Effects of Piper longum fruit, Piper sarmentosum root and Quercus infectoria nut gall on caecal amoebiasis in mice

The anti-amoebic effects of crude methanol extracts of Piper longum fruit, Piper sarmentosum root and Quercus infectoria nut gall against Entamoeba histolytica infecting the caecum of mice were studied. Caecal amoebiasis in mice was induced by injection of Entamoeba histolytica trophozoites directly into the caecum. The mice were then treated orally with the extract, a standard drug (metronidazole), or vehicle p.o. for five consecutive days, beginning 24 h after the infection and were examined on the sixth day. At a dose of 1000 mg/kg per day, the extracts of Piper longum fruit, Piper sarmentosum root and Quercus infectoria nut gall had a curative rate of 100, 40 and 26%, respectively. At a concentration of 500 and 250 mg/kg/day, extract from Piper longum fruit was still effective in 93 and 46% of the cases, respectively, while extract from Piper sarmentosum root at a dose of less than 1000 mg/kg per day did not cure any mice from amoebiasis. Extract of Quercus infectoria nut gall at a concentration of 500 and of 250 mg/kg per day cured 26 and 13% of mice, respectively. Metronidazole at a concentration of 125 and of 62.5 mg/kg per day had a curative rate of 100 and 60%, respectively. The severity of caecal wall ulceration was reduced in mice which received the extract and metronidazole as compared to the control animals.     

Screening of selected indigenous plants of Cambodia for antiplasmodial activity

The in vitro antiplasmodial activity of 117 aqueous, methanol and dichloromethane extracts derived from different parts of 28 indigenous wild plant species was studied. These plants are commonly used in Cambodian traditional medicine. The plant extracts were tested for in vitro activity against a chloroquine resistant Plasmodium falciparum strain (W2). Nine extracts were moderately active with IC(50) values ranging between 5 and 10 microg/ml, 17 extracts were active with IC(50) values ranging between 1 and 5 microg/ml. These 26 extracts derived from eight plants belong to six families. The most active extracts were dichloromethane and came from Stephania rotunda and Brucea javanica with IC(50) values of 1 microg/ml and a selectivity index > or = 25. It is interesting to note that some aqueous extracts were as active as dichloromethane extracts especially aqueous extracts of Stephania rotunda, Brucea javanica, Phyllanthus urinaria and Eurycoma longifolia with IC(50) values of < or = 4 microg/ml. These results are in agreement with statements of healers on traditional uses of these plants for the treatment of malaria and/or fever. In this study, we report the antiplasmodial potential activity of eight plant species from Cambodia. Among them four are tested for the first time.     

Inhibitory effects of sudanese medicinal plant extracts on hepatitis C virus (HCV) protease

One hundred fifty-two methanol and water extracts of different parts of 71 plants commonly used in Sudanese traditional medicine were screened for their inhibitory effects on hepatitis C virus (HCV) protease (PR) using in vitro assay methods. Thirty-four extracts showed significant inhibitory activity (>/=60% inhibition at 100 microg/mL). Of these, eight extracts, methanol extracts of Acacia nilotica, Boswellia carterii, Embelia schimperi, Quercus infectoria, Trachyspermum ammi and water extracts of Piper cubeba, Q. infectoria and Syzygium aromaticum, were the most active (>/=90% inhibition at 100 microg/mL). From the E. schimperi extract, two benzoquinones, embelin (I) and 5-O-methylembelin (II), were isolated and found as potent HCV-PR inhibitors with IC(50) values of 21 and 46 microM, respectively. Inhibitory activities of derivatives of I against HCV-PR as well as their effects on other serine proteases were also investigated.Copyright 2000 John Wiley & Sons, Ltd.     

Screening of Indonesian medicinal plant extracts for antibabesial activity and isolation of new quassinoids from Brucea javanica

Boiled extracts derived from 28 Indonesian medicinal plants were screened for their antibabesial activity against Babesia gibsoni in vitro. Of these extracts, the fruit of Brucea javanica was the most active in inhibiting parasite growth at a concentration of 10 microg/mL. Bioassay-guided fractionation of the fruit extract of Br. javanica led to the isolation of two new quassinoids, bruceantinol B and bruceine J, and the structures of these compounds were elucidated on the basis of their spectroscopic data and by chemical transformation to known compounds. In addition, the known quassinoids bruceines A-D, bruceantinol, and yadanziolide A were isolated. Antibabesial activities were also examined in vitro, and bruceine A and bruceantinol were shown to be more potent than diminazene aceturate, a drug (IC50 = 103 ng/mL) used clinically against B. gibsoni, with IC50 values of 4 and 12 ng/mL, respectively.     

