Isolation Of Active Compounds Research Articles

Gum Arabic Increases Phagocytosis of Escherichia coli by Blood Leukocytes of Young and Old Healthy Volunteers.

Gum arabic, a polysaccharide exudate from Acacia senegal (L.) Willdenow trees, has already been used by African native people in natural medicine. Using whole-blood samples from young (20-35 years) and older (>80 years) healthy volunteers (each group n = 10), the effect of an aqueous solution of GA on phagocytosis of Escherichia coli was examined with a gentamicin protection assay. Whole-blood samples of each volunteer were stimulated with GA and as a control with CpG oligodeoxynucleotides (Toll-like receptor -9 agonists) for 2 h, then co-incubated with E. coli for 30 min and thereafter treated with gentamicin for up to 240 min to kill extracellular bacteria. Then, whole-blood cells were lysed with distilled water, and colony-forming units were counted by quantitative plating. Cytokine enzyme-linked immunosorbent assay for the detection of TNF-α and IL-6 was performed using the blood supernatant. The GA concentration tested (20 mg/mL) did not affect the viability of eukaryotic cells. Phagocytosis of E. coli by whole-blood leukocytes derived from young (p = 0.008) and older (p = 0.004) healthy volunteers was increased by 120.8% (young) and 39.2% (old) after stimulation with GA. In contrast, CpG only stimulated the bacterial phagocytosis by cells derived from young volunteers (p = 0.004). Stimulation of whole blood with GA increased the intracellular killing of E. coli in young (p = 0.045) and older volunteers (p = 0.008) and induced a TNF-α release in whole blood collected from older volunteers but not from younger ones (p = 0.008). These data encourage the isolation of active compounds of GA and the initiation of clinical trials addressing the preventive effect of GA on bacterial infections.

Radical scavenging dihydroxycinnamic natural compounds from Trianthema pentandra

BackgroundTrianthema pentandra is a promising plant with numerous medical applications. Previous studies have confirmed that the plant is strongly cytotoxic in brine shrimp lethality tests and has antibacterial effects. However, the compounds responsible for these biological activities have not been identified. This study aimed to screen plants in an antiradical assay using 1,1-diphenyl-2-picrylhydrazyl (DPPH). This assay was used to guide the isolation of active compounds, which were identified at the molecular structural level by spectroscopic methods. MethodsThe plant was extracted using ethanol, labelled F1 and fractionated by solvents of different polarities (F2 chloroform, F4 ethyl acetate, F5 aqueous methanol, and F6 n-hexane). The ethyl acetate and aqueous methanol (F4 and F5) fractions were selected for further purification based on their yields and activities. They were run on chloroform-methanol and n-hexane-ethyl acetate gradients, respectively. Fractions resulting from column chromatography were further screened for DPPH antioxidant activity, upon which fraction F5–1–077 had unusually high activity (IC50 = 3.57 µg/ml). Further purification of these fractions through recrystallization and high-performance liquid chromatography (HPLC) led to the isolation of three compounds. Results: Among these compounds, two were identified and characterized using FT-IR, LC-MS, and complete nuclear magnetic resonance (NMR) data, and 2,3-dihydroxycinnamic acid ethyl ester and its analog acid were isolated from the ethyl acetate fraction (F4). The former compound has been proven to have good activity in comparison with standards, ascorbic acid, and butylated hydroxytoluene (BHT), even at a low concentration of 5 µg/ml with an IC50 value of 0.13 µg/ml in the DPPH assay. The molecular docking data supported the potent activity of the compound with binding affinity, ∆G = -6.4 kcal/mol compared to the ascorbic acid (∆G = -5.0 kcal/mol) used as standard. ConclusionThis study serves as a groundbreaking foundation for the investigation of the natural dihydroxycinnamic compounds present in this plant.

