Coleus forskolin extracts

Chemical composition
The chemical composition of Coleus forskohlii is diverse. At present, researchers have continuously discovered new chemical components in its roots, aerial parts and cultivated products. The isolated chemical components mainly include terpenes, flavonoids, sterols, volatile oils, etc. Terpenes are its main active ingredients.
1. Sesquiterpenes and monoterpenoid glycosides
α-Cedrol, Cuminyl-O-β-D-glucopyranosyl-(1-2)-β-D-galactop-yrano-side, Coleoside, 4β, 7β, 11-enantioeudesmantriol, Coleoside B.
2. Diterpenoid components
(1) Cynanchal diterpenes
Cynanchal diterpenes, also known as labdanane diterpenes, are the focus of research. The basic skeleton of its chemical structure is 8,13-epoxy-14-ene-11-one cynanchal diterpenes. Forskolin is its representative.
(2) Abietane-type diterpenes
Coleon S, Coleon T, 14-deoxycoleon U, Demethylcryptojaponol.
(3) Phytanes compounds
A phytanes compound, corcetin-dialdehyde, was isolated from Coleus forskohlii from India.
3. Triterpenoids
The triterpenoids isolated from Coleus forskohlii include: α-amyrin, Coleonolic acid, 3β,28-dihydroxy-12-ene-ursane, 2α,3β,19α-trihydroxyoleanolic acid-12-ene-28-acid (Arjunic acid), 2α,3β,19α,23-tetrahydroxyoleanolic acid-12-ene-28-acid (Arjunic acid), 2α,3α,19α-trihydroxyursane-12-ene-28-acid (Euscaphic acid), 2α,3α,19α,23-tetrahydroxyursane-12-ene-28-acid (Euscaphic acid), and Betulinic acid.
4. Flavonoids
A flavonoid compound, Genkwanin, was isolated from Coleus forskohlii.7 Sterol compounds include β-sitosterol, ergosterol-6,22-diene-5α,8α-epidioxy-3β-ol (ergosterol-5,8-peroxide), and ergosterol-6,9(11),22-triene-5α,8α-epidioxy-3β-ol.
5. Sterols
The sterols isolated from Coleus forskohlii mainly include β-sitosterol, carotene, stigmasterol, ergosterol-6,22,diene-5α,8α-cyclodioxy-3β-ol and ergosterol-6,9(11),22-triene-5α,8α-cyclodioxy-3β-ol.
6. Other compounds
Caffeic acid, guaiacol petroleum ether, rosmarinic acid, chamaecydin, colexanthone.
Introduction to characteristic chemical components: A diterpenoid substance extracted from the root of Coleus forskohlii, a plant of the Indian Lamiaceae family. Its chemical name is 7β-acetoxy-8,13α-epoxy-12,6β,9α-trihydroxy 14-ene-11-one diterpene. Named Forskolin, also known as Coleonol (Chinese name: Forskolin; Coleus; Forskolin), it is a useful experimental tool drug that has a strong and specific stimulating effect on the adenylate cyclase of eukaryotic cells, thereby increasing the concentration of cAMP.
Pharmacological effects
1. Effect of reducing intraocular pressure
The basic and clinical pharmacological studies on the three forskolin analogs isolated from Coleus forskohlii, isoforskolin, deacetylforskolin and 1-acetyl-forskolin, showed that the three compounds all have in vitro cyclic adenosine monophosphate activation activity, and can reduce normal rabbit intraocular pressure or inhibit high intraocular pressure in water-loaded rabbits to varying degrees. It is speculated that 1-acetylforksolin is active after metabolism in vivo.
2. Antiasthmatic and antispasmodic effect
Ethyl acetate extract of Coleus forskohlii has a strong antiasthmatic and antispasmodic effect. The antiasthmatic pharmacodynamics and acute toxicity experiments were analyzed and evaluated. The results showed that its antispasmodic potency is 145 times that of aminophylline, while its toxicity is much lower than that of aminophylline.
3. Antihypertensive effect
1-acetoxyforskolin and isofroskolin extracted from Coleus forskohlii can effectively reduce the blood pressure of anesthetized rats, and the effect is rapid and lasting, showing a dose-dependent relationship, while there is no significant effect on parameters such as heart rate or no statistically significant difference. However, whether it has more advantages than the currently widely used clinical first-line antihypertensive drugs needs further verification.
4. Inhibition of platelet aggregation
Isoforskolin can inhibit ADP, and the inhibitory effect has no obvious selectivity for the three platelet activation pathways. Its mechanism of action may be related to the direct activation of adenylate cyclase by isoforskolin and the increase of cAMP levels in platelets. Its anticoagulant effect and bleeding risk need further evaluation and investigation.
5. Anti-tumor effect
The extract of Coleus forskohlii has significant anti-tumor activity. It is reported that the research on its anti-tumor effect is focused on forskolin, and similar effects of other ingredients have not been reported. Forskolin can significantly increase the activity of cellular adenylate cyclase and the accumulation of cAMP, and the maintenance of cAMP levels can effectively regulate cell proliferation and differentiation.
Clinical application
1. Application history
It has a long history of use. In India, the whole herb is decocted and taken for the treatment of colds, coughs and respiratory diseases, etc., with significant efficacy. Ancient India called it a "panacea".
2. Modern clinical application
(1) Treatment of asthma and acute and chronic bronchitis
The compound granules made of Coleus forskohlii combined with Peucedanum chinense and Licorice are used to treat asthma and bronchitis with good efficacy. In addition, they have good antipyretic effect, no significant effect on important organs and blood system, and no serious adverse reactions. A clinical study on the treatment of pediatric bronchial asthma with the compound coleus granules made with Coleus forskohlii as the main drug found that the plasma cAMP concentration increased significantly after 1 week of use, with statistical significance. It is highly effective and low toxic, and can quickly relieve cough and asthma. It is an effective drug for the treatment of asthma.
(2) Treatment of lung heat disease
The compound coleus granules made of Coleus forskohlii combined with Peucedanum chinense, Apricot kernel and other Chinese medicines were used to treat 35 cases of acute lung heat syndrome, and compared with the Chinese patent medicine Xiaokechuan syrup. The results showed that its treatment efficiency reached 91.43%, which was better than the control group. In addition, it also had a certain effect on acute bronchitis and asthma, indicating that the compound preparation has a good effect on lung diseases.
Safety investigation
The acute toxicity of Coleus Forskohlii oral liquid to mice, the long-term toxicity to rats, and the general pharmacology of rabbits were studied. No one died at the end of the experiment after oral administration of high, medium and low doses. Autopsy and histopathological microscopy showed no significant difference from the control group. Cage-side symptoms, growth weight, hematological indicators, and blood sugar, liver and kidney functions were all normal. At normal doses, there was no significant effect on the respiratory, circulatory and nervous system functions of anesthetized rabbits, indicating that the oral liquid of Coleus Forskohlii is safe.