Evaluation of the antidiarrheal and antioxidant properties of Justicia hypocrateriformis

Content: Justicia hypocrateriformis Vahl (Acanthaceae) is used as an herbal remedy for diarrhea in Cameroon folk medicine.

Objective: This study evaluates the antidiarrheal and antioxidant properties of the aqueous extract of J. hypocrateriformis (JH).

Materials and methods: Preliminary phytochemical screening and an acute toxicity testing of the extract were carried out. The antidiarrheal activity of JH extract (100, 250, and 500?mg/kg) was assessed at curative and preventive levels in castor oil-induced diarrhea in mice. The antioxidant activity was measured by ferric reducing antioxidant power (FRAP), total phenolic content, and radical scavenging activity.

Results: A high lethal dose (LD₅₀) of 14.35?g/kg obtained in acute toxicity implies the extract is not toxic. Phytochemical screening revealed the presence of phenols, tannins, flavonoids, saponins, anthraquinones, and anthocyanins. JH showed a significant protection against castor oil-induced diarrhea as evidenced by a decrease in the number of defecation and wet stool. JH (100–500?mg/kg, p.o.) produced a non-significant dose-dependent decrease in castor oil-induced intestinal transit in the preventive study. In the curative and in healthy mice study, the decrease was only significant at 500?mg/kg. JH possessed a radical scavenging activity with an IC₅₀ of 9.93?mg/ml compared to 4.90?mg/ml for catechin. JH FRAP of 2703.77?±?0?mg/g (catechin equiv) and phenolic concentration of 14?169.99?±?612.39?mg/g (catechin equiv) were also obtained.

Conclusion: Justicia hypocrateriformis extract possesses antidiarrheal activity supported by its antioxidant potential and phytochemical constituents.     

Evaluation of Antidiarrheal Potential of Emblica officinalis.

ABSTRACT

The antidiarrheal potential of the methanol extract of the fruit of Emblica officinalis. Gaertn. Euphorbiaceae was evaluated using several experimental models of diarrhea in Wistar albino rats. The methanol extract showed a significant inhibitory effect on rats with diarrhea induced by castor oil and magnesium sulfate. The methanol extract produced a significant reduction in gastrointestinal motility in charcoal meal tests in rats. It also significantly inhibited PGE₂-induced enteropooling as compared to control animals. The results obtained establish the efficacy and substantiate the use of this herbal remedy as a nonspecific treatment for diarrhea in folk medicine.     

Antidiarrheal mechanism of Carpolobia lutea leaf fractions in rats

Context: Carpolobia lutea G. Don (Polygalaceae) leaf is reputable as an antidiarrheal agent among the Efik and Ibibio tribe of Akwa Ibom State, Nigeria. The crude extract is reported to show antidiarrheal and antiulcer effects in rodents.

Objective: The isolation and characterization of drug molecules from the leaf fraction with antidiarrheal bioactivity and determination of mechanism of action are reported.

Material and methods: Gradient extraction by maceration yielding n-hexane, chloroform, ethyl acetate, and ethanol fractions (770?mg/kg) were used to establish the fractions suitable for drug discovery. The antidiarrheal effect of the leaf fractions of Carpolobia lutea was evaluated using castor oil–induced diarrhea, castor oil–induced intestinal transit, and enteropooling.

Results: Results indicate that all fractions produced a significant (p?<?0.01–0.001) decrease in castor oil–induced diarrhea in rats. This effect was not antagonized by isosorbide dinitrate (150?mg/kg, p.o), diphenoxylate (5?×?10^?3 mg/kg p.o) and yohimbine (1?mg/kg, s.c.) except for the chloroform fraction. The ethyl acetate fraction produced 100% inhibition of intestinal transit, an effect greater than pure drug. Phytochemical analysis of the ethyl acetate fraction yielded polyphenolic compounds.

Conclusion: The leaf fractions contain two types of antidiarrheal agents, one mediating its effect through α₁-presynaptic adrenoceptor while the other does not. Polyphenols isolated may in part lend credence for observed antidiarrheal activity.     

