Antimalarial and antiplasmodial activity of husk extract and fractions of Zea mays

Context: Zea mays L. (Poacae) husk decoctions are traditionally used in the treatment of malaria by various tribes in Nigeria.

Objective: To assess the antimalarial and antiplasmodial potentials of the husk extract and fractions on malaria parasites using in vivo and in vitro models.

Materials and methods: The ethanol husk extract and fractions (187–748?mg/kg, p.o.) of Zea mays were investigated for antimalarial activity against Plasmodium berghei using rodent (mice) malaria models and in vitro activity against chloroquine sensitive (Pf 3D7) and resistant (Pf INDO) strains of Plasmodium falciparum using the SRBR green assay method. Median lethal dose and cytotoxic activities against HeLa and HEKS cells were also carried out. The GCMS analysis of the most active fraction was carried out.

Results: The husk extract (187–748?mg/kg, p.o.) with LD₅₀ of 1874.83?mg/kg was found to exert significant (p?P. berghei infection in suppressive, prophylactive and curative tests. The crude extract and fractions also exerted prominent activity against both chloroquine sensitive (Pf 3D7) and resistant (Pf INDO) strains of P. falciparum with the ethyl acetate fraction exerting the highest activity with IC₅₀ values of 9.31?±?0.46?μg/mL (Pf 3D7) and 3.69?±?0.66?μg/mL (Pf INDO). The crude extract and fractions were not cytotoxic to the two cell lines tested with IC₅₀ values of?>100?μg/mL against both HeLa and HEKS cell lines.

Discussion and conclusion: These results suggest that the husk extract/fractions of Zea mays possesses antimalarial and antiplasmodial activities and these justify its use in ethnomedicine to treat malaria infections.     

In vivo antiplasmodial activities of aqueous extract of Bridelia ferruginea stem bark against Plasmodium berghei berghei in mice

Context: Bridelia ferruginea Benth (Euphorbiaceae) is an indigenous medicinal plant in Nigeria. It is usually a gnarled shrub which sometimes reaches the size of a tree in suitable condition. Decoctions of parts of this plant have been employed in ethno medicine in many parts of Africa for treatment of many ailments including malaria fever.

Objective: In vivo antiplasmodial activity of aqueous stem bark extract of BF was investigated against Plasmodium berghei-infected mice.

Materials and methods: The aqueous stem bark extract of BF (100–400?mg/kg) was administered orally to P. berghei-infected mice in both early and established models of antiplasmodial studies.

Results: The extract exhibited significant (p?<?0.05) antiplasmodial activity in early and established infection tests with a considerable mean survival time comparable to that of chloroquine, 10?mg/kg. The oral LD₅₀ obtained was greater than 5000?mg/kg in mice.

Discussion and conclusions: The findings show that aqueous stem bark extract of Bridelia ferruginea possesses considerable antiplasmodial activity which can be developed in malaria therapy.     

Antimalarial,antiplasmodial and analgesic activities of root extract of Alchornea laxiflora

Context: Alchornea laxiflora (Benth.) Pax. &; Hoffman (Euphorbiaceae) root decoctions are traditionally used in the treatment of malaria and pain in Nigeria.

Objective: To assess the antimalarial, antiplasmodial and analgesic potentials of root extract and fractions against malarial infections and chemically-induced pains.

Material and methods: The root extract and fractions of Alchornea laxiflora were investigated for antimalarial activity against Plasmodium berghei infection in mice, antiplasmodial activity against chloroquine sensitive (Pf 3D7) and resistant (Pf INDO) strains of Plasmodium falciparum using SYBR green assay method and analgesic activity against experimentally-induced pain models. Acute toxicity study of the extract, cytotoxic activity against HeLa cells and GCMS analysis of the active fraction were carried out.

