Extracts of Bolivian plants,Copaifera reticulata and Heisteria pallida inhibit in vitro free radical-mediated DNA damage

The presence of different extracts of antiinflammatory plants Copaifera reticulata and Heisteria pallida in a reaction medium containing calf thymus DNA in a free radical generating system protected DNA against oxidative damage in terms of deoxyribose oxidation. The highest antioxidant activity was obtained using the methanol extract of C. reticulata (IC₅₀=3 μg/mL), followed by the aqueous extracts of H. pallida (IC₅₀=257 μg/mL) and C. reticulata (IC₅₀=380 μg/mL). Both dichloromethane extracts and the methanol extract of H. pallida showed a decreased antioxidant activity at higher concentrations. These results suggest that these extracts are capable of suppressing the in vitro oxidative degradation of DNA. © 1997 John Wiley & Sons, Ltd.     

Antiviral activity in vitro of Cupressus sempervirens on two human retroviruses HIV and HTLV

A proanthocyanidin polymer fraction (MW 1500–2000 daltons) from Cupressus sempervirens L. (Cupressaceae) exhibited true antiviral activity in vitro against two retroviruses, HIV and HTLV III B. In comparison with AZT no toxicity was observed with PPC at concentrations of 50 μg/mL which exceeded the IC₅₀ values (1.5 to 15 μg/mL for HIV and 5 to 25 μg/mL for HTLV). © 1998 John Wiley & Sons, Ltd.     

In Vitro activities of plant extracts from Saudi Arabia against malaria,leishmaniasis, sleeping sickness and Chagas disease

The in vitro activity of the methanol extracts of 51 plants randomly collected from the Kingdom of Saudi Arabia and some of their fractions (petroleum ether, chloroform, ethyl acetate and aqueous) were evaluated against Plasmodium falciparum, Trypanosoma brucei brucei, T. cruzi and Leishmania infantum, as well as toxicity against MRC‐5 fibroblast cells. Ten crude methanolic extracts that demonstrated potent and adequately selective antiprotozoal activity were subjected to solvent fractionation using petroleum ether, ethyl acetate and chloroform. Only three samples showed promising antiprotozoal activity. Argemone ochroleuca (CHCl₃ fraction) showed pronounced activity against P. falciparum_GHA (IC₅₀ 0.32 μg/mL) and T. cruzi (IC₅₀ 0.30 μg/mL) with low cytotoxicity against MRC‐5 cells (CC₅₀ 11.6 μg/mL). Capparis spinosa (EtOAc fraction) showed pronounced activity against P. falciparum_GHA with an IC₅₀ 0.50 μg/mL in the absence of toxicity against MRC‐5 cell line (CC₅₀ > 30 μg/mL). Heliotropium curassavicum (CHCl₃ fraction) showed similar activity against P. falciparum (IC₅₀ 0.65 μg/mL; MRC‐5 CC₅₀ > 30 μg /mL). These three extracts will be subjected for further extensive studies to isolate and identify their active constituents. Copyright © 2010 John Wiley & Sons, Ltd.     

Evaluation of Turkish seaweeds for antiprotozoal, antimycobacterial and cytotoxic activities

As part of our continuing research on seaweeds, crude MeOH extracts of two green, three brown and six red algae collected from Marmara, Black, Aegean and Mediterranean Seas were screened. Four parasitic protozoa, i.e. Plasmodium falciparum, Trypanosoma brucei rhodesiense, T. cruzi, Leishmania donovani and the tubercle bacillus Mycobacterium tuberculosis were used as test organisms for the in vitro assays. The selective toxicity of the extracts was also determined against mammalian L6 cells. All seaweed extracts were active against T. brucei rhodesiense; the Dasya pedicellata extract was the most potent (IC₅₀ value 0.37 µg/mL). The same extract also weakly inhibited the growth of T. cruzi (IC₅₀ 62.02 µg/mL). All seaweed extracts also showed leishmanicidal activity (IC₅₀ values 16.76–69.98 µg/mL). The majority of the extracts also exhibited antiplasmodial potential and the most potent extracts were those from D. pedicellata (IC₅₀ 0.38 µg/mL), Codium bursa (IC₅₀ 1.38 µg/mL) and Caulerpa rasemosa (IC₅₀ 3.12 µg/mL). One brown and two red algal extracts showed some weak activity against Mycobacterium tuberculosis (MIC values 125–256 µg/mL). Except for the extract of Dasya pedicellata, none of the extracts displayed any cytotoxicity. This is the second study investigating the antiprotozoal activities of Turkish marine algae and identifies Dasya pedicellata, an understudied algal species, as a candidate for further studies. Copyright © 2010 John Wiley & Sons, Ltd.     

