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1.
Andrologia ; 53(6): e14046, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-33756011

RESUMO

Gross alterations in the morphology of spermatozoa, teratozoospermia, invariably render them incapable of fertilisation. One of the contributory factors to teratozoospermia is failure of spermatozoon to shed the cytoplasmic droplet even after their arrival at epididymis. Quassia amara and quassin are of medicinal value with special reference to malaria. Nevertheless, there are also reports implicating Quassia/quassin in male reproductive toxicity. We were interested in finding if its therapeutic application would jeopardise male fertility. So, we tested it for male reproductive toxicity by analysing, among other aspects, abnormal sperm morphologies, and made a systematic analysis of the spermatozoa of treated mice before they are spermiated and until they arrive at the cauda epididymis. The spermatozoa not only failed to shed the cytoplasmic droplet during epididymal transit but swell to a very large size and were angulated, resulting in Dag-like defect or lasso shape. A link between cytoplasmic droplet that was retained and lasso shape of tail was indicated. This article traces the structural changes in spermatozoa that lead to angulation, flexion and coiling of the tail, caused due to retention of cytoplasmic droplet, and explains one of the mechanisms of toxicant-induced teratozoospermia.


Assuntos
Quassia , Quassinas , Animais , Epididimo , Masculino , Camundongos , Extratos Vegetais/toxicidade , Espermatozoides
2.
J Ethnopharmacol ; 267: 113546, 2021 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-33181284

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Quassia amara L. recently came into the spotlight in French Guiana, when it became the object of a biopiracy claim. Due to the numerous use records throughout the Guiana shield, at least since the 18th century, a thorough investigation of its origin seemed relevant and timely. In the light of the Convention on Biological Diversity (CBD) and the Nagoya protocol, questions about the origin of local knowledge are important to debate. AIM OF THE STUDY: Defining cultural biogeography as the dynamics through space and time of biocultural complexes, we used this theoretical framework to shed light on the complex biogeographical and cultural history of Q. amara. We explored in particular the possible transfer of medicinal knowledge on an Old World species to a botanically related New World one by enslaved Africans in Suriname. MATERIALS AND METHODS: Historical and contemporary literature research was performed by means of digitized manuscripts, archives and databases from the 17th to the 21st century. We retrieved data from digitized herbarium vouchers in herbaria of the Botanic Garden Meise (Belgium); Naturalis Biodiversity Center (the Netherlands); Missouri Botanical Garden, the Smithsonian National Museum of Natural History, the Field Museum (USA); Royal Botanic Gardens Kew (UK); the IRD Herbarium, French Guiana and the Museum National d'Histoire Naturelle (France). Vernacular names were retrieved from literature and herbarium specimens and compared to verify the origin of Quassia amara and its uses. RESULTS: Our exploration of digitized herbarium vouchers resulted in 1287 records, of which 661 were Q. amara and 636 were Q. africana. We observed that the destiny of this species, over at least 300 years, interweaves politics, economy, culture and medicine in a very complex way. Quassia amara's uses are difficult to attribute to specific cultural groups: the species is widely distributed in Central and South America, where it is popular among many ethnic groups. The species spread from Central to South America during the early 18th century due to political and economic reasons. This migration possibly resulted from simultaneous migration by religious orders (Jesuits) from Central America to northern South America and by Carib-speaking Amerindians (from northern South America to Suriname). Subsequently, through colonial trade networks, Q. amara spread to the rest of the world. The absence of African-derived local names in the Guiana shield suggests that Q. africana was not sufficiently familiar to enslaved Africans in the region that they preserved its names and transferred the associated medicinal knowledge to Q. amara. CONCLUSIONS: Cultural biogeography has proven an interesting concept to reconstruct the dynamics of biocultural interactions through space and time, while herbarium databases have shown to be useful to decipher evolution of local plant knowledge. Tracing the origin of a knowledge is nevertheless a complex adventure that deserves time and interdisciplinary studies.


Assuntos
Escravização , Conhecimentos, Atitudes e Prática em Saúde/etnologia , Medicina Tradicional , Fitoterapia , Extratos Vegetais/farmacologia , Política , Quassia , Características Culturais , Escravização/história , Etnobotânica , Guiana Francesa , História do Século XVII , História do Século XVIII , História do Século XIX , História do Século XX , História do Século XXI , Medicina Tradicional/história , Fitoterapia/história , Extratos Vegetais/história , Extratos Vegetais/isolamento & purificação , Quassia/química , Quassia/classificação
3.
Biomed Pharmacother ; 99: 198-204, 2018 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29334662

