Renoprotective effect of umbelliferone in high-fat diet/streptozotocin-induced type 2 diabetic rats

Objective: To evaluate the renoprotective effect of umbelliferone in high-fat diet/streptozotocin-induced type 2 diabetic rats. Methods: We established a streptozotocin-induced type 2 diabetic model in male Wistar rats. The rats were fed with high-fat diet (45 kcal％ lard fat) and injected with 35 mg/kg streptozotocin. Diabetic rats were treated with umbelliferone for 8 weeks. At the end of the experimental period, the serum and kidney were used for measuring biochemical parameters, protein expression and histological analysis. Results: After 8-week treatment, umbelliferone decreased fasting plasma glucose, concentrations of malondialdehyde and monocyte chemoattractant protein-1 in the plasma and tissues. It also significantly reduced serum creatinine, blood urea nitrogen, serum advanced glycation end products, as well as kidney weight in type 2 diabetic rats (P<0.05). Moreover, umbelliferone reduced the 24-h urine albumin, but increased 24-h urine creatinine excretion (P<0.05). In renal protein expression, umbelliferone decreased the levels of transforming growth factor-β1 and fibronectin while increasing the levels of superoxide dismutase and catalase (P<0.05). Renal histological examination revealed an enlarged glomerular size in diabetic rats, which was smaller in umbelliferone-treated diabetic rats. Conclusions: Umbelliferone alleviates renal dysfunction in diabetes via decreasing hyperglycemia, oxidative stress, inflammation and glycation.

Renoprotective effect of umbelliferone in high-fat diet/streptozotocin-induced type 2 diabetic rats

To evaluate the renoprotective effect of umbelliferone in high-fat diet/streptozotocin-induced type 2 diabetic rats. Methods: We established a streptozotocin-induced type 2 diabetic model in male Wistar rats. The rats were fed with high-fat diet (45 kcal% lard fat) and injected with 35 mg/kg streptozotocin. Diabetic rats were treated with umbelliferone for 8 weeks. At the end of the experimental period, the serum and kidney were used for measuring biochemical parameters, protein expression and histological analysis. Results: After 8-week treatment, umbelliferone decreased fasting plasma glucose, concentrations of malondialdehyde and monocyte chemoattractant protein-1 in the plasma and tissues. It also significantly reduced serum creatinine, blood urea nitrogen, serum advanced glycation end products, as well as kidney weight in type 2 diabetic rats (P<0.05). Moreover, umbelliferone reduced the 24-h urine albumin, but increased 24-h urine creatinine excretion (P<0.05). In renal protein expression, umbelliferone decreased the levels of transforming growth factor-b1 and fibronectin while increasing the levels of superoxide dismutase and catalase (P<0.05). Renal histological examination revealed an enlarged glomerular size in diabetic rats, which was smaller in umbelliferone-treated diabetic rats. Conclusions: Umbelliferone alleviates renal dysfunction in diabetes via decreasing hyperglycemia, oxidative stress, inflammation and glycation.

Umbelliferone ameliorates renal function in diabetic nephropathy rats through regulating inflammation and TLR/NF-κB pathway / 中国天然药物

Diabetic nephropathy (DN) is a leading cause of renal failure, contributing to severe morbidity and mortality in diabetic patients. Umbelliferae (Umb) has been well characterized to exert protective effects in diabetes. However, the action and mechanism of Umb in DN remains unclear. In this work, we studied the effect of Umb in a streptozotocin (STZ)-induced DN rat model and explore its underlying mechanism. DN rats were treated withUmb (20, 40 mg·kg) orirbesartan (15 mg·kg) for 4 weeks. Levels of serum glucose, insulin, blood uric acid, creatinine, triglycerides (TG) and total cholesterol (TC) were measured bycommercial assay kits, respectively. Histopathological changes andinflammatory cytokine levels including IL-6, IL-1β and TNF-α in the kidney were also evaluated. Alterations in the expression of podocin, CD2AP and TLR/NF-κB were assessed by western blotting. Our results showed that Umb reduced renal injury in DN rat model, as evidenced by the decrease in blood glucose, 24 h urinary protein, serum creatinine, and blood uric acid. Umb also significantly ameliorated the renal histopathological alteration, and down-regulated the expression of epithelial-to-mesenchymal transition-related molecular markers podocin and CD2AP. Moreover, Umb inhibited TLR2, TLR4, MyD88 expressions, NF-κB activation and considerably reduced levels of other downstream inflammatory molecules (TNF-α, IL-6, IL-1β). These findings indicated that Umb improved renal function through regulating inflammation and TLR/NF-κB pathway, suggesting the potential efficacy of Umb in DN treatment.