Results: The root extract (75–225?mg/kg, p.o.) with LD₅₀ of 748.33?mg/kg exerted significant (p?P. berghei infection in suppressive, prophylactive and curative tests. The root extract and fractions also exerted moderate activity against chloroquine sensitive (Pf 3D7) and resistant (Pf INDO) strains of P. falciparum with the ethyl acetate fraction exerting the highest activity with IC₅₀ value of 38.44?±?0.89?μg/mL (Pf 3D7) and 40.17?±?0.78?μg/mL (Pf INDO). The crude extract was not cytotoxic to HeLa cells with LC₅₀ value >100?μg/mL. The crude extract and ethyl acetate fraction exerted significant (p?Discussion and conclusions: These results suggest that the root extract/fractions of A. laxiflora possess antimalarial, antiplasmodial and analgesic potentials and these justify its use in ethnomedicine to treat malaria and pain.     

Landolphia owariensis leaf extracts reduce parasitemia in Plasmodium berghei-infected mice

Context Landolphia owariensis P. Beauv. (Apocyanaceae) leaf is used in southeast Nigeria to treat malaria.

Objective This study evaluated the antiplasmodial activity of L. owariensis leaf extract and fractions, also the phytoconstituents were standardized and analyzed.

Methods The effects of daily, oral administrations of 200, 400 and 800?mg/kg of L. owariensis leaf extract (LOE), its hexane (LOHF), ethyl acetate (LOEF) and methanol (LOMF) fractions on early, established and residual infections in Plasmodium berghei-infected albino mice were evaluated in vivo. The extract and fractions were subjected to phytochemical analysis and HPLC fingerprinting, and the acute toxicity of LOE was evaluated.

Results The extract and fractions elicited 29–86, 18–95 and 75–96% significant (p?<?0.001) suppression of parasitemia in early, established and residual infections, respectively. The ED₅₀ values for suppressive activity of LOE, LOHF, LOEF and LOMF were 266.56, 514.93, 392.95 and 165.70?mg/kg, respectively. The post-day 30-survival index was 16.7–50, 16.7, 16.7–66.7 and 50–83.3% for LOE, LOHF, LOEF, and LOMF, respectively. Extract-treated mice significantly (p?<?0.001) gained weight and had reduced mortality compared with negative control (untreated) mice. An oral LD₅₀ value >5000?mg/kg in mice was established for LOE. The LOMF showed the greatest antiplasmodial activity in all the models, suggesting that the antimalarial activity of the plant may be attributed to alkaloids, flavonoids, saponins and tannins present in the fraction.

Conclusion Results demonstrate the antiplasmodial activity of L. owariensis leaf, and provide a pharmacological rationale for its ethnomedicinal use as an antimalarial agent.     

An evaluation of the anti-inflammatory,antipyretic and analgesic effects of hydroethanol leaf extract of Albizia zygia in animal models

Context: The leaves of Albizia zygia (DC.) J.F. Macbr. (Leguminosae-Mimosoideae) are used in Ghanaian traditional medicine for the treatment of pain, inflammatory disorders and fever (including malaria).

Objectives: The present study evaluated the anti-inflammatory, antipyretic and analgesic effects of the hydroethanol leaf extract of Albizia zygia (AZE) in animal models.

Materials and methods: The anti-inflammatory and antipyretic effects of AZE were examined in the carrageenan-induced foot oedema model and the baker’s yeast-induced pyrexia test respectively. The analgesic effect and possible mechanisms of action were also assessed in the formalin test.

Results: AZE (30–300?mg/kg, p.o.), either preemptively or curatively, significantly inhibited carrageenan-induced foot edema in 7-day-old chicks (ED₅₀ values; preemptive: 232.9?±?53.33?mg/kg; curative: 539.2?±?138.28?mg/kg). Similarly, the NSAID diclofenac (10–100?mg/kg, i.p.) significantly reduced the oedema in both preemptive (ED₅₀: 21.16?±?4.07?mg/kg) and curative (ED₅₀: 44.28?±?5.75?mg/kg) treatments. The extract (30–300?mg/kg, p.o.) as well as paracetamol (150?mg/kg, p.o.) also showed significant antipyretic activity in the baker’s yeast-induced pyrexia test (ED₅₀ of AZE: 282.5?±?96.55?mg/kg). AZE and morphine (1–10?mg/kg, i.p.; positive control), exhibited significant analgesic activity in the formalin test. The analgesic effect was partly or wholly reversed by the systemic administration of naloxone, theophylline and atropine.