RESUMO

BACKGROUND: Tetrapleura tetraptera (TT) and Quassia undulata (QU) are two predominant tropical ethnobotanicals with various medicinal values but are commonly used in folklore for the treatment of mental illness without justifiable mechanisms of action. AIM OF THE STUDY: To investigate the effects of aqueous extracts from TT fruits and QU leaves on the spatial and non-spatial working memory, antioxidant status and activities of neuronal marker enzymes of scopolamine-induced amnesic rats and thus, understand the possible mechanism of action of these plants. MATERIALS AND METHODS: Fifty-five albino rats were divided into eleven groups. Group I (normal rats) received normal saline (p.o), Group II-V (normal rats) administered with 50 and 300 mg/kg of each extract group VI (induced rats) received 2 mg/kg of scopolamine (i.p.), groups VII-X (induced rats) pretreated with 50 and 300 mg/kg of TT and QU extracts (p.o) before scopolamine administration, group XI (induced rats) treated with 2.5 mg/kg of donepezil. The treatment lasted for 14 days and amnesia was induced by a single dose of 2 mg/kg of scopolamine on the last day. Spatial (Y-maze) and non-spatial (novel objectect recoginiton test) working memories of the rats were tested. Thereafter, the animals were sacrificed and homogenates of isolated brain samples were assayed for cholinesterase activity and malondialdehyde (MDA) content. The phenolic characterisation of the samples was also carried out using HPLC-DAD chromatography. RESULTS: Administration of 2 mg/kg of scopolamine brought about a decrease in spatial and non-spatial memory indeces, increase in acetylcholinesterase and butyrylcholinesterase activities, as well as increased MDA content compared to the control. However, pretreatment with both extracts improved both spatial and non-spatial working memories and ameliorated the increased enzyme activities and MDA contents. Furthermore, the HPLC-DAD characterization of the extracts revealed the presence of p-coumaric acid, rutin, catechin, ellagic acid, quercetin, caffeic acid, chlorogenic acid and galic acid. CONCLUSION: The ability of the extracts to improved cognitive function and ameliorate impairment in cholinergic enzyme activities and antioxidant status in scopolamine-induced amnesic rats could help justify the possible neuroprotective properties of TT and QU and also explain possible mechanism of action of these ethnobotanicals as obtained in folklore medical practices.


Assuntos
Amnésia/tratamento farmacológico , Amnésia/fisiopatologia , Antioxidantes/farmacologia , Colinérgicos/farmacologia , Memória de Curto Prazo/efeitos dos fármacos , Extratos Vegetais/uso terapêutico , Quassia/química , Tetrapleura/química , Acetilcolinesterase/metabolismo , Animais , Encéfalo/enzimologia , Cromatografia Líquida de Alta Pressão , Etnobotânica , Comportamento Exploratório , Feminino , Peroxidação de Lipídeos/efeitos dos fármacos , Aprendizagem em Labirinto/efeitos dos fármacos , Extratos Vegetais/farmacologia , Ratos , Escopolamina , Água/química
4.
J Ethnopharmacol ; 206: 290-297, 2017 Jul 12.
Artigo em Inglês | MEDLINE | ID: mdl-28576580

RESUMO

Biopiracy accusations are common in the world of biodiversity research. At the end of 2015, a French NGO accused researchers from the Institut de Recherche pour le Développement (IRD) of biopiracy. These researchers had applied for a patent for a natural bioactive molecule against malaria and cancer, the Simalikalactone E, isolated from Quassia amara L. (Simaroubaceae) leaves. This biopiracy allegation triggered a huge wave of attacks from the media and social networks, and vehement recrimination from political officials in French Guiana against researchers who have been accused of ethical misconduct, by stealing the traditional knowledge of indigenous people. These accusations were made in the contentious context of the ratification of the Nagoya Protocol in the frame of implementing the French law on biodiversity, nature and landscapes. So, in an atmosphere of heightened emotions it is crucial to understand the issues behind these accusations. We describe herein the genesis of our discovery, present the detractors' arguments, and discuss the consequences of such biopiracy denunciations for scientific research. We also address our concerns about the gap between rhetoric and reality and the real impact of the Nagoya Protocol on biodiversity conservation.


Assuntos
Patentes como Assunto , Plantas Medicinais , Quassia , Biodiversidade , Guiana Francesa
5.
Phytochem Anal ; 28(3): 210-216, 2017 May.
Artigo em Inglês | MEDLINE | ID: mdl-28028887