Antinociceptive and antioxidant potential of the crude ethanol extract of the leaves of Ageratum conyzoides grown in Bangladesh

Abstract

Context: Ageratum conyzoides Linn. (Asteraceae) is an annual herbaceous plant with a long history of traditional medicinal and agricultural uses; it is usually grown in the northeast part of Bangladesh.

Objective: The ethanol extract of the plant leaves was evaluated for preliminary phytochemical screening with its antinociceptive and antioxidant activities.

Materials and methods: The preliminary phytochemical analysis was performed on the basis of standard procedures. The analgesic activity of the extract was investigated using the acetic acid-induced writhing method in mice. Five complementary tests such as DPPH free radical scavenging, nitric oxide (NO) scavenging, reducing power, Fe⁺⁺ ion chelating ability and total phenolic content were used for determining antioxidant activities.

Results: The results of preliminary phytochemical analysis showed the presence of alkaloids, reducing sugars, saponins, gums, steroids, tannins and flavonoids. The extract possessed a significant dose-dependent DPPH free radical scavenging activity with an IC₅₀ value of 18.91?μg/ml compared to ascorbic acid (IC₅₀: 2.937?μg/ml) and butylated hydroxyanisole (IC₅₀: 5.10?μg/ml). The IC₅₀ value of the extract for NO scavenging (41.81?μg/ml) was also found to be significant compared to the IC₅₀ value of ascorbic acid (37.93?μg/ml). Moreover, the extract showed reducing power activity and Fe⁺⁺ ion chelating ability. The total phenolic amount was also calculated as quite high (378.37?mg/g of gallic acid equivalents) in the crude ethanol extract.

Discussion and conclusion: Therefore, the obtained results tend to suggest the antinociceptive and antioxidant activities of the ethanol extract of the plant leaves and justify its use in folkloric remedies.     

Anti-acetylcholinesterase activity and antioxidant properties of extracts and fractions of Carpolobia lutea

Context: There is an unmet need to discover new treatments for Alzheimer’s disease. This study determined the anti-acetylcholinesterase (AChE) activity, DPPH free radical scavenging and antioxidant properties of Carpolobia lutea G. Don (Polygalaceae).

Objective: The objective of this study is to quantify C. lutea anti-AChE, DPPH free radical scavenging, and antioxidant activities and cell cytotoxicity.

Materials and methods: Plant stem, leaves and roots were subjected to sequential solvent extractions, and screened for anti-AChE activity across a concentration range of 0.02–200?μg/mL. Plant DPPH radical scavenging activity, reducing power, and total phenolic and flavonoid contents were determined, and cytotoxicity evaluated using human hepatocytes.

Results: Carpolobia lutea exhibited concentration-dependent anti-AChE activity. The most potent inhibitory activity for the stem was the crude ethanol extract and hexane stem fraction oil (IC₅₀?=?140?μg/mL); for the leaves, the chloroform leaf fraction (IC₅₀?=?60?μg/mL); and for roots, the methanol, ethyl acetate and aqueous root fractions (IC₅₀?=?0.3–3?μg/mL). Dose-dependent free radical scavenging activity and reducing power were observed with increasing stem, leaf or root concentration. Total phenolic contents were the highest in the stem: ～632?mg gallic acid equivalents/g for a hexane stem fraction oil. Total flavonoid content was the highest in the leaves: ～297?mg quercetin equivalents/g for a chloroform leaf fraction. At 1?μg/mL, only the crude ethanol extract oil was significantly cytotoxic to hepatocytes.

Discussion and conclusions: Carpolobia lutea possesses anti-AChE activity and beneficial antioxidant capacity indicative of its potential development as a treatment of Alzheimer’s and other diseases characterized by a cholinergic deficit.     

