Antihistamine and antiinflammatory activities of barbaloin

Organic Health Protocol

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Inhibitory effect (ID 50) of barbaloin on antigen (dinitrophenyl-bovine serum albumin) and compound 48/80-induced histamine from mast cells degranulation was shown to

Aloe Vera Anatomy Images

Figure 14.1 Structure of barbaloin, aloesin and aloenin.

Aloenin 0ch3

Figure 14.1 Structure of barbaloin, aloesin and aloenin.

be 0.02 and 0.06mg/ml, respectively, and barbaloin was focused as an important constituent in Kidachi aloe. Anti-inflammatory activity of barbaloin was exhibited by the monitoring of carrageenin-induced edema in rats and 28.8% inhibition was reported, while that of indomethacin was 48.2% (Yamamoto etal., 1991).

Structure of aloesin esters

In a course of study on cathartic components, aloeresin together with barbaloin was shown to be antibiotic. Aloeresin was hydrolyzed into p-coumaric acid, ferulic acid and aloesin. Aloeresin A indicated a p-coumaroyl group located at C-2" position in aloesin (Makino etal, 1974). Since then, a series of aloesin and aloesol (which is hydrogenated at a ketone group in aloesin), was isolated from A. vera leaf extract, and isoaloeresin D showed anti-inflammatory and antioxidative activities (Hutter etal, 1996; Lee etal, 2000).

Skin-whitening aloesin esters

It is well known that Kidachi aloe extract shows skin-whitening activity and the active component is barbaloin. Recently, aloesin esters as well as barbaloin, were found as the active inhibitory components against mushroom tyrosinase, which converts tyrosine into melanin. The active components were determined to feruloyl- and ^-coumaroyl aloesin (Yagi etal, 1987a). The skin-whitening activity of semi-synthetic aloesin derivatives was demonstrated by monitoring on rat melanoma cells (KB cells) and in clinical tests (Jones, 1999).

Structure of aloenin and its dermatological studies

As one of the phenolic constituents in Kidachi aloe extract, aloenin (O-glycoside of a substituted phenylpyran-2-one) was isolated (Hirata and Suga, 1977). Aloenin was found in 12% of all Aloe species, particularly in Section Eualoe, subsection Magnae and Grandes, and utilized as a marker substance of Kidachi aloe preparations in JHNFA. Aloenin promoted hair growth in depilated mice and had recuperative effects on tape-stripped human skin as determined from parameters such as shape factor of corneocytes, thick abrasion, nuclear ghosts and cellular arrangement of corneocytes. Administration of aloenin before the carragenin-induced rat inflammatory edema by interperitoneal route inhibited swelling by 41.7% (Yamamoto etal, 1993).

Acceleration of gastric secretion by barbaloin

Effect of Kidachi aloe extract on the gastric secretion in rats after pyloric ligation was examined by oral administration of the powder, mainly contained barbaloin. The results showed that powdered aloe leaf significantly increased total acid amount and acid output in gastric secretion, suggesting gastrostimulating activity of the extract (Tanizawa etal, 1980).

Antihistamine activity of aloeulcin

The chemical properties and inhibition on histamine synthetic enzyme of a new substance, aloeulcin, were demonstrated. The action of aloeulcin, which was fractionated by ethanol-precipitation followed by chromatographical separation, was observed in both in vitro and in vivo experiments (Yamamoto, 1970).

Gastrointestinal function of aloeulcin

Aloeulcin, a new principle of Cape aloe (corrected to Kidachi aloe by author), and its gastrointestinal function, was demonstrated and aloeulcin inhibited gastric secretion, ulcer index and pH, on the L-histamine-induced aggravation of Shay rat's ulcer (Yamamoto, 1973).

Anti-inflammatory active components

The effect of aloenin, barbaloin and aloe extract was demonstrated on mast cell degranulation and porcine platelet aggregation. Barbaloin showed inhibitory activity on histamine released from mast cells induced by compound 48/80 at a concentration of lpg/ml, IC50 of barbaloin was about 40pg/ml (Nakagome etal., 1986).

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Aloe and Your Health

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