Conclusion: The results suggest that AZE possesses anti-inflammatory, antipyretic and analgesic properties, which justifies its traditional use. Also, the results show the involvement of the opioidergic, adenosinergic and the muscarinic cholinergic pathways in the analgesic effects of AZE.     

Antiplasmodial activity of aqueous extract of Berberis aristata roots against Plasmodium berghei-infected BALB/c mice

Abstract

Context: The rising problem of resistance to present antimalarial drugs stresses the need to look for newer antiplasmodial components with effective modes of action. The roots of Berberis aristata DC. (Berberidaceae) are used in the traditional medicine for malaria in various parts of India.

Objective: The objective of this study was to evaluate antiplasmodial activity of B. aristata roots extract for the validation of its traditional medicinal use.

Material and methods: Aqueous root extract of Berberis aristata (AREBA) was screened for its in vitro as well as in vivo antiplasmodial activity against lethal rodent malaria parasite Plasmodium berghei NK65. In vitro activity was evaluated against schizont maturation of P. berghei using various concentrations ranging from 1 to 100?µg/mL. For in vivo studies, AREBA at the doses of 150, 250, 350, and 650?mg/kg/d was administered to P. berghei infected BALB/c mice orally for 4 consecutive days (D0–D3).

Results: AREBA showed in vitro antiplasmodial activity with an IC₅₀ value of 40?µg/mL. In vivo studies demonstrated a variable dose-dependent chemosuppression with higher efficacy at lower doses. At a dose of 350?mg/kg/d, the suppressive and preventive activities were found to be 67.1% and 53.9%, respectively, followed by enhancing mean survival period up to 12.8?d for the curative assay versus 7.5?d for the untreated mice.

Discussion and conclusion: These results provide relevant scientific evidences for the traditional medicinal use of this plant as malaria remedy and further advocates the isolation and characterization of active antiplasmodial principle from this plant.     

Effective antidiabetic and antioxidant fractions of Otostegia persica extract and their constituents

Context: Otostegia persica (Burm.) Boiss. (Lamiaceae), “Goldar” in Persian, is widely used in the folk medicine of south Iran for control of diabetes mellitus.

Objective: In the present study, hypoglycemic and antioxidant effects of different fractions of the O. persica extract were investigated and constituents of effective fractions were elucidated.

Materials and method: Different concentrations (100–400?mg/kg) of aqueous infusion (AI) of flowering aerial parts of the plant (traditional preparation) and all fractions of the O. persica extract (i.p. injection) were tested for antidiabetic activity in streptozocin-induced diabetic NMRI mice. Blood glucose level was measured at time 0 and intervals of 1, 2, 4, and 6?h later. Antioxidant activities of different fractions of the plant extract and pure compounds (0.1, 0.5, and 1?mg/ml) were determined with the DPPH method. Four compounds were isolated and identified from potent fractions.

Results and discussion: Antidiabetic activity demonstrated that the effect of the methanol fraction at a dose of 300?mg/kg was equivalent with glibenclamide, and at a dose of 400?mg/kg was comparable with glibenclamide and insulin (p?>?0.05). The EC₅₀ of the methanol fraction was 307.12?mg. Methanol and ethyl acetate fractions showed antioxidant activities (both IC₅₀ equal to 0.49?mg/ml), so these fractions were selected for the purification of compounds. Chrysoeriol from ethyl acetate and three apigenin derivatives (6-methylapigenin, apigenin-7-O-glucoside, and echinaticin) from the methanol fraction were isolated and identified (new for the species). Chrysoeriol exhibited potent antioxidant activity comparable with vitamin E and BHT (p?>?0.05).