Antidiarrheal Activity of the Aqueous Extract of Punica granatum. (Pomegranate) Peels

Abstract

The antidiarrheal effects of the aqueous extract of Punica granatum. L. (Punicaceae) peels were evaluated in rats. Studies were carried out on the isolated rat ileum, gastrointestinal motility in vivo., and on castor oil–induced diarrhea in rats. The results revealed that the extract exhibited a concentration-dependent inhibition of the spontaneous movement of the isolated rat ileum and attenuated acetylcholine-induced contractions. The extract (100, 200, 300, and 400 mg/kg) also caused a dose-dependent decrease of gastrointestinal transit and markedly protected rats against castor oil–induced diarrhea enteropooling. The intraperitoneal injection LD₅₀ of the extract was found to be 1321 ± 15 mg/kg in mice. A preliminary phytochemical screening of the aqueous extract of Punica granatum. peels gave positive tests for tannins, flavonoids, and alkaloids. The results obtained showed that the aqueous extract of Punica granatum. peels may contain some biologically active principles that may be active against diarrhea, and this may be the basis for its traditional use for gastrointestinal disorders.     

Free radical scavenging activity and chemical constituents of Urvillea ulmaceae

The methanol extract of Urvillea ulmaceae Kunth (Sapindaceae) aerial parts and the hexane, ethyl acetate, and hydromethanol fractions were evaluated for their free radical scavenging activity with the DPPH assay. Among all the tested fractions, the ethyl acetate fraction was the most active, exhibiting an IC₅₀ of 16.33?μg/mL, comparable to that of the commercial antioxidant BHT. Fractionation of the ethyl acetate fraction through chromatographic methods afforded trans-N-methyl-5-hydroxypipecolic acid, epicatechin, and proanthocyanidin A2 as the main constituents. Epicatechin and proanthocyanidin A2 showed potent DPPH radical scavenging activity, with IC₅₀ values of 18.34 and 11.45?μg/mL, respectively. A new compound, trans-N-methyl-5-hydroxypipecolic acid, did not show any antioxidant effect (IC₅₀?>?500?μg/mL).     

Chemical profile and biological activities of Veronica thymoides subsp. pseudocinerea

Abstract

Context: In Turkey, Veronica species (Plantaginaceae) have been used as a diuretic and for wound healing in traditional medicine.

Objective: To examine the fatty acid and essential oil profiles, the antioxidant, anticholinesterase, antimicrobial, and DNA damage effects of Veronica thymoides P.H. Davis subsp. pseudocinerea M.A. Fischer as a potential source of natural active compounds.

Materials and methods: GC/MS was used to analyze essential oil and fatty acid obtained from whole plant. The antioxidant activity was evaluated by the β-carotene-linoleic acid test system, DPPH-free and ABTS cation radicals scavenging, and cupric reducing antioxidant capacity assays. The anticholinesterase and antimicrobial activities were determined by Ellman and broth macrodillution methods, respectively. The effect of the methanol extract on DNA cleavage was investigated.

Results: Hexatriacontene (21.0%) was found to be the main constituent in essential oil, and linoleic acid (25.2%) and palmitic acid (20.6%) in fatty acid. Methanol extract demonstrated the best IC₅₀ values in lipid peroxidation (49.81?±?0.31?µg/ml) and DPPH-free radical scavenging activity (15.32?±?0.17?µg/ml). Methanol and water extracts possessed strong ABTS cation radical scavenging activity with IC₅₀ values 9.15?±?0.28 and 8.90?±?0.14?µg/ml, respectively. The acetone extract exhibited moderate butyrylcholinesterase inhibitory activity. The highest antimicrobial activity was determined in methanol extract against Escherichia coli with 31.25?µg/ml MIC value. Inhibition of methanol extract on plasmid DNA cleavage by OH radicals was found to be 93.32% at 500?µg/ml.

Conclusion: The methanol extract having strong antioxidant and DNA damage effects could be investigated phytochemically to find natural active compounds.     

In vitro antioxidant and anti-cholinesterase activities of Rhizophora mucronata

Context: Rhizophora mucronata Lam. (Rhizophoraceae), commonly known as Asiatic mangrove, has been used traditionally among Asian countries as folk medicine.

Objective: This study investigates the cholinesterase inhibitory potential and antioxidant activities of R. mucronata.

Materials and method: Rhizophora mucronata leaves were successively extracted using solvents of varying polarity and a dosage of 100–500?µg/ml were used for each assay. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities were assessed according to the method of Ellman. In vitro antioxidant activity was assessed using free radical scavenging, reducing power, and metal-chelating activity (duration – 3 months). Total phenolic and flavonoid content were quantified spectrophotometrically. Compound characterization was done using column chromatography, NMR, FTIR, and LC-MS analysis.