Chemical constituents of Viola yedoensis / 中草药

Objective To investigate the chemical constituents of the whole plants of Viola yedoensis. Methods The chemical constituents were isolated and purified by column chromatography over silica gel and Sephadex LH-20, as well as on the semi-preparative HPLC. The structures of the isolates were identified by the NMR spectroscopic method. Results Twenty-three compounds were isolated and their structures were identified as pubinernoid A (1), (2R,6R,9R)-2,9-dihydroxy-4-megastigmen-3-one (2), 3S,5R-dihydroxy-6R,7-megastigmadien-9-one (3), dehydrovomifoliol (4), blumenol A (5), blumenol B (6), oleanolic acid (7), 2α,3α-dihydroxyurs-12-ene-28-oic acid (8), 1α,2α,3β-trihydroxyolean-12-ene-28-oic acid (9), 2α,19α-dihydroxyursolic acid (10), 3α-hydroxyfriedel-2-one (11), 7-oxopetrosterol (12), 7-oxositosterol (13), syringaresinol (14), lariciresinol (15), daphneticin (16), umbelliferone (17), trans-p-hydroxycinnamic acid methyl ester (18), p-hydroxyphenylpropionic acid (19), p-hydrobenzaldehyde (20), p-methoxybenzaldehyde (21), p-methoxybenzoic acid (22), and 5-hydroxymethyl-2-furfural (23). Conclusion Compounds 1-16 and 18-23 are isolated from the genus Viol for the first time, and compound 17 is isolated from the plant for the first time.

Justicia pectoralis, a coumarin medicinal plant have potential for the development of antiasthmatic drugs?

ABSTRACT Justicia pectoralis Jacq., Acanthaceae, is a medicinal plant found Central America. In the Northeast of Brazil, it is popularly known as "chambá" being extensively used in homemade preparations for the treatment of cough, bronchitis and asthma. The species is part of a public phytotherapy program in Brazil entitled "Farmácias Vivas", National Record of Plants of Interest to the National Health System and the National Formulary of Herbal medicines. This paper aims to critically review the available scientific literature regarding the health promoting effects of J. pectoralis var. stenophylla. The traditional uses, phytochemistry, pharmacological activities, toxicology, quality control and potential interactions with conventional drugs were included in the present review. Botanical, chemical and pharmacognostical studies stablished several parameters useful for quality control of plant drug, extracts and phytomedicine from aerial parts of J. pectoralis using as markers two bioactive coumarins. A wide range of evidence have demonstrated the anti-inflammatory, anti-nociceptive, anti-spasmodic, smooth muscle relaxant and anxiolytic effects of J. pectoralis and its chemical constituents. Pilot clinical studies showed the efficacy of a syrup preparation of J. pectoralis in the treatment of mild and moderate asthma. The pharmacological potential make these medicinal plants good candidates for the development of new phytomedicine for the treatment of asthma. However, a strong collaboration to bridge the gap between preclinical and clinical study is still necessary for the development of an effective medicine from J. pectoralis.

