RESUMO
Alzheimer's disease (AD) is the most common cause of dementia in the elderly, with some known classical factors. Cicer arietinum (Leguminosae) is a source of protein for humans and contains albumin, globulin, glutelin, and prolamin. The protein content of two cultivars of C. arietinum, Hashem and Mansour, was isolated to evaluate their inhibition activity against acetylcholinesterase (AChE), butyrylcholine esterase (BChE), and ß-amyloid peptide (ßA) aggregation. Sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) and molecular docking were also applied to evaluate the content and determine the potential of each chickpea protein to interact with AChE, respectively. Obtained data showed that proteins from both cultivars could inhibit AChE with IC50 of 17.73 (0.03) and 22.20 (0.06) µg/mL, respectively, with no activity on BChE. The 50 µg/mL protein concentration of each cultivar suppressed ßA accumulation (Mansour: 25.66% and Hashem: 21.69%) and showed biometal chelating activity. SDS-PAGE analysis revealed relatively different protein patterns, though the Mansour cultivar contained some protein bands with molecular weights of 18, 24, and 70 kDa were estimated to belong to vicilin and legumin, which were absent in the Hashem protein mass. Molecular docking showed that legumin and especially vicilin have good potential to interact with AChE. The chickpea proteins showed inhibitory activity against AChE, which might be due to the vicilin and legumin fractions. The characterization of the inhibitory effect of each protein band could be promising in finding new therapeutic peptide candidates to treat Alzheimer's in the future, although more experimental work is needed in this issue.
Assuntos
Doença de Alzheimer , Cicer , Humanos , Idoso , Doença de Alzheimer/tratamento farmacológico , Doença de Alzheimer/metabolismo , Cicer/química , Cicer/metabolismo , Acetilcolinesterase/metabolismo , Simulação de Acoplamento Molecular , Peptídeos beta-Amiloides , Inibidores da Colinesterase/farmacologiaRESUMO
CONTEXT: As an alternative approach, administration of phytotherapeutic agents in management of benign prostate hyperplasia (BPH), is rapidly growing each day. Different authors have indicated effectiveness of Viola odorata L. (Violaceae), Echium amoenum Fisch. & C.A.Mey. (Boraginaceae) and Physalis alkekengi L. (Solanaceae) in treatment of BPH. However, none have reported the beneficial outcomes of the mixture yet. OBJECTIVE: This study evaluates the therapeutical effects of V. odorata, E. amoenum and P. alkekengi mixture on symptomatic BPH patients. MATERIALS AND METHODS: Eighty six symptomatic BPH patients with International Prostate Symptom Score (IPSS) of more than 13 and prostate volume of more than 30 cm3 were randomly allocated to receive a two-week course of placebo (control group) or 1 mL of mixed hydro-alcoholic solution of P. alkekengi, E. amoenum and V. odorata extracts (1.5, 1 and 1.5% respectively) (treatment group). RESULTS: IPSS score of incomplete urination (42.3 ± 2.04%), frequency of urination (20.08 ± 1.02%), intermittency (40.78 ± 2.16%), urgency (60.91 ± 3.14%), weak stream (50.58 ± 2.14%), straining (55.67 ± 2.53%) and nocturia (40.14 ± 1.89%) in treatment group were significantly decreased after treatment compare to placebo receiving group. Furthermore, the prostate volume (16.92 ± 0.89%) and extant urine volume (28.12 ± 1.36%) also significantly decreased in treatment group compared to control group. No significant side effects or abnormalities in biochemical tests and urinalysis were observed throughout the study. DISCUSSION AND CONCLUSIONS: Based on results, mentioned mixture is safe and effective in improving life quality of patients suffering from BPH.
