Alkaloid Fraction Research Articles

Rapid Detection of Eight Volatile Alkaloids from Caryota mitis Lour. by LC-MS/MS and Antimicrobial Effects of their Extracts

Caryota mitis Lour. palm belongs to Family: Arecaceae. Pyridine and piperidine alkaloids are the most bioactive secondary metabolites reported in this Family. The dried leaves of Caryota mitis Lour. were subjected to defatting using n-hexane. The alkaloids were extracted from the defatted powder (marc) by acid base method. Eight pyridine/ piperidine alkaloids were detected by LC-MS and reported for the first time in the genus Caryota. The alkaloid fraction as well as other plant extract fractions showed antibacterial and antifungal activities (MIC) against selected strains.

Phenotype behavioral impairment after the administration of Xylopia Aromatica to male Balb-c mice and cytotoxicity to breast and cancer cell lines

Background: Crude extract obtained from the stem of Xylopia aromatica (Annonaceae, EB149) known as pimenta-de-macaco, a traditional Brazilian medicinal and edible plant, showed cytotoxicity against leukemia cell lines. Despite the initial findings, no information regarding its influence on behavioral phenotype (BP) has been previously reported. Objective: The objective was to assess the effect on EB149 on BP in male mice and to perform a bioguide-fractionation aimed at the verification of the cytotoxic potential against breast and prostate cancer cell lines. Materials and Methods: BP was assessed by observation in an open cage and subsequent analysis in an open field (OF) at 15, 30, 60, 120, and 180 min, after intraperitoneal administration of X. aromatica, in a two-stage experimental delineation. Results: EB149 impaired general activity, piloerection, defecation, breathing, auricular and corneal reflexes, tail squeeze, response to touch, hindquarter fall, surface-righting reflex, body tone, and grip reflex in the first stage. In the second stage, general activity, tail squeeze, touch response, and breathing were impaired, and a decrease in locomotion frequency in OF was also observed. All behavioral changes were recovered during the period of experiment in both stages. The LD50 of EB149 was 1.944 g/kg. Two fractions obtained from EB149 named FSIST, which contains sitosterol and stigmasterol as major compounds, and total alkaloid fraction, which contains total alkaloids, showed cytotoxicity against breast and prostate cancer cell lines. Conclusions: The traditional plant X. aromatica EB149 organic extract showed cytotoxicity against breast and prostate cancer cell lines and the recovery of behavioral impairment related to general activity, tail squeeze, touch response, breath, and locomotion frequency, causing no harm to male lab mice. Abbreviations used: MMA/ICMBio/SISBIO: Ministerio do Meio Ambiente/Instituto Chico Mendes de Conservacao da Biodiversidade/Sistema de Autorizacao e Informacao em Biodiversidade; CGen/IBAMA/MMA: Conselho de Gestao do Patrimonio Genetico/Instituto Brasileiro do Meio Ambiente e dos Recursos Naturais Renovaveis/Ministerio do Meio Ambiente; AM: Amazonas State; UNIP: Universidade Paulista; g: Gram; mg: Milligram; μg: Microgram; kg: Kilogram; I. P: Intraperitoneal; CEUA/ICS/UNIP: Comissao de etica no Uso de Animais/Instituto de Ciencias da Saude/Universidade Paulista; BP: Behavioral phenotype; OF: Open-field apparatus; NLD: Nonlethal dose; LD: Lethal dose; ANOVA: analysis of variance; FCHCl3: Fraction chloroform; FBuOH: Fraction buthanol; FH2O: Fraction water; FHEX: Fraction hexane; FDCM: Fraction dichloromethane; FMeOH: Fraction methanol; TLC: Thin-layer chromatography; U. V.: Ultraviolet; TAF: Total alkaloid fraction; nm: Nanometer; CC: Column chromatography; ATLC: Analytical thin-layer chromatography; NMR: Nuclear magnetic resonance apparatus; FSIST: Fraction containing sitosterol and stigmasterol; NC: Naive control; VC: Vehicle control; DIA: Diazepam

