The Anti-Serotonin Effect of Parthenolide Derivatives and Standardised Extract from the Leaves of Stizolophus balsamita

Abstract

The presence of dominant active compounds in standardised methanol extract from the leaves of Stizolophus balsamita (S. balsamita) was examined using HPLC with a diode-array detector. The extract and three dominant parthenolide derivatives were tested with Serotonin Research ELISA for their ability to inhibit the serotonin release from platelets. The antiserotonin effect of the extract was compared with that of parthenolide, a compound with proven antiserotonin and antimigraine effects. This study aimed to evaluate the ability of natural parthenolide derivatives to inhibit serotonin release from platelets. Izospiciformin, stizolin and stizolicin were analysed along with the standardised alcohol extract of S. balsamita leaves, which also contained four other parthenolide derivatives. All the analysed substances were found to inhibit serotonin release from platelets as compared with the control sample, which had 100% of serotonin released. Izospiciformin had the most significant impact (97.98% serotonin release inhibition). The effect of the methanol extract of S. balsamita on the serotonin release inhibition was also statistically significant.

Biologically Active Compounds in Stizolophus balsamita Inflorescences: Isolation, Phytochemical Characterization and Effects on the Skin Biophysical Parameters

“…They inhibit the release of 5-HT from platelets more effectively than parthenolide, and the izospiciformin ( 1 ) shows the most potent effect [ 42 ]. It is worth noticing that all isolated germacranolides, along with the three elements characteristic for a parthenolide (4,5-epoxide, lactone ring and exo-methylene), have an additional substituent on C-8, which significantly increases the potency of the antiserotonin effect compared to parthenolide [ 42 ]. Stizolicin ( 3 ) also has remarkable cytotoxic and antiparasitic activities [ 3 ].…”

Antifungal Activity of the Sesquiterpene Lactones from Psephellus bellus

“…The OH group signal at C-8 of compounds 11 and 12 was observed at 1.85 ppm. The characteristic signals indicated the presence of the 4α,15-epoxy group in compound 13 of oxirane protons (doublets of H-15 and H-15' at δ = 3.34 and 3.07 ppm with J (15, 15') = 4.2 Hz) [12][13][14]16,17,20]. The mixture of compounds 2-4 was identified using the TLC method (Figure 2).…”

“…Guaianolides are the most commonly appearing type of lactones [9]. Either in isolated form or extracts, they show broad biological properties, including anti-inflammatory, antibacterial, antiviral (including against SARS-CoV-2) [10], antihelminthic [11], and antimigraine [12] activities.…”

“…Cebellins L (1), O (2), K (3), N (4), A (11), and B (12) all have an ester on C-2. The characteristic features in the structure of these four guaianolides distinguish them from compounds occurring in the other Centaureinae plants.…”

“…The other nine sesquiterpene lactones from P. bellus are also lipophilic: 19-deoxychlorojanerin (5), 17,18-epoxy-19-deoxychlorojanerin (6), cebellin M (7), 8-desacyloxy-8α-(2methyloaryloxy)-subluteolide (8), repin (9), centaurepensin (10), cebellin A (11), cebellin B (12), and acroptilin (13).…”