Assuntos
Echium/química , Extratos Vegetais/uso terapêutico , Hiperplasia Prostática/tratamento farmacológico , Solanaceae/química , Viola/química , Adulto , Idoso , Método Duplo-Cego , Humanos , Masculino , Pessoa de Meia-Idade , Fitoterapia , Extratos Vegetais/efeitos adversos , Extratos Vegetais/isolamento & purificação , Plantas Medicinais , Próstata/efeitos dos fármacos , Próstata/patologia , Hiperplasia Prostática/diagnóstico , Hiperplasia Prostática/fisiopatologia , Qualidade de Vida , Fatores de Tempo , Resultado do Tratamento , Micção/efeitos dos fármacosRESUMO
CONTEXT: Otostegia persica (Burm.) Boiss. (Lamiaceae), "Goldar" in Persian, is widely used in the folk medicine of south Iran for control of diabetes mellitus. OBJECTIVE: In the present study, hypoglycemic and antioxidant effects of different fractions of the O. persica extract were investigated and constituents of effective fractions were elucidated. MATERIALS AND METHOD: Different concentrations (100-400 mg/kg) of aqueous infusion (AI) of flowering aerial parts of the plant (traditional preparation) and all fractions of the O. persica extract (i.p. injection) were tested for antidiabetic activity in streptozocin-induced diabetic NMRI mice. Blood glucose level was measured at time 0 and intervals of 1, 2, 4, and 6 h later. Antioxidant activities of different fractions of the plant extract and pure compounds (0.1, 0.5, and 1 mg/ml) were determined with the DPPH method. Four compounds were isolated and identified from potent fractions. RESULTS AND DISCUSSION: Antidiabetic activity demonstrated that the effect of the methanol fraction at a dose of 300 mg/kg was equivalent with glibenclamide, and at a dose of 400 mg/kg was comparable with glibenclamide and insulin (p > 0.05). The EC50 of the methanol fraction was 307.12 mg. Methanol and ethyl acetate fractions showed antioxidant activities (both IC50 equal to 0.49 mg/ml), so these fractions were selected for the purification of compounds. Chrysoeriol from ethyl acetate and three apigenin derivatives (6-methylapigenin, apigenin-7-O-glucoside, and echinaticin) from the methanol fraction were isolated and identified (new for the species). Chrysoeriol exhibited potent antioxidant activity comparable with vitamin E and BHT (p > 0.05). CONCLUSION: The present study confirmed the folklore usage of O. persica for antidiabetic properties.
Assuntos
Antioxidantes/uso terapêutico , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Lamiaceae , Extratos Vegetais/uso terapêutico , Animais , Antioxidantes/química , Antioxidantes/isolamento & purificação , Diabetes Mellitus Experimental/metabolismo , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Masculino , Camundongos , Componentes Aéreos da Planta , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Resultado do TratamentoRESUMO
Lythrum salicaria L. (Lythraceae), a herbaceous plant growing widely in Iran, has been well known for many centuries for its astringent and styptic properties. A phytochemical investigation of this plant, based on spectroscopic analysis, identified fourteen compounds: 5-hydroxypyrrolidin-2-one (1), umbelliferone-6-carboxylic acid (2), 3,3',4'-tri-O-methylellagic acid-4-O-beta-D-(2"-acetyl)-glucopyranoside (3), 3,3',4'-tri-O-methylellagic acid-4-O-beta-D-glucopyranoside (4), daucosterol (5), phytol (6), dodecanoic acid (7), oleanolic acid (8), 3,3',4'-tri-O-methylellagic acid (9), corosolic acid (10), beta-sitosterol (11), peucedanin (12), buntansin (13), and erythrodiol (14). All compounds, except for 8 and 11, have been isolated from L. salicaria for the first time. Cytotoxic activities of the compounds were examined against three cancerous cell lines, colon carcinoma (HT-29), leukemia (K-562), and breast ductal carcinoma (T47D), and Swiss mouse embryo fibroblast (NIH-3T3) cells using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and methotrexate as positive control. Compounds 5, 10, 11, and 14 were the most active against the HT-29 cell line with IC50 values of 192.7, 36.8, 38.2, and 12.8 microg/mL, respectively. Compounds 14, 11, 5, and 10 were 6.4, 2.8, 2.6, and 1.4 times, respectively, more selective than methotrexate. Compound 5 was the most active against the K-562 cell line (IC50 = 50.2 microg/mL), with a selectivity exceeding that of methotrexate 13.3 times. The results of the cytotoxic assay confirmed that growth and proliferation of the cancer cell lines are predominantly influenced by triterpene derivatives and sterols of this plant.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Lythrum/química , Extratos Vegetais/farmacologia , Animais , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , CamundongosRESUMO
