Screening antiacne potency of Indonesian medicinal plants: antibacterial,lipase inhibition,and antioxidant activities

Indonesian medicinal plants were screened as potential sources of antiacne agents. The screening methods were performed using antibacterial assay against Propionibacterium acnes, lipase inhibitor assay, and antioxidant assay. The results showed that from 40 plant materials extracted with methanol and 50% ethanol in water, Caesalpinia sappan was the best extract based on the combined activities: antibacterial (minimum inhibitory concentration 0.13 mg/ml; minimum bactericidal concentration 0.25 mg/ml), lipase inhibitory [50% inhibitory concentration (IC₅₀) 120.0 μg/ml], and antioxidative (IC₅₀ 6.47 μg/ml). Another prospective extract is Intsia palembanica based on its lipase inhibitory activity (IC₅₀ 4.1 μg/ml) and antioxidant activity (IC₅₀ 3.87 μg/ml). Part of this report was presented at the 58th Annual Meeting of the Japan Wood Research Society, Tsukuba, March 2008     

Screening of Indonesian plants for tyrosinase inhibitory activity

In our efforts to find new tyrosinase inhibitory materials, we investigated 44 Indonesian plants belonging to 24 families for tyrosinase inhibitory activity. The extracts of 5 Artocarpus woods showed potent tyrosinase inhibitory activity (over 80% at 100 μg/ml) similar to a positive control, kojic acid. In Artocarpus woods, the extracts of the sapwoods showed stronger inhibitory activity than those of the heartwoods. Chlorophorin was isolated as one of the active compounds in the sapwood of Artocarpus heterophyllus. The content of chlorophorin in sapwood was higher than that in heartwood. Part of this paper was presented at the 53rd (Fukuoka, March 2003) and 54th (Hokkaido, August 2004) Annual Meetings of the Japan Wood Research Society, and the 5th International Wood Science Symposium (Kyoto, September 2004)     

Effects of Morus alba leaf extract on the production of nitric oxide, prostaglandin E2 and cytokines in RAW264.7 macrophages

Morus alba leaf methanolic extract and its fractions (chloroform, butanol, and aqueous fractions) were found to inhibit NO production in LPS-activated RAW264.7 macrophages without an appreciable cytotoxic effect at concentration from 4 to 100 microg/ml. LPS-induced PGE2 production was significantly reduced only by butanol fraction. In addition, M. alba leaf extract and its fractions significantly decreased the production of TNF-alpha. These findings suggest that M. alba leaf extract seems to be able in suppressing inflammatory mediators. Moreover, the inhibitory activities on COX-2 and iNOS of its butanol fraction are warranted for further elucidation of active principles for development of new antiinflammatory agents.     

Screening of medicinal and ornamental plants for insecticidal and growth regulating activity

Extracts of 121 medicinal and ornamental plants were screened for insecticidal and growth regulating activity to milkweed bug, Oncopeltus fasciatus Dallas. The most effective extracts stemmed from Inula helenium L., Rumex crispus L., R. acetosa L., Asarum europaeum L., and Calendula officinalis L. All these extracts exerted growth inhibiting activities and moderate or low acute toxicity. Most promising were extracts of dried roots of I. helenium. Besides a moderate chronic toxicity which reduced the fitness of the milkweed bug, the treatment produced overaged nymphs, supernumerary nymphs, disturbances of the moulting process, morphological defects, delay of adult maturation and reduction of fecundity. In addition, I. helenium extracts had a strong antifeedant effect when topically applied and very strong repellent effect when applied to the food (peeled sunflower kernels). It is obvious that the extract contains several active constituents. Such a cocktail may reduce the threat of rapid resistance development.     

Antibacterial and antifungal activity of Indonesian ethnomedical plants

Methylene chloride and methanol extracts of 20 Indonesian plants with ethnomedical uses have been assessed for in vitro antibacterial and antifungal properties by disk diffusion method. Extracts of the six plants: Terminalia catappa, Swietenia mahagoni Jacq., Phyllanthus acuminatus, Ipomoea spp., Tylophora asthmatica and Hyptis brevipes demonstrated high activity in this bioassay system. These findings should stimulate the search for novel, natural product such as new antibacterial and antifungal agents.     