Antioxidant, Immunomodulatory and Fungicidal Potential of Different Extracts of Raphanus Raphanistrum L. Var. Caudatus

Background: Reactive oxygen species (ROS) have been implicated in the pathogenesis of various diseases, emphasizing the importance of antioxidants in maintaining cellular homeostasis. Raphanus raphanistrum, commonly known as wild radish, has been traditionally used for its medicinal properties, including antioxidant, immunomodulatory, and antifungal effects. The plant is rich in bioactive compounds such as flavonoids, isothiocyanates, and vitamins, which contribute to its therapeutic potential. Objective: This study aimed to evaluate the antioxidant, immunomodulatory, and antifungal activities of Raphanus raphanistrum extracts and to compare these activities with standard controls. Methods: Fresh Raphanus raphanistrum plants were collected, and extracts were prepared using methanol, chloroform, and water. The antioxidant activity was assessed using the DPPH radical scavenging assay. Immunomodulatory activity was evaluated through the luminol-enhanced chemiluminescence assay in whole blood and polymorphonuclear leukocytes (PMNS), measuring the oxidative burst. The antifungal activity was determined using the agar disk diffusion method against six pathogenic fungi. The statistical analysis was performed using SPSS version 25, with results presented as mean ± standard deviation for antioxidant and antifungal assays, and mean ± standard error for immunomodulatory activity. Results: The methanol extract exhibited significant antioxidant activity with DPPH scavenging percentages ranging from 56.55% at 150 µg/ml to 87.08% at 850 µg/ml. Immunomodulatory activity showed IC50 values of 37.8 µg/ml in whole blood and 18.9 µg/ml in PMNS for the methanol extract. The antifungal activity against Candida albicans showed zones of inhibition increasing from 15 mm at 150 µg/ml to 22 mm at 850 µg/ml. These activities were compared to standard controls, including ascorbic acid for antioxidant, ibuprofen for immunomodulatory, and miconazole for antifungal assays, demonstrating the extracts' competitive potential. Conclusion: Raphanus raphanistrum extracts showed promising antioxidant, immunomodulatory, and antifungal activities, indicating their potential as natural alternatives for the prevention and treatment of related diseases. Further in vivo studies and isolation of active compounds are recommended to fully understand the mechanisms and therapeutic applications.

Isolation of active compounds from Streptomyces sennicomposti GMY01 and cytotoxic activity on breast cancer cells line

The occurrence of resistance to anticancer and the emergence of serious side effects due to chemotherapy is one of the main problems in cancer treatment, including breast cancer. The need for effective anticancer with a specific target is urgently required. Streptomyces are widely known as the potential producers of new anticancer molecules. Previously reported that the methanol extract of Streptomyces sennicomposti GMY01 isolated from Krakal Coast, Gunungkidul had very strong cytotoxic activity against MCF-7 and T47D breast cancer cells with IC50 values of 0.6 and 1.3 μg/mL, respectively. The following study aimed to isolate and identify active compounds of the S. sennicomposti GMY01 and evaluate its cytotoxic activity. The study was started by re-culturing and re-fermented optimization of S. sennicomposti GMY01 in a larger volume, then the bacteria were extracted using methanol following the bioassay-guided isolation of the extract obtained. The active compounds obtained were then structurally determined using UV/Vis spectroscopy, Fourier Transform-Infrared (FT-IR), Liquid Chromatography-Mass Spectroscopy (LC-MS), 1H NMR, and 13C NMR and analyzed for their cytotoxic activity using MTT assay on MCF-7 and normal Vero cells line. The results showed that the culture of the S. sennicomposti GMY01 using Starch Nitrate Broth (SNB) media yields the best results compared to other culture media. An active anticancer compound namely mannotriose was successfully isolated from the methanol extract with an IC50 value of 5.6 μg/mL and 687 μg/mL against the MCF-7 and Vero cells lines, respectively, indicating that this compound showed strong cytotoxic activity with high selectivity.

Phytochemical Analysis and Evaluation of Genotoxic, Antigenotoxic Effects in Bacterial Models, and Hypoglycemic Activity of Epilobium angustifolium L. with Bioguided Isolation of Active Compounds.