The Effect of Alkaloidal Fraction from Annona squamosa L. against Pathogenic Bacteria with Antioxidant Activities

Background: Annona squamosa is used in different places such as India as a general tonic to enrich blood, relieve vomiting, cancer, as a vermicide, for skin complaints and also applied to wounds and ulcers. The purpose of the study was to evaluate the antibacterial and antioxidant properties from of the alkaloidal fraction of A. squamosa. Methods: Well diffusion assay, minimum inhibitory concentration and the minimum bactericidal concentration (MBC) were used to evaluate antibacterial activity against Staphylococcus aureus, Escherichia coli, Bacillus cereus, Pseudomonas aeruginosa, MRSA and Helicobacter pylori. DPPH and SOD assays were used to evaluate antioxidant activity. LC-MS analysis was used to identify alkaloids and scanning electron microscopy studies that revealed mode of action. Results: Alkaloidal fraction of A. squamosa exhibited significant inhibition against the tested bacteria. Extracted alkaloids from the leaves of A. squamosa showed high level of antioxidant activities. LC-MS analyses of alkaloids of the plant were identified as corydine, sanjoinine, norlaureline, norcodeine, oxanalobine and aporphine in the leaves of A. squamosa. SEM analysis of the interaction of these substances with the bacteria showed morphological changes of cell wall and lysis of the targeted bacterial cells. Conclusions: It could be concluded that the alkaloids isolated from A. squamosa showed good antibacterial and antioxidant activity. The results suggest the alkaloids can be a new source of antimicrobial agents against pathogenic bacteria and antioxidant source.

DIURETIC, ANTIDIURETIC AND LAXATIVE ACTIVITIES OF ANTHOCLEISTA VOGELII EXTRACTS IN RATS

Background: Anthocleista vogelii Planch is a medicinal plant used by traditional healers in the treatment of Malaria, hypertension, ulcer, obesity, diabetes, and as a diuretic and purgative in Africa. Therefore, the present study sought to evaluate the diuretic, antidiuretic and laxative activities of the root bark of A. vogelii extracts and fractions in male Sprague-Dawley rats.
 Materials and methods: Sixty rats were placed in 10 groups which included: control (normal saline), furosemide/sodium picosulfate (25 mg/kg) as standard drugs, methanol extracts (250 mg/kg and 500 mg/kg), and 125 mg/kg and 250 mg/kg of saponin, flavonoid and neutral alkaloid fractions of A. vogelii. The drugs/extracts/fractions were administered orally using normal saline as the vehicle.
 Results: The 500 mg/kg methanol extracts (ME) significantly increased (p

Measurement of Alkaloids Achyranthes Aspera Linn Level Using Thin Layer Chromatography Method and High-Performance Liquid Chromatography

One of the plants with the potential to be developed into a raw material for anti-breast cancer drugs is jarong (Achyranthes aspera linn). Allegedly alkaloid of Achryranthes aspera linn leaves showed anticancer activity in vitro in mice myeloma cells is extremely potent. In vivo study showed that the alkaloid Achyranthes aspera linn causes apoptosis and healing in breast cancer cells in mice induced by benzopyrene. Alkaloids of Achyranthes aspera linn leaves as anticancer been listed on Incestual Property Rights (IPR) since October 12, 2012, with number P00201299839. This study aims to prove the existence of alkaloids in the leaves of Achyranthes aspera linn using thin layer chromatography (TLC), determine the level of alkaloids in the leaves alkaloid fraction of Achyranthes aspera using High-Performance Liquid Chromatography (HPLC) and alkaloid fraction dose as an anticancer and dosing for the study. Alkaloid qualitative measurement results with thin layer chromatography showed alkaloid in orange. Alkaloid levels using HPLC has a retention time of 3.482 minutes, a wavelength of 254 nm, there are 13 kinds of chemical substances with the major components amounted to 52.36% alkaloids, the other component is the green substance with a peak area of 13.0624%, while other chemical substances in a very small peak area of between 0.428% until 8.3598%. Alkaloid fraction dose of Achyranthes aspera used in the study as anticancer is controlled the dose of 0 mg/kg, 1 treatment dose of 60 mg/kg, 2 treatment dose of 75 mg/kg and 3 treatment dose of 90 mg/kg. Keywords: Alkaloids, Achyranthes aspera linn, TLC, HPLC.