BACKGROUND: There are several plants have been used worldwide in the folk medicine with high incidence for treatment of human disorders, of which Lythrum salicaria belongs to the Lythraceae family has traditionally reputation for some medicinal usage and recently many biological and pharmacological activity of the plant have been studied. METHODS: In this study, microscopic characterizations of the aerial parts of the plant were determined. Moreover, the plant extract (aqueous methanol 80%) was subjected to an anti-diabetic activity test (in a rat model of streptozocin induced diabetes), anti-Helicobacter pylori (using disc diffusion method) along with antioxidant activity against DPPH (stable free radical) tests. Besides, total flavonoids, phenols, tannins, as well as polysaccharides contents have been assessed using spectroscopic methods. RESULTS: The microscopic properties of the plant fragments revealed anomocytic stomata, conical shape trichomes, and abundant spherical pollen grains as a characteristic pattern for the aerial parts of the plant. The extract of the plant at concentration of 15 g/kg showed mild lowering activity on blood glucose level to 12.6% and 7.3% after 2 and 3 h of administration. Additionally, clinically isolated H. pylori strain was inhibited with the plant extract at concentration of 500 mg/mL (zone of inhibition: 17 ± 0.08 mm). Moreover, IC50 values for DPPH inhibition of the plant extract, vitamin E, BHA were examined as 13.5, 14.2, and 7.8 µg/mL, respectively. Total flavonoids, phenols, tannin, and polysaccharides contents of the extract were successfully evaluated as 5.8 ± 0.4 µg QE/mg EXT, 331 ± 3.7 µg GAE/mg EXT, 340 ± 2.3 µg TAE/mg EXT, 21 ± 0.2 µg GE/mg EXT, respectively. CONCLUSIONS: The results suggested that L. salicaria has low anti-diabetic and anti-Helicobacter pylori effects, but high antioxidant activity, just the same as positive standard (vitamin E), which might be attributed to the high content of phenolic compounds in the extract.
Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Diabetes Mellitus Experimental/tratamento farmacológico , Radicais Livres/metabolismo , Helicobacter pylori/efeitos dos fármacos , Hipoglicemiantes/administração & dosagem , Lythrum/química , Extratos Vegetais/farmacologia , Animais , Helicobacter pylori/isolamento & purificação , Humanos , Hipoglicemiantes/uso terapêutico , Úlcera Péptica/microbiologia , Extratos Vegetais/química , Plantas Medicinais/química , Antro Pilórico/microbiologia , Ratos , Ratos Wistar , EstreptozocinaRESUMO
BACKGROUND: Melia azedarach L. is an important medicinal plant that is used for variety of ailments in Iranian traditional medicine. Azadirachta indica A. Juss is its allied species and possesses similar properties and effects. The present study was undertaken to investigate anticancer activity of these M. azedarach in comparison with A. indica on cancer cell lines and also to evaluate their safety in humans by testing them on normal cell line. The study also aimed to determine the active components that are responsible for medicinal effects of M. azedarach in traditional usages. METHODS: In this study, the cytotoxic activity of crude extracts from M. azedarach and A. indica leaves, pulps and seeds as well as three main fractions of their leaf extracts were assayed against HT-29, A-549, MCF-7 and HepG-2 and MDBK cell lines. MTT assay was used to evaluate their cytotoxic activities. Methanol leaf fraction of M. azedarach as the safest leaf fraction in terms of cytotoxicity was subjected for phytochemical study. RESULTS: Results of the present study indicated that seed kernel extract of M. azedarach had the highest cytotoxic activity and selectivity to cancer cell lines (IC50 range of 8.18- 60.10 λg mL-1). In contrast to crude seed extract of A. indica, crude pulp and crude leaf extracts of this plant showed remarkably stronger anti-prolifrative activity (IC50 ranges of 83.45 - 212.16 λg mL-1 and 34.11- 95.51 λg mL-1 respectively) than those of M. azedarach (all IC50 values of both plants > 650 λg mL-1). The phytochemical analysis led to the isolation of four flavonol 3-O-glycosides including rutin, kaempferol-3-O-robinobioside, kaempferol-3-O-rutinoside and isoquercetin along with a purin nucleoside, β-adenosine. CONCLUSIONS: The anti-prolifrative potentials of extracts from different parts of M. azedarach and A. indica were determined. By comparison, methanol leaf fraction of M. azedarach seems to be safer in terms of cytotoxicity. Our study shows that flavonols are abundant in the leaves of M. azedarach and these compounds seem to be responsible for many of medicinal effects exploited in the traditional uses.