RESUMO

INTRODUCTION: The genus Quassia is a promising source of secondary metabolites with biological potential including antimalarial and cytotoxic activities. Limited data are available on the phytochemistry and pharmacology of Quassia silvestris Cheek & Jongkind, a Cameroonian medicinal plant used to treat various ailments. OBJECTIVES: To carry out the bioassay-guided fractionation and LC-HR-ESI-MS analyses of the leaves extract from Q. silvestris; to purify the active fractions and isolate the major compounds using different chromatographic and spectroscopic methods. The obtained compounds will be evaluated for their biological activity. MATERIAL AND METHODS: Following the cytotoxic screening and LC-HR-ESI-MS profiling of fractions obtained from partition of the methanolic extract of Q. silvestris leaves, the CH2 Cl2 -soluble fraction which exhibited the highest cytotoxicity was retained for further investigations. RESULTS: Sixteen squalene-derived metabolites were identified with oxasqualenoid derivatives being the most predominant. Among the isolates, structure elucidation of two new oxasqualenoids quassiols E (1) and F (2), were achieved by NMR (one-dimensional (1D) and two-dimensional (2D)) and MS methods. The newly characterised compounds 1 and 2, together with the known tetraol (3) and 3-oxo-oleanoic acid (16) displayed moderate cytotoxicity. CONCLUSION: The identification and structural characterisation of highly oxidised squalene derived metabolites from this plant may provide important insight data for further pharmacological investigations. The LC-HR-ESI-MSn method reported here could be developed as a rapid and efficient tool for the analyses of structurally related compounds in the genera Quassia, Simarouba, and Eurycoma of the subfamily Simarouboideae. Copyright © 2016 John Wiley & Sons, Ltd.


Assuntos
Antineoplásicos Fitogênicos/química , Cromatografia Líquida/métodos , Quassia/química , Espectrometria de Massas por Ionização por Electrospray/métodos , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Fracionamento Químico , Furanos/química , Humanos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Extratos Vegetais/análise , Folhas de Planta/química , Plantas Medicinais/química , Piranos/química , Quassia/classificação , Esqualeno/química
6.
Appetite ; 107: 268-273, 2016 12 01.
Artigo em Inglês | MEDLINE | ID: mdl-27522037

RESUMO

Triggering of gastro-intestinal bitter taste receptors might have implications for appetite and food intake, but the evidence in humans is mixed and limited to acute studies. We previously reported that 15-days consumption of drinks with purified Hoodia gordonii extract and its taste-matched control both produced similar, significant energy intake (EI) reductions in females in an in-patient setting, with no significant differences between treatments. In that study the control was matched to Hoodia flavour and bitterness using Raisin Flavour (RF), Sucrose Octa Acetate (SOA) and Quassia Extract (QE). As triggering of gastrointestinal bitter receptors might have produced shared effects on EI, our objective here was to assess the effects of sustained exposure to capsules containing the same bitter RF + SOA + QE mix itself on EI, compared to a non-bitter placebo. In this randomized, double-blind study, sixty slightly overweight women in parallel groups consumed twice-daily capsules without (placebo) or with the tastant mixture (0.88 mg SOA, 0.088 mg QE, 0.22 mg RF) on days 1-14. On day 0 all subjects received placebo capsules at 0800 and 1600, ad libitum meals at 0900, 1300, 1700, and snacks after 1900. On day 14 these test procedures were repeated. Changes in EI on days 14 versus 0 between treatment groups were assessed using ANCOVA. Total EI differences on days 14 versus 0 were not significant (mean active-placebo treatment difference -109 kcal, SE 71, P = 0.13), nor was this significant when analyzed separately for each meal within the test day. Body weight changes were negligible. In conclusion, sustained exposure to these encapsulated bitter tastants did not significantly affect EI in overweight females.


Assuntos
Ingestão de Energia , Sobrepeso/dietoterapia , Paladar , Adolescente , Adulto , Apetite , Índice de Massa Corporal , Cápsulas , Método Duplo-Cego , Feminino , Humanos , Pessoa de Meia-Idade , Extratos Vegetais/administração & dosagem , Quassia/química , Lanches , Sacarose/administração & dosagem , Sacarose/análogos & derivados , Resultado do Tratamento , Vitis/química , Adulto Jovem
8.
Shokuhin Eiseigaku Zasshi ; 56(5): 185-93, 2015.
Artigo em Japonês | MEDLINE | ID: mdl-26537647

RESUMO

A novel HPLC-based method employing molar absorption coefficient ratios to 4-hydroxybenzoic acid (4HBA) was developed for the determination of quassin and neoquassin in Jamaica quassia extract, which is used as a food additive in Japan. Based on comparisons of quantitative NMR (qNMR) spectra and HPLC chromatograms of an artificial mixture of quassin, neoquassin, and 4HBA, the molar absorption coefficient ratios of quassin and neoquassin to 4HBA were determined as 0.84 and 0.85, respectively. Quassin and neoquassin were quantified in food additives by qNMR and HPLC based on molar absorption coefficient ratios using 1,4-bis(trimethylsilyl)benzene-d4 and 4HBA as internal standards, respectively. The differences in quantitation values between qNMR and HPLC analyses were below 1.2%. Our proposed novel HPLC-based quantitation method employing the molar absorption coefficient ratios is a reliable tool for determining levels of quassin and neoquassin in food additives and processed foods.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Aditivos Alimentares/química , Extratos Vegetais/química , Quassia/química , Quassinas/análise , Análise de Alimentos/métodos , Hidroxibenzoatos , Espectroscopia de Ressonância Magnética/métodos
9.
Phytochem Anal ; 26(2): 111-8, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25431121

