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Ber and other Jujubes monograph.pdf - Crops for the Future

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<strong>and</strong> Halpern, 1983). The mechanism which ziziphin used was identified as taste<br />

modification. On comparison with known gymnemic acids, effects suggest that<br />

net dissociation of ziziphins from taste receptor membranes <strong>and</strong>/or inactivation<br />

in <strong>the</strong> membrane may be much faster than with gymnemic acids. The<br />

compound is considered useful as a taste modifier resulting in reduced sugar<br />

intake <strong>and</strong> <strong>the</strong>reby reducing obesity in diabetic or overweight people (Suttisri et<br />

al., 1995).<br />

2.4.2 Permeability enhancement activity<br />

Delivery of certain classes of drugs such as peptides creates problems in<br />

transportation across cell membranes <strong>and</strong> subsequent diminished<br />

bioavailability. To overcome this barrier, permeability enhancers can be used to<br />

aid <strong>the</strong> passage of drugs across cell membranes. To assess <strong>the</strong> permeability<br />

enhancing activity of Z. jujuba, an aqueous extract of seeds was compared to<br />

two members of a known series of permeability enhancement agents belonging<br />

to <strong>the</strong> alkylglycosides. Cell culture systems were observed after transepi<strong>the</strong>lial<br />

electrical resistance (TEER) recorded <strong>the</strong> results of application of <strong>the</strong> three<br />

agents <strong>and</strong> changes in cell monolayer resistance. Lowering of resistance across<br />

a cell monolayer is an indication of ei<strong>the</strong>r <strong>the</strong> opening of tight junctions <strong>and</strong>/or<br />

<strong>the</strong> fluidisation of cell membranes. Z. jujuba extract lowered cell resistance<br />

more rapidly in a given time period than <strong>the</strong> alkylglycosides <strong>and</strong> allowed full<br />

recovery of cells in a relatively short time period. It appears that <strong>the</strong> extract of<br />

Z. jujuba may be more efficient as a permeability enhancer than <strong>the</strong> two<br />

alkylglycosides. It remains to fur<strong>the</strong>r analyse <strong>the</strong> extract to determine <strong>the</strong> active<br />

agent or agents (Eley <strong>and</strong> Hossein, 2002).<br />

2.4.3 Cytotoxic effect (chem<strong>o<strong>the</strong>r</strong>apy)<br />

The in vitro cytotoxicities of <strong>the</strong> triterpenoic acids extracted from Z. jujuba<br />

were tested against tumour cell lines . The lupane-type triterpenes showed high<br />

cytotoxic activities. The cytotoxic activities of 3-O-p- coumaroylalphitolic<br />

acids were found to be better than those of non-coumaroic triterpenenoids.<br />

These results suggest that <strong>the</strong> coumaroyl moiety at <strong>the</strong> C-3 position of <strong>the</strong><br />

lupane-type triterpene may play an important role in enhancing cytotoxic<br />

activity (Lee et al., 2003).<br />

The triterponic acid, betulinic acid, extracted from Z. jujuba <strong>and</strong> Z. mauritiana,<br />

showed selective toxicity against cultured human melanoma cells (Kim et al.,<br />

1998). Betulinic acid is currently undergoing preclinical development (Pisha et<br />

al., 1995). It is thought that betulinic acid may also be effective against <strong>o<strong>the</strong>r</strong><br />

types of cancer. Recently, considerable in vitro evidence has demonstrated that<br />

betulinic acid is effective against small- <strong>and</strong> non-small-cell lung, ovarian,<br />

cervical, <strong>and</strong> head <strong>and</strong> neck carcinomas. Published data suggest that betulinic<br />

acid induces apoptosis (Kim et al., 1998; Liu et al., 2004) in sensitive cells in a<br />

p53- <strong>and</strong> CD95-independent fashion (Eiznhamer <strong>and</strong> Xu, 2004).<br />

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