Chemical constituents from plant of Stelleropsis tianschanica / 中草药

Objective: To study the chemical constituents from the arerial parts of Stelleropsis tianschanica. Methods: The constituents were isolated and purified by silica gel chromatography repeatedly, and the structures were identified by spectra analysis and chemical methods. Results: Thirteen compounds were isolated from S. tianschanica and the structures were identified as (+)-pinoresinol (1), (-)-pinoresinol (2), 3'-desmethylarctigenin (3), arctigenin (4), pluviatolide (5), umbelliferone (6), 4-(3,4- dimethoxybenzyl)-3-(4-hydroxy-3-methoxybenzyl)-tetrahydrofuran-2-ol (7), daphnogitin (8), daphnetone (9), blumenol B (10), loliolide (11), 4'-hydroxyacetophenone (12), and 4'-hydroxybenzoic acid (13). Conclusion: Compounds 1-13 were all obtained for the first time from the plant of S. tianschanica and the genus Stelleropsis Pobed.

Phenolic constituents from roots of Artocarpus heterophyllus / 中草药

Objective: To investigate the phenolic constituents from the roots of Artocarpus heterophyllus. Methods: Compounds were isolated from the roots of the plant by column chromatography over ODS, MCI GEL CHP-20P, Sephadex LH-20 and by preparative HPLC. Their structures were identified by the analysis of their physicochemical properties and the spectral data of NMR and MS. Results: Seventeen phenolic compounds were isolated from the roots of the plant, namely 1-O-feruloylglycerol (1), hypargystilbene A (2), oxyresveratrol (3), 2', 3, 4', 5, 5'-pentahydroxy-cis-stilbene (4), resveratrol (5), ethyl 2, 4-dihydroxybenzoate (6), ethyl 3, 4-dihydroxybenzoate (7), umbelliferone (8), 8-(3, 3-dimethylallyl)-6, 7-dihydroxycoumarin (9), morachalcone A (10), artocarpanone (11), styracifolin C (12), cudraflavone C (13), heterophyllin (14), cycloheterophyllin (15), artonin A (16), and artonin B (17). Conclusion: It is the first report of the occurrence of compound 9 as a natural product. Compounds 1, 4, and 6 are isolated from the plants of Moraceae family for the first time. Compound 8 is first obtained from the plants of Artocarpus J. R. et G. Forst., while compounds 3, 5, 10, 11, 14, and 15 are first found in A. heterophyllus.

Anti-Alzheimer's disease potential of coumarins from Angelica decursiva and Artemisia capillaris and structure-activity analysis

OBJECTIVE@#To use structure-activity analysis to study the anti-Alzheimer's disease (anti-AD) activity of natural coumarins isolated from Angelica decursiva and Artemisia capillaris, along with one purchased coumarin (daphnetin).@*METHODS@#Umbelliferone, umbelliferone 6-carboxylic acid, scopoletin, isoscopoletin, 7-methoxy coumarin, scoparone, scopolin, and esculetin have been previously isolated; however 2'-isopropyl psoralene was isolated from Angelica decursiva for the first time to evaluate their inhibitory effects against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE1) enzyme activity. We scrutinized the potentials of coumarins as cholinesterase and BACE1 inhibitors via enzyme kinetics and molecular docking simulation.@*RESULTS@#Among the test compounds, umbelliferone 6-carboxylic acid, esculetin and daphnetin exhibited potent inhibitory activity against AChE, BChE and BACE1. Both esculetin and daphnetin have a catechol group and exhibit significant anti-AD activity against AChE and BChE. In contrast, presence of a sugar moiety and methoxylation markedly reduced the anti-AD activity of the coumarins investigated in this study. With respect to BACE1 inhibition, umbelliferone 6-carboxylic acid, esculetin and daphnetin contained carboxyl or catechol groups, which significantly contributed to their anti-AD activities. To further investigate these results, we generated a 3D structure of BACE1 using Autodock 4.2 and simulated binding of umbelliferone 6-carboxylic acid, esculetin and daphnetin. Docking simulations showed that different residues of BACE1 interacted with hydroxyl and carboxylic groups, and the binding energies of umbelliferone 6-carboxylic acid, esculetin and daphnetin were negative (-4.58, -6.25 and -6.37 kcal/mol respectively).@*CONCLUSIONS@#Taken together, our results suggest that umbelliferone 6-carboxylic acid, esculetin and daphnetin have anti-AD effects by inhibiting AChE, BChE and BACE1, which might be useful against AD.