RESUMO

INTRODUCTION: Simalikalactone E (SkE) from Quassia amara, has been proved to be a valuable anti-malarial and anti-cancer compound. As SkE is very scarce, methods of quantitation are needed in order to optimise its isolation process and to determine pharmacokinetic data. OBJECTIVE: To validate methods using liquid chromatography coupled to mass spectrometry for the quantitation of SkE in plant extracts and in biological fluids. METHODS: High- and ultrahigh-performance liquid chromatography (UHPLC) coupled to ion trap mass spectrometry (MS) with single ion monitoring detection and to triple quadrupole-linear ion trap tandem mass spectrometry with multiple reaction monitoring detection methods were developed. Validation procedure was realised according to the International Conference on Harmonisation guideline. Methanol extracts of dried Quassia amara leaves, and mouse-blood samples obtained after various routes of administration, were analysed for SkE. RESULTS: Methods were validated and gave similar results regarding the content of SkE expressed per kilogram of dry leaves in the traditional decoction (160 ± 12 mg/kg) and in the methanol extract (93 ± 2 mg/kg). The recovery of the analyte from mouse blood ranged from 80.7 to 119.8%. Simalikalactone E was only detected using UHPLC-MS/MS (0.2 ± 0.03 mg/L) in mouse blood after intravenous injection: none was detected following intraperitoneal or oral gavage administration of SkE. CONCLUSION: The LC-MS methods were used for the quantitation of SkE in plant extracts and in mouse blood. These methods open the way for further protocol optimisation of SkE extraction and the determination of its pharmacokinetic data.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Quassia/química , Quassinas/isolamento & purificação , Espectrometria de Massas em Tandem/métodos , Animais , Masculino , Camundongos , Extratos Vegetais/química , Plantas Medicinais , Quassinas/sangue , Quassinas/química
10.
Artigo em Inglês | MEDLINE | ID: mdl-25392586

RESUMO

BACKGROUND: Botanical and microbial insecticides have been increasingly used for the control of mosquito given their efficacy and documented nontoxic effects on non-target organisms. The discovery of new insecticides is imperative because of the development of resistance by the mosquitoes to the readily available insecticides. The aim of this study was therefore to isolate and characterize compounds from a local medicinal plant, Quassia africana Baill and Baill (Simaroubaceae) that were toxic to Anopheles gambiae. MATERIAL AND METHODS: The methanol extracts of the leaves, stem and roots of Quassia africana were tested against fourth instar larvae of An. gambiae. The root extract was partitioned into hexane, chloroform and ethyl acetate and the resulting extracts screened for larvicidal properties. The extracts and the fraction with the highest bioactivity were subjected to repeated column chromatography and isolated compounds evaluated for potential toxicity to An. gambiae larvae. The structure of the active compound was elucidated using spectroscopic techniques. The root extract showed the strongest activity profile (LC50 = 17.58 µg/mL). The chloroform soluble fraction obtained after partitioning the crude extract into solvents based on polarities was the most toxic. Further bio-activity-guided chromatographic separation of the chloroform fraction of the root extract led to the identification and isolation of a simalikalactone D as the larvicidal compound in Q. africana (LC50 = 1.25 µg/mL). RESULTS: Results suggest that Q. africana may serve as a source for vector control agent for malaria. CONCLUSION: Simalikalactone D was identified as the larvicidal compound in Q. africana (LC50 = 1.25 µg/mL).


Assuntos
Anopheles/efeitos dos fármacos , Insetos Vetores/efeitos dos fármacos , Inseticidas/farmacologia , Malária , Extratos Vegetais/farmacologia , Quassia/química , Quassinas/farmacologia , Animais , Larva/efeitos dos fármacos , Malária/prevenção & controle , Malária/transmissão , Folhas de Planta , Raízes de Plantas
11.
J Ethnopharmacol ; 148(3): 895-900, 2013 Jul 30.
Artigo em Inglês | MEDLINE | ID: mdl-23711829