Conclusion: The present study confirmed the folklore usage of O. persica for antidiabetic properties.     

Evaluation of antinociceptive and antidiarrhoeal properties of Manilkara zapota leaves in Swiss albino mice

Context Manilkara zapota (L.). P. Royen. (Sapotaceae) has been used in folk medicine to treat pain, diarrhoea, inflammation, arthralgia, and other disorders.

Objective Screening of Manilkara zapota leaves ethanol extract and its different solvent soluble fractions for possible antinociceptive and antidiarrhoeal activities in Swiss albino mice.

Materials and methods The extract and various fractions (200 and 400?mg/kg body weight; p.o.) were tested for peripheral and central antinociceptive activity by acetic acid-induced writhing and radiant heat tail-flick method, respectively; castor oil-induced diarrhoeal model was used to evaluate antidiarrhoeal activity at both doses. All the samples were administered once in a day and the duration of study was approximately 5?h.

Results Ethanol extract (400?mg/kg), petroleum ether fraction (400?mg/kg), and ethyl acetate fraction (400?mg/kg) showed significant peripheral antinociceptive activity having 59.89, 58.24, and 46.7% (p?<?0.001) of writhing inhibition, respectively, which is comparable with that of standard diclofenac (59.34% inhibition). The ethanol extract (400?mg/kg) and petroleum ether fraction (400?mg/kg) also showed promising central analgesic activity having 74.15 and 82.15% (p?<?0.001) elongation of reaction time, respectively, at 90?min after administration of sample which is also similar to that obtained by morphine (85.84% elongation). In antidiarrhoeal activity screening, ethanol extract (200 and 400?mg/kg) showed significant inhibition of defecation by 53.57 and 60.71%, respectively (p?<?0.001) compared with that of loperamide (71.42%).

Discussion and conclusion The findings of the studies demonstrated antinociceptive and antidiarrhoeal activities of M. zapota leaves which could be the therapeutic option against pain and diarrhoeal disease.     

Comparison of protective and curative potential of Daucus carota root extract on renal ischemia reperfusion injury in rats

Abstract

Context: Daucus carota Linn (Apiaceae), a useful vegetable, is traditionally used in treating kidney and hepatic dysfunctions.

Objective: To evaluate the protective and curative potential of D. carota root extract on renal ischemia reperfusion injury in rats.

Materials and methods: Wistar rats were selected with 8?+?8 groups (n?=?6). Renal pedicles of rats were occluded for 45?min and allowed for reperfusion period. In protective and curative studies, 14 days prior and 14 days after the induction of ischemia/reperfusion (I/R), rats received petroleum ether extract (PEE 250 and 500?mg/kg), fractional methanol extract (FME 250 and 500?mg/kg) and direct methanol extract (DME 250 and 500?mg/kg) of Daucus carota root, orally, once daily.

Results: PEE at a dose of 500?mg/kg significantly (p?<?0.001) reduced the levels of serum creatinine (0.853–3.090?mg/dl), uric acid (1.300–3.500?mg/dl) and urea (58.26–132.00?mg/dl) compared to disease control. FME at a dose of 500?mg/kg body weight significantly (p?<?0.001) reduced the levels of serum creatinine (0.960–3.090?mg/dl), uric acid (1.700–3.500?mg/dl) and urea (77.17–132.00?mg/dl) compared to disease control. DME at a dose of 500?mg/kg body weight significantly (p?<?0.001) reduced the levels of serum creatinine (1.173–3.090?mg/dl), uric acid (2.267–3.500?mg/dl) and urea (84.75–132.00?mg/dl) compared to disease control.

Discussion and conclusion: Findings demonstrate that postconditioning with the D. carota root extract significantly improves kidney function in I/R rats.     

