RESUMO
Background: There are thousands of species of known medicinal plants in the world. Ruta angustifolia L. has been widely used in traditional medication for jaundice and liver disease. Previous studies have shown that R. angustifolia leaves can inhibit the hepatitis C virus in Huhit culture cells, reduce the value of NS3 protein, and possess a synergistic effect in combination with antiviral drugs. Therefore, this plant is potential to be developed as a drug candidate. Characteristics of plants including microscopic, physicochemical properties, and phytochemical profiles are necessary information to ensure the quality of raw material in drug development. Objective: This study was carried out to examine the microscopic and physicochemical including the standardized parameter of R. angustifolia leaves to fulfil the quality raw materials as traditional medicine. Methods: Simplicia of R. angustifolia leaves obtained from Jombang, East Java, were observed under a microscope and determined its physicochemical properties referred to the Materia Medica Indonesia V. The TLC and HPLC profiles of extract were determined as well. Results: Microscopic analysis were conducted by transfection sections and the presence of epidermis cells, palisade, mesophyll with stomata, and Ca-oxalate crystal were found. The standard parameter obtained value of loss of drying, extractive value in water and ethanol, and ash value. The TLC and HPLC profiles of leaves extract demonstrated to contain with flavonoid, terpenoids, and alkaloids. Conclusion: Ruta angustifolia obtained from Jombang, east Java, has a specific character in microscopic analysis. The physicochemical properties analysis of R. angustifolia leaves as a raw material met the requirements according to Materia Medica Indonesia V.
RESUMO
BACKGROUND: Malaria continues to be a global problem due to the limited efficacy of current drugs and the natural products are a potential source for discovering new antimalarial agents. Therefore, the aims of this study were to investigate phytochemical properties, cytotoxic effect, antioxidant, and antiplasmodial activities of Sonchus arvensis L. leaf extracts both in vitro and in vivo. METHODS: The extracts from S. arvensis L. leaf were prepared by successive maceration with n-hexane, ethyl acetate, and ethanol, and then subjected to quantitative phytochemical analysis using standard methods. The antimalarial activities of crude extracts were tested in vitro against Plasmodium falciparum 3D7 strain while the Peter's 4-day suppressive test model with P. berghei-infected mice was used to evaluate the in vivo antiplasmodial, hepatoprotective, nephroprotective, and immunomodulatory activities. The cytotoxic tests were also carried out using human hepatic cell lines in [3(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] (MTT) assay. RESULT: The n-hexane, ethyl acetate, and ethanolic extracts of S. arvensis L. leaf exhibited good in vitro antiplasmodial activity with IC50 values 5.119 ± 3.27, 2.916 ± 2.34, and 8.026 ± 1.23 µg/mL, respectively. Each of the extracts also exhibited high antioxidant with low cytotoxic effects. Furthermore, the ethyl acetate extract showed in vivo antiplasmodial activity with ED50 = 46.31 ± 9.36 mg/kg body weight, as well as hepatoprotective, nephroprotective, and immunomodulatory activities in mice infected with P. berghei. CONCLUSION: This study highlights the antiplasmodial activities of S. arvensis L. leaf ethyl acetate extract against P. falciparum and P. berghei as well as the antioxidant, nephroprotective, hepatoprotective, and immunomodulatory activities with low toxicity. These results indicate the potential of Sonchus arvensis L. to be developed into a new antimalarial drug candidate. However, the compounds and transmission-blocking strategies for malaria control of S. arvensis L. extracts are essential for further study.