This study examined the effects of methanol extract and its sub-extracts from Epilobium angustifolium on α-glucosidase and α-amylase activity. Secondary metabolites and amino acids were quantified using LC-MS/MS. Dichloromethane sub-extract displayed the highest activity and was chosen for further investigation. Despite the widespread use of E. angustifolium, genotoxicity studies were conducted to assess its safety. Dichloromethane significantly inhibited α-glucosidase (IC50 =17.340 μg/mL), making it approximately 293 times more effective than acarbose. Six known compounds, including gallic acid (1), a mixture of quercetin-3-O-α-galactoside (2a) and quercetin-3-O-α-glucoside (2b), quercetin-3-O-α-glucuronic acid (3), quercetin-3-O-α-rhamnoside (4), and kaempferol-3-O-α-rhamnoside (5) were identified. Quercetin-3-O-α-rhamnoside exhibited the highest inhibition of α-glucosidase (IC50 =1735±85 μM), making it 3.70 times more effective than acarbose. Dichloromethane also showed significant antigenotoxic activity against mutagenesis induced by NaN3, 9-AA, 4-NPD, and MNNG. Gallic acid was found in the highest abundance (13253.6931 ng/mL) in the methanolic extract. Furthermore, L-Aspartic acid was the most concentrated amino acid (363.5620 nmol/mL) in the methanolic extract.

Skrining fitokimia dan isolasi senyawa steroid/triterpenoid dari ekstrak n-heksana biji nangka (Artocarpus heterophyllus Lam).

Jackfruit (Artocarpus heterophyllus Lam) is a plant that can grow well in tropical regions such as Indonesia. Jackfruit seeds contain steroid/triterpenoid chemical compounds, including several types of steroids that are useful as ingredients in medicines, such as estrogen, progestin, and cardenolides. The research aims to conduct phytochemical testing and isolate steroid/triterpenoid compounds from jackfruit seeds. This research uses experimental methods, including the compound extraction process using the maceration method and the isolation of active compounds via column chromatography. Identification of pure isolates was carried out using UV spectrophotometry and IR spectrophotometry. The results of phytochemical screening showed the presence of steroid/triterpenoid compounds, glycosides, and alkaloids in the samples. The isolate has a purple color with an RF value of 0.25, and the maximum absorption peak is located at a wavelength of 208.20 nm, indicating the presence of a chromophore group. IR spectrophotometry results show the presence of OH, aliphatic -CH, CH2, CH3, C=O, C-O, and C=C. This research concludes that the isolate obtained belongs to the steroid/triterpenoid compound group.

13C NMR-based dereplication using MixONat software to decipher potent anti-cholinesterase compounds in Mesua lepidota bark

A bio-assay guided fractionation strategy based on cholinesterase assay combined with 13C NMR-based dereplication was used to identify active metabolites from the bark of Mesua lepidota. Eight compounds were identified with the aid of the 13C NMR-based dereplication software, MixONat, i.e., sitosterol (1), stigmasterol (2), α-amyrin (3), friedelin (6), 3β-friedelinol (7), betulinic acid (9), lepidotol A (10) and lepidotol B (11). Further bio-assay guided isolation of active compounds afforded one xanthone, pyranojacareubin (12) and six coumarins; lepidotol A (10), lepidotol B (11), lepidotol E (13), lepidotin A (14), and lepidotin B (15), including a new Mammea coumarin, lepidotin C (16). All the metabolites showed strong to moderate butyrylcholinesterase (BChE) inhibition. Lepidotin B (15) exhibited the most potent inhibition towards BChE with a mix-mode inhibition profile and a Ki value of 1.03 µM. Molecular docking and molecular dynamics simulations have revealed that lepidotin B (15) forms stable interactions with key residues within five critical regions of BChE. These regions encompass residues Asp70 and Tyr332, the acyl hydrophobic pocket marked by Leu286, the catalytic triad represented by Ser198 and His438, the oxyanion hole (OH) constituted by Gly116 and Gly117, and the choline binding site featuring Trp82. To gauge the binding strength of lepidotin B (15) and to pinpoint pivotal residues at the binding interface, free energy calculations were conducted using the Molecular Mechanics Generalized Born Surface Area (MM-GBSA) approach. This analysis not only predicted a favourable binding affinity for lepidotin B (15) but also facilitated the identification of significant residues crucial for the binding interaction.