Antimicrobial and antioxidant activities of traditional Thai herbal remedies for aphthous ulcers

Four medicinal plants (Quercus infectoria, Kaempferia galanga, Coptis chinensis and Glycyrrhiza uralensis) as well as one traditional Thai treatment for aphthous ulcers based on these four plants were tested for antimicrobial activity. MIC values for a range of bacteria and Candida albicans were determined, with both type strains and clinical isolates being used. Antioxidant activity was determined using the ABTS radical scavenging assay. Among the four plants, Q. infectoria showed antimicrobial activity against Staphylococcus aureus with an MIC of 0.41 mg/mL, while C. chinensis showed antifungal activity against C. albicans with an MIC of 6.25 mg/mL. Activity was also shown against a range of other organisms including Salmonella typhi, Serratia marcescens, Vibrio cholerae, Vibrio parahaemolyticus, Pseudomonas aeruginosa and Enterococcus faecalis. The antimicrobial activity of the traditional aphthous ulcer preparation (a powder) was comparable to that for the individual plant extracts, however, incorporation of the powder into a gel formulation resulted in the loss of almost all activity. All extracts, with the exception of K. galanga, also showed good antioxidant activity. This study supports the traditional use of these plants and suggests that they may also be useful in the treatment of other infections.     

Inhibition of Naja kaouthia venom activities by plant polyphenols

Plant polyphenols from the aqueous extracts of Pentace burmanica, Pithecellobium dulce, Areca catechu and Quercus infectoria were tested for their inhibitory activities against Naja kaouthia (NK) venom by in vitro neutralization method. The first three extracts could completely inhibit the lethality of the venom at 4 LD50 concentration and the venom necrotizing activity at the minimum necrotizing dose while also inhibited up to 90% of the acetylcholinesterase activity of NK venom at much lower tannin concentrations than that of Quercus infectoria. The ED50 of plant tannins in inhibiting NK venom activities varied according to condensed tannins and their content in the extracts. Molecular docking of the complexes between alpha-cobratoxin and either hydrolysable or condensed tannins at their lowest energetic conformations were proposed. The anti-venom activities of these plant polyphenols by selectively blocking the nicotinic acetylcholine receptor and non-selectively by precipitation of the venom proteins were suggested.     

Quercus infectoria: a candidate for the control of methicillin-resistant Staphylococcus aureus infections

Acetone, ethyl acetate, 95% ethanol and aqueous extracts of Quercus infectoria (Q. infectoria) demonstrated significant antibacterial activities against all strains of methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-susceptible Staphylococcus aureus (MSSA). Inhibition zones were in the range 11.75-16.82 mm. Both MRSA and MSSA strains exhibited minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values at 0.13 and 0.13-1.00 mg/mL, respectively. At 2 MIC, the growth of two representative MRSA strains was continually inhibited for at least 20 h. Surviving MRSA cells were not detected within 12-14 h after treatment with the extract at 4 MIC concentration. Staphylococcus aureus ATCC 25923 demonstrated similar results.     

Activity against multidrug-resistant Mycobacterium tuberculosis in Mexican plants used to treat respiratory diseases

The increase of multidrug-resistant Mycobacterium tuberculosis (MDR-TB) demands the search for alternative antimycobacterial drugs. The aim of this study was to evaluate plants used in Mexican traditional medicine to treat respiratory diseases for activity against MDR-TB. A group of 22 plants was screened for activity against Mycobacterium tuberculosis H37Rv and Mycobacterium avium at concentrations from 50 to 200 microg/mL. The antimycobacterial effect was determined by a microcolorimetric assay with Alamar blue dye. None of the aqueous extracts had antimycobacterial activity. Hexane extracts from Artemisia ludoviciana, Chamaedora tepejilote, Lantana hispida, Juniperus communis and Malva parviflora, and methanol extracts from Artemisia ludoviciana and Juniperus communis inhibited the growth of Mycobacterium tuberculosis. Mycobacterium avium was inhibited by Juniperus communis hexane extract and by Malva parviflora methanol extract. The active extracts were tested against monoresistant variants of Mycobacterium tuberculosis H37Rv (isoniazid, rifampin, streptomycin and ethambutol resistant) and the hexane extract of Lantana hispida showed the best activity. Lantana hispida hexane extract was also active against a group of MDR-TB clinical isolates. In contrast, it did not inhibit the growth of non-tuberculous mycobacteria. The hexane extract of Lantana hispida was fractionated by column chromatography and one of its fractions (FVI) inhibited the growth of all the MDR-TB clinical isolates at concentrations up to 25 microg/mL. This study supports the fact that selecting plants by ethnobotanical criteria enhances the probability of finding species with activity against mycobacteria, and our results point to Lantana hispida as an important source of potential compounds against MDR-TB.     

