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Labdanum resin from Cistus ladanifer L. as a source of compounds with anti-diabetic, neuroprotective and anti-proliferative activity
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Advisor(s)
Abstract(s)
Labdanum resin or “gum” can be obtained from Cistus ladanifer L. by two different extraction methods: the Zamorean and the Andalusian processes. Although its main use is in the fragrance
and perfumery sectors, ethnobotanical reports describe its use for medicinal purposes in managing
hyperglycemia and mental illnesses. However, data concerning the bioactivities and pharmacological applications are scarce. In this work, it was found that the yield of labdanum resin extracted
by the Andalusian process was 25-fold higher than the Zamorean one. Both resins were purified
as absolutes, and the Andalusian absolute was purified into diterpenoid and flavonoid fractions.
GC-EI-MS analysis confirmed the presence of phenylpropanoids, labdane-type diterpenoids, and
methylated flavonoids, which are already described in the literature, but revealed other compounds,
and showed that the different extracts presented distinct chemical profile. The potential antidiabetic
activity, by inhibition of α-amylase and α-glucosidase, and the potential neuroprotective activity,
by inhibition of acetylcholinesterase, were investigated. Diterpenoid fraction produced the higher
α-amylase inhibitory effect (~30% and ~40% at 0.5 and 1 mg/mL, respectively). Zamorean absolute
showed the highest α-glucosidase inhibitory effect (~14% and ~24%, at 0.5 and 1 mg/mL, respectively). Andalusian absolute showed the highest acetylcholinesterase inhibitory effect (~70% and
~75%, at 0.5 and 1 mg/mL, respectively). Using Caco-2 and HepG2 cell lines, Andalusian absolute
and its purified fractions showed moderate cytotoxic/anti-proliferative activity at 24 h exposure
(IC50 = 45–70 µg/mL, for Caco-2; IC50 = 60–80 µg/mL, for HepG2), whereas Zamorean absolute did
not produce cytotoxicity (IC50 ≥ 200.00 µg/mL). Here we show, for the first time, that labdanum
resin obtained by the Andalusian process, and its fractions, are composed of phytochemicals with
anti-diabetic, neuroprotective and anti-proliferative potential, which are worth investigating for
the pharmaceutical industry. However, toxic side-effects must also be addressed when using these
products by ingestion, as done traditionally.
Description
Keywords
α-amylase α-glucosidase Acetylcholinesterase Cytotoxic activity Labdanum resin Labdane-type diterpenoids Methylated flavonoids
Citation
FRAZÃO, David F. [et al.] (2024) - Labdanum resin from Cistus ladanifer L. as a source of compounds with anti-diabetic, neuroprotective and anti-proliferative activity. Molecules. N.º 29, 2222. DOI: https://doi.org/10.3390/molecules29102222