Screening of medicinal plants from Iranian traditional medicine for acetylcholinesterase inhibition

To find new herbal compounds with an acetylcholinesterase (AChE) inhibitory effect, this study focused on herbal drugs and resins which have been used in Iranian traditional medicine for the treatment of cognitive disorders. Forty drugs were selected from authoritative written documents of Iranian traditional medicine. Each drug was extracted by accelerated solvent extraction using dichloromethane followed by methanol. The 80 extracts were screened for AChE inhibitory activity by a TLC bioautography method. The inhibiting effect of the 32 most active extracts was measured by a microplate colorimetric assay. Due to the best activity, the seeds of Peganum harmala L. were investigated in detail. From the TLC bioautography assay the alkaloids harmaline and harmine were identified as active compounds. This result was confirmed by means of HPLC‐DAD. The IC₅₀ values were 41.2 μg/mL for the methanol extract, 95.5 μg/mL for the dichloromethane extract, 8.4 μg/mL for harmaline and 10.9 μg/mL for harmine. The concentrations of active compounds in the extracts were determined by a fast and precise HPLC method. As the amounts of harmaline and harmine in the extracts were correlated with the IC₅₀ values of the extracts, it can be concluded that these two alkaloids are responsible for the AChE inhibitory activity of P. harmala. Copyright © 2011 John Wiley & Sons, Ltd.     

Antiviral activity of daphnoretin isolated from Wikstroemia indica

The ethanol extract of Wikstroemia indica was fractionated with organic solvents of different polarities, and various fractions were screened for their antiviral activity against respiratory syncytial virus (RSV) using a cytopathic effect (CPE) reduction assay. The ethyl acetate fraction was most active against RSV with 50% inhibition concentration (IC₅₀) value < 3.9 μg/mL and a selectivity index (SI) > 64.1. Further isolation and purification of the fraction led to a purified compound, daphnoretin. Daphnoretin was tested for its anti‐RSV activity using a plaque reduction assay and found active against RSV, with an IC₅₀ value of 5.87 μg/mL and SI value of 28.17. The mode of antiviral action study revealed that daphnoretin could slightly inhibit the early events of the viral infection but its effect was mainly on the later phase of the replication cycle. Copyright © 2009 John Wiley & Sons, Ltd.     

Antimycobacterial,antiprotozoal and cytotoxic potential of twenty‐one brown algae (phaeophyceae) from British and Irish waters

In the continuation of our research on seaweeds, crude extracts of 21 brown algae collected from the south coast of England and the west coast of Ireland were screened for in vitro trypanocidal, leishmanicidal and antimycobacterial activities. Mammalian stages of a small set of parasitic protozoa; i.e. Trypanosoma brucei rhodesiense, T. cruzi and Leishmania donovani, and the tubercle bacillus Mycobacterium tuberculosis were used as test organisms. The extracts were also evaluated for selectivity by testing on a mammalian cell line (L6 cells). Only four extracts were moderately active against T. cruzi, whereas all algal extracts showed significant activity against T. brucei rhodesiense, with Halidrys siliquosa and Bifurcaria bifurcata (Sargassaceae) being the most potent (IC₅₀ values 1.2 and 1.9 μg/mL). All algal extracts also displayed leishmanicidal activity, with H. siliquosa and B. bifurcata again being the most active (IC₅₀s 6.4 and 8.6 μg/mL). When tested against M. tuberculosis, only the B. bifurcata extract was found to have some antitubercular potential (MIC value 64.0 μg/mL). Only three seaweed extracts, i.e. H. siliquosa, B. bifurcata and Cystoseira tamariscifolia showed some cytotoxicity. To our knowledge, this is the first study on the antiprotozoal and antimycobacterial activity of brown algae from British and Irish waters. Copyright © 2010 John Wiley & Sons, Ltd.     