Results: Methanolic leaf extract (500?µg/ml) exhibited the highest inhibitory activity against AChE (92.73?±?0.54%) and BuChE (98.98?±?0.17%), with an IC₅₀ value of 59.31?±?0.35 and 51.72?±?0.33?µg/ml, respectively. Among the different solvent extracts, methanolic extract exhibited the highest antioxidant activity with an IC₅₀ value of 47.39?±?0.43, 401.45?±?18.52, 80.23?±?0.70, and 316.47?±?3.56?µg/ml for DPPH, hydroxyl, nitric oxide radical, and hydrogen peroxide, respectively. Total polyphenolic and flavonoid contents in methanolic extract were observed to be 598.13?±?1.85?µg of gallic acid equivalent and 48.85?±?0.70?μg of rutin equivalent/mg of extract. Compound characterization illustrated (+)-catechin as the bioactive compound responsible for cholinesterase inhibitory and antioxidant activities.

Conclusion: The presence of rich source of flavonoids, in particular catechin, might be responsible for its cholinesterase inhibitory and antioxidant activities.     

Phytochemical analysis,antiproliferative and antioxidant activities of Chrozophora tinctoria: a natural dye plant

Context: Chrozophora tinctoria (L.) A. Juss. (Euphorbiaceae) is known as ‘dyer’s-croton’ and used to obtain dye substances. Recently, natural antioxidants and colorants have been of interest because of their safety and therapeutic effects.

Objective: This study investigates the antiproliferative and antioxidant activities of the various extracts and fractions from C. tinctoria and analyzes their phytochemical contents.

Materials and methods: The aerial parts of C. tinctoria were extracted with water, ethyl acetate, n-butanol, and methanol/chloroform. Phenolic compounds and other constituents of the extracts were analyzed by HPLC/TOF-MS. The ethyl acetate extract (EA) was fractionated by flash chromatography. The extracts, fractions, and major phenolic compounds were investigated for their antiproliferative activities on human cervical adenocarcinoma (HeLa) cell line at the concentrations of 5–100?μg/mL by using BrdU ELISA assay during 24?h of incubation. DPPH radical scavenging activities (5–150?μg/mL) and total phenolic contents of the samples were also evaluated.

Results: 4-Hydroxybenzoic acid (268.20?mg/kg), apigenin-7-glucoside (133.34?mg/kg), and gallic acid (68.92?mg/kg) were the major components of EA. CT/E-F6 (IC₅₀?=?64.59?±?0.01?μg/mL) exhibited the highest antiproliferative activity. CT/E-F2 (IC₅₀=?14.0?±?0.0?μg/mL) and some fractions displayed higher radical scavenging activity compared to synthetic antioxidant BHT (IC_50?=_?23.1?±?0.0?μg/mL). Among the main phenolics, gallic acid exhibited the highest antiproliferative and radical scavenging abilities (IC_50?<_?5?μg/mL).

Conclusion: In this study, we have determined the biologically active fractions and their high effects may be attributed to the presence of gallic acid.     

Leishmanicidal and cytotoxic activities of Nigella sativa and its active principle,thymoquinone

Abstract

Context: Leishmaniasis is a complex disease with a broad spectrum of clinical presentations.

Objective: We evaluated the anti-leishmanial effects of Nigella sativa L. (Ranunculaceae) against Leishmania tropica and Leishmania infantum with an in vitro model.

Materials and methods: Antileishmanial effects of essential oil and methanolic extract of N. sativa (0–200?µg/mL) and thymoquinone (0–25?µg/mL) on promastigotes of both species and their cytotoxicity activities against murine macrophages were evaluated using the MTT assay at 24, 48, and 72?h. Moreover, their leishmanicidal effects against amastigotes were investigated in a macrophage model, for 48 and 72?h.