Antiprotozoal screening of the Cuban native plant Scutellaria havanensis

Context: Scutellaria havanensis Jacq. (Lamiaceae) is a native medicinal herb with a history of use in Cuba.

Objective: This study screens the antiprotozoal activity of S. havanensis.

Materials and methods: Chloroform and methanol extracts from leaves and stems were evaluated in vitro at doses between 0.015 and 200?μg/mL against protozoan parasites: Plasmodium berghei, Trichomonas vaginalis and Leishmania amazonensis. Chloroform and methanol extracts were characterized by GC/MS. Cytotoxicity against mouse peritoneal macrophages was tested in parallel.

Results: Scutellaria havanensis extracts exhibited IC₅₀ values between 7.7 and 32.2?μg/mL against trophozoites of P. berghei and T. vaginalis; while the extracts were inactive against L. amazonensis promastigotes. Trichomonicidal activity of methanol extract exhibited the best selectivity but chloroform extract showed the highest antiplasmodial, trichomonicidal and cytotoxic activity. The majority of compounds in the chloroform extract were hydroxy and/or methoxyflavones (77.96%), in particular, wogonin (48.27%). In methanol extract, wogonin (5.89%) was detected. Trichomonicidal effect of wogonin was moderate (IC_50?=_?56?μM) and unspecific with respect to macrophages (SI?=?2). On the contrary, antiplasmodial activity of wogonin were particularly active (IC_50?=_?15?μM) demonstrating a higher selectivity index (SI?=?7.4).

Conclusions: Wogonin is an active principle compound of the chloroform extract of S. havanensis against P. berghei and T. vaginalis trophozoites, whereas the methanol extract of S. havanensis should be investigated more deeply as a trichomonicide. Our findings suggest that wogonin is potentially useful for the development of antimalarial alternative treatments.     

Hydroalcoholic extract of Myrtus communis can alter anxiety and sleep parameters: a behavioural and EEG sleep pattern study in mice and rats

Context: Myrtus communis L. (Myrtaceae), myrtle, is an evergreen shrub with strong antibacterial, anti-inflammatory, antihyperglycemic and antioxidant activities. Also, it is used as a sedative-hypnotic plant in Iranian traditional medicine.

Objective: This study evaluates the effect of 80% ethanolic extract of M. communis leaves on sleep and anxiety in mice and rats.

Materials and methods: Male NMRI mice were subjected to open field, righting reflex, grip strength and pentylentetrazole-induced seizure tests. Male Wistar rats were used to evaluate the alterations in rapid eye movement (REM) and non-REM (NREM) sleep. They were treated with 25–400?mg/kg doses of the extract intraperitoneally.

Results: The applied doses (50–200?mg/kg) of M. communis extract increased vertical (ED_50?=_?40.2?±?6.6?mg/kg) and vertical and horizontal activity (ED_50?=_?251?±?55?mg/kg), while treatment with 200 and 400?mg/kg attenuated muscle tone significantly compared to vehicle treated animals (p?<?0.001 for all) in a dose-independent manner. Also, a significant hypnotic and not anticonvulsant effect was observed when animals were treated with 200?mg/kg of the extract (p?<?0.01). In this regard, electroencephalography results showed that REM sleep time was decreased (2.4?±?0.5%), while total and NREM sleep times were increased significantly compared to the control group of mice (82.5?±?7.6%).

Discussion and conclusion: The data show the anxiolytic and muscle relaxant effect of the extract without anticonvulsant activities. The anxiolytic, myorelaxant and hypnotic effects without effect on seizure threshold are in line with the effect of a alpha 2 GABA receptor agonist.     

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.     

Mechanistic assessment of the analgesic,anti-inflammatory and antipyretic actions of Dalbergia saxatilis in animal models

Context: Aqueous root extract of Dalbergia saxatilis, Hook, f., (Leguminosae) (DS) is reported useful for toothache, pains, and fever, but not scientifically proven.

Objective: This study determined its effectiveness in pain, inflammation, and fever, applying scientific models.