Antiprotozoal,antimycobacterial and cytotoxic potential of twenty‐three British and Irish red algae

As part of our continuing research on seaweeds, we have screened the crude extracts of 23 red marine algae collected from England and Ireland. The clinically important blood‐stage life forms of Trypanosoma brucei rhodesiense, T. cruzi, Leishmania donovani and Mycobacterium tuberculosis were used as test organisms in the in vitro assays. The selectivity of the extracts was determined by using mammalian skeletal myoblast (L6) cells. All algal extracts showed activity against T. brucei rhodesiense, with Corallina officinalis and Ceramium virgatum being the most potent (IC₅₀ values 4.8 and 5.4 μg/ml), whilst none of the algal extracts inhibited the growth of T. cruzi. Except for Porphyra leucosticta, extracts from all seaweeds also showed leishmanicidal activity with IC₅₀ values ranging from 16.5 to 85.6 μg/ml. Only the crude extract of Calliblepharis jubata showed some weak activity against Mycobacterium tuberculosis (MIC value 256 μg/ml), while the others were inactive at this concentration. Corallina officinalis was the only seaweed that displayed some marginal cytotoxicity (IC₅₀ value 88.6 μg/ml), and all remaining extracts were non‐toxic towards L6 cells at 90 μg/ml concentration. To our knowledge, this is the first study reporting antiprotozoal and antimycobacterial activity of British and Irish red algae. Copyright © 2010 John Wiley & Sons, Ltd.     

Antioxidant activity of yellow dock (Rumex crispus L., Polygonaceae) fruit extract

The methanol extract of ripe Rumex crispus L. fruits was evaluated for its antioxidant potential by assays for ferric‐reducing antioxidant power (FRAP), DPPH‐free radical scavenging activity (DPPH) and the influence on lipid peroxidation in liposomes (LP). Considerable activity was observed in all test systems (FRAP: 9.9 mmol Fe²⁺/g; DPPH IC₅₀: 3.7 μg/mL; LP IC₅₀: 4.9 μg/mL), comparable to that of BHT (FRAP: 8.0 μg/mL; DPPH IC₅₀: 19.4 μg/mL; LP IC₅₀: 3.5 μg/mL), but lower than the activity of ascorbic acid, rutin and quercetin, used as positive control substances. The in vivo effects were evaluated in several hepatic antioxidant systems (activities of LPx, GSH‐Px, Px, CAT and XOD, as well as GSH content), after treatment with the studied yellow dock extract in different doses, or in combination with carbon tetrachloride (CCl₄). Pretreatment with the R. crispus extract inhibited CCl₄‐induced oxidative stress by decreasing LPx and increasing GSH content in a dose dependent manner, bringing the levels of antioxidant enzymes to near control values. Copyright © 2010 John Wiley & Sons, Ltd.     

Antimalarial activity and cytotoxicity of Ficus pyrifolia and Rhus (=Baronia) taratana leaf extracts

Ethanolic leaf extracts of Ficus pyrifolia (Moraceae) and Rhus(= Baronia) taratana (Anacardiaccae), said to possess antimalarial effects in traditional herbal medicines, were tested against Plasmodium falciparum in vitro using an isotropic semi-microtest and in vivo in the 4 day suppressive test in Plasmodium berghei infected mice. Although the in vitro test showed moderate or low activity (IC₅₀ = 18 μg/mL and 80 μg/mL, respectively), the in vivo bioassays demonstrated significant activity with 67%, 52% and 48% suppression of parasitaemia with 80, 320, 2.5 mg/kg day^?1 of Ficus pyrifolia, Rhus taratana and chloroquine, respectively. The two plant extracts showed low cytotoxicity.     

