Median lethal dose, antimalarial activity, phytochemical screening and radical scavenging of methanolic Languas galanga rhizome extract

The methanolic extract of Languas galanga rhizomes was investigated for antimalarial activity against Plasmodium berghei (NK65) infections in mice. The median lethal dose was determined to ascertain the safety of the extract in ICR mice of both sexes. The antimalarial activities during early and established infections, as well as the prophylactic activity were evaluated. Phytochemical screening and radical scavenging activity of the extract were also investigated to elucidate the possible mechanism of the antimalarial properties. The acute oral toxicity (LD??) of Languas galanga extract in mice was established to be 4.998 mg/kg. The extract of Languas galanga rhizomes demonstrated significant antiplasmodial activity in all the three models of the antimalarial evaluations. Phytochemical screening revealed the presence of some vital antiplasmodial constituents such as terpenoids and flavonoids. The extract also exhibited a moderate capacity to scavenge the free radicals. The rhizome extract of Languas galanga thus possesses antimalarial activity, which explains the rational usage of this plant in traditional Malaysian medicine.     

Profiling of Piper betle Linn. cultivars by direct analysis in real time mass spectrometric technique

Piper betle Linn. is a traditional plant associated with the Asian and southeast Asian cultures. Its use is also recorded in folk medicines in these regions. Several of its medicinal properties have recently been proven. Phytochemical analysis showed the presence of mainly terpenes and phenols in betel leaves. These constituents vary in the different cultivars of Piper betle. In this paper we have attempted to profile eight locally available betel cultivars using the recently developed mass spectral ionization technique of direct analysis in real time (DART). Principal component analysis has also been employed to analyze the DART MS data of these betel cultivars. The results show that the cultivars of Piper betle could be differentiated using DART MS data.     

Biological activities of Peristrophe bivalvis extracts: promising potential for anti-snake venoms against Naja kaouthia and Trimeresurus albolabris venoms

This study evaluates the in vitro anti-snake venom potential of Peristrophe bivalvis (PB) extracts against Naja kaouthia (NK) and Trimeresurus albolabris (TA) venoms, including inhibition of cytotoxic effects and enzymatic activities, and the binding-precipitation of extracts and venom proteins analysis. In addition, the antioxidant, cytotoxic and in vivo acute oral toxic activities of PB extracts are also reported. The in vitro cytotoxic and enzymatic analysis reveals that the ethanol extracts of stems and leaves of PB showed good anti-snake venom activity against NK and TA venoms. In addition, the antioxidant result indicated that only the ethanol extract of leaves exhibited weak DPPH radical-scavenging activity. The ethanol whole-plant extract of PB also showed no cytotoxicity against four cell lines. Moreover, the in vivo acute oral toxicity result of the ethanol whole-plant extract showed that all treated rats did not exhibit abnormal toxic signs or deaths.     

Phytotoxic, antifungal activities and acute toxicity studies of the crude extract and compounds from Diospyros canaliculata

In?vitro biological activities including phytotoxic, antifungal activities as well as acute toxicity of the methanol extract, fractions and/or isolated compounds from the stem bark of Diospyros canaliculata were investigated. Well agar diffusion and macrodilution assays were used for investigating the antifungal activity. A phytotoxicity assay was performed against Lemna minor while an acute toxicity assay was performed in mice via oral administration. As a result, plumbagin (5-hydroxy-2-methyl-1,4-naphtoquinone) and two known pentacyclic triterpenes (lupeol and lupenone) were isolated from the extract. With regards the antifungal activities, the inhibition zones varied from 16.51 to 24.86 mm and from 20.50 to 25.10 mm for the extract and plumbagin, respectively. The minimum inhibitory concentrations of the extract and plumbagin ranged between 12.5-25 and 0.78-1.56 μg mL(-1), respectively. At 50 μg mL(-1), the hexane fraction showed phytotoxic activities similar to paraquat, the standard phytotoxic inhibitor. The extract was found to be non-toxic to mice after administration per os. Based on the current findings, we can conclude that this extract is non toxic, with significant phytotoxic and antifungal properties due to the presence of plumbagin.     