Results: The findings showed that essential oil (L. tropica IC₅₀ 9.3?μg/mL and L. infantum IC₅₀ 11.7?μg/mL) and methanolic extract (L. tropica IC₅₀ 14.8?μg/mL and L. infantum IC₅₀ 15.7?μg/mL) of N. sativa, particularly thymoquinone (L. tropica IC₅₀ 1.16?μg/mL and L. infantum IC₅₀ 1.47?μg/mL), had potent antileishmanial activity on promastigotes of both species after 72?h. In addition, essential oil (L. tropica IC₅₀ 21.4?μg/mL and L. infantum IC₅₀ 26.3?μg/mL), methanolic extract (L. tropica IC₅₀ 30.8?μg/mL and L. infantum IC₅₀ 34.6?μg/mL), and thymoquinone (L. tropica IC₅₀ 2.1?μg/mL and L. infantum IC₅₀ 2.6?μg/mL) mediated a significant decrease in the growth rate of amastigote forms of both species. Thymoquinone (CC₅₀ 38.8?μg/mL) exhibited higher cytotoxic effects against murine macrophages than the other extracts.

Conclusion: N. sativa, especially its active principle, thymoquinone, showed a potent leishmanicidal activity against L. tropica and L.infantum with an in vitro model.     

Bioactive potential of endophytic Myrothecium sp. isolate M1-CA-102, associated with Calophyllum apetalum

Context: Endophytes colonizing medicinal plants are diverse, constituting a rich bioresource for novel natural products.

Objective: Myrothecium sp. isolate M1-CA-102 was the most promising among the 16 Myrothecium isolates screened. The bioactive potential of the crude extract from the Calophyllum apetalum Willd. endophytic Myrothecium sp. (Alb. &; Schwein.) Ditmar (Incertae sedis) isolate M1-CA-102 and its thin layer chromatography (TLC) fractions were screened based on antioxidant, anti-inflammatory, antimicrobial activities, and cytotoxicity.

Materials and methods: The antioxidant activity was measured by 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2′-azinobis-(3-ethylbenzthiazoline-6-sulfonic acid (ABTS) radical scavenging capacities. Further, 15-lipoxygenase (15-LOX) and human cyclooxygenase-2 (COX-2) inhibition were assessed at different concentrations (25, 50, and 100?μg/mL for the crude extract, 5, 25, and 50?μg/mL for the TLC fractions). DNA-nicking assay as an indicator of the capacity of extracts to scavenge hydroxyl radical was recorded at a concentration of 50?μg/mL. Cell cytotoxicity was recorded by colorimetric 3-(4,5-dimethylthylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Antibacterial (Bacillus subtilis) and anti-Candida (Candida albicans) assays were performed by the microdilution method.

Results: The DPPH and ABTS IC₅₀ values of M1-CA-102 extract were 10 and 6?μg/mL compared with 6.1 and 7.03?μg/mL for the positive control quercetin. The cytotoxicity IC₅₀ value of M1-CA-102 extract was 37?μg/mL, while the M-I TLC fraction was 21?μg/mL. The M1-CA-102 extract gave an IC₅₀ value of 58 and 8?μg/mL for 15-LOX and COX-2, respectively. The MIC values for antimicrobial activity for M1-CA-102 extract ranged from 35 to 54?μg/mL, while for the TLC fractions, it ranged from 91 to 515?μg/mL.

Conclusion: The results indicate that Myrothecium M1-CA-102 isolated from C. apetalum is a potential source of natural metabolites of pharmaceutical importance.     

Pharmacological and computer-aided studies provide new insights into Millettia peguensis Ali (Fabaceae)

Millettia peguensis, popular for its ethnopharmacological uses, was employed to evaluate its different pharmacological properties in this study. The analgesic studies of the plant have been performed by acetic acid-induced writhing and formalin-induced licking tests respectively, whereas the antidiarrheal experiment was done by castor oil-induced diarrheal test. Besides, antioxidant, cytotoxic, antimicrobial, thrombolytic evaluations were performed by DPPH scavenging with phenol content determination, brine shrimp lethality, disc diffusion and clot lysis methods respectively. Moreover, in silico study of the phytoconstituents was carried out by molecular docking and ADME/T analysis.The methanol extract of Millettia peguensis (MEMP) revealed significant biological activity in the analgesic and antidiarrheal test (p < 0.001) compared to the standards. Antioxidant assay displayed promising IC₅₀ values (15.96 μg/mL) with the total phenol content (65.27 ± 1.24 mg GAE/g). In the cytotoxicity study, the LC₅₀ value was found to be 1.094 μg/mL. Besides, MEMP was highly sensitive to the bacteria but less liable to clot lysis. Furthermore, phytoconstituents exposed potential binding affinity towards the selected receptors, whereas the ADME/T properties indicated the drug likeliness of the plant. The outcomes of these findings suggest the therapeutic potential of this plant against pain, diarrhea, inflammation, and tissue toxicity.     

