The antiplasmodial activity of spermine alkaloids isolated from Albizia gummifera

In the present study the methanolic extract of Albizia gummifera was fractionated into various fractions. These fractions were tested against choroquine sensitive (NF54) and resistant (ENT30) strains of Plasmodium falciparum. All other fractions apart from the alkaloidal fraction showed low activity with IC 50 above 3 microg/ml. The alkaloidal fraction exhibited strong activity against NF54 and ENT30 with IC 50 of 0.16+/-0.05 and 0.99+/-0.06 microg/ml, respectively. Five known spermine alkaloids were isolated from the alkaloidal fraction. These alkaloids exhibited activities against NF54 and ENT30 with IC 50 ranging from 0.09+/-0.02 to 0.91+/-0.10 microg/ml. Four of the alkaloids were further evaluated for in vivo activity against rodent malaria parasite Plasmodium berghei. The alkaloids showed percentage chemosuppression of parasitaemia in mice ranging from 43 to 72%. The use of the extracts A. gummifera for treatment of malaria in traditional medicine seems to have a scientific basis.     

Molluscicidal activity of Aglaia duperreana and the constituents of its twigs and leaves

The methanol (MeOH) extract of the twigs and leaves of Aglaia duperreana was investigated for its molluscicidal activity against Pomacea canaliculata. The extract was found to exhibit significant molluscicidal activity. The ethyl acetate soluble fraction of the extract showed the most potent molluscicidal activity among different solvent fractions. The bioactivity-guided chemical investigation of the ethyl acetate soluble fraction led to a new triterpenoid along with 15 known compounds. Their structures were elucidated by spectroscopic methods, including one- and two-dimensional nuclear magnetic resonance techniques as well as mass spectroscopic analysis. The molluscicidal activities of compounds 2-16 against P. canaliculata were also investigated. Naringenin trimethyl ether showed significant molluscicidal activity with a median lethal concentration (LC(50)) of 3.9 μg/mL, which was indicated higher potency than the positive control, tea saponin (LC(50)=4.5 μg/mL).     

Antioxidant activity and total phenolic content in Cirsium five species from north-east region of Poland

Methanolic extracts from inflorescences and leaves of five Cirsium species: C. arvense, C. oleraceum, C. palustre, C. rivulare and C. vulgare and CHCl3, Et2O, EtOAc, n-BuOH fractions obtained from those extracts were investigated for their antioxidant activity. The antioxidant activity measurement, expressed as Total Antioxidant Status, ranged from 0.98 to 2.71 mM/l. The total phenolic content of the samples varied from 12 to 804 mg/g. There was a positive correlation between the total phenolic content and antioxidant activity for MeOH extracts and EtOAc fractions (R2=0.95, 0.8 respectively).     

Insecticidal activity of Vitex mollis

Organic extracts from the leaves of Vitex mollis were assessed for their toxic effect on fall armyworm neonate larvae (Spodoptera frugiperda), an important insect pest of corn. The extracts showed insecticidal and insect growth regulatory activity, being CHCl(3)-MeOH (1:1) extract the most active, also found to be toxic in the Artemia salina test.     

Anti-HBV activities of Streblus asper and constituents of its roots

The extracts from leaves, heartwood, barks and roots of the Streblus asper were investigated for anti-HBV activities, separately. The results suggested that the MeOH extracts of the heartwood, barks, and roots exhibited good anti-HBV activities. Further investigations displayed that ethyl acetate and n-butanol soluble parts of their MeOH extracts showed more significant anti-HBV activities. Moreover, a new lignan, together with 11 known compounds, was isolated from n-butanol-soluble part of MeOH extract of the roots of S. asper. The structures were elucidated by spectroscopic methods, including 1D NMR ((1)H NMR, (13)C NMR), 2D NMR (HMQC, HMBC) and HR-EI-MS experiments. Compounds 1-3 were evaluated for their anti-HBV activities. Honokiol showed significant anti-HBV activity with IC(50) values of 3.14μM and 4.74μM for HBsAg and HBeAg with no cytotoxicity respectively, while lamivudine (3TC, positive control) exhibited weak anti-HBV activity with IC(50) values of 11.81μM and 25.80μM for HBsAg and HBeAg respectively.     

Study on the antimicrobial activity of Hymatanthus sucuba

The antimicrobial activity of Hyamatantus sucuba roots methanol extract, fractions prepared from this extract (n-hexane, CHCl(3), EtOAc, and n-butanol) and some isolated compounds were evaluated against some Gram(+) and Gram(-) bacteria and yeasts.     