In vitro antifungal activity of extract and plumbagin from the stem bark of Diospyros crassiflora Hiern (Ebenaceae)

In this study the methanol/dichloromethane (1:1) extract and plumbagin isolated from extract of stem barks of Diospyros crassiflora were tested for their antifungal activity against 12 strains of yeast pathogens and filamentous fungi: Candida albicans, Candida glabrata, Candida krusei, Candida tropicalis, Cryptococcus neoformans, Aspergillus niger, Aspergillus flavus, Alternaria sp., Cladosporium sp., Geotrichum candidum, Fusarium sp. and Penicillium sp. The growth of all fungi strains tested was inhibited by the extract and plumbagin. The diameter of inhibition zones varied from 12 to 18 mm and from 21 to 35 mm for the extract and plumbagin, respectively. The MIC values ranged from 12.5 to 25 mg/mL for the extract and 0.78-3.12 microg/mL for plumbagin. It is therefore suggested that extracts from the stem bark of Diospyros crassiflora could be used traditionally in the treatment of fungal infections. Compared with ketoconazole used as a standard antifungal, plumbagin could be considered as a promising antifungal agent.     

Screening of Chinese and Mongolian herbal drugs for anti-human immunodeficiency virus type 1 (HIV-1) activity

Water and methanol extracts of 30 Chinese and Mongolian medicinal plants were tested for their human immunodeficiency virus type-1 (HIV-1) inhibitory activity. Of the 60 extracts, 23 showed anti-HIV activity. Bioassay-guided fractionation of one of the most active extracts, the methanol extract of the root tuber of Stephania cepharantha, led to the isolation of two alkaloids, aromoline and FK-3000 as potent inhibitory substances. They completely inhibited the cytopathic effects of HIV-1 on MT-4 cells at 31.3 and 7.8 microg/mL, respectively.     

Anti-proliferative and mutagenic activities of aqueous and methanol extracts of leaves from Pereskia bleo (Kunth) DC (Cactaceae)

The anti-proliferative effects of the aqueous and methanol extracts of leaves of Pereskia bleo (Kunth) DC (Cactaceae) against a mouse mammary cancer cell line (4T1) and a normal mouse fibroblast cell line (NIH/3T3) were evaluated under an optimal (in culture medium containing 10% foetal bovine serum (FBS)) and a sub-optimal (in culture medium containing 0.5% FBS) conditions. Under the optimal condition, the aqueous extract showed a significant (p<0.05) anti-proliferative effect at 200 microg/mL and 300 microg/mL in 4T1 cells and 300 microg/mL in NIH/3T3 cells, whereas the methanol extract did not show any notable anti-proliferative effect in these cell lines, at any of the concentrations tested. Under the sub-optimal condition, the aqueous extract showed a significant (p<0.05) anti-proliferative effect at 200 microg/mL and 300 microg/mL in NIH/3T3 cells, whilst the methanol extract showed a significant (p<0.05) anti-proliferative effect at 200 microg/mL and 300 microg/mL in both cell lines. An upward trend of apoptosis was observed in both 4T1 and NIH/3T3 cells treated with increasing concentrations of the aqueous extract. The level of apoptosis observed at all the concentrations of the aqueous extract tested was consistently higher than necrosis. There was a significant (p<0.05) increase in the level of necrosis observed in the 4T1 cells treated with 300 microg/mL of the methanol extract. Generally, the level of necrosis was noted to be higher than that of apoptosis in the methanol extract-treated cells. The mutagenicity assay performed showed that in the absence of S-9 liver metabolic activation, the extract was not mutagenic up to the concentration of 165 microg/mL . However, in the presence of S-9 liver metabolic activation, the aqueous extract was mutagenic at all the concentrations tested. This study shows that both the aqueous and methanol extracts of the leaves from Pereskia bleo (Kunth) DC (Cactaceae) do not have appreciable anti-proliferative effect on the 4T1 and NIH/3T3 cells as the EC(50) values obtained are greater than 50 microg/mL when tested under optimal culture condition. Moreover, the aqueous extract may form mutagenic compound(s) upon the metabolisation by liver enzymes.     