Assuntos
Antimaláricos , Malária Falciparum , Malária , Sonchus , Humanos , Animais , Camundongos , Antimaláricos/uso terapêutico , Extratos Vegetais/química , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Malária/tratamento farmacológico , Etanol , Malária Falciparum/tratamento farmacológico , Compostos Fitoquímicos/uso terapêuticoRESUMO
Malaria is still a global health problem. Plasmodium is a single-cell protozoan parasite that causes malaria and is transmitted to humans through the female Anopheles mosquito. The previous study showed that Sonchus arvensis L. callus has antiplasmodial activity. Several treatments are needed for callus quality improvement for antimalarial compound production. This study aimed to examine the effect of dolomite [CaMg(CO3)2] on growth (morpho-anatomical structure and biomass), secondary metabolite production, and in vitro antiplasmodial activity of S. arvensis L. callus. In this study, leaf explants were grown in Murashige and Skoog medium with a combination of 2,4-dichlorophenoxyacetic acid (2,4-D, one mg/L) and 6-benzyl amino purine (BAP, 0.5 mg/L) with dolomite (50, 75, 100, 150, and 200 mg/L). The 21 days callus ethanolic and methanolic extract were analyzed by gas chromatography-mass spectrometry (GC-MS) and thin-layer chromatography (TLC). The antiplasmodial test was performed on a blood culture infected with Plasmodium falciparum strain 3D7 using the Rieckmann method. The results showed that dolomite significantly affected callus growth, metabolite profile, and in vitro antiplasmodial activity. Dolomite (150 mg/L) showed the highest biomass (0.590 ± 0.136 g fresh weight and 0.074 ± 0.008 g dry weight). GC-MS analysis detected four compounds from callus ethanolic extract. Pelargonic acid, decanoic acid, and hexadecanoic acid were major compounds. One new terpenoid compound is based on TLC analysis. S. arvensis L. callus has antiplasmodial activity with the IC50 value of 5.037 µg/mL. It was three times lower than leaf methanolic extract and five times lower than leaf ethanolic extract.
Assuntos
Antimaláricos/farmacologia , Carbonato de Cálcio/farmacologia , Magnésio/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Metabolismo Secundário , Sonchus/crescimento & desenvolvimento , Sonchus/metabolismo , Biomassa , Metabolômica , Extratos Vegetais/farmacologia , Técnicas de Embriogênese Somática de Plantas , Metabolismo Secundário/efeitos dos fármacosRESUMO
OBJECTIVES: Osteoporosis is an ailment described by a skeletal degradation of bone skeletal dominating to increases the chance of fracture. In order to find out the bone formation agents from Baung Forest plants, this research analyzed the effects of 96% ethanol extract of several plants from Baung Forest on antioxidant activity and the effect of osteoblast differentiation-related to the bone formation on the most potent extract. METHODS: The antioxidant effect and osteoblast differentiation of 96% ethanol extracts were evaluated by measuring DPPH scavenging and alkaline phosphatase in p-nitrophenyl phosphate effects by the enzyme-linked immunosorbent assay (ELISA) reader method, respectively. RESULTS: The 96% ethanol extract of Elaeocarpus serratus L. from Baung Forest had the strongest DPPH radical scavenging as anti oxidant (82.17%) and stimulated osteoblast differentiation (116%). Then, this extract had been fractionated based on polarity to become hexane, ethyl acetate, butanol, and aqueous fractions. All the fractions stimulated their alkaline phosphatase (ALP) activity to 138.11 ± 9.72%, 108 ± 5.05%, 148.56 ± 8.47, and 144.58 ± 1.04, respectively. CONCLUSIONS: The extract and fractions of E. serratus L. can successfully inhibit DPPH radical scavenging value and increase ALP activities as markers of osteoblast functions.
Assuntos
Osteogênese , Extratos Vegetais , Fosfatase Alcalina , Antioxidantes , Etanol , Florestas , Extratos Vegetais/farmacologiaRESUMO
BACKGROUND: In previous studies, Cassia spectabilis DC leaf has shown a good antiplasmodial activity. Therefore, this study is a follow-up study of the extract of leaf of C. spectabilis DC on its in vitro and in vivo antiplasmodial activity and mechanism as an antimalarial. METHODS: The extract was fractionated, sub-fractionated and isolated to obtain the purified compound. In vitro antiplasmodial activity test against Plasmodium falciparum to find out the active compound. In vivo test against P. berghei ANKA-infected mice was conducted to determine prophylactic activity and antiplasmodial activity either alone or in combination with artesunate. The inhibition of heme detoxification test as one of the antimalarial mechanisms was carried out using the Basilico method. RESULTS: The results showed that active antimalarial compound isolated from C. spectabilis DC leaf had a structural pattern that was identical to (-)-7-hydroxycassine. Prophylactic test of 90% ethanolic extract of C. spectabilis DC leaf alone against P. berghei ANKA-infected mice obtained the highest percentage inhibition was 68.61%, while positive control (doxycycline 13 mg/kg) was 73.54%. In combination with artesunate, 150 mg/kg three times a day of C. spectabilis DC (D0-D2) + artesunate (D2) was better than the standard combination of amodiaquine + artesunate where the inhibition percentages were 99.18 and 92.88%, respectively. The IC50 of the extract for the inhibitory activity of heme detoxification was 0.375 mg/ml which was better than chloroquine diphosphate (0.682 mg/ml). CONCLUSION: C. spectabilis DC leaf possessed potent antiplasmodial activity and may offer a potential agent for effective and affordable antimalarial phytomedicine.