RESUMO
Seven undescribed sesquiterpene derivatives, Azerins A-G (3-6, 8, 14 and 15), three known sesquiterpene phenols, kopetdaghin A (1), kopetdaghin B (2) and latisectin (7), together with five known sesquiterpene coumarins (9-13), were isolated from the roots of Dorema glabrum. The structures were elucidated by comprehensive 1D- and 2D-NMR spectral analysis as well as HR-ESI-MS. Compounds were assessed for their in vitro antiprotozoal activity against Trypanosoma brucei rhodesiense, T. cruzi, Leishmania donovani, and Plasmodium falciparum. Cytotoxic potentials of the compounds were also tested on L6 rat skeletal myoblasts. Azerin G (15) showed a potent preferential growth inhibitory activity against T. b. rhodesiense with IC50 value of 0.01 µM and selectivity index of 329. Compounds 1, 4, 7 and 8 were also found as the most active compounds with selective growth inhibitory effects toward P. falciparum with selectivity indices ranging from 11.6 to 16.7 (IC50: 1.8-24.6 µM).
Assuntos
Antiprotozoários , Ferula , Leishmania donovani , Sesquiterpenos , Trypanosoma cruzi , Animais , Ratos , Estrutura Molecular , Antiprotozoários/farmacologia , Sesquiterpenos/farmacologia , Sesquiterpenos/química , Espectroscopia de Ressonância Magnética , Plasmodium falciparum , Trypanosoma brucei rhodesiense , Concentração Inibidora 50 , Testes de Sensibilidade ParasitáriaRESUMO
Medicinal plants such as Leutea avicennae Mozaff. (Apiaceae) have been shown some biological potential for preventing and treating diseases. Fractions and isolated compounds were tested on colon carcinoma (HT-29), cervical carcinoma (HeLa), breast carcinoma (MCF-7), and mouse embryonic fibroblast (NIH/3T3) cell lines. The BSLT method was used for the assessment of the general toxicity of the petroleum ether (PET), chloroform (CHCl3), ethyl acetate (EtOAc), and methanol (MeOH) fractions obtained from the aerial parts of L. avicennae. 1H-NMR and 13 C-NMR spectroscopy were used for structure elucidation. Five compounds, including two coumarins, osthole and umbelliferone, a diterpene phytol, ß-sitosterol, and lauric acid, were isolated for the first time from L. avicennae. Osthole showed potent cytotoxic activity against MCF-7 and HT-29 cell lines with IC50 values of 4.23 ± 0.26 and 12.11 ± 0.13 µg/mL, respectively. Phytol demonstrated potent cytotoxic activity towards MCF-7 and HeLa cell lines with IC50 values of 6.80 ± 0.08 and 12.27 ± 0.18 µg/mL, respectively.
