لخّصلي

Bitter principles are a diverse group of non-alkaloid, non-glycoside natural products characterized by their bitter taste. Traditionally used as appetite stimulants before meals, they encompass various chemical classes including phenolics, lactones, furanochromones, and furanocoumarins. Examples include humulone and lupulone (hops), with sedative effects; santonin (Artemisia cina), an effective anthelmintic against roundworms; artemisinin (Artemisia annua), a potent antimalarial active against chloroquine-resistant strains and effective against cerebral malaria due to high lipid solubility; and elephantopin (Elephantopus elatus), exhibiting antitumor activity (e.g., against leukemia). Santonin's chemical test involves a violet-red color change with alcoholic KOH. Artemisinin's antimalarial activity relies on its endoperoxide moiety.

Bitter Principles
A group of natural products which are non-
homogenous from the chemical point of view, they
have in common a bitter taste and are neither alkaloids
nor glycosides. They traditionally used in liquid
medicaments to stimulate appetite and are usually
administered before meals.
They belong to different chemical groups such as:
• Phenolics
• Lactones
• Furanochromones
• Furanocoumarins
• Other bitter principles
I- Phenolic bitter principles
1- Humulone & Lupulone
isopentene
Occurrence: In Hops (Humulus lupulus) Family Cannabinaceae
Uses: Humulone and lupulone have sedative effect
II- Lactone bitter principles
1- Santonin
Occurrence: Santonica “dried unexpanded flower heads of
Artemisia cina, F. Compositae.
Chemical test:
When santonin is warmed with alcoholic KOH, it gives a violet red
colour.
Uses: Anthelmintic, very efficient
against round worms (Ascariasis), with
less effect on thread worms
4
2- Artemisinin
• Occurrence: ″Artemisia flower″ dried unexpanded flower heads of
Artemisia annuna, Family: Compositae.
• Uses: Animalarial, equal in potency to chloroquine. The presence of
an endoperoxide moiety is essential for its antimalarial activity.
• There are two reasons for the great interest of artemisinin and its
derivatives:
a- Active against chloroquine resistant strains of Plasmodium
falciparum.
b- The high lipid solubility ensures rapid penetration into CNS; so,
it’s a first-line drug for the treatment of fatal cerebral malaria.
3. Elephantopin
• Occurrence: Elephantopus elatus, family:
Compositae.
• Uses: Antitumor agent (against leukemia).
• N.B. Elephantopin is a sesquiterpene lactone
containing two lactone rings and an epoxide function
(cyclic ether).