Assuntos
Antimaláricos/farmacologia , Cassia/química , Heme/metabolismo , Malária/parasitologia , Extratos Vegetais/farmacologia , Plasmodium berghei/efeitos dos fármacos , Plasmodium falciparum/efeitos dos fármacos , Animais , Antimaláricos/isolamento & purificação , Antimaláricos/uso terapêutico , Artesunato/uso terapêutico , Cloroquina/análogos & derivados , Cloroquina/farmacologia , Cetonas , Malária/tratamento farmacológico , Masculino , Camundongos Endogâmicos BALB C , Fitoterapia , Piperidinas , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Folhas de Planta/química , Plasmodium berghei/metabolismo , Plasmodium falciparum/metabolismoRESUMO
Cassia siamea leaf has been proven in vitro and in vivo to have a strong antimalarial activity with Cassiarin A as its active compound. To obtain a source of C. siamea medicinal plant with high level of active antimalarial compound (Cassiarin A), a valid method for determining Cassiarin A level is needed. For this reason, this research conducts the validation of the Cassiarin A content with determination method using thin-layer chromatography (TLC) densitometry which includes the determination of selectivity (Rs), linearity (r), accuracy, precision, limit of detection (LOD), and limit of quantification (LOQ). Cassiarin A was chromatographed on silica gel 60 F254 TLC plate using chloroform : ethanol (85 : 15 v/v) as a mobile phase. Cassiarin A was quantified by densitometric analysis at 368 nm. The linear regression analysis data for the calibration plots showed good linear relationship with r = 0.9995. The method was validated for precision, recovery, repeatability. The minimum detectable amount was found to be 0.0027 µg/spot, whereas the limit of quantitation was found to be 0.008 µg/spot. The results of this validation are then used to determine the Cassiarin A level of C. siamea leaf from various regions in Indonesia. Based on the results of the study, it can be concluded that the TLC-densitometry method can be used to determine level of the Cassiarin A compound with the advantages of being fast, easy, accurate, and inexpensive. In addition, it showed that C. siamea leaves from Pacitan have the highest level of Cassiarin A compared to other areas studied.
Assuntos
Cassia/química , Cromatografia em Camada Fina/métodos , Densitometria/métodos , Compostos Heterocíclicos com 3 Anéis/análise , Folhas de Planta/química , Calibragem , Indonésia , Limite de Detecção , Plantas Medicinais/químicaRESUMO
BACKGROUND: Each part of H. annuus plants is traditionally used as medicinal remedies for several diseases, including malaria. Antimalarial activity of the leaf and the seed has already been observed; however, there is no report about antimalarial activity of the other parts of H. annuus plants. In this study, we assess in vitro and in vivo antimalarial activity of each part of the plants and its mechanism as antimalarial agent against inhibition of heme detoxification. OBJECTIVE: To investigate the antimalarial activity of various parts of H. annuus. METHODS: Various parts of the H. annuus plant were tested for in vitro antimalarial activity against Plasmodium falciparum 3D7 strain (chloroquine-sensitive), in vivo antimalarial activity against P. berghei using Peters' 4-day suppressive test in BALB/c mice, curative and prophylaxis assay, and inhibition of heme detoxification by evaluating ß-hematin level. RESULTS: Ethanol extract of the roots showed the highest antimalarial activity, followed by ethanol extract of leaves, with IC50 values of 2.3 ± 1.4 and 4.3 ± 2.2 µg/mL, respectively and the percentage inhibition of P. berghei of 63.6 ± 8.0 and 59.3 ± 13.2 at a dose of 100 mg/kg, respectively. Ethanol extract of roots produced an ED50 value of 10.6 ± 0.2 mg/kg in the curative test and showed an inhibition of 79.2% at a dose of 400 mg/kg in the prophylactic assay. In inhibition of heme detoxification assay, root and leaf ethanol extracts yielded a lower IC50 value than positive (chloroquine) control with a value of 0.4 ± 0.0 and 0.5 ± 0.0 mg/mL, respectively. CONCLUSION: There were promising results of the ethanol extracts of root of H. annuus as a new source for the development of a new plant-based antimalarial agent.