RESUMO
Objectives: Influenza A virus (IAV) is a contagious illness. Different species of Scutellaria genus are used as a traditional remedy to reduce influenza symptoms. This study aimed to investigate the anti-influenza capacity of several species of Iranian Scutellaria and identify active compounds of the most potent species for the first time. Materials and Methods: Some Iranian species of Scutellaria were collected from different regions of Iran, including S. pinnatifida with mucida, viridis, and alpina subspecies; S. tournefortii; S. tomentosa; S. persica. They were fractionated to chloroform and methanol. The total phenols and flavonoids of samples were examined by the folin-ciocalteau and aluminum-flavonoid complex methods, respectively. The 50% cytotoxic concentrations (CC50) on MDCK cells and non-cytotoxic concentrations (NCTC) were determined by MTT assay. The percentage of cell protection against IAV and their effect on virus titer were investigated in pre-, post-, and co-penetration treatment groups. Phytochemicals of the most effective species were isolated by various chromatographic methods and identified by different spectroscopic methods. Results: Methanol fraction of S. pinnatifida subsp. viridis demonstrated the highest amounts of flavonoid content and best activity against influenza A virus in all combination treatments, which reduced the virus titer by 5 logs with no cytotoxicity. Kaempferol-3-O-glucoside, quercetin-3-O-glucoside, apigenin-4'-methoxy-7-O-glucoside, luteolin, and luteolin-7-O-glucoside were purified and identified from this species. Conclusion: Scutellaria pinnatifida subsp. viridis can be introduced as a source of flavonoids with acceptable anti-influenza activity. S. tomentosa also showed potent antiviral effects and is a candidate for elucidation in further studies.
RESUMO
The n-butanolic fraction of a methanolic extract (80%) from aerial parts of Ajuga chamaecistus ssp. tomentella was analysed using different chromatographic methods. Column (CC) and high-performance liquid chromatography (HPLC) were used for isolation and purification. 13C, H NMR, H-H COSY, HSQC, HMBC, and ESI-MS were employed for identification of the compounds isolated from this fraction. The structures of the compounds were determined to be cis-melilotoside (1), trans-melilotoside (2), lavandulifolioside (3), 20-hydroxyecdysone (4), leonoside B (5), martynoside (6), ajugalactone (7), makisterone A (8), and 24-dehydroprecyasterone (9). This is the first report on the presence of cis- and trans-melilotoside in Ajuga species. Cytotoxic evaluation of the n-butanolic fraction, cis- and trans-melilotoside against cancer (T47D, HT-29, and Caco-2) and normal (NIH 3T3) cell lines by the mitochondrial tetrazolium test (MTT) showed no cytotoxic effects up to 400 microg/mL. The results of this study suggest that melilotoside, phenylethyl glycosides, and phytoecdysteroids are the main constituents of the n-butanolic fraction of Ajuga chamaecistus ssp. tomentella.
Assuntos
Ajuga/química , Antineoplásicos Fitogênicos/farmacologia , Extratos Vegetais/farmacologia , Células 3T3 , Animais , Antineoplásicos Fitogênicos/química , Linhagem Celular Tumoral , Humanos , Espectroscopia de Ressonância Magnética , Camundongos , Extratos Vegetais/química , Espectrometria de Massas por Ionização por ElectrosprayRESUMO
BACKGROUND AND THE PURPOSE OF THE STUDY: The early stage of diabetes mellitus type 2 is associated with postprandial hyperglycemia. Hyperglycemia is believed to increase the production of free radicals and reactive oxygen species, leading to oxidative tissue damage. In an effort of identifying herbal drugs which may become useful in the prevention or mitigation of diabetes, biochemical activities of Polygonum hyrcanicum and its constituents were studied. METHODS: Hexane, ethylacetate and methanol extracts of P. hyrcanicum were tested for α-glucosidase inhibitory, antioxidant and radical scavenging properties. Active constituents were isolated and identified from the methanolic extract in an activity guided approach. RESULTS: A methanolic extract from flowering aerial parts of the plant showed notable α-glucosidase inhibitory activity (IC50 = 15 µg/ml). Thirteen phenolic compounds involving a cinnamoylphenethyl amide, two flavans, and ten flavonols and flavonol 3-O-glycosides were subsequently isolated from the extract. All constituents showed inhibitory activities while compounds 3, 8 and 11 (IC50 = 0.3, 1.0, and 0.6 µM, respectively) were the most potent ones. The methanol extract also showed antioxidant activities in DPPH (IC50 = 76 µg/ml) and FRAP assays (1.4 mmol ferrous ion equivalent/g extract). A total phenol content of 130 mg/g of the extract was determined by Folin-Ciocalteu reagent. CONCLUSION: This study shows that P. hyrcanicum contains phenolic compounds with in vitro activity that can be useful in the context of preventing or mitigating cellular damages linked to diabetic conditions.