PXR mediated induction of CYP3A4, CYP1A2, and P-gp by Mitragyna speciosa and its alkaloids.

Kratom (Mitragyna speciosa), a native herb of Southeast Asia, is widely known for its psychoactive properties. Recent increase in the use of kratom as a recreational drug has increased the risk of its interaction with conventional drugs if taken concomitantly. A few reports are available related to the effects of kratom on the activity of cytochrome P450 enzymes (CYPs), but there are no reports of its effects on pregnane X receptor (PXR), a transcription factor that regulates the expression of CYPs and P-glycoprotein (P-gp). This study was carried out to evaluate the effects of a methanolic extract of kratom leaves, an alkaloid rich fraction and its 5 indole and 4 oxindole alkaloids on PXR activation and the resulting changes in the mRNA expression of PXR target genes (CYP3A4, CYP1A2, and P-gp). A significant activation of PXR was observed by the extract (3-fold), alkaloidal fraction (4-fold) and all 9 alkaloids (4- to 6-fold) that was associated with an increased mRNA expression which resulted into an increase in the activity of CYP3A4, CYP1A2, and P-gp. These results indicate that high consumption of Mitragyna speciosa extract along with the conventional drugs may lead to potential herb-drug interactions due to its effects on PXR.

Computational Chemistry Study of Natural Alkaloids and Homemade Databank to Predict Inhibitory Potential Against Key Enzymes in Neurodegenerative Diseases.

Cissampelos sympodialis Eichl is used in folk medicine for the treatment of various inflammatory diseases; several alkaloids have been isolated from this species and some of them have anti-allergic, immunomodulatory and spasmolytic activities. Treatment of rats with the total tertiary alkaloid fraction showed an antidepressant effect. One of the depression causes can be the deficiency of monoamines, which is a factor displayed in patients with Alzheimer's disease. Theoretical studies using in silico methods have aided in the process of drug discovery. From this perspective, we applied ligand-based-virtual associated with structure-based-virtual screening of alkaloids from C. sympodialis Eichl and 101 derivatives proposed by us are promising leads against some important targets (BACE, GSK-3β and MAO-A). From the ChEMBL database, we selected a diverse set of 724, 1898 and 1934 structures, which had been tested against BACE, GSK-3β and MAO-A, to create Random Forest (RF) models with good overall prediction rate, over 78%, for cross-validation and test set. Compounds 24 and 47 presented activity against GSK-3β and MAO-A simultaneously. The natural alkaloids roraimine and simpodialine-β-N-oxide presented activity against BACE and liriodenine against MAO-A. The top 20 compounds with best docking performance per enzyme were selected and validated through the RF model. All 9 compounds classified as active in RF model for BACE are bisbenzylisoquinoline alkaloids and were present in the top docking scoring, demonstrating a consensus on results. Affinities of bisbenzylisoquinoline alkaloids, including two secondary metabolites (roraimine and simpodialine-β-N-oxide), with BACE suggest that this skeleton can be used as a model to design new antagonists of this enzyme.