Antiviral activity against human immunodeficiency virus type 1 (HIV-1) and type 2 (HIV-2) of ethnobotanically selected Ethiopian medicinal plants

Ethiopian medicinal plants used for the treatment of a variety of ailments including infectious diseases were screened for activity against human immunodeficiency virus type 1 (HIV-1) and type 2 (HIV-2). Seventy-one polar and nonpolar extracts derived from 21 plants belonging to 14 families were tested for inhibition of viral replication using HIV-1 (III(B)) and HIV-2 (ROD) strains. Selective inhibition of viral growth was assessed by the simultaneous determination of the in vitro cytotoxicity of each of the extracts against MT-4 cells. Six extracts made from the root bark of Bersama abyssinica Fresen, the leaves of Combretum paniculatum Vent., and Dodonaea angustifolia L.f., and the stem bark of Ximenia americana L. displayed antiviral activity at concentrations that were nontoxic to MT-4 cells. The highest selective inhibition of HIV-1 replication was observed with the acetone fraction of C. paniculatum and the methanol fraction of D. angustifolia which showed selectivity indices (ratio of 50% cytotoxic concentration to 50% effective antiviral concentration) of 6.4 and 4.9, and afforded cell protection of viral induced cytopathic effect of 100% and 99%, respectively, when compared with control samples. The greatest degree of antiviral activity against HIV-2 was achieved with the acetone extract of C. paniculatum (EC(50): 3 microg/mL), which also showed the highest selectivity index (32). The 50% cytotoxic concentration ranged from 0.5 microg/mL for the hexane extract of D. angustifolia L.f., the most cytotoxic of the extracts tested, to >250 microg/mL for some extracts such as the methanol fraction of Alcea rosea L., the least toxic tested. Only the polar extracts that were obtained by extraction with hydroalcohol, methanol or acetone exhibited inhibition of viral growth at subtoxic concentrations. The results obtained in this study enable the selection of extracts which show some specificity of action and support the further investigation of these extracts for their potential as new lead antiretroviral compounds.     

Effective medicinal plants against enterohaemorrhagic Escherichia coli O157:H7

The stimulating effect of subinhibitory concentrations of antibiotics on the production of verocytotoxin (VT) by enterohaemorrhagic Escherichia coli (EHEC) O157:H7 has been claimed. The purpose of this study was to find an alternative, but bioactive medicine for the treatment of this organism. Fifty-eight preparations of aqueous and ethanolic extracts of 38 medicinal plant species commonly used in Thailand to cure gastrointestinal infections were tested for their antibacterial activity against different strains of Escherichia coli, including 6 strains of Escherichia coli O157:H7, Escherichia coli O26:H11, Escherichia coli O111:NM, Escherichia coli O22; 5 strains of Escherichia coli isolated from bovine; and Escherichia coli ATCC 25922. Inhibition of growth was primarily tested by the paper disc agar diffusion method. Among the medicinal plants tested, only 8 species (21.05%) exhibited antimicrobial activity against Escherichia coli O157:H7. Acacia catechu, Holarrhena antidysenterica, Peltophorum pterocarpum, Psidium guajava, Punica granatum, Quercus infectoria, Uncaria gambir, and Walsura robusta demonstrated antibacterial activity with inhibition zones ranging from 7 to 17 mm. The greatest inhibition zone against Escherichia coli O157:H7 (RIMD 05091083) was produced from the ethanolic extract of Quercus infectoria. Minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) were determined by the agar microdilution method and agar dilution method in petri dishes with millipore filter. Both aqueous and ethanolic extracts of Quercus infectoria and aqueous extract of Punica granatum were highly effective against Escherichia coli O157:H7 with the best MIC and MBC values of 0.09, 0.78, and 0.19, 0.39 mg/ml, respectively. These plant species may provide alternative but bioactive medicines for the treatment of Escherichia coli O157:H7 infection.     

Inhibition of enteric parasites by emulsified oil of oregano in vivo

Oil of Mediterranean oregano Oreganum vulgare was orally administered to 14 adult patients whose stools tested positive for enteric parasites, Blastocystis hominis, Entamoeba hartmanni and Endolimax nana. After 6 weeks of supplementation with 600 mg emulsified oil of oregano daily, there was complete disappearance of Entamoeba hartmanni (four cases), Endolimax nana (one case), and Blastocystis hominis in eight cases. Also, Blastocystis hominis scores declined in three additional cases. Gastrointestinal symptoms improved in seven of the 11 patients who had tested positive for Blastocystis hominis.     