RESUMO
Trigonella genus is a member of Fabaceae family, which is used as medicinal plant. The aim of this study was investigation of phytochemicals and some biological activities of Trigonella teheranica for the first time. The essential oils (EOs) of different parts (leaves, fruits and roots) were obtained and analyzed by GC-MS. Also, their chloroform and methanol extracts were prepared, too. The antimicrobial effects, antioxidant activities and cytotoxic effects against cancer (MDA-MB-231, MRC5 and HT-29) cell lines were investigated. N-hexadecanoic acid was the major compound of leaves and fruits EOs, and hexanal was abundant component of roots EO. The extracts showed stronger antibacterial effects than volatile oils against Gram-positive bacteria such as Staphylococcus aureus and Bacillus subtilis. All methanol extracts showed strong antioxidant effects, while the volatile oils, especially of leaves was the most effective in cytotoxic assay. Also, three derivatives of coumaric acid were isolated and identified from T. teheranica.
Assuntos
Óleos Voláteis , Trigonella , Antioxidantes/farmacologia , Metanol/química , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Compostos Fitoquímicos/farmacologia , Óleos Voláteis/química , Antibacterianos/químicaRESUMO
The Phytochemical profiling of the root extract of Salvia leriifolia, an endemic plant of Iran, was investigated and 16 abietane diterpenes were isolated, and three were original compounds. 1D and 2D NMR and HRMS performed structural elucidation. The absolute configuration of the previously unreported compounds was determined by circular dichroism (ECD). The cytotoxicity of the isolated compounds was investigated against AGS, MIA PaCa-2, HeLa, and MCF-7 cell lines by the MTT assay. The known diterpene pisiferal possesses high cytotoxicity against all investigated cell lines at a concentration between 9.3 ± 0.6 and 14.38 ± 1.4 µM.
Assuntos
Antineoplásicos Fitogênicos , Antineoplásicos , Diterpenos , Salvia , Abietanos/química , Abietanos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Diterpenos/química , Humanos , Estrutura Molecular , Salvia/químicaRESUMO
The reversed-phase (RP) preparative HPLC analyses of the MeOH extract of the aerial parts of Artemisia armeniaca yielded four prenylated coumarins, 7-hydroxy-8-(4-hydroxy-3-methylbutoxy)coumarin (named armenin), 8-hydroxy-7-(4-hydroxy-3-methylbutoxy)coumarin (named isoarmenin), lacarol, and deoxylacarol, together with five other compounds, including three flavonoid glycosides, quercetin 3-O-ß-D-glucopyranoside, rutin, and kaempferol 3-O-ß-D-glucopyranoside, and chlorogenic acid, and tryptophan. (10E,12Z)-9-Hydroxyoctadeca-10,12-dienoic acid (ß-dimorphecolic acid) was isolated from the CH(2)Cl(2) extract. Armenin and isoarmenin were new coumarins. Structures of all compounds were determined by spectroscopic means, including UV, MS, 1D- and 2D-NMR. The in vitro free-radical-scavenging property of the extracts and isolated compounds was evaluated by the 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay.