Proanthocyanidin-enriched extract from Myrothamnus flabellifolia Welw. exerts antiviral activity against herpes simplex virus type 1 by inhibition of viral adsorption and penetration

Aim of the study

Extracts from the aerial parts of the South African resurrection plant Myrothamnus flabellifolia Welw. have been used traditionally against infections of the upper respiratory tract and skin diseases. A polyphenol-enriched extract was investigated for potential antiviral effects against herpes simplex virus type 1 (HSV-1) and adenovirus, and the underlying mode of action was to be studied.

Materials and methods

Antiviral effects of an acetone-water extract (MF) from Myrothamnus flabellifolia on HSV-1 and adenovirus type 3 were tested in infected Vero cells by plaque reduction assay, MTT test and immunofluorescence. The influence of the extract on the HSV-1 envelope glycoprotein D was shown by Western blot. Organotypic full thickness skin models consisting of multilayer skin equivalents were used for the investigation of MF effects on HSV-1 replication.

Results

MF exhibited strong antiviral activity against HSV-1. The HSV-1-specific inhibitory concentration (IC₅₀) was determined as 0.4 μg/mL and the cytotoxic concentration (CC₅₀) against Vero cells as 50 μg/mL. A selectivity index (SI) (ratio of CC₅₀ to IC₅₀) of approximately 120 was calculated when MF was added to the virus inoculum for 1 h at 37 °C prior to infection. The replication of adenovirus 3 was not affected by MF.MF abolished virus entry into the host cell by blocking viral attachment to the cell surface. When added after attachment at a concentration of >6 μg/mL, the extract also inhibited penetration of HSV-1 into the host cell. Polyphenolic compounds from MF directly interacted with viral particles, leading to the oligomerisation of envelope proteins as demonstrated for the essential viral glycoprotein D (gD). Using organotypic full thickness tissue cultures, it was shown that treatment of HSV-1 infected cultures with the MF resulted in reduced viral spread.

Conclusions

A polyphenol-enriched extract from Myrothamnus flabellifolia strongly acts against HSV-1 by blocking viral entry into the cells.     

Antihyperlipidemic Components of Cassia auriculata Aerial Parts: Identification Through In Vitro Studies

Cassia auriculata (Caesalpiniaceae) is a common Asian beverage and medicinal plant widely used in tradition medicine for diabetes, hyperlipidemia and various other disease conditions. Previous studies on crude extracts of C. auriculata have documented the scientific basis for some of its traditional medicinal uses. The present study investigates the antilipase activity of the ethanol extract of the aerial parts along with the previously isolated compounds (kaempferol‐3‐O‐rutinoside, rutin, kaempferol, quercetin and luteolin). The crude extract displayed inhibitory activity against pancreatic lipase with IC₅₀ of 6.0 ± 1.0 µg/mL. The most active antilipase compound was kaempferol‐3‐O‐rutinoside with IC₅₀ value (2.9 ± 0.50 μM) only about twice weaker than the standard antilipase drug, orlistat (IC₅₀ = 1.45 ± 0.26 μM). Luteolin, quercetin and rutin were found to be weak pancreatic lipase inhibitors (IC₅₀ over 100 μM), whereas kaempferol showed no activity up to 250 μM. The antihyperlipidemic effect of C. auriculata could be attributed to direct lipase inhibitory effect of the plant constituents. Copyright © 2012 John Wiley & Sons, Ltd.     

Screening of New Zealand Plant Extracts for Inhibitory Activity Against HIV-1 Protease

231 Ethanol/aqueous extracts from New Zealand plants were screened for inhibitory activity against HIV-1 protease using fluorogenic and HPLC assays. Among the examined extracts, Pseudotsuga menziesii , Elaeocarpus hookerianus , Pernettya macrostigma and Cassinia leptophylla showed significant inhibition at a concentration of 50 μg/mL in the HPLC confirmation assay. The IC₅₀ values of these extracts to HIV-1 protease on its synthetic peptide substrate were 9.63, 9.74, 27.62 and 60.73 μg/mL, respectively. The derivatives of dihydroquercetin and [5′5′]-bisdihydroquercetin from Pseudotsuga menziesii could be the causative compounds for the inhibition.     