Cytotoxicity and antihyperglycemic effect of minor constituents from Rhizoma Coptis in HepG2 cells

Generally, berberine, coptisine, palmatine, and jatrorrhizine were considered as the main bio-active compounds in Rhizoma Coptis (RC). Little attention was paid to investigate the pharmacological activity of minor constituents in RC. The present study was designed to separate the minor compounds, and the cytotoxicity and antihyperglycemic effect of these compounds in HepG2 cells were also studied. Palmatine (1), berberine (2), coptisine (3), epiberberine (4), columbamine (5), and jatrorrhizine (6) from RC ethanol extract were isolated by high speed counter current chromatography (HSCCC) in one run. The remaining fraction (about 50% of extract in HSCCC) was further isolated by traditional column chromatography methods to yield magnoflorine (7), ferulic acid (8), and choline (9). Another four alkaloids, namely groenlandicine (10), berberrubine (11), oxyberberine (12), 8-oxo-coptisine (13), also were obtained from CHCl₃ extracts. Especially, choline was first isolated from RC. Cell assay indicated that the minor fractions excluding compounds 1-6 showed obvious glucose lowering activity. In addition, the minor monomers also exhibited moderate glucose lowering activity. The combination of berberine and ferulic acid showed synergistic effect on antihyperglycemic. The combination of alkaloids 1-6 was same so. All compounds had different cytotoxicity in HepG2 cells within the test concentration. Of them, berberrubine showed the strongest cytotoxicity. The results suggested that combined action of variety constituents contributed to the antihyperglycemic effets and low cytotoxicity of RC extract in HepG2 cells.     

Antimicrobial activity of Leucas aspera flowers

The methanol extract of Leucas aspera flowers, its fractions, the alkaloidal residue and the expressed flower juice, tested for antimicrobial activity, showed good antibacterial activity for methanol extract and methanol fraction with maximum activity for the alkaloidal residue.     

COX-2 and sPLA2 inhibitory activity of aqueous extract and polyphenols of Rhizophora mangle (red mangrove)

The aqueous extract of Rhizophora mangle bark and its polyphenolic fractions showed remarkable in vitro antiinflammatory activity in a preliminary study. The low molecular weight fraction exhibited cyclooxygenase-2 inhibitory activity while the total aqueous extract and the low molecular weight fraction showed secretory phospholipase A(2) inhibitory activity.     

Activity of Berberis aetnensis root extracts on Candida strains

The antifungal activity of methanolic extract and alkaloidal fraction of Berberis aetnensis against Candida species was investigated. The crude extract was active against Candida species, this activity being higher than that of the alkaloidal fraction and berberine.     

Anti-hyperglycemic action of apigenin-6-C-β-fucopyranoside from Averrhoa carambola

A stimulatory effect of apigenin-6-C-β-fucopyranoside (1) on glucose uptake was observed when rat soleus muscle was incubated with 1, 10 and 100μM of this flavonoid glycoside. The presence of specific insulin signaling inhibitors, such as wortmannin, an inhibitor of phosphoinositide 3-kinase (PI3K), RO318220, an inhibitor of protein kinase C (PKC), PD98059, an inhibitor of mitogen-activated protein kinase (MEK), and HNMPA(AM)(3), an insulin receptor tyrosine kinase activity inhibitor showed that apigenin-6-C-β-fucopyranoside triggers different metabolic pathways in skeletal muscle. The oral administration of crude extract, fractions and isolated flavonoids (apigenin-6-C-β-fucopyranoside (1) and apigenin-6-C-(2″-O-α-rhamnopyranosyl)-β-fucopyranoside (2)) from Averrhoa carambola leaves exhibited a potential hypoglycemic activity in hyperglycemic normal rats. Additionally, both flavonoids significantly increased the muscle and liver glycogen content after an acute treatment. The results indicate that A. carambola can be regarded as a potent antihyperglycemic agent with insulin secretagogue and insulin mimetic properties.     

Hepatoprotective activity of Beta vulgaris against CCl4-induced hepatic injury in rats

Ethanolic extract of Beta vulgaris roots given orally at doses of 1000, 2000 and 4000 mg/kg exhibited significant dose-dependent hepatoprotective activity against carbontetrachloride (CCl(4))-induced hepatotoxicity in rats. Hepatotoxicity and its prevention were assessed by serum markers viz. cholesterol, triglyceride, alanine amino transferase and alkaline phosphatase.     

Antidiarrhoeal activity of Cyperus rotundus

The methanol extract of Cyperus rotundus rhizome, given orally at the doses of 250 and 500 mg/kg b.w., showed significant antidiarrhoeal activity in castor oil induced diarrhoea in mice. Among the fractions, tested at 250 mg/kg, the petroleum ether fraction (PEF) and residual methanol fraction (RMF) were found to retain the activity, the latter being more active as compared to the control. The ethyl acetate fraction (EAF) did not show any antidiarrhoeal activity.     

