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Lysine derivatives Alkaloids

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(1)

Lysine derivatives Alkaloids

• Drugs containing secondary metabolites with pyridine

and piperidine rings are Herba Lobelia and Cortex

Granati

• Lycopodium alkaloids are also derivatized fron lysine.

(2)

• Punica granatum (Punicaceae), cortex and roots and

branches. Inner side of barks is smooth and yellow.

• Plant contains volatile liquid alkaloids 0.5-0.9%.

• Major alkaloids are pelletierine and pseudopelletierine.

Cortex Radicis Granati (Nar Kök Kabuğu)

N

O

H

(3)

• Pelletierine and pseudopelletierine are antihelminthic. 22% of the bark consist of tannins.

• Barks are used to obtain pelletierine sulphate. • Because of the toxic effects, plant and

obtained salts are not used anymore for medicinal purposes.

(4)

Seed Oil

Increases the skin elasticity.

Topically anticancer activity

occurs.

Punica preparations

(5)

Pelletierine

tannate;

yellowish,

odourless,

amorphous powder with astringent effect.

Effective specifically against tapewarms, taenias.

Used only for adults (too toxic).

(6)

Lobelia inflata (Campanulaceae),

Herba collected in the end of flowering period.

Naturally grows in USA and Canada. Also cultivated in Netherlands.

Firstly used by American natives. (Indian Tobacco). In 1813 suggested to use in asthma.

Alkaloid ratio 0.2-0.4%.

L. nicotianaefolia is the official lobelia in India. Alkaloid amount is high in the flowering period.

(7)

Not less than 0.25-0.3 % alkaloid amount. (BP 1988)

In this type of alkaloids there are substituents in 2. and 6. C.

The structure can be symetrically or not.

Symetric Lobelidiol (alkol grubu), Lobelidion (keton grubu)

Non symetric Lobeline. 3 assymetric c atoms which means the optically activity. Lobinin N CH3 H5C2 O OH Lobelanin N CH3 O O

(8)

Herba Lobelia preparations;

Spasmodic

Used for asthma and chronic bronchitis

Takes place in the prepartions used to give up smoking. Controlled studies indicate that herba lobelia preparations are ineffective to give up smoking.

(9)

Lobeline slightly soluble in water, good soluble in alcohol.

Lobeline is a respiratory stimulant.

Lobeline HCl; injectable preparations (IM or SC) are used for respiratory stimulant. Used in respiratory problems in surgeries and especially for new born babies.

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