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Aqueous extracts from Ceiba pentandra (Malvaceae/Bombacoideae) and Quassia africana (Simaroubaceae) are used as crude medicines for the management of sickle cell anemia (SCA) in the Democratic Republic of Congo (DR Congo). Since it is postulated that the pathogenesis of SCA is associated with an increased blood coagulation activity, the present study is conducted to determine the effect of the two extracts on the coagulation by assessing the thrombin activity and the plasma clotting time. MATERIALS AND METHODS: Thrombin activity was measured by chromogenic assay in the presence of the aqueous extracts (10, 100 or 200 µg/ml); and plasma clotting times were measured by activated partial thromboplastin time (APTT) and prothrombin time (PT) in the presence of C. pentandra (10, 100 or 200 µg/ml) and Q. africana (5, 20 or 50 µg/ml). RESULTS: Reduced thrombin activity and prolonged plasma clotting time measured by APTT were observed in the presence of C. pentandra extract only. However, plasma clotting time measured by PT was not modified by the use of the two extracts. CONCLUSIONS: This study suggests that the aqueous extract of C. pentandra may contain active components that reduce the thrombin activity and prolong the plasma clotting time by affecting the coagulation intrinsic pathway.


Assuntos
Coagulação Sanguínea/efeitos dos fármacos , Ceiba , Extratos Vegetais/farmacologia , Anemia Falciforme , República Democrática do Congo , Humanos , Medicina Tradicional Africana , Tempo de Tromboplastina Parcial , Casca de Planta , Raízes de Plantas , Tempo de Protrombina , Quassia , Trombina/metabolismo
12.
J Drugs Dermatol ; 12(3): 312-5, 2013 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-23545914

RESUMO

BACKGROUND: Seborrheic dermatitis (SD) is a chronic mild skin disorder with high prevalence. Various treatment options are available, including topical antifungals and anti-inflammatories. Antifungal and anti-inflammatory properties of Quassia amara have been reported. AIM: To check the efficacy and safety of a topical gel with 4% Quassia amara extract and compare it with topical 2% ketoconazole and 1% topical ciclopiroxolamine in the treatment of facial SD. METHODS: A group of 60 patients displaying facial SD were randomly distributed in 3 groups and given either a topical gel with 4% Quassia amara extract, a topical gel with 2% ketoconazole, or a topical gel with 1% ciclopirox olamine for 4 weeks. Disease severity was assessed at the start and weekly along treatment, as well as 4 weeks after the end of treatment. In each selected area, severity of erythema, scaling, pruritus, and papules were scored from 0 to 3, the sum of these values representing the score of SD on the face. This evaluation was conducted at each visit. The decrease in SD score with all 3 products was compared at each visit. At each stage, overall improvement, safety, and tolerability were also assessed. RESULTS: Of the 60 patients, 54 (90%) completed the study. The 3 therapeutic options resulted to be very effective, with a significant advantage in efficacy for 4% Quassia extract. For the other 2 drugs, the results were in line with those previously published in the literature. CONCLUSION: Topical gel with 4% Quassia extract represents a new, safe, and effective treatment for facial SD.


Assuntos
Antifúngicos/uso terapêutico , Dermatite Seborreica/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Quassia/química , Administração Cutânea , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Antifúngicos/administração & dosagem , Antifúngicos/efeitos adversos , Ciclopirox , Dermatite Seborreica/patologia , Método Duplo-Cego , Dermatoses Faciais/tratamento farmacológico , Dermatoses Faciais/patologia , Feminino , Géis , Humanos , Cetoconazol/administração & dosagem , Cetoconazol/uso terapêutico , Masculino , Pessoa de Meia-Idade , Extratos Vegetais/administração & dosagem , Extratos Vegetais/efeitos adversos , Piridonas/administração & dosagem , Piridonas/uso terapêutico , Adulto Jovem
13.
Rev. bras. plantas med ; 15(3): 368-372, 2013. graf
Artigo em Inglês | LILACS | ID: lil-684153

RESUMO

The anti-hyperglycemic effect of wood powder of Quassia amara (QA) was evaluated in normal and in alloxan diabetes-induced rats. After a 12 h fast and glycemic check, the animals were orally given 0.9% of saline (control group), metformin (500 mg/kg) or QA (200 mg/kg) and, 30 minutes later, they received an oral glucose dose (1g/kg). The blood glucose level was measured after 30, 60, 90 and 120 minutes. From the oral glucose dose, QA showed anti-hyperglycemic effects, similar to metformin, only in the diabetic animals (p<0.01) when compared to the control group. Although the anti-hyperglycemic mechanism of action of QA was not investigated, a mechanism similar to metformin can be suggested, since both presented similar results for the conditions tested, that is, normal and diabetic rats. It is believed that the use of QA in diabetics could help to control the blood glucose levels and be useful as an alternative therapy.