Cytotoxic activity of physodic acid and acetone extract from Hypogymnia physodes against breast cancer cell lines

Context: Lichens produce specific secondary metabolites with different biological activity.

Objective: This study investigated the cytotoxic effects of physodic acid, in addition to the total phenolic content and cytotoxic and antioxidant activity of acetone extract from Hypogymnia physodes (L.) Nyl. (Parmeliaceae).

Materials and methods: Cytotoxicity of physodic acid (0.1–100?μM) was assessed in MDA-MB-231, MCF-7 and T-47D breast cancer cell lines and a nontumorigenic MCF-10A cell line using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, neutral red uptake and crystal violet assays during 72?h of incubation. An MTT assay was also used to assess the cytotoxic effects of the acetone extract (0.1–100?μg/mL) in the MDA-MB-231, MCF-7, T-47D breast cancer cell lines after 72?h. The total phenolic content of the acetone extract, expressed as the gallic acid equivalent, was investigated using Folin-Ciocalteu reagent. The antioxidant activity of the extract was assessed by 2,2-diphenyl-1-picrylhydrazyl and ferric-reducing antioxidant power assays.

Results: The cytotoxic activity of physodic acid appeared to be strong in the tumorigenic cell lines (IC₅₀ 46.0–93.9?μM). The compound was inactive against the nontumorigenic MCF-10A cell line (IC_50?>100?μM). The acetone extract showed cytotoxicity in the breast cancer cell lines (IC₅₀ 46.2–110.4?μg/mL). The acetone extract was characterized by a high content of polyphenols, and it had significant antioxidant activity.

Discussion and conclusion: Physodic acid and acetone extract from H. physodes displayed cytotoxic effects in the breast cancer cell lines. Furthermore, acetone extract from H. physodes possessed significant antioxidant properties.     

Antidiarrheal potential of standardized extract of Rhododendron arboreum Smith flowers in experimental animals

Objective:

To investigate standardized ethyl acetate fraction of Rhododendron arboreum (EFRA) flowers for antidiarrheal activity in experimental animals.

Materials and Methods:

A simple sensitive high performance thin layer chromatography (HPTLC) method was used for the determination of hyperin in EFRA. The standardized fraction was investigated for castor oil, magnesium sulfate-induced diarrhea, measurement of gastrointestinal transit using charcoal and castor oil-induced enteropooling.

Results:

The concentration of hyperin in flowers of R. arboreum was found to be 0.148% by HPTLC. Oral administration of EFRA at 100, 200 and 400 mg/kg exhibited dose-dependent and significant (P<0.05-0.001) antidiarrheal potential in castor oil and magnesium sulfate-induced diarrhea. EFRA at doses of 100, 200 and 400 mg/kg also produced significant (P<0.05-0.001) dose-dependent reduction in propulsive movement in castor oil-induced gastrointestinal transit using charcoal meal in rats. EFRA was found to possess an antienteropooling in castor oil-induced experimental animals by reducing both weight and volume of intestinal content significantly.

Conclusion:

These findings demonstrate that standardized ethyl acetate fraction of R. arboreum flowers has potent antidiarrheal activity thus justifying its traditional use in diarrhea and have great potential as a source for natural health products.KEY WORDS: Antidiarrheal, enteropooling, gastrointestinal motility, high performance thin layer chromatography, Rhododendron arboreum     

In vitro Antioxidant and Antibacterial Activities of Methanol Extract of Kyllinga nemoralis