Development of practicum guideline active compound isolation base on medical plant in Sasambo Society, Indonesia

The people of NTB have many distinctive cultures and cuisines. The use of plants is traditional medicine. This study aims to develop practical guidelines based on the medicinal plant sasambo, NTB. Development design is Research & Development with a 4D model (define, design, develop, and disseminate). The results of laboratory experiments are outlined in practicum guidelines for student activities. Chemistry lecturers in chemistry and natural product chemistry constructively validate the procedures. The analytical method uses Aiken's V formula and percentage agreement. The results of the expert validation show that the practicum guidelines meet very valid criteria with an Aiken value of 0.86. The guidelines also received positive responses from students and expert validators with an average practicality level of 88.6% with very practical criteria. Guidelines can be applied to learning with a percentage agreement of 100%. The cultural richness applied to learning can increase motivation learning and encourage students to be creative in developing products from the Sasambo milk medicinal plant.

Efficacy of Four different Botanical sources on some Human and Fish Pathogenic Bacteria

Bacteria are becoming resistant to new generation antibiotics day by day, which in turn lead us to find new antibacterial compounds of plant origin. Objective of this study was to assess in-vitro antibacterial activities of methanol extractives of fruits of four plants namely Kleinhovia hospita, Callistemon citrinus, Barringtonia acutangula and Polyalthia suberosa against four human and eight fish pathogenic bacteria by measuring the zone of inhibition (in mm), Minimum Inhibitory Concentration and Minimum Bactericidal Concentration. Characterization and isolation of active compounds through phytochemical screening, FT-IR analysis, Thin Layer Chromatography (TLC) and GC-MS analysis were done in most effective extract i.e., in C. citrinus fruit methanol extract among four tested plant extracts. All the tested bacteria (human and fish pathogens) were found to be susceptible to all four plant extracts used. Highest zone of inhibition (20.17±0.24mm) was found in C. citrinus fruit extract against Gram-positive bacterium, Staphylococcus aureus (MTCC 2940) indicating more sensitivity of Gram-positive bacteria than the Gram-negative bacteria examined. Presence of several bioactive compounds as detected through FT-IR, TLC and GC-MS analysis might be accountable for the significant efficacy of fruit methanolic extract of C. citrinus as antibacterial agent against both human and fish pathogenic bacteria.

Isolation of active compound as anti acne from ethanol extract Artocarpus camansi leaves

Acne vulgaris or acne is a chronic inflammatory skin disease in adolescents and adults affecting one self-confidence. The result of the research shows the ethanol extract, subfraction, pure isolate, and gel extract of Artocarpus camansi are active in inhibiting the growth of Propionibacterium acnes. The ethanol extract with the highest inhibition zone was at the concentration of 0.5 and 2% with 9.1±0.62 mm and 8.5±0.7 mm with the activity of 47.07% and 43% respectively (in comparison with the chloramphenicol 30 μg 19.33±0.47mm). The gel extract had the highest activity at 2%, with an inhibition zone of 8±0.50 mm and the activity of 43.97%. Anti-acne activity for all subfractions had an activity of 32.5-33.3% while the pure isolate was at 42.10 - 45.63%. Physical properties of the gel extract were evaluated for four weeks by examining the pH test obtained with a range of 5.8-6.7, viscosity in the range of 18460-19668 cP, spreadability in the range of 5.45-7.20 cm, adhesion observation above 4 seconds, and homogeneity in a concentration of 0.5-7.5%. The pure isolate has a melting point of 147 ℃, presumed to be γ-sitosterol and appropriate with the screening phytochemicals results with the presence of steroid.

An efficient isolation and purification of broad partition coefficient range ginsenosides from roots of Panax quinquefolium L. by linear gradient counter-current chromatography coupled with preparative high-performance liquid chromatography.