Effects of methanolic extract and fractions from Litsea cubeba bark on the production of inflammatory mediators in RAW264.7 cells

Both the methanolic extract and its fractions (0.01 mg/ml) from Litsea cubeba bark were found to inhibit NO and PGE2 production in LPS-activated RAW264.7 macrophages without significant cytotoxicity at less than 0.01 mg/ml concentration. Moreover, L. cubeba bark extract and its fractions significantly decreased the activity of myeloperoxidase catalyzing oxidation of chloride to HOCl and O2- production was reduced by methanol extract (0.05 mg/ml), chloroform fraction (0.025-0.05 mg/ml) and butanol fraction (0.005 mg/ml). These findings suggest that L. cubeba is beneficial for inflammatory conditions and may contain compound(s) with anti-inflammatory properties.     

Screening of Argentinian plants for pesticide activity

Aerial parts of 27 plant species native to Argentina were tested in anti-insect, germination inhibition and bactericide bio-assays. In antifeedant assays on Epilachna paenulata larvae, 11 species showed strong feeding deterrent effects (higher than 90% at 200 microg/cm(2)). Twelve plants strongly inhibited the germination of Avena sativa seeds, but only six inhibited Raphanus sativum germination at 10 mg/ml. Four plants showed complete growth inhibition of Escherichia coli at a concentration of 2 mg/ml.     

New sesquiterpenoids from the dried flower buds of Tussilago farfara and their inhibition on NO production in LPS-induced RAW264.7 cells

Three new sesquiterpenoids, 1α-(3″-ethyl-cis-crotonoyloxy)-8-angeloyloxy-3β,4β-epoxy-bisabola-7(14),10-diene (1), 7β-angeloyloxy-14-hydroxy-notonipetranone (2) and 1α-hydroxy-7β-(4-methylsenecioyloxy)-oplopa-3(14)Z,8(10)-dien-2-one (3) were isolated from ethanolic extract of the dried flower buds of Tussilago farfara L., along with nine known sesquiterpenoids (4-12). All of these compounds were evaluated for their effect on the inhibition of nitric oxide (NO) production induced by lipopolysaccharide in macrophage cell line RAW 264.7 and exhibited inhibitory activity on NO production in a dose-dependent manner. 7β-(4-Methylsenecioyloxy)-oplopa-3(14)E,8(10)-dien-2-one (8) was proved to be the best among these tested sesquiterpenoids with an IC(50) value of 10.80 μM.     

Screening of Costus speciosus extracts for antioxidant activity

Different parts of Costus speciosus were investigated for their polyphenol content and antioxidant activity.     

Antifungal activity of some Himalayan medicinal plants and cultivated ornamental species

Extracts of roots of Rumex nepalensis, Berberis aristata, Arnebia benthamii, bark of Taxus wallichiana, Juglans regia and petals of Jacquinia ruscifolia were tested for their antifungal activity against twelve different fungal pathogens. Ethanolic extracts of R. nepalensis and J. ruscifolia extracts showed a broad spectrum of activity.     

Screening of some rare endemic Italian plants for inhibitory activity on 5-lipoxygenase

The extracts of four rare plants found on the islands of Sicily, Vulcano and Marettimo, Southern Italy, were screened for their inhibitory effect on the production of leukotriene B4 by 5-lipoxygenase in intact cells. The methanol extracts of pods of Cytisus aeolicus and aerial parts of Thymus richardii were the most active extracts, inhibiting almost completely the leukotriene B4 production at 200 and 50 microg/ml, respectively.     