RESUMO
A new spiro heterocycle, decarboxyportentol acetate (1) was isolated from the barks of Laumoniera bruceadelpha Nooteboom (Simaroubaceae), together with 3,4-dehydrotheaspirone (2), and their structures were elucidated by 2D NMR analysis. 3,4-Dehydrotheaspirone (2) showed potent antiplasmodial activity against Plasmodium falciparum 3D7.
Assuntos
Antimaláricos/farmacologia , Simaroubaceae/química , Compostos de Espiro/farmacologia , Antimaláricos/química , Estrutura Molecular , Plasmodium falciparum/efeitos dos fármacos , Compostos de Espiro/químicaRESUMO
A new indole alkaloid, leucoridine A N-oxide (1), consisting of two units of a strychnan type of skeleton, was isolated from the leaves of Leuconotis griffithii. Its structure was elucidated by various spectroscopic means such as NMR and MS, and also by chemical means. Antiplasmodial activity against Plasmodium falciparum 3D7 of indole alkaloids isolated from L. griffithii was investigated.
Assuntos
Antimaláricos/química , Antimaláricos/farmacologia , Apocynaceae/química , Alcaloides Indólicos/química , Alcaloides Indólicos/farmacologia , Extratos Vegetais/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Extratos Vegetais/químicaRESUMO
Two new acyclic diterpenes, melidianolic acids A (1) and B (2), have been isolated from the bark of Aphanamixis grandifolia. Their structures were elucidated on the basis of spectroscopic and chemical methods. Melidianolic acids A (1) and B (2) showed antimalarial activity against Plasmodium falciparum 3D7 with IC50 of 6.1 and 7.3 microg/mL, respectively.
Assuntos
Antimaláricos/química , Antimaláricos/farmacologia , Diterpenos/química , Meliaceae/química , Animais , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Conformação Molecular , Rotação Ocular , Casca de Planta/química , Extratos Vegetais/química , Plasmodium falciparum/efeitos dos fármacosRESUMO
Three new alkaloids, cassiarins C-E (1-3), and a new chromone, 10,11-dihydroanhydrobarakol (4), which showed moderate antiplasmodial activity against Plasmodium falciparum 3D7, were isolated from flowers of Cassia siamea, and the structures of 1-4 were elucidated by 2D NMR analysis and chemical transformation. Cassiarin D (2) was a dimeric compound consisting of 5-acetonyl-7-hydroxy-2-methylchromone and cassiarin C (1), and cassiarin E (3) was a dimer of cassiarins A and C (1).
Assuntos
Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Antimaláricos/isolamento & purificação , Antimaláricos/farmacologia , Cassia/química , Compostos Heterocíclicos com 3 Anéis/isolamento & purificação , Compostos Heterocíclicos com 3 Anéis/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Alcaloides/química , Animais , Antimaláricos/química , Flores/química , Compostos Heterocíclicos com 3 Anéis/química , Indonésia , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Testes de Sensibilidade ParasitáriaRESUMO
New quassinoids, delaumonones A (1) and B (2) have been isolated from the bark of Laumoniera bruceadelpha NOOTEBOOM (Simaroubaceae) and the structures were elucidated by 2D NMR analysis and a chemical correlation. Delaumonones showed an antimalarial activity against Plasmodium falciparum.
