , Folhas de Planta/química , Caules de Planta/química , Proantocianidinas/análise , Salmonella typhimurium/efeitos dos fármacos , Salmonella typhimurium/genética
5.
Planta Med ; 84(12-13): 881-885, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29929205

RESUMO

Strychnogucine B is a bisindole alkaloid previously isolated from Strychnos icaja that possesses promising in vitro antiplasmodial properties. This compound was synthesized in four steps from (-)-strychnine. As no acute toxicity was observed at the highest tested cumulative dose of 60 mg/kg, its in vivo antimalarial activity was determined intraperitoneally at 30 mg/kg/d in a Plasmodium berghei murine model. In the Peters's 4-d suppressive test, this alkaloid suppressed the parasitaemia by almost 36% on day 5 and 60% on day 7 compared to vehicle-treated mice. In addition to this interesting antimalarial activity, it showed moderate in vitro antitrypanosomal activity but no in vivo activity in an acute Trypanosoma brucei model. It was also inactive in vitro on Leishmania mexicana promastigotes. This highlights its selective antimalarial efficacy and leads to further investigation to assess its potential as new antimalarial lead compound.


Assuntos
Alcaloides/farmacologia , Antimaláricos/farmacologia , Plasmodium berghei/efeitos dos fármacos , Estricnina/análogos & derivados , Strychnos/química , Tripanossomicidas/farmacologia , Alcaloides/química , Animais , Antimaláricos/química , Modelos Animais de Doenças , Feminino , Leishmania mexicana/efeitos dos fármacos , Camundongos , Estricnina/química , Estricnina/farmacologia , Tripanossomicidas/química , Trypanosoma brucei brucei/efeitos dos fármacos
6.
PLoS One ; 13(4): e0195786, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29649320

RESUMO

Natural substances are used in folk medicines to treat injuries. Strychnos pseudoquina has scarring, antipyretic, and antimalarial actions. The present study aimed to analyze the effect of S. pseudoquina on cutaneous wound healing in rats. The S. pseudoquina extract was submitted to phytochemical prospection. The levels of flavonoids and total phenolic compounds in the extract were 50.7 mg/g and 2.59 mg/g, respectively. Thirty Wistar rats were individualized in cages with food and water ad libitum (registration no. 730/2014). After anesthesia, three circular wounds (12mm diameter) were made in the animals, which were randomly separated into five treatments: Sal, saline; VO, ointment vehicles (lanolin and Vaseline); SS, positive control (silver sulfadiazine 1%); LE 5, freeze-dried extract 5%; and LE 10, lyophilized extract 10%. The animals were treated with the ointment daily for 21 days. Every seven days, the area and the rate of wound contraction were evaluated. Tissue samples were removed for histopathological analysis of the number of mast cells, elastic and collagen fibers, and biochemical analyses, quantification of malondialdehyde (MDA), carbonylated proteins (PCN), superoxide dismutase (SOD), catalase (CAT), transforming growth factor ß (TGF-ß), Interleukin 10 (IL-10) and tumor necrosis factor (TNF). The number of mast cells, collagen and elastic fibers in the rat wounds were higher in the treatments with the plant. The extract also stimulated the activity of antioxidant enzymes, particularly SOD, presenting high levels, and maintained low levels of PCN. The TGF-ß and IL-10 concentration was higher in the LE5 and LE10 treatment of the extract than in the Sal, OV and SS treatments on day 7. The ointment based on S. pseudoquina closed the wound faster and accelerated wound healing in animals.


Assuntos
Cicatriz/patologia , Extratos Vegetais/farmacologia , Strychnos/química , Cicatrização/efeitos dos fármacos , Animais , Cicatriz/tratamento farmacológico , Colágeno/genética , Colágeno/metabolismo , Citocinas/genética , Citocinas/metabolismo , Expressão Gênica , Imuno-Histoquímica , Masculino , Ratos , Ferimentos e Lesões/tratamento farmacológico , Ferimentos e Lesões/etiologia , Ferimentos e Lesões/patologia
7.
Biomed Res Int ; 2017: 9538351, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29057272