O efeito anti-hiperglicemiante do pó do lenho de Quassia amara (QA) foi avaliado em ratos normais e diabéticos aloxana induzidos. Após jejum de 12 horas e verificação da glicemia, os animais receberam administração oral de salina 0.9% (grupo controle), metformina (500 mg/kg) ou QA (200 mg/kg) e 30 minutos depois carga oral de glicose (1g/kg). A glicemia foi medida nos próximos 30, 60, 90 e 120 minutos. A partir da carga oral de glicose, a QA mostrou efeito anti-hiperglicemiante, similar a metformina, somente nos animais diabéticos (p<0.01) quando comparados ao grupo controle. Embora o mecanismo de ação anti-hiperglicemiante da QA não tenha sido investigado, podemos sugerir um mecanismo semelhante à metformina, visto que ambos apresentaram resultados similares nas duas condições testadas, ou seja, animais normais e diabéticos. Acredita-se que o uso de QA, em diabéticos, possa auxiliar no controle da glicemia e servir como terapia alternativa.


Assuntos
Animais , Masculino , Ratos , Aloxano/efeitos adversos , Quassia/análise , Diabetes Mellitus/fisiopatologia
14.
Exp Parasitol ; 130(4): 341-7, 2012 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-22374406

RESUMO

Quassia amara L. (Simaroubaceae) is a species widely used as tonic and is claimed to be an efficient antimalarial all over the Northern part of the Amazon basin. Quassinoid compound Simalikalactone D (SkD) has been shown to be one of the molecules responsible for the antiplasmodial activity of a watery preparation made out of juvenile fresh leaves of this plant. Because of its strong antimalarial activity, we decided to have a further insight of SkD pharmacological properties, alone or in association with classical antimalarials. At concentrations of up to 200µM, we showed herein that SkD did not exert any apoptotic or necrotic activities in vitro on lymphoblastic cells. However, an antiproliferative effect was evident at concentrations higher than 45nM. SkD was inefficient at inhibiting heme biomineralization and the new permeability pathways induced by the parasite in the host erythrocyte membrane. With respect to Plasmodium falciparum erythrocytic stages, SkD was almost inactive on earlier and later parasite stages, but potently active at the 30th h of parasite cycle when DNA replicates in mature trophozoites. In vitro combination studies with conventional antimalarial drugs showed that SkD synergizes with atovaquone (ATO). The activity of ATO on the Plasmodium mitochondrial membrane potential was enhanced by SkD, which on its own had a poor effect on this cellular parameter.


Assuntos
Antimaláricos/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Plasmodium yoelii/efeitos dos fármacos , Quassia/química , Quassinas/farmacologia , Linhagem Celular/efeitos dos fármacos , Permeabilidade da Membrana Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Membrana Eritrocítica/efeitos dos fármacos , Membrana Eritrocítica/metabolismo , Eritrócitos/efeitos dos fármacos , Eritrócitos/parasitologia , Heme/metabolismo , Humanos , Concentração Inibidora 50 , Extratos Vegetais/farmacologia , Folhas de Planta/química
15.
Bol. latinoam. Caribe plantas med. aromát ; 11(2): 172-187, mar. 2012. ilus
Artigo em Espanhol | LILACS | ID: lil-647629

RESUMO

Quassia amara L. popularly known as “quasia”, is a shrubby plant from Tropical America. The wood, bark and leave are used in either folk medicine or in procuring phytotherapeutic drugs. The aim of the present work was to analize morphoanatomical and micrographic features which might provide assistance in the identification, analysis and standardization of Quasia amara L wood, bark and leaves. Results. Anatomical study showed white yellowish and diffuse porous wood, confluent paratracheal parenchyma. Rays width 1 cell wide and 8-30 cells high. CaOx crystals are absent. Cortex, 1-4 mm thick, a periderm up to 12 layers phellem cells. Leaf, hipostomatic with dorsiventral mesophyll and high number of sclerosed idioblasts.


Quassia amara L. popularmente conocida como “quasia” es un planta arbustiva de América Tropical. El leño, corteza y hojas son usadas tanto en medicina popular como en la obtención de drogas fitoterapéuticas. El objetivo del presente trabajo es analizar características morfoanatómicas y micrográficas las cuales provean asistencia en la identificación, análisis y estandarización de la madera, corteza y hojas de Quassia amara L. Resultados. El estudio anatómico mostró leño, blanco amarillento, de porosidad difusa. Parénquima paratraqueal confluente. Radios de 1 célula de ancho y 8-30 hileras de alto. Faltan cristales CaOx. Corteza, 1-4 mm de espesor, una peridermis de hasta 12 estratos de células de súber. Hoja, hipoestomática, con mesófilo dorsiventral, con elevado número de idioblastos esclerosados.