The antioxidant, anti-inflammatory and antidiabetic activities of Sternbergia lutea ssp. lutea and Sternbergia lutea ssp. sicula

Determine a relationship between the neuroprotective activity and the antioxidant capacity of the Amaryllidaceae alkaloids in a model of Glu excitotoxicity in rat cortical neurons.Was evaluated several alkaloidal fractions isolated from Amaryllidaceae species, a family known to contain neuroprotective alkaloids, in a model of Glu excitotoxicity in rat cortical neurons. In addition, several mechanisms of antioxidant activity were used, and a theoretical study of the antioxidants was performed.The results of this study suggest that a possible neuroprotective mode of action of the alkaloidal fractions of Eucharis bonplandii (Kunth) Traub bulbs, Eucharis caucana Meerow bulbs, and Clivia miniata Regel leaves, is through their antioxidant activity and ability to stabilize free radicals generated from an excitotoxic process mediated by Glu. The chemical structure characterization and antioxidant activity of the fractions suggest that the phenol and enol groups in the structures of the alkaloids are critical for the stabilization of ROS and RNS. Additionally, the pair of free electrons on the N is spatially close to a hydroxyl group, which benefits the cleavage of this group and, consequently, the stabilization of the generated O.The versatility of the structures of the studied Amaryllidaceae alkaloids suggests that they have potential as neuroprotective agents against an oxidative stimulus.

Antioxidant Activity of Phenolic and Alkaloid Fractions Accumulated in Artemisia Judaica and Artemisia Herba Alba

Genus Artemisia are desert plants spread in the Egypt and Saudi Arabia. The methanol extract of the aerial parts of Artemisia herba alba and Artemisia judaica grown in the arid zones in the Northern regions of Saudi Arabia and North Sinai, in Egypt were subjected to the primary phytochemical analysis which, showed the presence of phenolic compounds, flavonoids, tannins and sterols. The GC-MS analysis of the methanolic extract exhibited numerous compounds, 11 compounds were identified as phenolic compounds, ferulic acid, ursodeoxycholic acid and derivatives of cinnamic acid (ethyl cinnamate). The highest phenolics content in A.herba alba grown in Saudi Arabia was observed for methyl cinnamate, (8.2 %) and the lowest methyl ferulate (0.02 %) for A. judica grown in Egypt. The quantization analysis of GC-MS revealed high amount of phenolic acid in the plant grow in Saudi Arabia than the plant collected from Egypt. The radical scavenging activities of two plant were studied by 1,1-diphenyl -2-pycrylhydrazyl (DPPH), EC (50) values were determined for A.herba alba and A.judaica (0.122, and 0.56 mg/ml) growing in Saudi Arabia and A.herba alba and A. judaica (1.7 and 0. 67 mg/ml ) growing in Egypt. Total alkaloid content was analysed and some alkaloid compounds was identified by GC-MS, viz. dasycarpidan-1-methanol, acetate, pseudosolasodine diacetate and morphinan4,5epoxy3,6-diol. Certain compounds were rich in Saudi plant but not detected in plants grown in Egypt, which reflect the role of environment adaptation of plant by accumulation of only certain compounds.

Pharmacokinetics, Tissue Distribution, and Elimination of Three Active Alkaloids in Rats after Oral Administration of the Effective Fraction of Alkaloids from Ramulus Mori, an Innovative Hypoglycemic Agent.

In this study, we systematically investigated the plasma pharmacokinetics, tissue distribution, and elimination of three active alkaloids after oral administration of the effective fraction of alkaloids from Ramulus Mori (SZ–A)—an innovative hypoglycemic agent—in rats. Moreover, the influences of other components in SZ–A on dynamic process of alkaloids were explored for the first time. The results showed that 1-deoxynojirimycin (DNJ), fagomine (FGM) and 1,4-dideoxy-1,4-imino-d-arabinitol (DAB) exhibited nonlinear pharmacokinetics following oral administration of SZ–A (40–1000 mg/kg). The prolonged t1/2 and greater area under concentration-time curve (AUC) versus time (AUC0–t) of DNJ for SZ–A than for purified DNJ has been observed after both oral and intravenous administration. It was found that other components in SZ–A could enhance the absorption of DNJ through the intestinal barrier. The major distribution tissues of DNJ, FGM, and DAB were the gastrointestinal tract, liver, and kidney. Three alkaloids were mainly excreted into urine and feces, but less into bile. Interestingly, the excess excretion of FGM was revealed to be partly due to the biotransformation of other components in SZ–A via gut microbiota. These information provide a rational basis for the use of SZ–A in clinical practice.