Anti-Alzheimer's disease potential of coumarins from Angelica decursiva and Artemisia capillaris and structure-activity analysis

Objective: To use structure-activity analysis to study the anti-Alzheimer's disease (anti-AD) activity of natural coumarins isolated from Angelica decursiva and Artemisia capillaris, along with one purchased coumarin (daphnetin). Methods: Umbelliferone, umbelliferone 6-carboxylic acid, scopoletin, isoscopoletin, 7-methoxy coumarin, scoparone, scopolin, and esculetin have been previously isolated; however 2'-isopropyl psoralene was isolated from Angelica decursiva for the first time to evaluate their inhibitory effects against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE1) enzyme activity. We scrutinized the potentials of coumarins as cholinesterase and BACE1 inhibitors via enzyme kinetics and molecular docking simulation. Results: Among the test compounds, umbelliferone 6-carboxylic acid, esculetin and daphnetin exhibited potent inhibitory activity against AChE, BChE and BACE1. Both esculetin and daphnetin have a catechol group and exhibit significant anti-AD activity against AChE and BChE. In contrast, presence of a sugar moiety and methoxylation markedly reduced the anti-AD activity of the coumarins investigated in this study. With respect to BACE1 inhibition, umbelliferone 6-carboxylic acid, esculetin and daphnetin contained carboxyl or catechol groups, which significantly contributed to their anti-AD activities. To further investigate these results, we generated a 3D structure of BACE1 using Autodock 4.2 and simulated binding of umbelliferone 6-carboxylic acid, esculetin and daphnetin. Docking simulations showed that different residues of BACE1 interacted with hydroxyl and carboxylic groups, and the binding energies of umbelliferone 6-carboxylic acid, esculetin and daphnetin were negative (-4.58, -6.25 and -6.37 kcal/mol respectively). Conclusions: Taken together, our results suggest that umbelliferone 6-carboxylic acid, esculetin and daphnetin have anti-AD effects by inhibiting AChE, BChE and BACE1, which might be useful against AD.

Anti-inflammatory and antioxidant effects of umbelliferone in chronic alcohol-fed rats

BACKGROUND/OBJECTIVES: Inflammation is associated with various types of acute and chronic alcohol liver diseases. In this study, we examined whether umbelliferone (7-hydroxycoumarin, UF) ameliorates chronic alcohol-induced liver damage by modulating inflammatory response and the antioxidant system. METHODS: Rats were fed a Liber-Decarli liquid diet containing 5% alcohol with or without UF (0.05 g/L) for 8 weeks, while normal rats received an isocaloric carbohydrate liquid diet. RESULTS: Chronic alcohol intake significantly increased serum tumor necrosis factor-alpha (TNF-alpha) and interleukin 6 levels and decreased interleukin 10 level; however, UF supplementation reversed the cytokines related to liver damage. UF significantly suppressed hepatic lipopolysaccharide binding protein, toll-like receptor 4 (TLR4), nuclear factor kappa B, and TNF-alpha gene expression increases in response to chronic alcohol intake. Masson's trichrome staining revealed that UF improved mild hepatic fibrosis caused by alcohol, and UF also significantly increased the mRNA expressions and activities of superoxide dismutase and catalase in liver, and thus, decreased lipid peroxide and mitochondrial hydrogen peroxide levels. CONCLUSIONS: The findings of this study indicate that UF protects against alcohol-induced liver damage by inhibiting the TLR4 signaling pathway and activating the antioxidant system.

Influencia del tiempo de cosecha sobre el contenido de cumarina y de umbeliferon hallado en los extractos de Justicia pectoralis Jacq. (tilo) / Harvest time influences on coumarin and umbelliferone contents in extracts of Justicia pectoralis Jacq. (tilo)