Compounds with tyrosinase inhibition, elastase inhibition and DPPH radical scavenging activities from the branches of Distylium racemosum Sieb. et Zucc

Twenty compounds were isolated from the ethanol extract of Distylium racemosum branches and their inhibitory activities on tyrosinase, elastase and free radicals evaluated. The isolated compounds were identified as dibenzofurans (1–4), abscisic acid (5), 6′‐O‐galloylsalidroside (6), catechin derivatives (7–11), gallic acid derivatives (12–14), tyrosol (15), flavonoids (16–18), lupeol (19) and 1,2,3,6‐tetragalloylglucose (20). For study of tyrosinase inhibition activities, when compared with arbutin (IC₅₀ 48.8 μg/mL), four compounds (8, 11, 13, 17) showed higher activities, with IC₅₀ values of 4.8, 30.2, 40.5 and 37.7 μg/mL, respectively. For the elastase inhibition test, dibenzofuran 1 showed greater activity than the positive control, oleanolic acid (IC₅₀ 9.7 μg/mL), with an IC₅₀ of 7.7 μg/mL. In the studies on DPPH radical scavenging activities, five compounds (11, 12, 13, 14, 15) showed higher activities than ascorbic acid (IC₅₀ 5.0 μg/mL), with IC₅₀ values of 4.6, 3.9, 2.9, 3.8 and 4.7 μg/mL, respectively. Copyright © 2011 John Wiley & Sons, Ltd.     

Screening of some Tanzanian medicinal plants for their trypanocidal and cytotoxic activities

The objective of the present study was to evaluate in vitro antitrypanosomal and cytotoxic activities of crude extracts of 20 traditionally used medicinal plants of Tanzania. A total of 40 extracts (dichloromethane and methanol) were screened for antiproliferative activity of bloodstream form of T. b. brucei and human leukaemia HL‐60 cell. Inhibition of cell proliferation was assessed using resazurin as vital stain. Of the 40 extracts tested, the dichloromethane extract from bark of Warburgia salutaris (Canellaceae) exhibited the most potent antitrypanosomal activity with an IC₅₀ value of 10.68 μg/ml. A dichloromethane extract from Lannea stuhlmannii (Anacardiaceae) was found to be the most cytotoxic extract against HL‐60 (IC₅₀ = 27.15 μg/ml). Out of the 20 plants tested, 5 plants exhibited trypanocidal activity with IC₅₀ values below 20 μg/ml. These 5 plants: Entandrophragma bussei (Meliaceae), Securidaca longepedunculata (Polygalaceae), Warburgia salutaris (Canellaceae), Zanha africana (Sapindaceae) and Zanthoxylum chalybeum (Rutaceae) could therefore serve as sources of lead compounds for treatment of trypanosomiasis. Copyright © 2009 John Wiley & Sons, Ltd.     

Inhibition of keratinocyte growth by different Nepalese Zanthoxylum species

A total of 11 methanol extracts obtained from four different Nepalese Zanthoxylum species were screened for their antiproliferative activity against the growth of human keratinocytes (HaCaT cells). The extract obtained from Z. armatum barks was highly active with an IC₅₀ value of 11 µg/mL. Also, the extracts ­obtained from Z. oxyphyllum barks and roots with IC₅₀ values of 53 and 57 µg/mL, respectively, showed potent activity. Their antiproliferative activity was not due to cytotoxic effects on cell membranes, as documented by the activity of lactate dehydrogenase released from the cytoplasm of keratinocytes, which did not exceed that of the control value. Rather, they also protected against radical‐induced ­damage to model membranes stimulated with 2,2′‐azo‐bis(2‐amidinopropane) dihydrochloride. Copyright © 1999 John Wiley & Sons, Ltd.     

Antiherpetic Activity of S1, an Algal Derived Sulphated Galactan

The sulphated galactan S1 isolated from the red seaweed Pterocladia capillacea proved to be a selective antiviral compound against herpes simplex virus types 1 and 2 (HSV-1 and HSV-2), human cytomegalovirus and pseudorabies virus. No cytotoxicity was observed with S1 at concentrations about 500 γ g/mL that were in excess of the IC₅₀ values (range from 3.2 to 12.0 γg/mL for the different herpesviruses assayed). The antiherpetic action of S1 was independent of the host cell and the antiviral assay. The kinetics of infectious virus adsorption to the host cell was highly inhibited in the presence of S1 whereas the subsequent stage of virus penetration was not affected. The binding of radiolabelled HSV-1 particles was inhibited in a dose dependent manner confirming that the mode of action of S1 could be attributable to an inhibition of initial virus attachment to the host cell.     