Antioxidant capacity and larvicidal and antifungal activities of essential oils and extracts from Piper krukoffii

The leaves and twigs of Piper krukoffii, collected in the Carajás National Forest, north Brazil, yielded essential oils (2.0% and 0.8%), the main constituents of which were myristicin (40.3% and 26.7%), apiole (25.4% and 34.1%) and elemicin (2.8% and 3.0%). The antioxidant activities of the oils, methanol extract and its sub-fractions were evaluated. The DPPH EC50 values varied from the ethyl acetate sub-fraction (73.4 +/- 3.7 microg/mL) to the methanol extract (24.9 +/- 0.8 microg/mL), and the ABTS TEAC values ranged in the same order from 265.7 to 349.2 microMol TE/g. These results indicated a significant antioxidant activity for the plant. The lignans (-)-kusunokin, yatein, (-)-hinokin and cubebin were identified in the methanol extract. The hydro-methanolic sub-fraction showed a high value for total phenol content (106.5 +/- 0.7 mg GAE/g), as well as 1H NMR signals for sugar moieties. Crude extracts and sub-fractions were also able to inhibit beta-carotene bleaching, varying from 22.4 to 47.1%. The oils from the leaves and twigs showed strong larvicidal (21.4 and 3.6 microg/mL) and fungicide (0.5 and 0.1 microg/mL) activities.     

Antioxidant, antitubercular and cytotoxic activities of Piper imperiale

Phenolic compounds are widely distributed in Nature and act as pharmacologically active constituents in many herbal medicines. They have multiple biological properties, most notably antioxidant, antibacterial and cytotoxic activities. In the present study an attempt to correlate the phenolic composition of leaf, flower and wood extracts of Piper imperiale, with antioxidant, antitubercular and cytotoxic activities was undertaken. The total phenol content ranged from 1.98 to 6.94 mg GAE/gDW among ethanolic extracts, and gallic acid, catechin, epicatechin, ferulic acid, resveratrol and quercetin were identified and quantified by HPLC. DPPH and ABTS assays showed high antioxidant activity of the leaf extract (EC(50ABTS) = 15.6 μg/mL, EC(50DPPH) = 27.3 μg/mL) with EC?? in the same order of magnitude as the hydroxyquinone (EC(50ABTS) = 10.2 μg/mL, EC(50DPPH) = 15.7 μg/mL). The flower extract showed strong antimicrobial activity against Mycobacterium tuberculosis H??Rv. All the extracts exhibited dose-dependent cytotoxic effects against MCF-7 cancer cells. This is the first time that a Piper extract has been found to be highly active against M. tuberculosis. This study shows the biological potential of Piper imperiale extracts and gives way to bio-guided studies with well-defined biological activities.     

Urine NMR Metabolomic Study on Biochemical Activities to Investigate the Effect of P. betle Extract on Obese Rats

Applied Biochemistry and Biotechnology - The present studies are to evaluate the ability of PB to induce weight loss and urine metabolite profile of Piper betle L. (PB) leaf extracts using...     

Antioxidant and Anti-Inflammatory Effects of Peganum harmala Extracts: An In Vitro and In Vivo Study