RESUMO

The effect of topical application of ointment based on Strychnos pseudoquina hydroethanolic extract in the cutaneous wounds healing in diabetic rats was evaluated. Samples of S. pseudoquina were submitted to phytochemical prospection and in vitro antioxidant assay. Thirty Wistar rats were divided into 5 groups: Sal-wounds treated with 0.9% saline solution; VH-wounds treated with 0.6 g of lanolin cream (vehicle); SS-wounds treated with silver sulfadiazine cream (10 mg/g); ES5- and ES10-wounds treated with an ointment of S. pseudoquina extract, 5% and 10%, respectively. Fragments of wounds were removed for histological and biochemical analysis every 7 days during 21 days. ES showed equivalent levels per gram of extract of total phenols and flavonoids equal to 122.04 mg for TAE and 0.60 mg for RE. The chlorogenic acid was one of the major constituents. S. pseudoquina extract presented high antioxidant potential in vitro. ES5 and ES10 showed higher wound healing rate and higher amount of cells, blood vessels, and type III and I collagen. The oxidative stress markers were lower in the ES5 and ES10 groups, while the antioxidants enzymes levels were higher. Ointment based on S. pseudoquina extract promotes a fast and efficient cutaneous repair in diabetic rats.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Tipo 1/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Cicatrização/efeitos dos fármacos , Animais , Cicatriz/tratamento farmacológico , Cicatriz/patologia , Diabetes Mellitus Experimental/complicações , Diabetes Mellitus Experimental/patologia , Diabetes Mellitus Tipo 1/complicações , Diabetes Mellitus Tipo 1/patologia , Humanos , Pomadas/administração & dosagem , Pomadas/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Fitoterapia/métodos , Extratos Vegetais/química , Ratos , Ratos Wistar , Pele/efeitos dos fármacos , Pele/patologia , Strychnos/química
8.
BMC Complement Altern Med ; 17(1): 13, 2017 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-28056932

RESUMO

BACKGROUND: Malaria is a major public health problem in the world which is responsible for death of millions particularly in sub-Saharan Africa. Today, the control of malaria has become gradually more complex due to the spread of drug-resistant parasites. Medicinal plants are the unquestionable source of effective antimalarials. The present study aimed to evaluate antiplasmodial activity and acute toxicity of the plant Strychnos mitis in Plasmodium berghei infected mice. METHODS: Standard procedures were employed to investigate acute toxicity and 4-day suppressive effect of crude aqueous and hydro-methanolic extracts of the leaves of Strychnos mitis against P. berghei in Swiss albino mice. Water, n-hexane and chloroform fractions, obtained from crude hydro-methanolic extract, were also tested for their suppressive effect against P. berghei. RESULTS: All crude extracts revealed no obvious acute toxicity in mice up to the highest dose administered (2000 mg/kg). All crude and solvent fractions of the leaves of Strychnos mitis inhibited parasitaemia significantly (p < 0.01). At the highest dose of 600 mg/kg, both aqueous and hydro-methanolic extracts demonstrated higher performance with 95.5 and 93.97% parasitaemia suppression, respectively. All doses of crude extracts and fractions of leaves of Strychnos mitis prolonged survival time of infected mice dose dependently. The highest two doses of the crude aqueous and hydro-methanolic extracts, and chloroform and aqueous fractions prevented weight loss in a dose dependent manner. Whereas, all doses of n-hexane fraction prevented loss of body weight but not in a dose dependent manner. The crude aqueous extract at the doses of 400 mg/kg and 600 mg/kg and hydro-methanolic extract at all dose levels significantly (p < 0.01) prevented packed cell volume reduction. Crude aqueous extract at a dose of 600 mg/kg and hydro-methanolic extract at all dose levels significantly prevented temperature reduction. Phytochemical screening of the crude aqueous and hydro-methanolic extracts revealed the presence of alkaloids, anthraquinones, glycosides, terpenoids, saponins, tannins and phenols. CONCLUSION: The results of this study provide support the traditional therapeutic use of Strychnos mitis for treatment of malaria. However, further in-depth study is needed to evaluate the potential of the plant towards the development of new antimalarial agent.


Assuntos
Antimaláricos/administração & dosagem , Malária/parasitologia , Extratos Vegetais/administração & dosagem , Plasmodium berghei/efeitos dos fármacos , Strychnos/química , Animais , Antimaláricos/química , Antimaláricos/isolamento & purificação , Humanos , Malária/tratamento farmacológico , Masculino , Camundongos , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Plasmodium berghei/fisiologia
9.
Nat Prod Res ; 31(2): 149-154, 2017 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-27545867

RESUMO

A novel pyrrole alkaloid, strychnuxin (1), along with five known compounds (2-6) was isolated from the fruit peels of Strychnos nux-blanda. The structures of all the isolated compounds (1-6) were fully characterised using spectroscopic data, as well as comparison with the previous literature data. Moreover, all isolated compounds were assessed for their α-glucosidase and acetylcholinesterase inhibitory activities.