As a famous health food, roots of Panax quinquefolium L. possessed immune regulation and enhancement of the central nervous system, in which ginsenosides are the main active component with different numbers and positions of sugars, causing different chemical polarities with a challenge for the separation and isolation. In this study, a fast and effective bilinear gradient counter-current chromatography was proposed for preparative isolation ginsenosides with a broad partition coefficient range from roots of Panax quinquefolium L. In terms of the established method, the mobile phases comprising n-butanol and ethyl acetate were achieved by adjusting the proportion. Coupled with the preparative HPLC, eleven main ginsenosides were successfully separated, including ginsenoside Rg1 (1), Re (2), acetyl ginsenoside Rg1 (3), Rb1 (4), Rc (5), Rg2 (6), Rb3 (7), quinquefolium R1 (8), Rd (9), gypenoside X VII (10) and notoginsenoside Fd (11), with purities exceeding 95% according to the HPLC results. Tandem mass spectrometry and electrospray ionization mass spectrometry were adopted for recognizing the isolated compound architectures. Our study suggests that linear gradient counter-current chromatography effectively separates the broad partition coefficient range of ginsenosides compounds from the roots of Panax quinquefolium L. In addition, it can apply to active compound isolation from other complicated natural products.

Column Chromatography Fractionation and Antioxidant Activity of Passiflora foetida Leaves

Available synthetic antioxidants have been reported to have mutagenic and toxic effects. On the other hand, natural antioxidants show their superiority as they are not or less toxic. Passiflora foetida has the potential as an antioxidant, but the investigation of the antioxidant activity of the P. foetida chromatography column fraction has not been reported. This studied aims to investigate the antioxidant activity of the column chromatographic fractions of P. foetida leaves. An antioxidant assay using the DPPH and FRAP methods. The extraction was carried out by graded maceration, then fractionation using column chromatography. The antioxidant activity test was carried out using the DPPH and FRAP methods. Thin Layer Chromatography analysis was performed to determine the chromatogram pattern. The EC50 using DPPH method from n-hexane extract: 129.035 µg/mL, ethyl acetate extract: 206.398 µg/mL, methanol extract: 97.453 µg/mL, while the EC50 using FRAP method from n-hexane extract: 67.851 µg/mL, ethyl acetate extract : 68.981 µg/mL, and methanol extract: 58.787 µg/mL. Column chromatography fractions have antioxidant activity, with FMetPF6 as the fraction with the best activity, with percent inhibition 41.85±1.96 at concentration 25 µg/mL (DPPH), and with percent antioxidant activity 26.03±0.84 at concentration 9 µg/mL (FRAP). Passiflora foetida leaves have great potential as an antioxidant; both the extract and its fractions have antioxidant activity. The FMetPF6 has the best activity compare to other extracts and fractions. Further analysis to determine the various compounds in FMetPF6 using LC-MS/MS will facilitate the active compound's isolation.

Isolation and Characterization of Galloylglucoses Effective against Multidrug-Resistant Strains of Escherichia coli and Klebsiella pneumoniae.

The search for new antibiotics against multidrug-resistant (MDR), Gram-negative bacteria is crucial with respect to filling the antibiotics development pipeline, which is subject to a critical shortage of novel molecules. Screening of natural products is a promising approach for identifying antimicrobial compounds hosting a higher degree of novelty. Here, we report the isolation and characterization of four galloylglucoses active against different MDR strains of Escherichia coli and Klebsiella pneumoniae. A crude acetone extract was prepared from Paeonia officinalis Linnaeus leaves, and bioautography-guided isolation of active compounds from the extract was performed by liquid–liquid extraction, as well as open column, flash, and preparative chromatographic methods. Isolated active compounds were characterized and elucidated by a combination of spectroscopic and spectrometric techniques. In vitro antimicrobial susceptibility testing was carried out on E. coli and K. pneumoniae using 2 reference strains and 13 strains hosting a wide range of MDR phenotypes. Furthermore, in vivo antibacterial activities were assessed using Galleria mellonella larvae, and compounds 1,2,3,4,6-penta-O-galloyl-β-d-glucose, 3-O-digalloyl-1,2,4,6-tetra-O-galloyl-β-d-glucose, 6-O-digalloyl-1,2,3,4-tetra-O-galloyl-β-d-glucose, and 3,6-bis-O-digalloyl-1,2,4-tri-O-galloyl-β-d-glucose were isolated and characterized. They showed minimum inhibitory concentration (MIC) values in the range of 2–256 µg/mL across tested bacterial strains. These findings have added to the number of known galloylglucoses from P. officinalis and highlight their potential against MDR Gram-negative bacteria.