Assuntos
Artemisia/química , Cumarínicos/isolamento & purificação , Sequestradores de Radicais Livres/isolamento & purificação , Compostos de Bifenilo/química , Cromatografia Líquida de Alta Pressão , Cumarínicos/farmacologia , Sequestradores de Radicais Livres/farmacologia , Isomerismo , Estrutura Molecular , Picratos/química , Componentes Aéreos da Planta/química , Extratos Vegetais/química , PrenilaçãoRESUMO
OBJECTIVES: The objective of this study was to evaluate larvicidal activity of native marine algae against main malaria vector Anopheles stephensi. STUDY DESIGN: The total 70% methanol (MeOH) extract and partition fractions of chloroform (CHCl3), ethylacetate (EtOAc), and MeOH from two algae, Sargassum swartzii and Chondria dasyphylla were investigated for larvicidal activities against late III and early IV instar larvae of malaria vector An. stephensi. RESULTS: Among all the fractions tested against larvae, EtOAc fraction of S. swartzii and C. dasyphylla, showed mortality rate of 96 and 95%, respectively. Probit analysis of logarithmic concentration from regression line exhibited the LC50 and LC90 values of 11.75 and 53.47 ppm respectively for S. swartzii and 10.62 and 56.39 ppm respectively for C. dasyphylla. CONCLUSION: This is the first report of larvicidal activities of two native algae against An. stephensi. We propose that the larvicidal activity of EtOAc fraction is related to the presence of semi- polar compounds. Further isolation and purification could lead to identify more potent compounds.
Assuntos
Anopheles/efeitos dos fármacos , Insetos Vetores/efeitos dos fármacos , Inseticidas/farmacologia , Rodófitas/química , Sargassum/química , Animais , Anopheles/parasitologia , Insetos Vetores/parasitologia , Inseticidas/isolamento & purificação , Larva/efeitos dos fármacos , Larva/parasitologia , Dose Letal Mediana , Malária/parasitologia , Plasmodium/fisiologia , Análise de RegressãoRESUMO
CONTEXT: Artemisia annua L. (Asteraceae), commonly known as sweet wormwood or Qinghao, is an annual herb/shrub native of Asia. The plant grows broadly in Caspian Sea shores in North of Iran. In China, the aerial parts of this plant are source of artemisinin, which is an antimalarial compound. OBJECTIVE: This study aimed to establish the scientific basis of reported ethnomedicinal use of A. annua as sedative agent. MATERIAL AND METHODS: The plants were gathered from Gilan Province in Iran. Plant aerial parts were extracted with methanol and concentrated in vacuum. Methanol extract was partitioned into chloroform, petroleum ether, and ethyl acetate. Each fraction was administered intraperitoneally (i.p.) in male mice with different concentrations (50, 100, and 200 mg/kg), and for evaluation of sedative activity, immobility time was determined. In effort to clarify the mechanism of action, flumazenil (3 mg/kg, i.p.) as a benzodiazepine (BZD) receptor antagonist was injected 15 min before chloroform fraction (200 mg/kg, i.p.). RESULTS: Compared with control group (saline-treated mice), the chloroform fraction significantly increased immobility time in a dose-dependent manner. Flumazenil decreased immobility time induced by chloroform fraction significantly. DISCUSSION AND CONCLUSION: The results of the present study suggest that A. annua growing in Iran has sedative effects, which are probably mediated via BZD receptors pathways.
Assuntos
Artemisia annua , Hipnóticos e Sedativos/farmacologia , Extratos Vegetais/farmacologia , Receptores de GABA-A/efeitos dos fármacos , Acetatos/química , Alcanos/química , Animais , Antídotos/farmacologia , Antimaláricos/farmacologia , Artemisininas/farmacologia , Clorofórmio/química , Diazepam/farmacologia , Relação Dose-Resposta a Droga , Flumazenil/farmacologia , Hipnóticos e Sedativos/química , Hipnóticos e Sedativos/metabolismo , Imobilização , Irã (Geográfico) , Masculino , Camundongos , Fitoterapia , Componentes Aéreos da Planta , Extratos Vegetais/química , Extratos Vegetais/metabolismo , Receptores de GABA-A/metabolismo , Solventes/químicaRESUMO
OBJECTIVE: Many pharmaceutical factories have dramatically improved the quality of herbal remedies in cancer treatment. The results of somestudies have shown anticancer effect of Astrodaucus genus. Therefore, the aim of this article was to review the chemical ingredients and biological effects of Astrodaucus genus especially A. persicus from the family Apiaceae (Umbelliferae). MATERIALS AND METHODS: Online databases ScienceDirect, PubMed, Scopus, and Google Scholar were searched using the keywords Astrodaucus, Apiaceae, Biologic, Phytochemistry, and Benzodioxole to retrieve studies published between 1970 and 2020. RESULTS: The Astrodaucus genus has two species, Astrodaucus persicus (Boiss.) Drude and Astrodaucus orientalis (L.) Drude. In this genus, 5 new biologically active phytochemicals with benzodioxole structure were introduced and their biological effects were assessed. CONCLUSION: Since many of the most commonly used anticancer drugs such as etoposide, teniposide, podophyllotoxin and sanguinarine have benzodioxole structureand according to the results of biological tests, it seems that more researchwith these perspectives should be done on this genus.