Assuntos
Frutas/química , Pirróis/química , Pirróis/farmacologia , Strychnos/química , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Extratos Vegetais/química , Sementes/química , Espectrometria de Massas por Ionização por Electrospray , Espectrofotometria Ultravioleta , Tailândia , alfa-Glucosidases
10.
J Appl Microbiol ; 121(6): 1519-1529, 2016 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-27566664

RESUMO

AIMS: To investigate the anti-HSV and anti-inflammatory effects of a standardized ethyl acetate extract (SEAE) prepared with the stem bark of Strychnos pseudoquina, along with two isolated compounds: quercetin 3-O-methyl ether (3MQ) and strychnobiflavone (SBF). METHODS AND RESULTS: The mechanisms of action were evaluated by different methodological strategies. SEAE and SBF affected the early stages of viral infection and reduced HSV-1 protein expression. Both flavonoids elicited a concentration-dependent inhibition of monocyte chemoattractant protein-1 (MCP-1), whereas 3MQ reduced the chemokine release more significantly than SBF. Conversely, both compounds stimulated the production of the cytokines TNF-α and IL-1-ß in LPS-stimulated cells, especially at the intermediate and the highest tested concentrations. CONCLUSIONS: SEAE and SBF interfered with various steps of HSV replication cycle, mainly adsorption, postadsorption and penetration, as well as with ß and γ viral proteins expression; moreover, a direct inactivation of viral particles was observed. Besides, both flavonoids inhibited MCP-1 selectively, a feature that may be beneficial for the development of new anti-HSV agents. SIGNIFICANCE AND IMPACT OF THE STUDY: The results indicated that the samples present anti-HSV and anti-inflammatory activities, at different levels, which is an interesting feature since cold and genital sores are accompanied by an inflammation process.


Assuntos
Antivirais/farmacologia , Biflavonoides/farmacologia , Herpesvirus Humano 1/efeitos dos fármacos , Quercetina/análogos & derivados , Strychnos/química , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Antivirais/química , Biflavonoides/química , Brasil , Linhagem Celular , Quimiocina CCL2/metabolismo , Chlorocebus aethiops , Citocinas/metabolismo , Herpesvirus Humano 1/fisiologia , Humanos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Quercetina/química , Quercetina/farmacologia , Células Vero
11.
Nat Prod Commun ; 11(6): 709-10, 2016 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-27534097

RESUMO

Strychnuxin (1), a new non-glucosidic iridoid, together with four known compounds, IX (2), loganetin (3), loganin (4) and sweroside (5), were isolated from the roots of Strychnos nux-blanda. The structures of all isolated compounds (1-5) were elucidated through their physical properties and by the use of spectroscopic methods, as well as comparisons with the previous literature. To the best of our knowledge, this is the first isolation of compounds 1-5 from this plant. All isolated compounds were evaluated for their in vitro cytotoxicity against five human cancer cell lines.


Assuntos
Medicamentos de Ervas Chinesas/química , Iridoides/química , Strychnos/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Humanos , Iridoides/isolamento & purificação , Iridoides/farmacologia , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Raízes de Plantas/química
12.
Artigo em Inglês | MEDLINE | ID: mdl-28480356

RESUMO

BACKGROUND: The study was aimed at determining the anti-inflammatory activity of fractions and extracts obtained from Strychnos spinosa leaves on a mediator of inflammation nitric oxide (NO). MATERIALS AND METHODS: Leaves were extracted with acetone and separated into fractions with different polarities by solvent-solvent fractionation. The Griess assay was used to determine the nitric oxide (NO) inhibitory activity. Cellular toxicity was determined by "using the MTT reduction assay". RESULTS: With the exception of the ethyl acetate fraction which had an IC50 >750 µg/mL, all extracts and fractions had significant nitric oxide-inhibitory activity. The most active being the water fraction, chloroform fraction and the dichloromethane/methanol extracts with IC50 values of 88.43 µg/mL, 96.72 µg/mL and 115.62 µg/mL, respectively. The extracts and fractions had low cytotoxicity on macrophage U937 cell lines. CONCLUSION: Extracts and fractions of Strychnos spinosa leaves may be promising sources of natural anti-inflammatory agents. Findings obtained from this study showed that Strychnos spinosa leaves possess promising anti-inflammatory action and could be used in the treatment of inflammation-related conditions.