Peganum harmala (P. harmala) belongs to the family Zygophyllaceae, and is utilized in the traditional medicinal systems of Pakistan, China, Morocco, Algeria, and Spain to treat several chronic health disorders. The aim of the present study was to identify the chemical constituents and to evaluate the antioxidant, anti-inflammatory, and toxicity effects of P. harmala extracts both in vitro and in vivo. Sequential crude extracts including 100% dichloromethane, 100% methanol, and 70% aqueous methanol were obtained and their antioxidant and anti-inflammatory effects evaluated both in vitro and in vivo. The anti-inflammatory effect of the extract was investigated using the carrageenan-induced paw edema method in mice, whereas the toxicity of the most active extract was evaluated using an acute and subacute toxicity rat model. In addition, we have used the bioassay-guided approach to obtain potent fractions, using solvent–solvent partitioning and reversed phase high performance liquid chromatography from active crude extracts; identification and quantification of compounds from the active fractions was achieved using electrospray ionization mass spectrometry and high performance liquid chromatography techniques. Results revealed that the 100% methanol extract of P. harmala exhibits significant in vitro antioxidant activity in DPPH assay with an IC₅₀ of 49 µg/mL as compared to the standard quercetin with an IC₅₀ of 25.4 µg/mL. The same extract exhibited 63.0% inhibition against serum albumin denaturation as compared to 97% inhibition by the standard diclofenac sodium in an in vitro anti-inflammatory assay, and in vivo anti-inflammatory against carrageenan-induced paw edema (75.14% inhibition) as compared to 86.1% inhibition caused by the standard indomethacin. Furthermore, this extract was not toxic during a 14 day trial of acute toxicity when given at a dose of 3 g/kg, indicating that the lethal dose (LD₅₀) of P. harmala methanol extract was greater than 3 g/kg. P. harmala methanolic fraction 2 obtained using bioassay-guided fractionation showed the presence of quinic acid, peganine, harmol, harmaline, and harmine, confirmed by electrospray ionization mass spectrometry and quantified using external standards on high performance liquid chromatography. Taken all together, the current investigation further confirms the antioxidant, anti-inflammatory, and safety aspects of P. harmala, which justifies its use in folk medicine.     

Antimicrobial Activity of Green Silver Nanoparticles Synthesized by Different Extracts from the Leaves of Saudi Palm Tree (Phoenix Dactylifera L.)

The Arabian desert is rich in different species of medicinal plants, which approved variable antimicrobial activities. Phoenix dactylifera L. is one of the medical trees rich in phenolic acids and flavonoids. The current study aimed to assess the antibacterial and antifungal properties of the silver nanoparticles (AgNPs) green-synthesized by two preparations (ethanolic and water extracts) from palm leaves. The characteristics of the produced AgNPs were tested by UV-visible spectroscopy and Transmitted Electron Microscopy (TEM). The antifungal activity of Phoenix dactylifera L. was tested against different species of Candida. Moreover, its antibacterial activity was evaluated against two Gram-positive and two Gram-negative strains. The results showed that AgNPs had a spherical larger shape than the crude extracts. AgNPs, from both preparations, had significant antimicrobial effects. The water extract had slightly higher antimicrobial activity than the ethanolic extract, as it induced more inhibitory effects against all species. That suggests the possible use of palm leaf extracts against different pathogenic bacteria and fungi instead of chemical compounds, which had economic and health benefits.     

Polarity Directed Appraisal of Pharmacological Potential and HPLC-DAD Based Phytochemical Profiling of Polygonum glabrum Willd

The present study was designed to evaluate polarity-dependent extraction efficiency and pharmacological profiling of Polygonum glabrum Willd. Crude extracts of leaves, roots, stems, and seeds, prepared from solvents of varying polarities, were subjected to phytochemical, antioxidant, antibacterial, antifungal, antidiabetic, and cytotoxicity assays. Maximum extraction yield (20.0% w/w) was observed in the case of an acetone:methanol (AC:M) root extract. Distilled water:methanol (W:M) leaves extract showed maximum phenolic contents. Maximum flavonoid content and free radical scavenging potential were found in methanolic (M) seed extract. HPLC-DAD quantification displayed the manifestation of substantial quantities of quercetin, rutin, gallic acid, quercetin, catechin, and kaempferol in various extracts. The highest ascorbic acid equivalent total antioxidant capacity and reducing power potential was found in distilled water roots and W:M leaf extracts, respectively. Chloroform (C) seeds extract produced a maximum zone of inhibition against Salmonella typhimurium. Promising protein kinase inhibition and antifungal activity against Mucor sp. were demonstrated by C leaf extract. AC:M leaves extract exhibited significant cytotoxic capability against brine shrimp larvae and α-amylase inhibition. Present results suggest that the nature of pharmacological responses depends upon the polarity of extraction solvents and parts of the plant used. P. glabrum can be considered as a potential candidate for the isolation of bioactive compounds with profound therapeutic importance.     