Phytochemical Analysis and In Vitro and In Vivo Pharmacological Evaluation of Parthenium hysterophorus Linn.

The main aim of this research was to explore Parthenium hysterophorus Linn phytochemically and pharmacologically. Phytochemical screening is important for the isolation of active compounds before bulk extraction. The crude extracts and their fractions were screened for enzyme (urease, α-glycosidase, and phosphodiesterase) inhibition assays, in vivo analgesic, anti-inflammatory, and sedative effects. Results indicated the presence of steroids, flavonoids, etc. The crude extracts such as methanol, hexane, aqueous, ethyl acetate, chloroform, and butanol exhibited excellent urease inhibitory activities with IC50 = 43.1 ± 1.24, 31.9 ± 2.21, 31.9 ± 2.21, 57.3 ± 1.27, 49.2 ± 2.16, and 35.3 ± 1.12, respectively, as compared to standard acetohydroxamic acid (20.3 ± 0.43). The extracts (methanol, hexane, aqueous, ethyl acetate, chloroform, and butanol) also showed promising α-glycosidase potency with IC50 = 13.1 ± 0.34, 21.2 ± 1.16, 23.1 ± 0.12, 84.2 ± 2.17, 118.6 ± 3.07, and 840 ± 1.73, respectively against acarbose (840 ± 1.73). The phosphodiesterase activity of the mentioned extracts was also excellent with IC50 = 131.1 ± 2.41, 197.2 ± 3.16, 24.2 ± 0.11, 62.4 ± 2.21, 152.4 ± 1.81, and 55.3 ± 2.15, respectively, against the standard (265.5 ± 2.25). Furthermore, butanol (14.96 ± 1.78), ethyl acetate (18.98 ± 1.71), and methanol (16.87 ± 1.00) showed dose-dependent analgesic effects with a maximum inhibition of acetic acid-induced writhes. Whereas, methanolic and butanol extracts exhibited maximum inhibition of inflammation in the carrageenan paw edema test. The aqueous (p < 0.01) and butanol (p < 0.01) extracts exhibited maximum a sedative effect followed by chloroform (p < 0.05), ethyl acetate (p < 0.05), and methanolic (p < 0.05) fractions as compared to the standard drug. The current research concluded that Parthenium hysterophorus Linn has important phytochemical constituents having inhibitory effects on urease, α-glycosidase, and phosphodiesterase enzymes. Furthermore, the plant has analgesic, anti-inflammatory, and sedative effects. The P. hysterophorus needs to further be explored for the candidate molecules responsible for the abovementioned activities.

Isolation of active compound from Nephelium lappaceum L. rind as an antioxidant

The consumption of rambutan (Nephelium lappaceum L.) results in a vast amount of rambutan rind. It is very interesting to explore rambutan rind as natural antioxidants. This study aimed to explore the antioxidant activities of rambutan rind in vitro and to correlate those activities with a group of compounds (phenolics and flavonoids). Rambutan rind was cleaned, dried using a conventional oven, powdered, and the powder obtained was subjected to maceration. The macerate was fractionated using petroleum ether and chloroform to get chloroform fraction. The sub fractionation was done toward chloroform fraction. The chloroform fraction and its subfractions were then subjected to antioxidant activity measurement, determination of phenolics and flavonoid contents, and the active compound present in the most active subfractions was isolated using column chromatography. The isolate was identified using several methods including thin-layer chromatography (TLC), Fourier transform infrared (FTIR) spectroscopy as well as gas chromatography-mass spectrometry (GC-MS). The results showed that the chloroform fraction and its subfractions were correlated with the phenolic and flavonoid contents found in rambutan rinds. The phenolic and flavonoid content of chloroform fraction was 32.32±0.79 and 55.05±3.900, respectively, whereas the IC50 of antioxidant activity was 49.77±0.22 for DPPH and 45.36±0.27 for ABTS. The reducing power was 34.478±0.245 (mg vitamin C equivalent/g sample) and the metal chelating activity was 332.753±0.695 (mg Na EDTA equivalent/g sample). The phenolic contents contributed towards the metal chelating activities compared to other antioxidant activities with an R 2 value of 0.8726, while flavonoid contents contributed more to ABTS radical scavenging activity with an R 2 value of 0.8916. One of the active compounds present in rambutan rind having antioxidant activity was identified as 1,2-benzenedicarboxylic acid. Thus, the under-utilized part of rambutan rind could be explored as a natural antioxidant to be used as a food supplement