Materials and methods: Swiss mice or Sprague–Dawley rats (n?=?5) were pretreated with distilled water, DS (100 or 200?mg/kg), or standard drug for 30?min. The analgesic activity was measured by acetic acid writhing, tail flick, tail immersion, tail clip, hot plate, and formalin pain tests; anti-inflammatory effects were determined via carrageenan and dextran rat paw oedema tests; antipyretic activity was measured by Escherichia coli lipopolysaccharide (ECL) and turpentine in rabbits, and d-amphetamine sulphate (d-AS) pyrexia test in rats.

Results: Writhing frequency inhibition was produced by 200?mg/kg DS (33.10%), aspirin (38.19%) and morphine (93.68%). Unlike morphine, DS did not produce significant prolongation of the reaction times in the hot-plate, tail immersion, tail flick, and tail clip tests. In the first and second phases of formalin test, respectively, % inhibition was: 200?mg/kg DS (25.70% and 0%), aspirin (4.76% and 67.33%), morphine (81.42% and 66.11%); for carrageenan and dextran tests, significant difference was recorded between 200?mg/kg DS and control up to 6?h. Significant reduction in ECL, turpentine and d-AS pyrexia was recorded at 100 and 200?mg/kg DS.

Conclusion: DS produces mild non-steroidal analgesic and anti-inflammatory, as well as significant antipyretic actions involving cyclooxygenase, α₂ adrenoceptor and interleukin-1 β1 due to any of glycosides, saponins or phenolic tannins.     

Antinociceptive,anti-inflammatory and antipyretic properties of an aqueous extract of Corchorus capsularis leaves in experimental animal models

The present study was carried out to establish the antinociceptive, anti-inflammatory and antipyretic properties of an aqueous extract of jute plant leaves, Corchorus capsularis L. (Tiliaceae), in experimental animals. The antinociceptive activity was measured using the abdominal constriction, hot plate and formalin tests, while the anti-inflammatory and antipyretic activities were measured using the carrageenan-induced paw edema and brewer’s yeast-induced pyrexia tests, respectively. The extract, obtained after 72 h soaking of the air-dried leaves in distilled water, freeze-drying for 72 h and then prepared in dosages of 11.57, 57.85, and 115.7 mg/kg, was administered subcutaneously (10 ml/kg) 30 min prior to subjection to the above mentioned assays. The extract was found to exhibit significant (antinociceptive, anti-inflammatory and anti-pyretic, activities in a dosage-independent manner. In conclusion, the aqueous extract of C. capsularis possesses antinociceptive and antipyretic activities and supports the previous claim of its traditional use to treat various ailments.     

In vitro immunomodulatory activity and in vivo anti-inflammatory and analgesic potential with gastroprotective effect of the Mediterranean red alga Laurencia obtusa

Context: Red algae have been recognized as a rich natural source of compounds possessing interesting biological and pharmacological activities.

Objective: This work investigates anti-inflammatory, analgesic and gastroprotective activities of MeOH/CH₂Cl₂ crude extract and its fractions F1 (50% MeOH) and F2 (80% MeOH) from the whole alga plant Laurencia obtusa Hudson (Rhodomelaceae).

Materials and methods: Anti-inflammatory activity was evaluated in vitro using cytometric bead array (CBA) technology to follow up the secretion of tumour necrosis factor alpha (TNF-α) in lipopolysaccharide activated THP-1 monocytic cells at doses of 10–250?μg/mL and in vivo using carrageenan-induced paw oedema in Wistar rats at doses of 25, 50, 100 and 200?mg/kg. Crude extract and fractions were tested at the doses of 25, 50, 100 and 200?mg/kg for peripheral and central analgesic activity by acetic acid-induced writhing test and hot-plate method, respectively, in Swiss albino mice. Gastroprotective activity was evaluated using HCl/ethanol-induced gastric ulcer test in rats at doses of 25, 50, 100 and 200?mg/kg.