Antimicrobial activity of Piper gaudichaudianum Kuntze and its synergism with different antibiotics

One of the oldest forms of medical practice is the use of plants for the treatment and prevention of diseases that affect humans. We have studied the antimicrobial activity and synergism of Piper gaudichaudianum Kuntze with different antibiotics. The crude extract from the leaves of P. gaudichaudianum was submitted to chromatographic separation, resulting in five fractions. Fraction F3 contained a chromone (2,2-dimethyl-6-carboxycroman-4-one), and fraction F2 contained isomers that are prenylated derivatives of benzoic acid [4-hydroxy-(3',7'-dimethyl-1'-oxo-octa-E-2'-6'-dienyl)benzoic acid and 4-hydroxy-(3',7'-dimethyl-1'-oxo-octa-2'-Z-6'-dienyl) benzoic acid]. The chemical structures of both compounds were determined by analysis of 1H-NMR, 13C-NMR, COZY, DEPT, HMQC, and HMBC spectral data, and by comparison with data in the literature. The crude extract, fraction F2, and fraction F3 showed good activity against Staphylococcus aureus, Bacillus subtilis, and Candida tropicalis. The two benzoic acid derivatives only showed activity against S. aureus and B. subtilis. The bioauthographic analysis showed an inhibition zone only in fraction F2. Fractions F2 and F3 showed synergism in combination with ceftriaxone, tetracycline, and vancomycin. Morphological changes in form and structure were found by scanning electron microscopy in S. aureus treated with the combination of fraction F2 with vancomycin.     

Antioxidant and toxicological evaluation of a Tamarindus indica L. leaf fluid extract

In the scientific community, there is a growing interest in Tamarindus indica L. leaves, both as a valuable nutrient and as a functional food. This paper focuses on exploring its safety and antioxidant properties. A tamarind leaf fluid extract (TFE) wholly characterised was evaluated for its anti-DPPH activity (IC₅₀ = 44.36 μg/mL) and its reducing power activity (IC₅₀ = 60.87 μg/mL). TFE also exhibited a high ferrous ion-chelating capacity, with an estimated binding constant of 1.085 mol L^? 1 while its influence over nitric oxide production in human leucocytes was irregular. At low concentrations, TFE stimulated NO output, but it significantly inhibited it when there was an increase in concentration. TFE was also classified as a non-toxic substance in two toxicity tests: the acute oral toxicity test and the oral mucous irritability test. Further toxicological assays are needed, although results so far suggest that TFE might become a functional dietary supplement.     

Inhibitory potential of Hydroxychavicol on Ehrlich ascites carcinoma model and in silico interaction on cancer targets

Abstract

Hydroxychavicol (HC), a major phenolic derivative isolated from the leaves of Piper betle L. is well known for its antibacterial, antifungal and antimutagenic properties. The present study evaluated the in vivo antitumor activity of HC against Ehrlich Ascites Carcinoma (EAC) cells in Swiss albino mice and in silico interaction of HC with the receptors involved in the cancer. Hydroxychavicol (200 and 400?mg/kg bw) was orally administered for 21 consecutive days and was effective in inhibiting the tumor growth in ascitic mouse model. HC consistently reduced the tumor volume, viable cell count, lipid peroxidation and elevated the life span of HC treated mice. Besides the hematological profiles, SGOT and SGPT levels reverted back to normal and oxidative stress markers GSH, SOD and CAT also increased in HC treated groups. In silico docking analysis revealed that HC possessed potent antagonist activity against all the cancer targets demonstrating its inhibitory activity.     