Chromatography Analysis of Fatty Acids, Volatile Compounds and Alkaloids of Ephedra alata Growing Wild in Southern Tunisia and Evaluation of their Antioxidant Activity

In order to provide more information about phytochemical composition of Tunisian Ephedra alata known for their medicinal uses, fatty acids, volatile compounds and alkaloids have been analyzed in fresh or dry plant materials whether powdered or not. Extraction was performed with hexane and ethanol in soxhlet extractor and all extracts were analyzed by GC-MS. Phosphomolybdenum, DPPH and FRAP methods were used to evaluate their antioxidant activities. The dry matter present a more diversified fatty acids composition dominated by palmitic acid, oleic acid and linolelaidic acid. Hydrocarbons represent the largest group of volatile compounds, followed by alcohols. The most known detected ephedrine-type alkaloid characteristic of the Ephedra genus are dominated by pseudoephedrine, norephedrine, ethylephedrine. Some other compounds are mentioned for the first time in E. alata alkaloids such as azetidine, 1,2- dimethyl-3-phenylaziridine, N-ethyl benzamide and N-methyl-mandelamide. Lower total antioxidant and anti-radicular effects were shown with hexane extracts and alkaloid fractions instead the ferric reducing antioxidant power test showed the highest results with obtained alkaloid from powdered fresh and dry plant materials. Lipids, volatile compounds and alkaloids in E. alata that have been assessed could provide possible roles in case of human breast cancer and health benefits and therefore a research on this plant might be of value in drug industry.

Toxicological profile and acetylcholinesterase inhibitory potential of Palicourea deflexa, a source of β-carboline alkaloids

Palicourea genus is chemically and taxonomically close to Psychotria genus, a well-known source of neuroactive alkaloids. It has been previously reported the pharmacological potential of these alkaloids in some targets related to the neurodegenerative process. In this context, this study was carried out in order to evaluate the toxic effects and acetylcholinesterase (AChE) inhibitory potential of Palicourea deflexa fraction of total alkaloids (FTA). P. deflexa FTA was analyzed by means of HPLC-DAD and HRMS-ESI. We performed toxicological screening through Fish Embryo Toxicity (FET) test using zebrafish embryo and abnormal developmental phenotypes were recorded daily. For AChE inhibition, zebrafish brains were used as enzymatic source and formation of thiolate dianion of 5,5′-Dithiobis(2-nitrobenzoic acid) (DTNB) was used to monitor acetylthiocholine hydrolysis. Lineaweaver–Burk double reciprocal plots were used to indicate mode of inhibition. Chemical analysis of the P. deflexa FTA allowed the identification of the main compound as harman-3-carboxylic acid. This fraction was evaluated in vivo for its toxicological effect. The zebrafish embryo test indicated that the FTA has a lethal concentration of 50% (LC50)=72.18μg/mL. Further, the FTA was evaluated for its AChE inhibitory profile, demonstrating an inhibitory concentration of 50% (IC50) of 50.65μg/mL. Lineaweaver–Burk double reciprocal plots indicated a mixed mode of inhibition. It is reported for the first time the toxicological and pharmacological profile of the alkaloid fraction of Palicourea deflexa in zebrafish models.