Results: Crude extract, F1 and F2 showed an interesting inhibition of TNF-α secretion with IC₅₀ values of 25, 52 and 24?μg/mL, respectively, and a significant anti-inflammatory activity in vivo (p?< 0.01), 3?h after carrageenan injection, the oedema inhibition was 55.37%, 52.18% and 62.86%, respectively, at the dose of 100?mg/kg. Furthermore, they showed a significant peripheral analgesic activity with 53.79%, 55.92% and 57.37% (p?< 0.01) of writhing inhibition, respectively. However, no significant activity was found in the hot-plate test. An interesting gastroprotective effect was observed with crude extract and its fractions F1 and F2 with a gastric ulcer inhibition of 65.48%, 77.42% and 81.29%, respectively, at the dose of 50?mg/kg.

Discussion and conclusion: These results suggest that L. obtusa might be used as a potential source of natural anti-inflammatory and analgesic agents with gastroprotective effect.     

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.     

In vivo Antimalarial Activities of Russelia Equisetiformis in Plasmodium Berghei Infected Mice

The rising problem of resistance to most commonly used antimalarials remains a major challenge in the control of malaria suggesting the need for new antimalarial agents. This work explores the antiplasmodial potential of ethanol extract of Russelia equisetiformis in chloroquine Plasmodium berghei infected mice. Swiss albino mice were intraperitoneally infected with chloroquine-resistant P. berghei (ANKA). Experimental mice were treated for four days consecutively with graded doses of plant extracts and standard antimalarial drugs (artesunate and chloroquine) at a dose of 10 mg/kg body weight used as control. The extract showed a dose-dependent activity in the chemosuppression of P. berghei parasites by 31.6, 44.7, 48.4 and 86.5% at doses of 100, 200, 400 and 800 mg/kg, while chloroquine (10 mg/kg) and artesunate produced 59.4 and 68.4%, respectively. The extract showed a significant decrease in parasitaemia (P<0.05). The level of parasitemia and decrease in weight in all the treated groups was significantly lower (P<0.05) compared with the infected but untreated mice. The plant extract was devoid of toxicity at the highest dose tested (5000 mg/kg). The study concluded that the ethanol extract of R. equisetiformis possesses antimalarial effect, which supports the folk medicine claim of its use in the treatment of malaria.     

Antioxidant,anticholinesterase and tyrosinase inhibition activities,and fatty acids of Crocus mathewii – A forgotten endemic angiosperm of Turkey

Context We report the first ever chemical/biochemical study on Crocus mathewii Kerndorff (Iridaceae) – a Turkish endemic angiosperm. This plant has never been explored for its phytochemistry and bioactivities.

Objective This study explores C. mathewii corm and aerial parts for the chemical and biological properties of hexane, ethyl acetate, methanol and water fractions of the extracts.

Material and methods Plant material (20 g) was extracted by methanol (250?mL?×?5, 3 days each) and fractioned into hexane, ethyl acetate, methanol and water. All fractions were subjected to β-carotene–linoleic acid, DPPH^·, ABTS^·+, CUPRAC, metal chelating and tyrosinase inhibition activities. Hexane fractions were submitted to GC–MS analysis.

Results Ethyl acetate fractions showed excellent IC₅₀ values in DPPH^· (aerial 36.21?±?0.76 and corm 33.87?±?0.02?mg/L) and ABTS^·+ (aerial 33.01?±?0.79 and bulb 27.87?±?0.33?mg/L); higher than the IC₅₀ of the standard α-tocopherol (DPPH 116.25?±?1.97; ABTS 52.64?±?0.37?mg/L), higher than BHA in DPPH (57.31?±?0.25?mg/L), but slightly lower in ABTS (19.86?±?2.73?mg/L). Methanol extract of aerial parts also showed higher activity than α-tocopherol in DPPH (85.56?±?11.51?mg/L) but slightly less (72.90?±?3.66?mg/L) than both the standards in ABTS. Linoleic (aerial 53.9%, corm 43.9%) and palmitic (aerial 22.2%, corm 18%) were found as the major fatty acids.

