Forskolin Coleus Anti-tumor Active Ingredient And Its Fingerprint

Coleus forskohlii(Wild.)Briq.belongs to the Coleus genus of Labitae.The decoction of the plant is used in local folk medicine against cough,congestive cardiomyopathy,asthma,acute and chronic bronchitis, dizziness and fluster.Modern pharmacological researches have shown that Coleus forskohlii Briq.has good therapeutic efficacy against tumor metastasis,bronchial asthma,congestive heart failure and so on.We went on separating from active fraction of Coleus forstohlii and combined with the similar portion.Then got 10 fractions(Fra.A to Fra. J).Screened the anti-tumor activity fractions by MTT assay and Hela cell used as test object.The results showed that the Fra.G,Fra.H and Fra.J have significant anti-tumor activity.The IC₅₀value is 121μg·mL^-1,150μg·mL^-1,80μg·mL^-1respectively.14 compounds from active fractions were isolated and purified by chromatography and identified 11 of them.Their structures have been determined as demethylcryptojaponol(G1),β-sitosterol(G2),14-deoxy coleon U(H1),5α,8α-epidioxy-(22E,20S,24R)-ergosta-6,22-alien-3β-ol(H2),1α,6β,7β-triacetoxy-8,13-epoxylabd-14-en-11-one(J1),1α, 9α-dihydroxy-6β,7β-diacetoxy-8,13-epoxylabd-14-en-11-one(J3),1α, 9α-dihydroxy-6β,7α-diacetoxy-8,13-epoxylabd-14-en-11-one(J4),1α, 6β-diacetoxy-8,13-epoxylabd-14-en-11-one(J5),7β,9α-dihydroxy-1α, 6β-diacetoxy-8,13-epoxylabd-14-en-11-one(J8),medicarpin(J9),isoforskolin(J16).Medicarpin(J9)was found from HERBA LABITAE for the first time.The structures of compound 63,H3 and J10 are being further identified.Screen the anti-tumor activity constituent from the above compounds by MTT assay and A375 cells,Hela ceils and HCT-8 cells used as test objects.H1,H2,G1,J5,J9,J10 and G3 showed significant antitumor activity.To develop the fingerprint of Coleus forskohli,11 batches of samples were analyzed by ELSD-HPLC and 18 common peaks were found in the fingerprints.The technical parameters of the fingerprints are consistent with the requirements of "Chinese medicine injectables fingerprint reader technology requirements(provisional)" which promulgated by national food and medicines Authority.The analysis method has good credibility and stability.Compared the fingerprints of Coleus forskohli which contain different growing area and periods,the result showed significant differences.So it provided some scientific basis for evaluating the quality of Coleus forskohlii replanted in different condition.