Qualitative and quantitative determination of main alkaloids of Chelidonium majus L. using thin-layer chromatographic-densitometric method

We present a new simple thin-layer chromatographic method designed for determination of the main alkaloids of Chelidonium majus L. In this study, we used roots and herb of the plant collected in spring and autumn. The alkaloid fractions were prepared according to modified pharmacopeial procedure [1]. In our method, we performed two-step elution onto silica gel plates. The first eluent consisted of chloroform, methanol, and water mixed with 70:30:4 proportion. The second eluent comprised of toluene, ethyl acetate, and methanol with 83:15:2 proportion. The described thin-layer chromatography (TLC) system allows qualitative and quantitative determination of the following alkaloids: sanguinarine, chelerythrine, chelidonine, coptisine, and berberine. For determination of protopine, eluent with n-buthanol, acetic acid, and water in 15:1.5:4 proportion was investigated. The dominant alkaloids observed in studied fractions were coptisine (1027.096 ± 13.367–287.474 ± 3.069 mg/100 g dry matter ± sdv) and chelidonine (1780.667 ± 263.522– 115.929 ± 14.694 mg/100 g dry matter ± sdv). The alkaloid detected in the least amount was chelerythrine (30.74 ± 7.526–1.143 ± 0.0651 mg/100 g dry matter ± sdv). The highest total amount of all alkaloids was determined in the fractions obtained from herbs in spring, and the lowest amount was detected in herbs autumn. Additionally, we compared amounts of studied alkaloids in different parts of plants (aerial parts and roots). The plants were collected in spring and autumn. Authors concluded that the presented method can be used as a valuable tool for screening studies on C. majus L.

Evaluation of antiplasmodial properties of a cyanobacterium, Spirulina platensis and its mechanism of action

The rapid emergence of antimalarial drug resistance necessitates a continual effort on novel drug discovery. A cyanobacterium, Spirulina platensis, is a potential antimalarial agent that has been widely consumed as food supplement in the form of crude extract. It is known to possess antiviral, antibacterial and antifungi activities. This study examined the antimalarial activities of several Spirulina formulas against Plasmodium falciparum 3D7, in vitro. The tested Spirulina formulas included commercially available capsule, crude extract and alkaloid fraction. Results showed that all tested formula possessed antimalarial activities with the Spirulina capsule exhibited the highest activities (IC50 = 2.16 μg/mL). Light and electron microscopies revealed interference of the Spirulina with the parasite hemozoin formation. In conclusion, all tested Spirulina formulas and fraction exhibited moderate to high antimalarial activities.

Effect of Extracts of Khat (<i>Catha edulis </i>F.) on Glucose Handling in Normoglycaemic, Diabetic, and Glucose Loaded Rodents

Khat (Catha edulis F., Celastraceae) is widely chewed for its euphoric effects and as recreational drug to improve performance. Although khat is also claimed to be useful in diabetic patients, conflicting results appear in the literature on the benefit of khat in managing diabetes. This study was therefore initiated to investigate the effect of khat on blood glucose homeostasis in rodents. Crude extract as well as flavonoid and alkaloid fractions of khat were used to investigate its effect in normoglycaemic, diabetic, and oral glucose loaded animals. Three doses of crude extract (100, 200, 400 mg/kg), four doses of flavonoid fraction (50, 100, 200, 400 mg/kg), and one dose of alkaloid fraction (200 mg/kg) were employed. Positive and negative controls were treated with 5 mg/kg glibenclamide and 2% Tween-80, respectively. Fractions and doses that provided prominent activity in diabetic mice were selected for oral glucose tolerance test. Blood was then taken from the tail vein at 0, 1, 2, 3 and 4 h to determine blood glucose level using commercial one touch glucometer. The flavonoid fraction at 200 and 400 mg/kg (p < 0.001) as well as the alkaloid fraction (p < 0.05) and glibenclamide (p < 0.05) produced a significant reduction in blood glucose level in normoglycaemic mice compared to the negative control. In diabetic mice, significant decline (p < 0.05) was noted with 400 mg/kg of the crude extract, 50, 100 and 400 mg/kg of the flavonoid fraction, and glibenclamide. In glucose loaded rats, 400 mg/kg of the crude extract was the only group that significantly lowered (p < 0.05) blood glucose level in comparison to vehicle-treated animals. Higher dose of the crude extract was shown to possess antidiabetic activity without producing hypoglycaemia. Antidiabetic effect could be primarily, if not exclusively, linked to the flavonoidal contents. However, since the flavonoid and alkaloid fractions were associated with hypoglycaemia, this effect seems to be counterbalanced by other constituents.Keywords: Catha edulis, flavonoids, alkaloids, blood glucose, diabetes