Discussion and conclusion Some fractions of C. mathewii showed higher antioxidant activities than the standards. There is a need to explore more about this plant.     

Antidiabetic,antilipidemic, and antioxidant activities of Gouania longipetala methanol leaf extract in alloxan-induced diabetic rats

Abstract

Context: Gouania longipetala Hemsl. (Rhamnaceae) is used in folkloric medicine for treating diabetes mellitus and its associated symptoms.

Objective: This study evaluated the antidiabetic antilipidemic and antioxidant activities of the plant methanol leaf extract.

Materials and methods: Diabetes was induced in rats by intraperitoneal injection of alloxan monohydrate (160?mg/kg). Three test doses (50, 100, and 150?mg/kg) of G. longipetala extract (GLE) were administered orally and the effects were compared with glibenclamide (2?mg/kg). The effect of GLE on hyperglycemia and sub-acute study for 21?d were carried out using its effect on fasting blood sugar (FBS) level. Serum biochemistry and antioxidant activity were evaluated. Histopathological evaluation of the pancreas was also done.

Results: The LD₅₀ of G. longipetala was found to be >4000?mg/kg. The extract significantly (p?<?0.0001) decreased the FBS levels of treated rats from 16.2?±?2.03 to 6.5?±?1.52?mM/L at 150?mg/kg within 24?h. The extract decreased FBS levels of rats by 62.0, 74.8, and 75.0% on day 21 at 50, 100, and 150?mg/kg, respectively. GLE reduced the level of malondiadehyde from 23.0?±?1.34?to 10.3?±?0.43?mg/dL, increased superoxide dismutase activities from 2.97?±?0.34 to 5.80?±?0.53?IU/L at 150?mg/kg, and improved the serum lipid profile of treated rats. GLE also caused restoration of the altered histopathological changes of the pancreas.

Discussion and conclusion: Gouania longipetala demonstrated significant antidiabetic, antilipidemic, and antioxidant activities that may be due to its multiple effects involving both pancreatic and extra-pancreatic mechanisms.     

Azadirachta indica extract–artesunic acid combination produces an increased cure rate of Plasmodium berghei-infected mice

Context: Available artemisinin-combination therapies (ACTs) are expensive. Various traditional herbal remedies for malaria involve plants, proven scientifically to have antiplasmodial effects, e.g., Azadirachta indica A. Juss. (Meliaceae).

Objective: Combination of an artemisinin-based compound and a medicinal herb extract will provide an indigenous alternative/herb-based ACT.

Materials and methods: The in vivo schizontocidal activity of the crude aqueous extract of 100, 500, and 1000?mg/kg of A. indica fresh leaves (NCE) and 6, 15, and 20?mg/kg of artesunic acid were determined, alone and in combination, while keeping the dose of artesunic acid constant at 15?mg/kg, using the Peter’s 4-day suppressive test and Swiss albino mice. The ED₅₀ was calculated from the dose-response relationships. Percentage survival and cure were also determined.

Results: The average yield of two extractions of NCE was 8.33?±?1.67%. Combination of 1000?mg/kg of NCE and 15?mg/kg of artesunic acid, produced a significant reduction of parasitemia (96.87%), compared to 20?mg/kg of artesunic acid alone (68.14%). The combination had an ED₅₀ of 0.58?mg/kg while that of artesunic acid alone was 8.814?mg/kg. The combinations of NCE with artesunic acid produced a cure, although the artesunic acid did not produce a cure in 30?d.

Discussion: NCE increased the activity of artesunic acid in terms of reduction in parasitemia, and increased survival time and cure rate.

Conclusion: The combination of an artemisinin and aqueous extract of neem leaf is possible, providing a potentiated reduction of parasitemia, and increased cure rate.