Chemical composition, anti-inflammatory, molluscicidal and free-radical scavenging activities of the leaves of Ficus radicans 'Variegata' (Moraceae)

The methanol crude extract of the leaves of Ficus radicans Roxb. 'Variegata' (Moraceae) and the n-hexane, ethyl acetate and aqueous methanol fractions resulting from its fractionation were evaluated for their anti-inflammatory, molluscicidal and free-radical scavenging activities. The crude extract and fractions exhibited significant inhibition of inflammation in both croton oil (CO)-induced ear oedema in mice (p<0.001) and carrageenan-induced rat paw oedema models (p<0.01). The molluscicidal assay against Biomphalaria glabrata showed a weak activity for the n-hexane fraction (DL(50)=?400 μg mL(-1)). A moderated 1,1-diphenyl-1-picrylhydrazyl (DPPH) free-radical scavenging activity was observed for the ethyl acetate fraction (IC(50)=?66.2 μg mL(-1)). Fractionation of the extracts through chromatographic methods afforded the coumarins 7-methoxycoumarin, 7-hydroxy-6-methoxycoumarin and methoxy-3,4-dihydrocoumarin, the steroids β-sitosterol and β-sitosterol 3-O-β-glucopyranoside, as well as a cinnamic acid derivative and a flavonoid identified as trans-4-methoxy-2-β-D-glucopyranosyloxy cinnamic acid and quercetin 3-O-β-D-xylopyranosyl-(1?→?2)-α-L-rhamnopyranoside, respectively. The compounds were identified on the basis of their NMR spectral data and comparison with those previously reported in the literature.     

In vitro bioactivity of essential oils and methanol extracts of Salvia reuterana from Iran

The chemical composition of the essential oils, antioxidant activity (DPPH and beta-carotene/linoleic acid assays) and total phenolic content (Foline-Ciocalteu) of the flowers and leaves of Salvia reuterana were determined. Essential oils extracted from the flowers and leaves by hydrodistillation were analyzed by GC and GC/MS. Forty-four constituents, representing 99.7-99.9% of the oils, were identified. The major components were germacrene D, benzoic acid hexyl ester, bicyclogermacrene, beta-gurjunene and ishwarene, constituting 33.7-31.9% of the oils. The highest radical-scavenging activity (DPPH test) was shown by the methanol extract of the flowers (IC50 = 77.6 microg/mL). In the beta-carotene/linoleic acid assay, the methanol extract of the leaves showed the highest inhibition (40.3%) which was only slightly lower than that shown by BHT (82.9%). The total phenolic contents of the methanol extracts of the flowers and leaves as gallic acid equivalents were 81.4 and 88.3 microg/mg, respectively. The plant also showed good antimicrobial activity against three strains of tested microorganisms.     

Antiinflammatory effect of Graptophyllum pictum (L.) Griff

The red leaves of Graptophyllum pictum (L.) Griff. (G. pictum) are used in Indonesian folk medicine. The present study was carried out to elucidate the antiinflammatory effect of the ethanol extract obtained from this crude drug. The extract was partitioned between ether and water, and then the water-soluble fraction was extracted with 1-butanol. The 1-butanol-soluble fraction was extracted with chloroform-acetone, hot methanol and water, successively, and the hot methanol-soluble fraction (fr.) was chromatographed (frs. I-III). The antiinflammatory activity of these fractions was investigated on carrageenin-induced edema in rats and acetic acid-induced vascular permeability as well as the writhing symptom in mice. The ethanol extract (p.o.) showed an antiinflammatory activity as well as an analgesic activity and these activities shifted to the water-soluble fraction, 1-butanol-soluble fraction, methanol-soluble fraction and fr. II, successively. It was found that fr. II contained flavonoids. These results suggest that these flavonoids are at least partly responsible for the antiinflammatory effect of the ethanol extract of G. pictum.     