Activity against drug resistant-tuberculosis strains of plants used in Mexican traditional medicine to treat tuberculosis and other respiratory diseases

Tuberculosis (TB) kills about 3 million people per year worldwide. Furthermore, TB is an infectious disease associated with HIV patients, and there is a rise in multidrug-resistant TB (MDR-TB) cases around the world. There is a need for new anti-TB agents. The study evaluated the antimycobacterial activity of nine plants used in Mexican traditional medicine to treat tuberculosis and other respiratory diseases. Nasturtium officinale showed the best activity (MIC = 100 microg/mL) against the sensitive Mycobacterium tuberculosis. The following plants were active also but at 200 microg/mL: Citrus sinensis, Citrus aurantifolia, Foeniculum vulgare, Larrea tridentata, Musa acuminata and Olea europaea. Contrary to the above data, activity against drug-resistant variants of M. tuberculosis was more evident, e.g. N. officinale was the most potent (MIC < or = 100 microg/mL) against the four mono-resistant variants tested; F. vulgare and O. europaea were active against all the resistant variants (MICs < or = 100 microg/mL). The most susceptible variant was the isoniazid resistant, being inhibited by C. aurantifolia, C. sinensis and O. europaea (MIC = 25 microg/mL). These data point to the importance of biological testing of extracts against drug-resistant M. tuberculosis isolates, and the bioguided assay of these extracts for the identification of lead compounds against MDR-TB isolates.     

In vitro anti-Helicobacter pylori activity of extracts of selected medicinal plants from North West Cameroon

ETHNOPHARMACOLOGICAL RELEVANCE: Helicobacter pylori, a gram negative microaerophilic bacterium is a major etiological agent in duodenal, peptic and gastric ulcers. The growing problem of antibiotic resistance by the organism demands the search for novel compounds from plant based sources. AIM OF STUDY: The present study is aimed at evaluating the antimicrobial activity of some selected medicinal plants on clinical isolates of H. pylori circulating in Cameroon in a bid to identify potential sources of cheap starting materials for the synthesis of new drugs. MATERIALS AND METHODS: Gastric biopsy samples were obtained from patients presenting with gastroduodenal complications. H. pylori was isolated from the specimens following standard microbiology procedures. The disk diffusion method was used to determine the susceptibility of 15 isolates to ten methanol plant extracts (Ageratum conyzoides, Scleria striatinux, Lycopodium cernua, Acanthus montanus, Eryngium foetidium, Aulutandria kamerunensis, Tapeinachilus ananassae, Euphorbia hirta, Emilia coccinea and Scleria verrucosa). The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) for the most active plant extracts were also determined by the agar dilution method. Results were analyzed statistically by the Fisher's exact test. RESULTS: All the plants tested demonstrated antimicrobial activity with zone diameters of inhibition ranging from 0-30mm. Of these, A. conyzoides, S. striatinux and L. cernua showed very potent antibacterial activity on the isolates. The lowest MIC and MBC recorded were 0.032mg/mL and 0.098mg/mL respectively. However, the MIC of the extracts ranged from 0.032-1.0mg/mL for S. striatinux; 0.063-0.5mg/mL for L. cernua and 0.063-1.0mg/mL for A. conyzoides. The MBC of the extracts ranged from 0.098-15.0mg/mL for S. striatinux; 0.098-12.5mg/mL for A. conyzoides, and 0.195-12.5mg/mL for L. cernua. The extracts had a wide spectrum of activity. The three most potent extracts possessed significant (P<0.05) inhibitory activities. CONCLUSION: The plant extracts may contain compounds with therapeutic activity.     

Evaluation of the anti-inflammatory and anti-proliferation tumoral cells activities of Antrodia camphorata, Cordyceps sinensis, and Cinnamomum osmophloeum bark extracts