INTRODUCTION: Justicia pectoralis Jacq. (Acanthaceae) is medicinal plant species commonly used in Cuba for the treatment of nervous disorders because of its sedative effect. Coumarin is one of its main active phytochemicals present in the extracts obtained from this plant and used as analytic marker in quality control. On the other hand, this compound contributes to the sedative effect attributed to this plant. OBJECTIVE: to evaluate the influence of harvest time on the coumarin and umbelliferone (7-hydroxycoumarin) in Justicia pectoralis extracts. METHODS: the experiment lasted two years. The harvest was performed at 4, 6 and 8 months after planting. Aqueous and hydroalcohol extracts were produced and the coumarin and umbelliferone contents were determined by high resolution liquid chromatography. RESULTS: the achieved results showed the presence of coumarin and umbelliferone in both extracts. Both methods can be used for the extraction of these components from the plant, although in the case of umbelliferone, the best extraction results were achieved by using aqueous extract. In both cases, the recovery percentages were more than 98 percent. This study confirmed that the harvest time significantly influences on the coumarin and umbelliferone contents. CONCLUSIONS: the best results are observed in the first two harvests (4 and 6 months at summer time), which indicates that the industry should process the vegetal material in these two periods of the year(AU)

INTRODUCCIÓN: Justicia pectoralis Jacq. (Acanthaceae) es una planta medicinal comúnmente usada en Cuba para el tratamiento de enfermedades nerviosas por su efecto sedante. La cumarina es uno de los fitocomponentes mayoritarios en los extractos obtenidos con esta planta y empleado como marcador analítico en los controles de calidad. Por otro lado, este componente contribuye con el efecto sedante atribuido a esta planta. OBJETIVO: evaluar la influencia del tiempo de cosecha sobre el contenido de cumarina y umbelliferona (7 hidroxicumarina) en extractos de Justicia pectoralis. MÉTODOS: se desarrolló el experimento durante 2 años. Se realizaron las cosechas a los 4, 6 y 8 meses de plantada. Se elaboraron extractos acuosos e hidroalcohólicos y se determinó el contenido de cumarina y umbelliferone por cromatografía líquida de alta resolución. RESULTADOS: se mostró la presencia de cumarina y umbelliferona en ambos extractos. Además, en el caso de la umbelliferona, los mejores resultados se alcanzaron al aplicar extracción acuosa. En ambos casos, los por cientos de recobrados fueron superiores al 98 por ciento. Se confirmó que el tiempo de cosecha influyó significativamente sobre el contenido de cumarina y umbelliferona. CONCLUSIONES: los mejores resultados se obtienen en la primeras dos cosechas (4 y 6 meses que coincide con el verano), lo que sugiere que el material de la planta debe procesarse por la industria en esos periodos del año(AU)

Relaxant effect of 7-ethoxy-4-methyl-2H-chromen-2-one by calcium channel blockade: computational and ex vivo studies.

Current work was conducted in order to determine the underlying mode of relaxant action of 7-ethoxy-4-methyl- 2H-chromen-2-one (1), a coumarin obtained by semisynthesis from umbelliferone (2), with significant relaxant effect in a concentration-dependent manner on tracheal rat rings pre-contracted with carbachol (1 μM). In a previous study it was demonstrated that compound 1 and 2 showed significant relaxant effect, being 1 the most active compound (Emax= 100% and EC50= 83 μM) even more active than theophylline an unspecific phosphodiesterases (PDE’s) inhibitor used as positive control. Moreover, pretreatment with 1 significantly shifted to the right the carbachol-induced contraction. On the other hand, compound 1 (83 μM) produces significant (100%) relaxant effect on the contraction induced by KCl (80 mM) and the CaCl2-induced contraction was significantly reduced by the coumarin 1 as nifedipine does (a L-type calcium channel blocker), used as positive control. Indomethacin (10 μM, unspecific COX inhibitor) significantly reduced 1-relaxation. Meanwhile, in the presence of isoproterenol (a  -adrenergic agonist), and K+ channel blockers glibenclamide (10 μM) and 2- AP (100 μM) the relaxant curve was not modified. Compound 1 was docked on an outer cavity located on the extracellular side of the human L-type calcium channel model (affinity energy -6.8 kcal/mol). However, compound 1 was also found on the same location as nifedipine with the same affinity energy (-6.3 kcal/mol) as previously described. Both conformations were stabilized by aliphatic interactions on both binding sites, primordially by a π-π interaction between FIVS6.7 and aromatic rings from compound 1. In conclusion, 7-ethoxy-4- methyl-2H-chromen-2-one (1) induces a significant relaxant action on rat trachea rings, through L-type calcium channel blockade and, as a second mechanism of action, by a possible intracellular cyclic AMP increasing.