The Immunosuppressive Effects of Globularia alypum Extracts

Responder lymphocytes were cultured with an equal number of irradiated stimulator lymphocytes from another donor for 6 days in RPMI 1640 (a modified Mc Coh's 5 A Medium). After 48 h incubation with PMA (phorbol 12-myristate), PHA (phytohaematogglutin) and 120 h with MLR (mixed lymphocytes reaction), the cells were labelled with ³H-thymidine. Cells were harvested in a scintillation counter Globularia alypum L. extracts were dissolved in HPLC quality ethanol or water and diluted in RPMI to concentrations ranging from 0.156–10 μg/mL. Extract solutions were added immediately after cell stimulation in the cell walls. Cyclosporin A was used as a control. Both the water and ethanol extracts of Globularia alypum L. demonstrated a dose response effect in all three systems of MLR, PHA and PMA with no statistical difference in water or ethanol extracts. The IC₅₀ were: PHA 1.14 μg/mL, PMA 1.05 μg/mL and MLR 2.06 μg/mL. The PHA and MLR IC₅₀ are approximately double the IC₅₀ for cyclosporin A (0.5 μg/mL). The effects of Glubularia alypum L. in PMA stimulated lymphocytes suggests it may suppress T cell function through a pathway that cyclosporin A does not effect.     

Antiprotozoal,antimycobacterial and cytotoxic potential of some british green algae

In the continuation of our search for natural sources for antiprotozoal and antitubercular molecules, we have screened the crude extracts of four green marine algae (Cladophora rupestris, Codium fragile ssp. tomentosoides, Ulva intestinalis and Ulva lactuca) collected from the Dorset area of England. Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani and Mycobacterium tuberculosis were used as test organisms in the in vitro assays. The selective toxicity of the extracts was also determined toward mammalian skeletal myoblast (L6) cells. The crude seaweed extracts had no activity against M. tuberculosis, but showed antiprotozoal activity against at least two protozoan species. All algal extracts were active against T. brucei rhodesiense, with C. rupestris being the most potent one (IC₅₀ value 3.7 μg/ml), whilst only C. rupestris and U. lactuca had moderate trypanocidal activity against T. cruzi (IC₅₀ values 80.8 and 34.9 μg/ml). Again, all four extracts showed leishmanicidal activity with IC₅₀ values ranging between 12.0 and 20.2 μg/ml. None of the extracts showed cytotoxicity toward L6 cells, indicating that their antiprotozoal activity is specific. This is the first study reporting antiprotozoal and antimycobacterial activity of British marine algae. Copyright © 2009 John Wiley & Sons, Ltd.     

Medicinal Plants Traditionally Used for Treatment of Obesity and Diabetes Mellitus – Screening for Pancreatic Lipase and α‐Amylase Inhibition

In order to find new pancreatic lipase (PL) and α‐amylase inhibitors from natural sources for the treatment of obesity and related diseases as diabetes mellitus II, 23 medicinal plants with weight‐reducing, serum glucose‐reducing or related potential were investigated. Methanolic and water extracts of the plants were evaluated by using two in vitro test systems. Our findings have shown that the methanolic extract of Hibiscus sabdariffa L. (Malvaceae) showed high inhibitory activities to PL (IC₅₀: 35.8 ± 0.8 µg/mL) and α‐amylase (IC₅₀: 29.3 ± 0.5 µg/mL). Furthermore, the methanolic extract of Tamarindus indica L. (Leguminosae) showed a high anti‐lipase (IC₅₀: 152.0 ± 7.0 µg/mL) and the aqueous extract a high anti‐amylase (IC₅₀: 139.4 ± 9.0 µg/mL) activity. This work provides a priority list of interesting plants for further study with respect to the treatment of obesity and associated diseases. Copyright © 2015 John Wiley & Sons, Ltd.