Induction of heme oxygenase-1 by Macleaya cordata extract and its constituent sanguinarine in RAW264.7 cells

Macleaya cordata (plume poppy) is used in traditional Chinese medicine for its anti-inflammatory and antibacterial activities. In this study, we examined whether M. cordata extract and/or its major alkaloid constituents, protopine, allocryptopine, sanguinarine and chelerythrine activate the Nrf2 signalling pathway which regulates the expression of cytoprotective enzymes including heme oxygenase-1 (HO-1) and thioredoxin 1. In murine macrophage RAW264.7 cells, M. cordata extract increased both mRNA and protein levels of HO-1. Of the alkaloids examined, only sanguinarine appeared to be responsible for these effects. At the concentration of 2 μM, sanguinarine induced nuclear accumulation of Nrf2, increased the expression of Hmox1 gene encoding HO-1 and elevated HO-1 protein levels. Sanguinarine-induced Hmox1 mRNA expression was suppressed by SB203580, a pharmacologic inhibitor of p38 mitogen-activated protein kinases (p38 MAPKs). The upregulation of HO-1 in RAW264.7 cells by sanguinarine was, however, accompanied by decrease in cell viability. Nonetheless, sanguinarine at micromolar, non-cytotoxic concentrations elevated protein levels of HO-1 and thioredoxin 1 in primary cultures of human hepatocytes. We conclude that sanguinarine may, under appropriate conditions, increase the capacity of the enzymatic antioxidant defence system via activation of the p38 MAPK/Nrf2 pathway.     

Radical scavenging, antioxidant and cytotoxic activity of Brazilian Caatinga plants

Extracts of 32 plants from the Brazilian northeastern semi-arid region called Caatinga were evaluated through DPPH radical scavenging assay, beta-carotene bleaching, and brine shrimp lethality tests (BST). Among the extracts studied Byrsonima cf. gardneriana, Mascagnia coriacea, Cordia globosa, Diodia apiculata and Hypenia salzmannii showed the highest activities in DPPH radical scavenging test. In the beta-carotene bleaching test the highest activities were observed for Passiflora cincinnata, Chamaecrista repens, B. cf. gardneriana, Rollinia leptopetala, Serjania glabrata, Diospyros gaultheriifolia, C. globosa, Mimosa ophtalmocentra, M. coriacea and Lippia cf. microphylla. In contrast, R. leptopetala, Zornia cf. brasiliensis and Leonotis nepetifolia were the most active species in the BST.     

Polyphenols from the stems of Morus alba and their inhibitory activity against nitric oxide production by lipopolysaccharide-activated microglia

Neuroinflammatory processes are involved in the pathogenesis of many neurodegenerative disorders. Microglial cells, the main immune cells of the central nervous system, represent a target of interest to search for naturally occurring anti-inflammatory products. In this study, we evaluated the anti-inflammatory properties of polyphenols obtained from the stems of Morus alba. This edible species, known as white mulberry, is frequently studied because of its traditional use in Asian medicine and its richness in different types of polyphenols, some of which are known to be phytoalexins. One new coumarin glycoside, isoscopoletin 6-(6-O-β-apiofuranosyl-β-glucopyranoside) (1) was mainly isolated by CPC (centrifugal partition chromatography) from this plant, together with seven known polyphenols (2–8). Their structures were established on the basis of spectroscopic analyses including extensive 2D NMR studies. The eight isolated compounds were evaluated for their inhibitory activities on nitric oxide (NO) production in lipopolysaccharide (LPS)-induced BV-2 microglial cells. The absence of cell toxicity is checked by a MTT assay.     