Chemical constituents from Lepidogrammitis drymoglossoides / 中草药

Objective: To study the chemical constituents from Lepidogrammitis drymoglossoides. Methods: The constituents were isolated and purified by various column chromatographies, and their structures were identified on the basis of chemical evidences and spectroscopic analysis including MS, 1H-NMR, and 13C-NMR. Results: Fourteen compounds were isolated and identified as β-ecdysterone (1), physcion (2), emodin (3), umbelliferone (4), scoparone (5), aesculetin (6), caffeic acid (7), chlorogenic acid (8), protocatechuic acid (9), pyrocatechualdehyde (10), gallic acid (11), 4-hydroxybenzoic acid methyl ester (12), docosanyl tetracosanoate (13), and hexadecanoic acid (14). Conclusion: Compounds 3-5, 8, and 11-13 are isolated from the plants of genus Lepidogrammitis Ching for the first time.

Chemical constituents in flowers of Rhododendron lapponicum / 中草药

Objective: To study the chemical constituents in the flowers of Rhododenron parvifolium, which is a traditional Tibet medicine. Methods: Silica gel column chromatography, HPLC, and Sephadex LH-20 column chromatography techniques were used for the separation and purification of the compounds. Their structures were determined on the basis of IR, MS, 1D, and 2D NMR spectral evidences. Results: Thirteen compounds were isolated from methanol extract in the flowers of R. parvifolium, and their structures were identified as parvifoliumol I (1), umbelliferone (2), scopoletin (3), 4', 5, 7-trihydroxyflavanone (4), 8-demethylfarrerol (5), farrerol (6), quercetin (7), rutin (8), eudesmin A (9), 4-hydroxybenzoic acid (10), 3, 5-dihydroxy toluene (11), oleanane (12), and kojic acid (13). Conclusion: Compound 1 is a new compound, which has a hexahydroxanthene skeleton. Compounds 9, 11, and 13 are obtained from the plants of Rhododendron L. for the first time.

Chemical constituents from aerial parts of Ligusticum sinense cv. chaxiong / 中草药

Objective: To study the chemical constituents from the aerial parts of Ligusticum sinense cv. chaxiong. Methods: The chemical constituents were separated and purified by silica gel, ODS column chromatography, and preparative HPLC. Their structures were determined by various of spectroscopic analyses. Results: Fourteen compounds were isolated from the petrol ester and CH2Cl2 fractions of 95% ethanol extract of the aerial parts of L. sinense cv. chaxiong, and their structures were identified as 5-hydroxy-3- butylphthalide (1), 3-hydroxy-octa-1, 5-dien-7-one (2), umbelliferone (3), pumbinernoid A (4), crocinervolide (5), (3R, 6R, 7E)-3- hydroxy-4, 7-megastignadien-9-one (6), senkyunolide G (7), scopoletin (8), (2Z)-3-(3, 4-dihydroxyphenyl)-2-propenal (9), (3S, 5R, 6S, 7E, 9R)-5, 6-epoxy-3, 9-dihydroxy-7-megastigmene (10), vomifoliol (11), dihydroactinidiolide (12), 7-hydroxy-3-butylphthalide (13), and senkyunolide A (14). Conclusion: Compounds 1-13 are isolated from this plant for the first time, compounds 1, 2, 4-6, and 9-13 are found from the plants of genus Ligusticum L. for the first time, and compound 1 is a new natural product.