The present study was designed to evaluate the antioxidant and antibacterial activity of methanol extract of Kyllinga nemoralis. Six different in vitro antioxidant assays including 2,2-diphenyl-1-picrylhydrazyl, hydroxyl radical, superoxide anion radical, hydrogen peroxide radical, ferric reducing antioxidant power assay and reducing power were carried out to ensure the scavenging effect of the plant on free radicals. In addition, total antioxidant capacity assay, total phenolic contents, tannins, flavonoids and flavonol contents of the plant were also analysed by the standard protocols. Kyllinga nemoralis exhibited high antioxidant activity on 2,2-diphenyl-1-picrylhydrazyl assay (IC₅₀= 90 μg/ml), superoxide radical scavenging assay (IC₅₀= 180 μg/ml) and hydrogen peroxide radical scavenging assay (IC₅₀= 200 μg/ml), compared with standards. These observations provide comprehensible supporting evidence for the antioxidant potential of the plant extract. Reducing power (IC₅₀= 213.16 μg/ml) and hydroxyl radical scavenging activity (IC₅₀= 223 μg/ml) of the plant extract was remarkable. The methanol extract of K. nemoralis exhibited significant antimicrobial activity against Gram-positive human pathogenic bacteria. Standard in vitro antioxidant assays assessed the electron donating ability of the plant extract in scavenging free radicals. The inhibitory effect of the plant extract against bacterial pathogens may be due to the presence of phytochemicals. Thus, the results suggest that Kyllinga nemoralis is a potential source of antioxidants and could serve as the base for drug development.     

In vitro assessment of selected Korean plants for antioxidant and antiacetylcholinesterase activities

Context: Antiacetylcholinesterase (AChE) drugs have been a main therapeutic treatment for Alzheimer’s disease because increased AChE levels play a key role in reducing neurotransmission.

Objectives: Extracts from 35 Korean plants were selected and screened for antioxidant and anti-cholinesterase activity to explore new sources derived from Korean natural resources that could be used as AD therapeutic agents.

Materials and methods: The antioxidant effect of extracts from 35 selected Korean plants was determined using two most common free radical scavenging assays using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2′-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS). Additionally, the effect of extracts, identified as antioxidants, on acetylcholinesterase inhibition was assessed by an acetylcholinesterase assay kit.

Results: Out of 36 extracts of 35 plants tested, Oenothera biennis L. (9.09?μg/mL), Saururus chinensis (Lour.) Baill. (9.52?μg/mL) and Betula platyphylla var. japonica (9.85?μg/mL) showed strong DPPH scavenging activity. Twelve other extracts also exerted moderate free radical scavenging activities with IC₅₀ values ranging from 10 to 50?μg/mL. Antioxidant capacity detected by ABTS assay was only significant in O. biennis (23.40?μg/mL), while the other extracts were weak or unable to reduce the production of ABTS. Based on the antioxidant activities of these plant extracts, 19 extracts with IC₅₀ values less than 100?μg/mL in DPPH assay were selected for further AChE inhibition assay. Among the extracts tested, the IC₅₀ value for Prunella vulgaris var. lilacina NAKAI (18.83?μg/mL) in AChE inhibitory activity was the lowest, followed by O. biennis (20.09?μg/mL) and Pharbitis nil Chosy (22.79?μg/mL).

Conclusions: Considering complex multifactorial etiology of AD, the extracts of P. vulgaris var. lilacina (aerial part), O. biennis (seed) and P. nil (seed) may be safe and ideal candidates for future AD modifying therapies.     

Unlocking the in vitro anti-inflammatory and antidiabetic potential of Polygonum maritimum

Context: Several Polygonum species (Polygonaceae) are used in traditional medicine in Asia, Europe and Africa to treat inflammation and diabetes.

Objective: Evaluate the in vitro antioxidant, anti-inflammatory and antidiabetic potential of methanol and dichloromethane extracts of leaves and roots of the halophyte Polygonum maritimum L.

Material and methods: Antioxidant activity was determined (up to 1?mg/mL) as radical-scavenging activity (RSA) of 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), copper (CCA) and iron (ICA) chelating activities and iron reducing power (FRAP). NO production was measured in lipopolysaccharide (LPS)-stimulated macrophages for 24?h at concentrations up to 100?μg/mL and antidiabetic potential was assessed by α-amylase and α-glucosidase inhibition (up to 10?mg/mL) assays. The phytochemical composition of the extracts was determined by gas chromatography-mass spectrometry (GC-MS).