Assuntos
Anti-Inflamatórios/farmacologia , Óxido Nítrico/antagonistas & inibidores , Extratos Vegetais/farmacologia , Folhas de Planta/química , Strychnos/química , Anti-Inflamatórios/química , Fracionamento Químico/métodos , Humanos , Extratos Vegetais/química , Células U937
13.
Nat Prod Res ; 30(4): 399-405, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-25752927

RESUMO

A new indole alkaloid strychnosinol (1) and a new phenolic-glycoside (2) were isolated from the bark and leaves of Strychnos fendleri Sprague & Sandwith, together with six known compounds reported for the first time in this species. The structures of these compounds were determined on the basis of spectroscopic data; mainly those obtained by using (1)H and (13)C NMR (1D and 2D) and mass spectrometry. Strychnosinol (1) and the phenolic glycoside (2) together with compounds 3-8 were evaluated for cytotoxicity against a panel of five tumour cell lines; IC50 values between 0.090 and 0.227 µM for the human tumour cell lines were observed for compound 2.


Assuntos
Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Indóis/isolamento & purificação , Indóis/farmacologia , Strychnos/química , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Fenóis/isolamento & purificação , Fenóis/farmacologia , Casca de Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Sais de Tetrazólio , Tiazóis
14.
Parasitol Res ; 114(12): 4625-35, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-26346453

RESUMO

The present study aimed to investigate the in vitro antileishmanial activity of strychnobiflavone flavonoid against Leishmania infantum, as well as its mechanism of action, and evaluate the ex vivo biodistribution profile of the flavonoid in naive BALB/c mice. The antileishmanial activity (IC50 value) of strychnobiflavone against stationary promastigote and amastigote-like stages of the parasites was of 5.4 and 18.9 µM, respectively; with a 50% cytotoxic concentration (CC50) value of 125.0 µM on murine macrophages, resulting in selectivity index (SI) of 23.2 and 6.6, respectively. Amphotericin B, used as a positive control, presented SI values of 7.6 and 3.3 for promastigote and amastigote-like stages of L. infantum, respectively. The strychnobiflavone was also effective in reducing in significant levels the percentage of infected macrophages, as well as the number of amastigotes per macrophage, after the treatment of infected macrophages using the flavonoid. By using different fluorescent probes, we investigated the bioenergetics metabolism of L. infantum promastigotes and demonstrated that the flavonoid caused the depolarization of the mitochondrial membrane potential, without affecting the production of reactive oxygen species. In addition, using SYTOX(®) green as a fluorescent probe, the strychnobiflavone demonstrated no interference in plasma membrane permeability. For the ex vivo biodistribution assays, the flavonoid was labeled with technetium-(99m) and studied in a mouse model by intraperitoneal route. After a single dose administration, the scintigraphic images demonstrated a highest uptake by the liver and spleen of the animals within 60 min, resulting in low concentrations after 24 h. The present study therefore demonstrated, for the first time, the antileishmanial activity of the strychnobiflavone against L. infantum, and suggests that the mitochondria of the parasites may be the possible target organelle. The preferential distribution of this compound into the liver and spleen of the animals could warrant its employ in the treatment of visceral leishmaniasis.


Assuntos
Antiprotozoários/farmacologia , Flavonoides/administração & dosagem , Leishmania infantum/efeitos dos fármacos , Leishmaniose Visceral/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Strychnos/química , Animais , Antiprotozoários/isolamento & purificação , Permeabilidade da Membrana Celular/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Feminino , Flavonoides/isolamento & purificação , Humanos , Leishmania infantum/fisiologia , Leishmaniose Visceral/parasitologia , Camundongos , Camundongos Endogâmicos BALB C , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Extratos Vegetais/isolamento & purificação , Espécies Reativas de Oxigênio/metabolismo , Distribuição Tecidual
15.
Toxins (Basel) ; 7(1): 138-55, 2015 Jan 14.
Artigo em Inglês | MEDLINE | ID: mdl-25594733

RESUMO

Tibetan ethnomedicine is famous worldwide, both for its high effectiveness and unique cultural background. Many poisonous plants have been widely used to treat disorders in the Tibetan medicinal system. In the present review article, some representative poisonous plant species are introduced in terms of their significance in traditional Tibetan medicinal practices. They are Aconitum pendulum, Strychnos nux-vomica, Datura stramonium and Anisodus tanguticus, for which the toxic chemical constituents, bioactivities and pharmacological functions are reviewed herein. The most important toxins include aconitine, strychnine, scopolamine, and anisodamine. These toxic plants are still currently in use for pain-reduction and other purposes by Tibetan healers after processing.