Studies on differentiation-inducing activities of triterpenes.

Differentiation-inducing activity of over 180 extracts of crude drugs and plants was tested using mouse myeloid leukemia cell line (M1). The methanol extracts of clove (Syzygium aromaticum Merrill et Perry, Myrtaceae) showed remarkable induction of differentiation of M1 cells into macrophage-like cells. From the extract, oleanolic acid (1) and crategolic acid (2) were isolated as the active components. We also tested other triterpenes, such as oleananes, ursanes and dammaranes, to investigate the structure-activity relationship. Some triterpene aglycones showed differentiation-inducing activity, but triterpene glycosides showed little activity. Furthermore, the differentiation-inducing activity of these triterpene compounds was tested against human acute promyelocytic leukemia cell line (HL-60).     

Antiproliferative activity of Luehea candicans Mart. et Zucc. (Tiliaceae)

Luehea candicans Mart. et Zucc. (Tiliaceae) is known as 'a?oita-cavalo' and is one of the most important medicinal plants found in the Brazilian cerrado. The crude methanolic extracts of the branches and leaves and their fractions were evaluated using the following cancer cell lines: MCF-7 (breast), NCI-ADR (breast expressing the multidrug resistance phenotype), NCI-460 (lung), UACC-62 (melanoma), 786-0 (kidney), OVCAR (ovarian), PCO-3 (prostate), HT-29 (colon) and K-562 (leukaemia). The crude methanolic extracts from the branches (B) and leaves (L) were able to inhibit the growth of the K-562 and 786-0 cell lines in a dose-dependent manner, with GI(50) values of 8.1 and 5.4 μg mL(-1), respectively. The hexane (L1), chloroform (L2) and methanol (L4) fractions derived from extract L showed a high selectivity and pronounced cytostatic activity against 786-0 (GI(50) ~ 40 μg mL(-1)). A significant amount of lupeol was isolated from fraction L2. The chloroform (B2) and methanol (B3) fractions derived from extract (B) exhibited less selectivity, showing the highest cytostatic activity against K-562, NCI-ADR, OVCAR, MCF-7 and NCI-460 cells, with GI(50) values between 27 and 40 μg mL(-1). Lupeol, betulin, a mixture of steroids, (-)-epicatechin, vitexin and liriodendrin were isolated from these active fractions.     

Chemical constituents of Piper betle Linn. (Piperaceae) roots

Column chromatography of the alcoholic extract of Piper betle roots furnished aristololactam A-II and a new phenyl propene, characterized as 4-allyl resorcinol, while the petroleum-ether extract yielded a diketosteroid, viz. stigmast-4-en-3,6-dione. All these compounds were characterized by spectroscopic means. Isolation of these compounds from this source is being reported here for the first time.     

Polyphenol contents and antioxidant activity of Brassica nigra (L.) Koch. leaf extract

Profound research has been done on the medicinal value of Brassica nigra (BN) seeds, and the leaves of the plant have been investigated in this study. The methanol extracts of the leaves were subjected to several in?vitro studies. The antioxidant activity of methanol extract was demonstrated with a wide range of concentration, 10-500?μg?mL(-1), and the antioxidant activity increased with the increase in concentration. Total phenol content was found to be 171.73?±?5.043 gallic acid equivalents and the total flavonoid content 7.45?±?0.0945 quercetin equivalents. Further quantification and identification of the compounds were done by HPTLC and GC-MS analyses. The predominant phenolic compounds determined by HPTLC were gallic acid, followed by quercetin, ferulic acid, caffeic acid and rutin. The free radical quenching property of BN leaf extract suggests the presence of bioactive natural compounds.