Antibacterial effect of Dryopteris crassirhizoma against methicillin-resistant Staphylococcus aureus

Methanol extract and its fractions (hexane, EtOAc, n-BuOH, and H2O) of Dryopteris crassirhizoma were investigated for antibacterial activity against methicillin-resistant Staphylococcus aureus. The hexane fraction showed a good antibacterial activity against all tested strains.     

Antiinflammatory activity of Sambucus ebulus hexane extracts

Hexane extracts of aerial parts (flowered browes), leaves and roots of Sambucus ebulus were investigated for their antiinflammatory activity in rats. Aerial parts and roots extracts produced statistically significant and dose dependent inhibition of edema induced by carrageenan at all doses when compared to the control groups. On the contrary, hexane extract of leaves did not show any activity up to 600 mg/kg i.p. The highest activity was showed in the aerial parts and roots that at 600 mg/kg i.p. inhibited inflammation by ca. 80% (78% for diclofenac at 100 mg /kg i.p.). No extracts exhibit toxicity when injected up to 2 g/ kg intraperitoneally in mice.     

Hypoglycemic effect of Bauhinia cheilandra in rats

The extract of the methanolic leaves of Bauhinia cheilandra (BC) was tested on glucose loaded and alloxan-induced diabetic rats. In both tests, the methanolic extract at doses of 300, 600, and 900 mg/kg, has shown a statistically significant and considerable hypoglycemic activity.     

Antinociceptive effect and acute toxicity of the Hyptis suaveolens leaves aqueous extract on mice

The aqueous extract of Hyptis suaveolens leaves was studied for their antinociceptive property in chemical and thermal models of nociception in mice. Oral administration of the aqueous extract (100, 200, and 400 mg/kg) dose-dependently reduced the number of writhings induced by acetic acid, decreased the licking activity of the early phase in formalin test and increased the reaction time in hot-plate test. The antinociceptive effect was significantly antagonized by naloxone (3 mg/kg; i.p.). Preliminary acute toxicity study showed that no animal death with doses up to 5 g/kg (p.o.).     

New withanolides from Mandragora officinarum: First report of withanolides from the Genus Mandragora

Two new withanolides named mandragorolide A (1) and mandragorolide B (2) were isolated from the MeOH extract of the whole plant of Mandragora officinarum of Jordanian origin, along with five known withanolides namely larnaxolide A (3), withanolide B (4), datura lactone 2 (5), withanicandrin (6) and salpichrolide C (7). Compound 3 has been reported only once before, from the leaves of Larnax glabra. This is the first report of withanolides of different biogenetic types from the genus Mandragora. Isolation of known fatty compounds, coumarins, sterols and tropane alkaloids was also achieved in this study.     

Mechanism-based CYP2D6 inactivation by acridone alkaloids of Indonesian medicinal plant Lunasia amara

Fourteen acridone alkaloids isolated from Lunasia amara Blanco were tested for their mechanism-based inhibition on human liver microsomal dextromethorphan O-demethylation activity, a prototype marker for cytochrome P450 2D6 (CYP2D6). Among the 14 compounds, 5-hydroxygraveroline (1), 8-methoxyifflaiamine (2), lunamarine (3), and lunine (12) increased their inhibitory activity with increasing preincubation time. Then, we further examined the possibility of mechanism-based inhibition on 5-hydroxygraveroline (1) and lunamarine (3), which showed the potent inhibition. Further investigations on 1 and 3 showed that the characteristic time- and concentration-dependent inhibition, which required a catalytic step with NADPH, was not protected by nucleophiles, and was decreased by the presence of a competitive inhibitor. Thus, 1 and 3 were concluded as mechanism-based inactivators of CYP2D6.     

Hepatoprotective activity of Clerodendrum inerme against CCl4 induced hepatic injury in rats

The ethanolic extract of Clerodendrum inerme leaves were screened for its hepatoprotective activity in CCl(4) (0.5 ml/kg, i.p) induced liver damage in Swiss albino rats at a dose of 200 mg /kg bw. The ethanolic extract of C. inerme significantly (P<0.001) decreases the serum enzyme alanine amino transferase (ALT), asparate amino transferase (AST), alkaline phosphates (ALP), triglycerides (TGL), total cholesterol (TC) and significantly increased the glutathione level. Silymarin (25 mg/kg), a known hepatoprotective drug used for comparison exhibited significant activity (P<0.001). The extract did not shown any mortality up to a dose of 2000 g/kg bw.