Assuntos
Plantas Tóxicas , Aconitum/química , Aconitum/toxicidade , Animais , Humanos , Medicina Tradicional , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/toxicidade , Plantas Tóxicas/química , Plantas Tóxicas/toxicidade , Solanaceae/química , Solanaceae/toxicidade , Strychnos/química , Strychnos/toxicidade , Tibet
16.
Rev Environ Health ; 30(1): 19-23, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25411981

RESUMO

The role of water in our daily lives cannot be highlighted enough, and ensuring the availability of pure water is an urgent need. Bleaching powder (calcium hypochlorite) and Strychnos potatorum Linn. seeds are commonly used in water purification as a disinfectant and anticoagulant, respectively, yet their safety levels have not been analyzed so far. Hence, a genotoxic assessment was conducted using Allium cepa chromosome aberration assay. Reduction in mitotic index and increase in abnormality percentage was observed for both, but this effect was dose dependent. All values were statistically significant at p<0.05%. Bleaching powder was found to be cytotoxic and genotoxic compared with the control. Abnormality percentage was found to be significantly high when compared with the positive control. Chromosome aberrations like binucleate condition, micronuclei formation, stickiness, and lesions could only be observed in root meristems treated with positive control and bleaching powder. The seeds of S. potatorum expressed mild cytotoxicity, but the genotoxic effect was found to be negligible when compared with positive control. Other chromosome aberrations observed included chromosome bridges, c-metaphases, chromosome laggards, shift in microtubule organizing centre, polyploidy, early movement of chromosomes, vagrant chromosomes, as well as diagonal, disturbed, and scattered arrangement of chromosomes. Thus, the genotoxic effect of bleaching powder warns people to use a safer choice of S. potatorum in water purification, whenever possible, as in the condition of muddy, coagulated water.


Assuntos
Compostos de Cálcio/toxicidade , Aberrações Cromossômicas/induzido quimicamente , Sementes/química , Strychnos/química , Purificação da Água/métodos , Precipitação Química , Desinfetantes/química , Desinfetantes/toxicidade , Cebolas/efeitos dos fármacos , Raízes de Plantas/citologia
17.
Chin J Nat Med ; 12(10): 760-7, 2014 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-25443369

RESUMO

AIM: The application of strychnine (S) is limited due to its toxicity; strychnine N-oxide (SNO) is a derivative of strychnine. The aim was to employ zebrafish embryos to investigate and compare the developmental toxicity induced by S and SNO. METHODS: The toxicity of S and SNO was examined through the hatching rate and survival rate. Morphological changes of the zebrafish were observed with a dissecting microscope. Apoptosis was detected through acridine orange (AO) staining and flow cytometry. Apoptotic genes were measured by RT-PCR. RESULTS: Embryo malformation was observed in the embryos exposed to S at 200 µmol·L(-1). When SNO concentration was increased to 1 mmol·L(-1), scoliolosis, and pericardial edema could be seen in some embryos. Results from fluorescence microscopy and flow cytometry analysis showed that S at 200 µmol·L(-1) induced apoptosis, whereas the apoptotic rate in the SNO-treated group (200 µmol·L(-1)) was much lower than that in the S group. RT-PCR analysis showed that p53 mRNA expression and the ratio of Bax/Bcl-2 in the S group were significantly altered compared with the control group (*P < 0.05). Moreover, Bax mRNA expression in both S and SNO group were significantly different from that in the control group (**P < 0.01). CONCLUSION: These results lead to the conclusion that SNO has significantly lower toxicity than S in zebrafish embryos.


Assuntos
Óxidos N-Cíclicos/toxicidade , Medicamentos de Ervas Chinesas/toxicidade , Estricnina/análogos & derivados , Estricnina/toxicidade , Strychnos/química , Peixe-Zebra/embriologia , Animais , Apoptose/efeitos dos fármacos , Feminino , Masculino , Estresse Oxidativo/efeitos dos fármacos , Proteínas Proto-Oncogênicas c-bcl-2 , Strychnos/efeitos adversos , Proteína Supressora de Tumor p53/genética , Proteína Supressora de Tumor p53/metabolismo , Peixe-Zebra/genética , Peixe-Zebra/metabolismo , Proteínas de Peixe-Zebra/genética , Proteínas de Peixe-Zebra/metabolismo
18.
Hong Kong Med J ; 20(4): 343-6, 2014 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-25104008