Effects of a nitric oxide donor and nitric oxide scavengers on Sorbus pohuashanensis embryo germination

The effects of an exogenous nitric oxide donor(sodium nitroprusside, SNP), a NO scavenger 2-phenyl-4,4,5,5-tetramethylimidazoline-1-oxyl-3-oxode(PTIO) and carboxy-PTIO potassium salt(c PTIO) on the embryo germination of Sorbus pohuashanensis were studied in a petri dish test. SNP at 0.5–5 mmol L-1 increased germination percentage, mean time to germination, germination index and germination energy compared with the control to different degrees. Treatment with 2 mmol L-1 SNP improved germination most significantly; embryo germination percentage for mother tree 1(91.11%) and mother tree 2(64.44%) were much higher than the control. In addition,excessive SNP levels did not enhance embryo germination.Combined treatment with SNP and an NO scavenger delayed embryo germination. Treatment with c PTIO inhibited embryo germination; germination percentage was 42.22% and was lower than that of the control. These results show that low concentrations of exogenous NO can enhance the embryo germination of S. pohuashanensis,providing a simple, effective way for promoting germination of S. pohuashanensis.     

Sesquiterpenes from the rhizomes of Alpinia japonica and their inhibitory effects on nitric oxide production

A novel norsesquiterpene (1), three new bisabolenes sesquiterpenes (2–4), along with 7 known compounds (5–11), were isolated from the rhizomes of Alpinia japonica. The structures of the new compounds were elucidated by analysis of spectroscopic data. The absolute configuration of C-1 in 3 was deduced via the circular dichroism data of the in situ formed [Rh₂(OCOCF₃)₄] complexes. Inhibitory effects of the isolates on nitric oxide production in lipopolysaccaride-activated RAW264.7 macrophages were evaluated. Compound 6 showed significant inhibitory activity with IC₅₀ value of 5.3 μΜ, and compounds 1, 3, 5 and 7–10 exhibited moderate inhibitory activities with IC₅₀ values between 24.5 and 46.3 μM.     

Inhibition of nitric oxide production on LPS-activated macrophages by kazinol B from Broussonetia kazinoki

The ethyl acetate soluble fraction of Broussonetia kazinoki at 50 microg/ml showed a significant inhibition (78.2%) of nitric oxide (NO) in lipopolysaccharide activated macrophages. Kazinol B, an isoprenylated flavan, was identified as the active principle. It inhibits the NO synthesis with an IC(50) of 21.6 microM.     

Indole alkaloids from the roots of Isatis indigotica and their inhibitory effects on nitric oxide production

Three rare indole-2-S-glycosides, indole-3-acetonitrile-2-S-β-D-glucopyranoside (1), indole-3-acetonitrile-4-methoxy-2-S-β-D-glucopyranoside (2) and N-methoxy-indole-3-acetonitrile-2-S-β-D-glucopyranoside (3), together with 11 known indole alkaloids were isolated from the roots of Isatis indigotica Fort. (Cruciferae). The structures of 1–3 were elucidated on the basis of mass spectrometry and extensive 1D and 2D NMR spectroscopy. All of the isolated compounds were tested for inhibitory activity against LPS-induced nitric oxide production in RAW 264.7 macrophages. A plausible biosynthesis pathway of 1–3 is also proposed.     

3, 4-seco-Labdane diterpenoids from the leaves of Callicarpa nudiflora and their inhibitory effects on nitric oxide production

As a part of our ongoing search for bioactive compounds from the leaves of Callicarpa nudiflora that inhibit nitric oxide (NO) production, the 90% EtOH fraction eluted by macroporous resin adsorption was found to show significant inhibitory activity against the production of NO in RAW 264.7 stimulated by lipopolysaccharide (LPS). Bioactivity-guided isolation of the fraction yielded three new bioactive diterpenoids, named ent-3, 4-seco-14-carbonyl-15, 16-epoxy-4(18), 8(17), 13(14)-labdatrien-3-oic acid (1), syn-3, 4-seco-12R-hydroxy-15, 16-epoxy-4(18), 8(17), 13(16), 14(15)-labdatetraen-3-oic acid (2) and syn-3, 4-seco-12S-hydroxy-15, 16-epoxy-4(18), 8(17), 13(16), 14(15)-labdatetraen-3-oic acid (3). Their structures and configurations were elucidated by comprehensive spectroscopic analysis. All the three compounds exhibited potent inhibitory activity on NO production in LPS-activated RAW 264.7 macrophage cells.