Chemical constituents in leaves of Morus atropurpurea and their α-glucosidase activity / 中草药

Objective: To study the chemical constituents in the leaves of Morus atropurpurea and their biological activity. Methods: The chemical constituents were isolated by silica gel, ODS, Sephadex LH-20 column chromatographies, as well as HPLC. Their structures were elucidated on the basis of physicochemical properties and spectral analysis. The inhibitory effect of the compounds on α-glucosidase was tested by pNP method. Results: Eighteen compounds were isolated from the leaves of M. atropurpurea. Their structures were identified as 1-deoxynojirinycin (1), fagomine (2), cytidine (3), 2-(1', 2', 3', 4'-tetrahydroxybutyl)-5-(2″, 3″, 4″-trihydroxybutyl)-pyrazine (4), 2-(1', 2', 3', 4'-tetrahydroxybutyl)-6-(2″, 3″, 4″-trihydroxybutyl)-pyrazine (5), 2-(1', 2', 3', 4'-tetrahydroxybutyl)-5-(1″, 2″, 3″, 4″-tetrahydroxybutyl)-pyrazine (6), quercetin 3-O-β-D-glucopyranoside (7), kaempferol 3-O-β- D-glucopyranoside (8), kaempferol 3-O-β-rutinoside (9), cichorioside (10), roseoside (11), phytol (12), umbelliferone (13), 1H-indole-3-aldehyde (14), ethyl trans-caffeate (15), sucrose (16), β-sitosterol (17), and daucosterol (18). Conclusion: Compounds 5, 6, 14, and 15 are isolated from the plants of Morus Stapf. for the first time, and compounds 3, 4, 7-13, and 16 are firstly reported from M. atropurpurea. Compounds 1-6 display the potential inhibitory activities on α-glucosidase.

Justicia pectoralis Jacq: , Acanthaceae: preparation and characterisation of the plant drug including chromatographic analysis by HPLC-PDA

Justicia pectoralis Jacq., Acanthaceae, é uma erva conhecida popularmente no Nordeste como chambá e, utilizada tradicionalmente no tratamento de doenças do trato respiratório, como a asma, tosse e bronquite. Essa espécie encontra-se na Relação Nacional de Plantas Medicinais de Interesse para o SUS. O objetivo do presente estudo foi elaborar protocolo para a preparação da droga vegetal a partir de J. pectoralis e realizar a sua caracterização visando seu emprego como matéria-prima farmacêutica. A parte aérea de J. pectoralis, após secagem em estufa com circulação e renovação de ar (35 °C) durante diferentes períodos de tempo (1-5 dias) mostrou a partir de 24 h de secagem um teor de umidade abaixo do valor máximo permitido para drogas vegetais. O pó da droga vegetal foi classificado como pó moderadamente grosso e, caracterizado quanto aos teores de cinzas totais, extrativos solúveis em água e etanol. Análise do extrato hidroalcoólico (etanol 20 por cento) de J. pectoralis por Cromatografia Líquida de Alta Eficiência (CLAE-DAD) determinou um teor de cumarina e umbeliferona de 16,2 e 0,81 mg/g da droga vegetal, respectivamente. As condições de preparação da droga vegetal e os parâmetros de controle de qualidade determinados para J. pectoralis no presente estudo são de interesse no desenvolvimento de fitoterápicos que empreguem esse matéria-prima ativa.

Justicia pectoralis Jacq., Acanthaceae, is a herb popularly known in Brazilian northeast as "chambá" and used in folk medicine for the treatment of respiratory tract conditions such as asthma, cough and bronchitis. This species is included in the National Register of Plants of Interest to the National Health System. The aim of the present study was to develop a protocol for the preparation of the plant drug from J. pectoralis and to characterise the plant drug for its use as a pharmaceutical raw material. The aerial parts of J. pectoralis, after drying chamber with forced air circulation (35 °C) for different periods of time (1-5 days), presented after one day a moisture content below the maximum allowed for plant drugs. The powder of the plant drug was classified as moderately coarse, and the total ashes content and the water- or ethanol-soluble extractives were determined. Analysis of hydroalcoholic (ethanol 20 percent) extract of J. pectoralis by high performance liquid chromatography-photo diode array (HPLC-PDA) determined the content of coumarin and umbelliferone (16.2 and 0.81 mg/g plant drug, respectively). The preparation conditions of the plant drug and the quality control parameters established for J. pectoralis in this study are of interest for the development of phytomedicines which use this active raw material.