RESUMO

Traditional Chinese medicine is commonly used locally, not only for disease treatment but also for improving health. Many people prepare soups containing herbs or herbal decoctions according to recipes and general herbal formulae commonly available in books, magazines, and newspapers without consulting Chinese medicine practitioners. However, such practice can be dangerous. We report five cases of poisoning from 2007 to 2012 occurring as a result of inappropriate use of herbs in recipes or general herbal formulae acquired from books. Aconite poisoning due to overdose or inadequate processing accounted for three cases. The other two cases involved the use of herbs containing Strychnos alkaloids and Sophora alkaloids. These cases demonstrated that inappropriate use of Chinese medicine can result in major morbidity, and herbal formulae and recipes containing herbs available in general publications are not always safe.


Assuntos
Aconitum/intoxicação , Alcaloides/intoxicação , Medicamentos de Ervas Chinesas/intoxicação , Medicina Tradicional Chinesa/efeitos adversos , Adulto , Idoso , Alcaloides/isolamento & purificação , Livros , Overdose de Drogas , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/química , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Sophora/química , Strychnos/química
19.
Trop Anim Health Prod ; 45(6): 1341-7, 2013 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-23456785

RESUMO

The efficacy of Solanum incanum and Strychnos spinosa aqueous fruit extracts was evaluated against cattle ticks in on-station experiments and laboratory tick bioassays. In the on-station experiment using cattle, fruit extracts were applied at three concentrations 5, 10, and 20 % (w/v) and compared with a commercial acaricide, Tickbuster (amitraz) spray (positive control) and no treatment (negative control). The treatments were applied at weekly intervals for 6 weeks as surface sprays on 32 Mashona cattle in a completely randomized design experiment. Ticks on individual cattle were identified, counted, and recorded daily. Peripheral blood samples were collected for parasite screening. In the laboratory, tick bioassays were conducted at four concentrations, 5, 10, 20, and 40% (w/v) fruit extracts compared to Tickbuster (amitraz) spray (positive control) and distilled water (negative control). The extracts were incubated with Rhipicephalus (Boophilus) decoloratus tick larvae and mortalities for each treatment level recorded after 24 and 48 h. The 5% Solanum incanum treatment had higher efficacy ratio (P < 0.05) than the other fruit extract concentrations of the same plant species. Efficacy ratio was higher (P < 0.05) in the 5% S. spinosa-treated cattle than in the untreated control but lower (P < 0.05) than that for the amitraz treatment. The bioassays indicated that there was a high efficacy ratio for the lowest fruit extract concentrations when ticks were exposed to acaricidal treatments for 48 h compared to 24 h. Overall, the results indicate that Solanum incanum and Strychnos spinosa individually have some acaricidal effect.


Assuntos
Acaricidas/efeitos adversos , Doenças dos Bovinos/prevenção & controle , Extratos Vegetais/efeitos adversos , Rhipicephalus/efeitos dos fármacos , Solanum/química , Strychnos/química , Infestações por Carrapato/veterinária , Animais , Bovinos , Doenças dos Bovinos/parasitologia , Relação Dose-Resposta a Droga , Frutas/efeitos adversos , Larva/efeitos dos fármacos , Larva/crescimento & desenvolvimento , Rhipicephalus/crescimento & desenvolvimento , Infestações por Carrapato/parasitologia , Infestações por Carrapato/prevenção & controle , Toluidinas/administração & dosagem
20.
Acta Pol Pharm ; 69(5): 939-43, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-23061291

RESUMO

The antidiabetic effect of seeds of Strychnos potatorum Linn. was evaluated in a model of diabetes mellitus using streptozotocin (40 mg/kg b.w., i.p.). Changes in fasting blood sugar were estimated periodically for 12 weeks along with weekly measurement of body weight, food and water intake for 4 weeks. The antidiabetic effects were compared with glipizide as the reference hypoglycemic drug. Strychnos potatorum Linn. (100 mg/kg p.o.) significantly reduced fasting blood sugar, the effects being comparable with glipizide (40 mg/kg, p.o.), an established hypoglycemic drug. It also increased body weight along with decreased food and water intake in streptozotocin-induced diabetic rats. Taken together, Strychnos potatorum Linn. shows promise as an effective hypoglycemic compound worthy of future pharmacological investigations.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Strychnos/química , Animais , Glicemia/efeitos dos fármacos , Peso Corporal/efeitos dos fármacos , Ratos , Ratos Wistar , Sementes/química
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