Ethnomedicinal Survey and Phytochemical Screening of Plants Used To Treat Epilepsy by Traditional Healers in Etche, Rivers State, Nigeria

Epilepsy is one of the oldest recorded medical ailments. Ethnomedicinal survey was carried out to identify and take a detailed list of the medicinal plant species used to treat epilepsy and assess how they are used in Etche Local Government Area (LGA) of Rivers State, Nigeria. Semi-structured questionnaires were used during the survey to conduct interviews with traditional healers and other knowledgeable individuals on the use of medicinal plants in the treatment of epilepsy. Twelve communities were randomly selected while a total of 54 respondents were purposively selected. The respondents consist of 82.5% males and 12.3% females, 43.9% were above 60 years while 28.1% were between 51-60 years. Traditional medicine practitioners (TMP) formed 75.4% of the respondents, primary occupation of other knowledgeable respondents on plants used for epilepsy were civil servants (8.8%), farming and trading (3.5%). A total of 25 medicinal plant species were recorded during the survey. Phytochemical screening was carried out on five medicinal plants based on frequency of mention, the screening showed presence of alkaloids, triterpenoids, steroids, saponins, tannins, flavonoids, anthraquinones, cardenolides and carbohydrates. Plant resources employed in the local treatment of epilepsy in Etche were documented. Further research on isolation of active compounds on frequently used plants for epilepsy is encouraged to harness their potentials.

Phenolic Composition, In-vitro Antioxidant and Enzyme Inhibition Activities of Cardaria draba Different Parts

The plant Cardaria draba (L.) Desv. subsp. draba (Brassicaceae), is traditionally used for various ailments in different cultures. We investigated different solvent extracts such as methanol, ethanol, and water extracts obtained from flowers, leaves, stems, and roots of C. draba for their chemical composition, as well as antioxidant and enzyme inhibition activities of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-glucosidase, α-amylase, and tyrosinase). RP-HPLC technique was used to determine the phenolic profile of each extracts. The antioxidant activities of the extracts were determined by using DPPH and ABTS method, total phenol and flavonoid content analysis, and iron chelating assay. Enzyme inhibitory potential was evaluated by 96-microplate method. According to the results, aqueous extract of flower demonstrated the highest total phenolic content (64.32 µgGAE/ mg), while leaf ethanol extract showed the highest total flavonoid content (141.47 µgQE/ mg) among all extracts. The methanol, and water extracts of flowers were the most effective DPPH scavenger while aqueous extract of flower was the most active on ABTS scavenging. It is shown that the extracts possess promising activity against α-glucosidase than α-amylase enzyme. The methanolic extract of flower showed anti-acetylcholinesterase activity, and the ethanolic extract of the stem exhibited the best anti-butyrylcholinesterase activity among the 12 extracts. As for the anti-tyrosinase activity, higher kojic acid equivalent values were found for the aqueous extracts of roots and leaves. In conclusion, the data obtained from this study may serve as the basis for the bioassay-guided isolation of active compounds and the development of novel drugs from Cardaria draba.

Magnetic Molecularly Imprinted Polymers: An Update on Their Use in the Separation of Active Compounds from Natural Products.

During the last few years, separation techniques using molecularly imprinted polymers (MIPs) have been developed, making breakthroughs using magnetic properties. Compared to conventional MIPs, magnetic molecularly imprinted polymers (MMIPs) have advantages in sample pretreatment due to their high specificity and selectivity towards analytes as a result of their larger specific surface areas and highly accessible specific binding sites. The techniques of isolation of active compounds from natural products usually require very long process times and low compound yields. When MMIPs are used in sample separation as Solid Phase Extraction (SPE) sorbents, the MMIPs are introduced into the dissolved sample and spread evenly, and they form bonds between the analyte and the MMIPs, which are then separated from the sample matrix using an external magnetic field. This process of separating analytes from the sample matrix makes the separation technique with MMIPs very simple and easy. This review discusses how to synthesize MMIPs, which factors must be considered in their synthesis, and their application in the separation of active compounds from natural products. MMIPs with magnetic core-shells made by co-precipitation can be a good choice for further development due to the high synthesis yield. Further optimization of the factors affecting the size and distribution of magnetic core-shell particles can obtain higher synthesis yields of MMIPs with higher adsorption capacity and selectivity. Thus, they can isolate target compounds from natural plants in high yields and purity.