The extracts of chloroform (1) and methanol (2) from Antrodia camphorata (AC), and chloroform (3) and n-butanol (4) fractions of methanol extract from Cordyceps sinensis (CS), and hexane (5), ethyl acetate (6), and methanol (7) from Cinnamomum osmophloeum bark (CO) were evaluated for their anti-inflammatory as well as tumor-cell growth inhibitory activities in vitro. All the tested extracts dose dependently inhibited the enhanced production of inflammatory mediators such as nitric oxide (NO) through reducing inducible NO synthase expression, and cytokines (tumor necrosis factor (TNF)-alpha and interleukin (IL)-12 in LPS/IFN-gamma activated murine peritoneal macrophages. In addition, extracts 1 from AC, and 5 and 6 from CO significantly arrest the mitogen-stimulated spleen cells in G0/G1 stage. On the other hand, all these extracts were also evaluated for their tumor-cell proliferation activities in different type of cancer cell lines such as Jurkat, HepG2, PC 3, Colon 205, and MCF 7 as well as normal PBMCs. Compared to untreated controls, the extracts 1, 2, and 4-7 were most active and inhibited Jurkat cells with IC50 value of 22, 40, 18, 4, 5, and 45 microg/ml, respectively. In addition, the extracts 5, 6, and 7 from CO showed potent growth inhibition of HepG2 and PC 3 with IC50 values of 35, 80, 55 microg/ml; and 42, 125, and 50 microg/ml, respectively. Similarly, the extracts 1 and 5 inhibited the growth of Colon 205 and MCF 7 cells with IC50 values of 65, 33; and 95 and 30 microg/ml, respectively. Interestingly, none of the tested extract has shown cytotoxicity towards normal PBMCs up to the concentration range studies (0-150 microg/ml). Taken together, these data suggest that the anti-inflammatory and anti-cancer properties of AC, CS, and CO might result from the growth inhibition of NO, TNF-alpha and IL-12, and tumor cells proliferation, respectively.     

鸦胆子油乳对肺癌 A549 细胞凋亡及血管内皮生长因子分泌的影响

 目的 观察鸦胆子油对肺癌 A549 细胞凋亡和血管内皮生长因子分泌的影响,以探讨其治疗肺癌的作用机制。 方法 用不同浓度鸦胆子油乳（ 0.5 , 1.25 , 2.5 , 3.75 g·L^-1 ）与 A549 细胞共育不同时间（ 6 , 24 , 48 h ）,采用流式细胞仪（ Annexin V 双标法、 DNA 含量测定和 凋亡细胞 DNA 片段原位末端检测等方法）检测凋亡细胞百分比,采用定量 Sandwich 酶免疫技术（ ELISA ）观察细胞血管内皮生长因子（ VEGF ）分泌量。 结果 3 种检测方法均表明, 中、高浓度鸦胆子油乳（ 2.5 , 3.75 g·L^-1 ）作用 6 h 以上,具有显著的诱导 A549 细胞凋亡的作用。 Annexin V 双标法和 DNA 凝胶电泳结果表明, 1.25 g·L^-1 的鸦胆子油乳作用 24 ~ 48 h ,也能诱导 A549 细胞凋亡。 2.5 g · L^-1 鸦胆子油乳作用 48 h 能使 A549 细胞分泌 VEGF 显著减少。 结论 鸦胆子油乳通过诱导肿瘤细胞凋亡,减少肿瘤细胞分泌 VEGF 发挥其治疗肺癌的作用。     

COX-1 and -2 activity of rose hip

The objective of this study was to investigate whether the clinically observed efficacy of rose hip in the treatment of osteoarthritis is due to inhibition of cyclooxygenase-1 and -2. Water, methanol, dichloromethane and hexane extracts of rose hip were tested for in vitro COX-1 and 2 activity. The organic solvent extracts showed good inhibition of both COX-1 and 2. The methanol extract was most active in both assays with IC(50) values of 12 microg/mL for COX-1 and 19 microg/mL for COX-2. The clinically observed effect might be due to inhibition of cyclooxygenase.     

Screening of selected basidiomycetes for inhibitory activity on Clostridium histolyticum collagenase and human leukocyte elastase

Collagenase and elastase play a critical role in the degradation of connective tissue. Aqueous and dichloromethane extracts of 15 Basidiomycetes were screened for their ability to inhibit the activity of collagenase and elastase. Collagenase (EC 3.4.24.3) was not inhibited by aqueous extracts, but by dichloromethane extracts in concentrations of 200 microg/mL. For seven extracts an IC(50) less than 200 microg/mL could be observed. Elastase (3.4.21.37) was inhibited by both aqueous and dichloromethane extracts of the Basidiomycetes, with the aqueous extracts active at concentrations of 200 microg/mL. Five extracts inhibited strongly, with an IC(50) 2-20 microg/mL. Except for four, all dichloromethane extracts inhibited the enzyme in concentrations of 2 microg/mL, nine of them very strongly at about 90%.