Antimalarial Activity of Solvent and Alkaloid Fractions of <i>Kleinia abyssinica</i>

In Ethiopia, the roots of Kleinia abyssinica (A. Rich.) A. Berger are used traditionally for the treatment of malaria. In the present study, the 80% methanol extract as well as solvent and alkaloid fractions prepared from the powdered roots of K. abyssinica were tested for their in vivo antimalarial activity using mice infected with Plasmodium berghei parasites in a four-day suppressive test. Preliminary investigation showed that the crude 80% methanol extract significantly (P < 0.05) inhibited parsitaemia of P. berghei in mice. Investigation of the activity of solvent fractions of the plant revealed that the petroleum ether and methanol fractions displayed better suppression than those of the chloroform and acetone fractions. However, the alkaloid extract obtained from the methanol fraction displayed maximum activity suppressing significantly (p < 0.05) the growth of P. berghei at dose levels of 100, 200, 400, and 800 mg/kg/day compared to the mice in the negative control group. The ED50 for the total alkaloid was found to be 60.77 mg/kg/day. In conclusion the present study confirmed the traditional uses of the plant in the treatment of malaria and that alkaloids contribute to the overall antimalarial activity. Keywords : Kleinia abyssinica , roots, four-day suppressive test, Plasmodium berghei, alkaloid fraction

Characterization of Pyrrolidine Alkaloids of Epipremnum aureum for Their Antitermite Activity Against Subterranean Termites with SEM Studies

Epipremnum aureum (Linden and Andre) G.S. Bunting (E. aureum) is an ornamental foliage rich in phytoconstituents and serves as a potential source of bioactive compounds possessing beneficial biological activities. The present study was carried out to isolate the pyrrolidine alkaloids of leaves with in vitro antitermite and antirepellant efficacy on paper and soil by direct-choice and no-choice assay. Spectrometric analysis of alkaloid fractions via Ultraviolet–visible spectroscopy (UV–VIS), Fourier transform infrared spectroscopy (FTIR) and gas chromatography mass spectrometry (GC–MS) helped in the characterization of pyrrolidine alkaloids. Superior antitermite activities were observed, associated with high levels of 5-Oxoproline as compare to Methyl 5-oxo-2-pyrrolidinecarboxylate. Presence of higher contents of 4-Morpholineethanol showed effective antitermite activity and even low levels of 3-Amino-4-Hydroxybutanoic acid and 1H-1,2,4-Triazol-3-amine, N-methyl- also exposed significant activities for repellence and mortality of termites. Repellence and percentage mortality of termites by these alkaloid fractions were similar in results when compared with the standard alkaloid Nicotine and chemical termiticide Monocrotophos. These findings were also supported by SEM studies. Pyrrolidine alkaloids present in E. aureum have exposed strong in vitro antitermite and antirepellant activities against subterranean termites Odontotermes obesus. These findings strongly support the use of E. aureum to bear potential termiticidal properties, however further details need to be carried out.

Identification of anti-inflammatory constituents in Phellodendri Cortex and Coptidis Rhizoma by monitoring the suppression of nitric oxide production.