Assuntos
Casca de Planta/anatomia & histologia , Folhas de Planta/anatomia & histologia , Madeira/anatomia & histologia , Quassia/anatomia & histologia , Casca de Planta/ultraestrutura , Folhas de Planta/ultraestrutura , Madeira/ultraestrutura , Fotomicrografia , Quassia/ultraestrutura
16.
Artigo em Inglês | MEDLINE | ID: mdl-23983328

RESUMO

The effects of Quassia amara extract (Q. amara) and its bioactive principles-quassin and 2-methoxycanthin-6-one on gastric ulceration were studied in albino rats. Q. amara (200-800 mg/kg p.o.; 5-20 mg/kg i.p) and 2-methoxycanthin-6-one (12.5, 25.0 and 50.0 mg/kg p.o; 1, 2 and 4 mg/kg i.p) but not quassin (12.5, 25.0 and 50 mg/kg p.o; 1, 2 and 4 mg/kg i.p) significantly inhibited gastric ulceration induced by indomethacin (40mg/kg). Administration of Q. amara (800 mg/kg p.o and 20 mg/kg i.p) and 2-methoxycanthin-6-one (12.5 mg/kg p.o; 4 mg/kg i.p) caused between 77%-85% cytoprotection against indomethacin (40 mg/kg, i.p) - induced gastric ulceration. Quassin did not cause any significant change in indomethacin-induced gastric ulceration. The inhibition of gastric ulceration produced by Q. amara and 2-methoxycanthin-6 one was accompanied by significant dose-dependent decreases (P< 0.01) in total gastric acidity. To investigate the probable mechanism of action, the individual effects of the extract and its principles alone and in combination with histamine (1 mg/kg) or cimetidine (0.12 mg/kg) on gastric acid secretion in situ were studied. Q. amara (20 mg/kg) and 2-methoxycanthin-6-one (4 mg/kg) but not quassin significantly (P< 0.01) inhibited the basal and histamine-induced gastric acid secretion. Inhibition of gastric acid secretion by Q. amara and 2-methoxycanthin-6-one was accentuated by cimetidine. The results suggest that Q. amara and its bioactive principle, 2-methoxycanthin-6-one possess antiulcer activity probably acting via histamine H2 receptor. This could be a potential source of potent and effective antiulcer agents.


Assuntos
Antiulcerosos/uso terapêutico , Carbolinas/uso terapêutico , Ácido Gástrico/metabolismo , Fitoterapia , Extratos Vegetais/uso terapêutico , Quassia/química , Úlcera Gástrica/tratamento farmacológico , Animais , Antiulcerosos/farmacologia , Carbolinas/farmacologia , Cimetidina/farmacologia , Relação Dose-Resposta a Droga , Histamina/farmacologia , Indometacina , Masculino , Extratos Vegetais/farmacologia , Quassinas/farmacologia , Ratos , Ratos Wistar , Úlcera Gástrica/induzido quimicamente
17.
J Clin Pharmacol ; 52(1): 84-8, 2012 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-21343346

RESUMO

BACKGROUND: There are various treatment options available for rosacea, depending on the subtype, but treatment is still generally unsatisfactory. Some studies have reported antiparasitic and anti-inflammatory properties of Quassia amara. AIM: To check the efficacy and safety of a topical gel with 4% Quassia amara extract in the treatment of various grades of rosacea. METHODS: A group of 30 patients with various grades of rosacea (I-IV) were investigated in a single-center, open-label study. They were treated with a topical gel with 4% Quassia amara extract for 6 weeks. Response was evaluated by the flushing, erythema, telangiectasia, papules, and pustules scores. At the end of therapy, overall improvement, safety, and tolerability were assessed. RESULTS: Twenty-seven of 30 patients (90%) completed the study. The treatment resulted to be very effective, and the results achieved were in line with those published with topical metronidazole and azelaic acid. Safety and tolerability were excellent. CONCLUSION: Topical quassia extract could be a new, efficient, and safe weapon in the armamentarium for the management of rosacea.


Assuntos
Extratos Vegetais/uso terapêutico , Quassia , Rosácea/tratamento farmacológico , Administração Tópica , Adulto , Idoso , Idoso de 80 Anos ou mais , Feminino , Géis , Humanos , Masculino , Pessoa de Meia-Idade , Resultado do Tratamento , Adulto Jovem
18.
Chin J Integr Med ; 17(12): 933-6, 2011 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-22139545

RESUMO

OBJECTIVE: To evaluate the therapeutic efficacy and side effects of oral Fructus bruceae oil combined with radiotherapy in the treatment of esophageal cancer. METHODS: A total of 80 patients with esophageal cancer were equally and randomly divided into two groups. The patients in Group A were treated with radiotherapy (60-65 Gy, 6-7 weeks) and oral Fructus bruceae oil (20 mL, 3 times per day for 12 weeks), while the patients in Group B were treated with radiotherapy alone. The short-term effect was evaluated by Response Evaluation Criteria in Solid Tumors (RECIST) and quality of life (QOL) was evaluated by the Karnofsky scoring (KFS). The outcome measures included complete remission (CR) rate, partial remission (PR) rate, effective rate as CR+PR, patients' QOL and adverse effects. RESULTS: After 12-week treatment, the CR and CR+PR were significantly higher in Group A than those in Group B (P <0.05). There was an improvement in esophageal obstruction of 87.5% and 60.0%, respectively, and in KFS of 84.6% and 43.9%, respectively, in Groups A and B. CONCLUSION: Oral medication with oral Fructus bruceae oil could effectively improve the efficacy of radiotherapy in esophageal cancer, including a reduction in esophageal obstruction, and also reduce the side effects of radiotherapy; thus it would be very promising for clinical application.