Insulin secretory and antidiabetic actions of Heritiera fomes bark together with isolation of active phytomolecules.

In folklore, Heritiera fomes (H. fomes) has been extensively used in treatment of various ailments such as diabetes, cardiac and hepatic disorders. The present study aimed to elucidate the antidiabetic actions of hot water extract of H. fomes (HWHF), including effects on insulin release from BRIN BD11 cells and isolated mouse islets as well as glucose homeostasis in high-fat-fed rats. Molecular mechanisms underlying anti-diabetic activity along with isolation of active compounds were also evaluated. Non-toxic concentrations of HWHF stimulated concentration-dependent insulin release from isolated mouse islets and clonal pancreatic β-cells. The stimulatory effect was potentiated by glucose and isobutyl methylxanthine (IBMX), persisted in presence of tolbutamide or a depolarizing concentration of KCl but was attenuated by established inhibitors of insulin release such as diazoxide, verapamil, and Ca2+ chelation. HWHF caused depolarization of the β-cell membrane and increased intracellular Ca2+. The extract also enhanced glucose uptake and insulin action in 3T3-L1 differentiated adipocytes cells and significantly inhibited in a dose-dependent manner starch digestion, protein glycation, DPP-IV enzyme activity, and glucose diffusion in vitro. Oral administration of HWHF (250 mg/5ml/kg b.w.) to high-fat fed rats significantly improved glucose tolerance and plasma insulin responses and it inhibited plasma DPP-IV activity. HWHF also decreased in vivo glucose absorption and intestinal disaccharidase activity while increasing gastrointestinal motility and unabsorbed sucrose transit. Compounds were isolated from HWHF with similar molecular weights to quercitrin (C21 H20 O11) ranging from 447.9 to 449.9 Da which stimulated the insulin release in vitro and improved both glucose tolerance and plasma insulin responses in mice. In conclusion, H. fomes and its water-soluble phytochemicals such as quercitrin may exert antidiabetic actions mediated through a variety of mechanisms which might be useful as dietary adjunct in the management of type 2 diabetes.

In vitro antiplasmodial activity of selected plants from the Colombian North Coast with low cytotoxicity.

Plants are an important option in the treatment of malaria, especially in endemic regions, and are a less expensive and more accessible alternative with a lower risk of toxicity. Colombia has a great diversity of plants, and evaluation of natural extracts could result in the discovery of new compounds for the development of antimalarial drugs. The purpose of this work was to evaluate the in vitro antiplasmodial activity and the cytotoxicity of plant extracts from the Colombian North Coast against Plasmodium falciparum. The antiplasmodial activity of 12 plant species from the Colombian North Coast that are used in traditional medicine was evaluated through in vitro cultures of P. falciparum, and the cytotoxicity of extracts of these species to human cells was determined. Plant extracts with high antiplasmodial activity were subjected to preliminary phytochemical screening. Extracts from five plants had promising antiplasmodial activity. Specifically, Bursera simaruba (Burseraceae) (bark), Guazuma ulmifolia Lam. (Malvaceae) (whole plant), Murraya exotica L. (Rutaceae) (leaves), Hippomane mancinella L. (Euphorbiaceae) (seeds), and Capparis odoratissima Jacq. (Capparaceae) (leaves). Extracts presented 50% inhibitory concentration values between 1 and 9 μg/ml. Compared to no extract, these active plant extracts did not show cytotoxic effects on mononuclear cells or hemolytic activity in healthy human erythrocytes. The results obtained from this in vitro study of antiplasmodial activity suggest that active plant extracts from the Colombian North Coast are promising for future bioassay-guided fractionation to allow the isolation of active compounds and to elucidate their mechanism of action against Plasmodium spp.