Results: The methanol leaf extract had the highest activity against DPPH? (IC₅₀ =?26?μg/mL) and ABTS⁺? (IC₅₀ =?140?μg/mL), FRAP (IC₅₀ =?48?μg/mL) and CCA (IC₅₀ =?770?μg/mL). Only the dichloromethane leaf extract (LDCM) showed anti-inflammatory activity (IC₅₀ =?48?μg/mL). The methanol root (IC₅₀ =?19?μg/mL) and leaf (IC₅₀ =?29?μg/mL) extracts strongly inhibited baker’s yeast α-glucosidase, but LDCM had higher rat’s α-glucosidase inhibition (IC₅₀ =?2527?μg/mL) than acarbose (IC₅₀ =?4638?μg/mL). GC-MS analysis identified β-sitosterol, stigmasterol, 1-octacosanol and linolenic acid as possible molecules responsible for the observed bioactivities.

Conclusions: Our findings suggest P. maritimum as a source of high-value health promoting commodities for alleviating symptoms associated with oxidative and inflammatory diseases, including diabetes.     

Biological activities of ethyl acetate extract of different parts of Hyssopus angustifolius

Context: Hyssopus angustifolius M. Bieb. (Lamiaceae) is one of the most important medicinal plants in Iranian traditional medicine for the treatment of lung inflammation, laryngitis and cough relief. Much attention has been paid to this medicinal plant because of its traditional uses.

Objective: The present study examined the antioxidant and antihemolytic activities of ethyl acetate extract of stems, leaf and flowers of Hyssopus angustifolius.

Materials and methods: Antioxidant activity of extracts was evaluated by employing six different models, i.e., DPPH, nitric oxide and hydrogen peroxide scavenging, metal chelating and reducing power activities and hemoglobin-induced linoleic acid system. Also, antihemolytic activity was evaluated against hydrogen peroxide-induced hemolysis.

Results: Flowers extract showed the better activity than leaf and stems extracts in DPPH radical scavenging activity (IC₅₀ was 275.4?±?7.6 μg mL^?1). Leaf, stems and flowers extracts showed good nitric oxide scavenging activity (IC₅₀ were 376.6?±?11.4 µg mL^?1 for flowers, 297.6?±?9.6 μg mL^?1 µg mL^?1 for leaves and 837.8?±?19.2 µg mL^?1 for stems). The leaf extract exhibited better hydrogen peroxide scavenging and Fe²⁺ chelating activity than stems and flowers extracts. In hemoglobin-induced linoleic acid system, all of the extracts exhibited very good activity. Also, extracts show weak reducing power activity. The ethyl acetate extract of leaf showed better antihemolytic activity than the flower and stems (IC₅₀ was 94.0?±?2.4 μg mL^?1).

Discussion and conclusion: These findings give a scientific basis to the traditional usage of Hyssopus angustifolius, also showing its potential as rich sources of natural antioxidant compounds.     

Antimalarial and free radical scavenging activities of rhizomes of Polygonatum verticillatum supported by isolated metabolites

Antimalarial activity of the crude extract of Polygonatum verticillatum rhizomes and its sequentially partitioned fractions were investigated against Plasmodium falciparum. The crude extract possessed notable activity (IC₅₀: 21.67?μg/mL) that enhanced reasonably upon fractionation. The antiparasitic potency of the n-hexane fraction was maximum (IC₅₀: 2.33?μg/mL) followed by chloroform (IC₅₀: 4.62?μg/mL). However, the remaining fractions showed insignificant activity in the assay. The extracts of the plant showed marked scavenging activity on stable free radical, DDPH. The most potent antioxidant was the chloroform fraction (IC₅₀: 90?μg/mL) followed by ethyl acetate (IC₅₀: 93?μg/mL) and n-butanol (IC₅₀: 95?μg/mL) fractions. In the brine shrimps lethality test, the extracts were found nontoxic with the exception of ethyl acetate fraction (LD₅₀: 492.846?μg/mL). The bioactivity-guided isolation resulted into 5-hydroxymethyl-2-furaldehyde (HMF) and diosgenin which strongly supports the present experimental findings.