Assuntos
Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/uso terapêutico , Neoplasias Esofágicas/tratamento farmacológico , Neoplasias Esofágicas/radioterapia , Administração Oral , Terapia Combinada , Medicamentos de Ervas Chinesas/efeitos adversos , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Fitoterapia , Quassia , Fatores de Tempo , Resultado do Tratamento
19.
Phytother Res ; 25(12): 1806-12, 2011 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-21480415

RESUMO

The aim of the present study was to evaluate the efficacy of a standardized methanol extract of Quassia amara L. (Family: Simaroubaceae) in nicotinamide-streptozotocin-induced diabetic rats. Non insulin dependent diabetes mellitus was induced by streptozotocin in rats pre-treated with nicotinamide. Diabetic rats were treated with oral doses of Quassia amara extract (QaE; 100 and 200 mg/kg) or glibenclamide (10 mg/kg; as standard). QaE and glibenclamide were administered as a suspension in 0.3% carboxy methyl cellulose for 14 days. Control animals received an equal volume of vehicle. Blood samples were collected by retro-orbital puncture on day 14, 1 h after last treatment. Plasma glucose, insulin and lipid parameters (total cholesterol, LDL-C, HDL-C and triglycerides) were measured using commercially available biochemical kits. The oral glucose tolerance test was performed to evaluate the effect of the extract on peripheral glucose utilization in normal rats. Both doses of QaE significantly (p < 0.01) reduced elevated fasting blood glucose levels in diabetic rats. In the oral glucose tolerance test, QaE treatment significantly increased (p < 0.05) the glucose tolerance compared with the vehicle. QaE and glibenclamide, effectively normalized dyslipidemia associated with streptozotocin-induced diabetes. The findings of the present study indicate that Quassia amara extract may be potentially valuable in the treatment of diabetes and associated dyslipidemia.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/farmacologia , Fitoterapia , Extratos Vegetais/farmacologia , Quassia/química , Animais , Glicemia , Colesterol/sangue , Diabetes Mellitus Experimental/induzido quimicamente , Teste de Tolerância a Glucose , Glibureto/administração & dosagem , Glibureto/farmacologia , Hipoglicemiantes/administração & dosagem , Masculino , Niacinamida , Extratos Vegetais/administração & dosagem , Ratos , Estreptozocina , Triglicerídeos/sangue
20.
Rev Biol Trop ; 59(1): 487-99, 2011 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-21513206

RESUMO

In Latin America and the Caribbean, precious wood species like mahoganies (Swietenia spp.) and cedars (Cedrela spp.) are seriously injured by the mahogany shootborer, Hypsipyla grandella (Zeller) (Lepidoptera: Pyralidae) larva, which bores into the main shoot of trees. In previous experiments focused on searching for a preventive method for managing this pest, a wood extract of bitterwood, Quassia amara L. ex Blom (Simaroubaceae) had been shown to cause phagodeterrence to larvae. Therefore, three fractions (water, methanol and diethyl ether) of a wood extract were tested for their phagodeterrence to larvae, by means of laboratory and greenhouse trials. Phagodeterrence was assessed by determining their effect on foliage consumption, mortality and signs of damage (number of orifices, sawdust piles, fallen shoots, number of tunnels and tunnel length) caused by larvae on Spanish cedar (C. odorata). Both the methanol and diethyl ether fractions caused phagodeterrence, by strongly reducing foliage consumption and signs of damage, while not causing larval mortality. The lowest concentration at which phagodeterrence was detected for the methanol fraction corresponded to 0.0625%, which is equivalent to a 1.0% of the bitterwood crude extract. However, results with the diethyl ether fraction were unsatisfactory, as none of the treatments differed from the solvent, possibly because of an adverse effect of the solvent on foliar tissues. Phagodeterrent principles from Q. amara derivatives may play an important role in dealing with H. grandella if they are complemented with other integrated pest management preventative tactics.


Assuntos
Lepidópteros/efeitos dos fármacos , Extratos Vegetais/farmacologia , Quassia/química , Animais , Comportamento Alimentar/efeitos dos fármacos , Larva/efeitos dos fármacos , Fatores de Tempo , Madeira/química
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