Phellodendri Cortex (Obaku in Japanese) and Coptidis Rhizoma (Oren), both of which contain berberine, have been used to prepare the kampo formula orengedokuto to treat inflammatory diseases, including dermatitis, gastric ulcers, and gastritis. These drugs are blended differently in other formulas, such as the use of Phellodendri Cortex in shichimotsukokato to treat hypertension and Coptidis Rhizoma in hangeshashinto to treat diarrhea and stomatitis. However, the differences in their medicinal properties are not well characterized. We prepared extracts from Phellodendron amurense bark (PAB) and Coptis chinensis rhizome (CCR) and separated them into alkaloid and non-alkaloid fractions. Anti-inflammatory effects were examined by monitoring the production of nitric oxide (NO), which is a pro-inflammatory mediator. A non-alkaloid fraction of the PAB extract suppressed NO production in hepatocytes more efficiently than that of the CCR extract. When each non-alkaloid fraction of the PAB and CCR extracts was administered to mice, the fractions of both extracts decreased the levels of mRNAs encoding inducible NO synthase and molecules in the interleukin-1β signaling pathway. Limonin and obakunone identified in the PAB non-alkaloid fraction suppressed NO production, exhibiting IC50 values of 16 and 2.6μM, respectively, whereas berberine and coptisine displayed IC50 values of 12 and 14μM, respectively. Limonin and obakunone reduced the expression of the iNOS gene, probably through the transcription factor nuclear factor-κB. Therefore, both limonoids and alkaloids may be responsible for the anti-inflammatory effects of the PAB extract, whereas alkaloids may be primarily responsible for those of the CCR extract. The different composition of the constituents may modulate the anti-inflammatory effects of Phellodendri Cortex and Coptidis Rhizoma.

Profiling of the Bioactive Compounds in Flowers, Leaves and Roots of Vinca sardoa

Vinca sardoa (Stern) Pignatti (Apocynaceae) is largely distributed in Sardinia where it is considered a typical endemism. Since the plant is used in traditional folk medicine, the aim of the present work was to identify and quantify the polyphenolic metabolites, due to the well-known importance of polyphenolic compounds, as well as to evaluate antioxidant activity in different parts of the plant. The compounds were identified and determined in the methanol extracts of leaves, flowers, and roots by developing different LC-MS/MS methods. The obtained data show that leaves possess the highest amount of polyphenols, in particular quinic acid (3401 mg/100 g), chlorogenic acid (1082 mg/100 g), caffeoylquinic acid isomer 1 (190 mg/100 g), and robinin (633 mg/100 g). Likewise, antioxidant tests showed that leaves possess the main radical scavenging activities in both ABTS (49.19 ± 3.41 μg/mL, 30.88 ± 3.04 μg/mL at time zero and after 50 min, respectively) and DPPH assays (223.97 ± 30.81 μg/mL, 109.52 ± 12.89 μg/mL at time zero and after 30 min, respectively). Taking into account that leaves differed most from flowers and roots in the content of caffeoylquinic acid and chlorogenic acid, of which antioxidant properties are widely recognized, it is reasonable to assume that these two compounds are involved in the differences described. The relationship between the high polyphenolic content and interesting antioxidant activities, justifies its use in ethnobotany and may be suggest a use of this specie, after removal of the alkaloid fraction, in the pharmaceutical, phytotherapy, and cosmetic industries.

An experimental design approach to obtain canthinone alkaloid-enriched extracts from Simaba aff. paraensis

The species of the genus Simaba (Simaroubaceae) are found in almost all Brazil and they are used by local population for the treatment of ulcers and malaria. The genus is characterized by the presence of quassinoids and canthinone alkaloids. There is a great interest in canthinones due to important biological activities associated with this class of alkaloids. In this study, methods were developed for obtaining enriched fractions of canthinone alkaloids from Simaba aff. paraensis using experimental factorial design analyzed by gas chromatography. Three alkaloids were detected: canthin-6-one, 4,5-dimethoxycanthin-6-one and the major 9-methoxycanthin-6-one. Within the experimental domain, factorial designs 22 helped establish the minimum amount of solvent and minimum time necessary to obtain extracts enriched in canthinone alkaloids from S. aff. paraensis barks by two extraction methods. These results represent a reduction in costs for obtaining canthinone alkaloids described for the first time in S. aff. paraensis.