Assuntos
Antimaláricos/isolamento & purificação , Antimaláricos/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Quassinas/isolamento & purificação , Quassinas/farmacologia , Simaroubaceae/química , Animais , Antimaláricos/química , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Células HL-60 , Humanos , Espectroscopia de Ressonância Magnética/normas , Modelos Moleculares , Conformação Molecular , Testes de Sensibilidade Parasitária , Casca de Planta/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Quassinas/química , Padrões de Referência , EstereoisomerismoRESUMO
Bioassay-guided purification from the seeds of Peganum harmala led to the isolation of harmine (1), harmaline (2), vasicinone (3), and deoxyvasicinone (4). Harmine (1) and harmaline (2) showed a moderate in vitro antiplasmodial activity against Plasmodium falciparum. Quinazoline alkaloid, vasicinone (3), showed a vasorelaxant activity against phenylephrine-induced contraction of isolated rat aorta.
Assuntos
Alcaloides/farmacologia , Peganum/química , Extratos Vegetais/farmacologia , Alcaloides/isolamento & purificação , Animais , Antimaláricos/isolamento & purificação , Antimaláricos/farmacologia , Harmalina/isolamento & purificação , Harmalina/farmacologia , Harmina/isolamento & purificação , Harmina/farmacologia , Fenilefrina , Extratos Vegetais/isolamento & purificação , Plasmodium falciparum/efeitos dos fármacos , Quinazolinas/isolamento & purificação , Quinazolinas/farmacologia , Ratos , Sementes , Vasodilatação/efeitos dos fármacos , Vasodilatadores/isolamento & purificação , Vasodilatadores/farmacologiaRESUMO
Two new cassane-type diterpenes, sucutiniranes A (1) and B (2), have been isolated from the seeds of Bowdichia nitida together with 6alpha-acetoxyvouacapane (3) and 6alpha,7beta-diacetoxyvouacapane (4), and the structures of 1 and 2 were elucidated by using 2D NMR data and chemical correlations. Sucutinirane A (1) and 3 showed a moderate cytotoxicity against human colon carcinoma COLO201 cells, and 6alpha,7beta-diacetoxyvouacapane (4) showed in vitro antiplasmodial activity against parasite Plasmodium falciparum 3D7.
Assuntos
Antimaláricos/farmacologia , Carcinoma/tratamento farmacológico , Neoplasias do Colo/tratamento farmacológico , Diterpenos/química , Plantas/metabolismo , Animais , Antimaláricos/química , Linhagem Celular Tumoral , Química Farmacêutica/métodos , Diterpenos/farmacologia , Desenho de Fármacos , Humanos , Espectroscopia de Ressonância Magnética , Modelos Químicos , Extratos Vegetais/farmacologia , Plasmodium falciparum/metabolismo , Sementes/metabolismoRESUMO
A new bischromone, chrobisiamone A (1) with an antiplasmodial activity has been isolated from the leaves of Cassia siamea and the structure was elucidated by 2D NMR analysis. Cyclization of 5-acetonyl-7-hydroxy-2-methylchromone (2) in the presence of ammonium acetate resulted in generation of cassiarin A (3) with an unprecedented tricyclic skeleton, supporting a biogenetic pathway proposed for 3.
Assuntos
Antimaláricos/farmacologia , Cassia/metabolismo , Cromonas/química , Compostos Heterocíclicos com 3 Anéis/química , Extratos Vegetais/química , Biomimética , Química Farmacêutica/métodos , Cromonas/síntese química , Cromonas/farmacologia , Desenho de Fármacos , Espectroscopia de Ressonância Magnética , Malária/prevenção & controle , Modelos Químicos , Modelos Moleculares , Folhas de Planta/metabolismoRESUMO
Two novel alkaloids with an unprecedented tricyclic skeleton, cassiarins A (1) and B (2), have been isolated from the leaves of Cassia siamea, and the structures were elucidated on the basis of spectroscopic data. Cassiarin A (1) showed a potent antiplasmodial activity.