In-vitro alpha amylase inhibitory activity of the leaf extracts of Adenanthera pavonina.

BACKGROUND: Diabetes has caused a major burden to the health sector in the developing countries and has shown an increasing trend among the urban population. It is estimated that most patients are with type II diabetes which could be easily treated with dietary changes, exercise, and medication. Sri Lanka carries a long history ayurvedic medicine where it uses the plant for treating many diseases. Therefore it is important to screen medicinal plants scientifically so they could be used safely and effectively in the traditional medical system and also be used for further investigations. Adenanthera pavonina is a plant used in the Ayurvedic medical system in Sri Lanka for treating many diseases including diabetics. We evaluated the anti-diabetic properties and the antioxidant properties of Adenanthera pavonina leaves. METHODS: The methanol extract of the leaves was sequentially extracted with petroleum ether and thereafter was partitioned between EtOAc, and water. The α-amylase inhibition assay was performed using the 3,5- dinitrosalicylic acid method. The antioxidant activities were measured using the DPPH free radical scavenging activity and the total phenolic content using Folin-Ciocalteu's reagent. The cytotoxicity of the extract was evaluated using the Brine shrimp bioassay. RESULTS: The IC50 values of α amylase inhibitory activity of MeOH, EtOAc, petroleum ether, and water were 16.16 ± 2.23, 59.93 ± 0.25, 145.49 ± 4.86 and 214.85 ± 9.72 µg/ml respectively and was similar to that of Acarbose (18.63 ± 1.21 (µg/ml). Antioxidant activities were also determined and the EtOAc fraction showed the highest total phenolic content (34. 62 ± 1.14 mg/g extract) and the highest DPPH scavenging activity with an IC50 of 249.92 ± 3.35 µg/ml. CONCLUSION: The leaf extracts of Adenanthera pavonina exhibit remarkable α-amylase inhibitory activity in the crude methanolic extract. Hence leaves of Adenanthera pavonina has a potential to be used as a regular green vegetable and also be investigated further in isolating pure compounds with anti-diabetic activity.

Tricolorin A, major phytogrowth inhibitor from Ipomoea tricolor.

The allelopathic potential of Ipomoea tricolor (Convolvulaceae), used in Mexican traditional agriculture as a weed controller, has been demonstrated by measuring the inhibitory activity of organic extracts on seedling growth of Amaranthus leucocarpus and Echinochloa crus-galli. Bioactivity-directed fractionation of the active CHCl3 extract led to the isolation of the allelopathic principle, which turned out to be a mixture of the so-called "resin glycosides" of convolvulaceous plants. The structure of tricolorin A, the major phytogrowth inhibitor present in the active fraction, was elucidated as (11S)-hydroxyhexadecanoic acid 11-O-alpha-L-rhamnopyranosyl-(1-->3)-O-alpha-L-[2-O-(2S-methylbutyryl)-4 -O- (2S-methylbutyryl)] rhamnopyranosyl-(1-->2)-O-beta-D-glucopyranosyl-(1-->2)-beta-D-fucopyran oside- (1,3"-lactone)[1], based on chemical methods and spectral analysis including 1H-1H COSY, 1H-13CHETCOR, long range 1H-13C COLOC, and selective INEPT experiments. Bioassays showed that radicle elongation of the two weed seedlings tested was inhibited by tricolorin A [1] with IC50 values ranging from 12 to 37 microM. Staphylococcus aureus was sensitive to compound 1 with an MIC value of 1.8 micrograms/ml. Significant cytotoxic activity against cultured P-388 and human breast cancer cells (ED50 2.2 micrograms/ml) was demonstrated for compound 1, and it also inhibited phorbol 12,13-dibutyrate binding using calf brain homogenate as a source of protein kinase C (IC50 43 microM).

Cytotoxicity of Hymenocallis expansa alkaloids.

From the bulbs and leaves of Hymenocallis expansa (Amaryllidaceae), three alkaloid constituents were identified: (+)-tazettine, (+)-hippeastrine, and (-)-haemanthidine. These alkaloids demonstrated significant cytotoxicity when tested against a panel of human and murine tumor cell lines.

(-)-Roemerine, an aporphine alkaloid from Annona senegalensis that reverses the multidrug-resistance phenotype with cultured cells.

A known aporphine alkaloid, (-)-roemerine [1], isolated from the leaves of Annona senegalensis, was found to enhance the cytotoxic response mediated by vinblastine with multidrug-resistant KB-V1 cells. In the absence of vinblastine, no significant cytotoxicity was observed with KB-3 or KB-V1 cells (ED50 > 20 micrograms/ml), and several other human tumor cell lines were also relatively insensitive. As indicated by its ability to inhibit ATP-dependent [3H]vinblastine binding to multidrug-resistant KB-V1 cell membrane vesicles, (-)-roemerine appears to function by interacting with P-glycoprotein. In addition to alkaloid 1, three inactive compounds [the aporphine alkaloid(-)-isocorydine (reported in the levo-configuration for the first time), and the lignans (+/-)-8,8'-bisdihydrosiringenin [2] (a new natural product), and (+)-syringaresinol] were also isolated.

Cytotoxic constituents of Bursera permollis.

Four cytotoxic lignans were isolated from the stem bark of Bursera permollis (Burseraceae), namely, deoxypodophyllotoxin (1), beta-peltatin methyl ether (2), picro-beta-peltatin methyl ether (3), and dehydro-beta-peltatin methyl ether (4). Also isolated was the inactive lignan, nemerosin (5). Compounds 1 and 2 were potently cytotoxic when evaluated against a panel of human cancer cell lines.

Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea.

By means of activity-directed chromatographic fractionation using cultured astrocytoma (ASK) cells, six dibenzocyclo-octadiene lignans were isolated from Steganotaenia araliacea stem bark. In addition to the most abundant analogue, steganangin [1], two other known compounds, steganacin [3] and steganolide A [6], and three new compounds, episteganangin [2], steganoate A [4], and steganoate B [5], were obtained. Episteganangin [2] was chemically correlated with the known ketone steganone [7]. All of these compounds demonstrated cytotoxic activity when tested against a panel of eleven human tumor cell lines, with the exception of steganoate A [4]. The magnitude of this activity tended to correlate with antimitotic activity observed with the ASK assay and in vitro inhibition of microtubule assembly. Steganacin [3] was less cytotoxic than colchicine, but more active in these latter two assay systems.