RESUMO
Four undescribed and 17 known diterpenoids were isolated from the roots of Zhumeria majdae Rech.f. & Wendelbo. Using 1D and 2D NMR spectroscopy, ECD spectroscopy, and HRESIMS data analysis, the structures of the undescribed compounds were elucidated. The anti-proliferative activity of isolated compounds was evaluated against HeLa and MCF7 cancer cell lines. The binding affinity of all compounds to HSP90, one of the targets for the modern anticancer therapy, was investigated using surface plasmon resonance. The results demonstrated that lanugon Q interacted with the chaperone. To explain its mechanism of action, experimental and computational tests were also conducted.
Assuntos
Diterpenos , Salvia , Diterpenos/farmacologia , Proteínas de Choque Térmico , Estrutura Molecular , Extratos Vegetais , Raízes de PlantasRESUMO
Vinca minor L. (Apocynaceae) is a medicinal plant that has long been used to treat cerebral and memory disorders in European folk medicine. Furthermore, it contains more than 50 alkaloids, some of them having bisindole structure such as the antineoplastic alkaloids present in Catharanthus roseus (L.) G. Don (Apocynaceae). In this study, the plant's alkaloid extract was divided into three fractions and the cytotoxic effects on cell proliferation of HT-29, Caco-2, T47D, and NIH/3T3 cell lines were examined. All alkaloid fractions showed a dose-dependent cytotoxic effect on the cell lines. IC(50) values confirmed that the growth and proliferation of NIH/3T3 cells were less affected in comparison to other cell lines.
Assuntos
Citotoxinas/toxicidade , Alcaloides de Vinca/toxicidade , Vinca , Animais , Células CACO-2 , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/fisiologia , Citotoxinas/isolamento & purificação , Células HT29 , Humanos , Camundongos , Células NIH 3T3 , Componentes Aéreos da Planta , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Alcaloides de Vinca/isolamento & purificaçãoRESUMO
Salvia reuterana Boiss. is an aromatic perennial plant traditionally used for its anxiolytic and sedative properties. In the present study, various fractions and essential oil of S. reuterana aerial parts were investigated to find its free radical scavenging principles. Hydroalcoholic fraction with IC50 value of 112.6 ±3.2 µg mL-1 in DPPH assay demonstrated the highest free radical scavenging activity and was selected to further phytochemical investigation. RP-18 and Sephadex LH-20 column chromatography of the hydroalcoholic fraction resulted in the isolation and structural elucidation of four phenolic derivatives, including apigenin-7-O-ß-D-glucopyranoside (1), luteolin-7-O-ß-D-glucopyranoside (2), rosmarinic acid (3), and luteolin (4). Isolated compounds showed potent free radical scavenging activities (5.1-34.2 µg mL-1), compared with BHT (21.30 ± 1.9 µg mL-1). Twenty four compounds were also identified in GC-MS analysis of the plant essential oil, of which benzyl benzoate (26.64%), n-hexyl benzoate (22.99%) and n-hexyl isovalerate (6.04%) were the main compounds. The results of the present study introduced S. reuterana as a valuable source of natural phenolic antioxidants which can be utilized in prevention of oxidative stress related diseases. Moreover, interesting composition of S. reuterana essential oil, dominated by non-terpenes compounds (76.17%) especially aromatic derivatives, make it an appropriate candidate for more detailed studies.