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Apiaceae Plants Growing in the East
Published in Mahendra Rai, Shandesh Bhattarai, Chistiane M. Feitosa, Ethnopharmacology of Wild Plants, 2021
Sherweit El-Ahmady, Nehal Ibrahim, Nermeen Farag, Sara Gabr
Twelve polyacetylenes were isolated from carrot, where falcarinol, falcarindiol and falcarindiol-3-acetate are the essential ones predominately found in the roots. The other nine polyacetylenes isolated are: (E)-isofalcarinolone, falcarindiol-8-acetate, 1,2-dihydrofalcarindiol-3-acetate, (E)-falcarindiolone-8-acetate, (E)-falcarindiolone-9-acetate, 1,2-dihydrofalcarindiol, (E)-1-methoxyfalcarindiolone-8-acetate, (E)-1-methoxy-falcarindiolone-9-acetate, and panaxydiol (Schmiech et al. 2009, Dawid et al. 2015). Their distribution has been shown to be linked to the cultivars and the concentration of polyacetylenes found, maybe 10–20 times more in wild type of carrots than domesticated carrots (Pferschy-Wenzig et al. 2009, Dawid et al. 2015).
Inhibiting Insulin Resistance and Accumulation of Triglycerides and Cholesterol in the Liver
Published in Christophe Wiart, Medicinal Plants in Asia for Metabolic Syndrome, 2017
Ethylacetate extract of Oenanthe javanica (Blume) DC. (Figure 3.29) given to spontaneous type 2 diabetic Goto–Kakizaki rats at a single oral dose improved glucose tolerance in oral glucose tolerance at 90 minutes.373 From this extract, the polyacetylene falcarindiol inhibited the expression of glucose-6 phosphatase, (the rate-controlling enzyme of gluconeogenesis), as well as glycogen synthetase kinase 3β in H4IIE rat hepatoma at a concentration of 50 µM.373 It must be recalled that insulin binding to its hepatic receptor induced the inhibition of glucose-6 phosphatase and glycogen synthetase kinase-3β to command glycogen synthesis.374 It would be of interest to examine the protective effect of falcarindiol on hepatic insulin signaling.
Schefflera Genus (Araliaceae)
Published in Parimelazhagan Thangaraj, Medicinal Plants, 2018
Puthanpura Sasidharan Sreeja, Karuppusamy Arunachalam, Parimelazhagan Thangaraj
The two lupane type triterpenoid saponins, 3β-O-(α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranosyl)-lup-20(29)-ene-28-O-β-D-glucopyranosyl ester and 3β-O-α-L-arabinopyranosyl-lup-20(29)-ene-28-O-β-D-glucopyranosyl ester, were isolated from S. rotundifolia to inhibit proliferation activity for J774.A1, HEK-293 and WEHI-164 cells (Braca et al. 2004). But the oleanane type triterpenoid saponins 3β-O-[β-D-glucopyranosyl-(1→2)-β-D-glucopyranosyl-(1→3)-β-D-xylopyranosyl)-16α-hydroxyolean-12-en-28-O-(β-D-galactopyranosyl) ester-30-oic acid and 3β-O-[β-D-glucopyranosyl-(1→3)-β-D-xylopyranosyl)-16α-hydroxyolean-12-en-28-O-(β-D-galactopyranosyl) ester-30-oic acid isolated from S. faguetigueti possesses significantly more inhibitory proliferative activity for these three cell lines (Cioffi et al. 2003). Falcarindiol; C18-acetylenverbindung; 3α-hydroxyoleane-12; 28-dioic acid methyl ester (methyl ester 22); 3α-hydroxylup-20(29)-ene-23; 28-dioic acid methyl ester; a mixture of γ-tocopherol, docosyl and tetracosyl; 4-hydroxy-trans-cinnamate of docosyl and tetracosyl; and a mixture of hexacosyl 4-hydroxy-cis-cinnamate were obtained from S. taiwaniana and shows inhibitory activity towards the HUGC, HONE1 cell to a certain extent and t-murrolol possess significant cytotoxic activity against A-549 (EC50 3.2 μg/mL), MCF (EC50 0.6 μg/mL) and HT-29 cells (EC50 1.8 μg/mL) (Kuo et al. 2002). Liu et al. (2005) found that the Chrysophanol, 2, 6-dimethoxy-p-benzoquinone separated from the dense pulse S. venulosa, and could inhibit K562 cells, thus showing a value-added activity, and separated ten palmitic acid also inhibits the proliferation activity on FT210 cells. Yao et al. (2009) found that the essential oil of S. heptaphylla possessed significant antiproliferative activity against the human cancer cell lines MCF-7, A375 and HepG2 cells.
Synergetic Inhibition of Human Colorectal Cancer Cells by Combining Polyyne-Enriched Fraction from Oplopanax elatus and Irinotecan
Published in Nutrition and Cancer, 2019
Jin Wang, Li Shao, Chong-Zhi Wang, Hong-Hao Zhou, Chun-Su Yuan, Wei-Hua Huang
Caspase family proteases have been considered as a key factor of apoptosis (26,27). It’s reported that falcarindiol, one of main polyynes from O. elatus, could induce cancer cells death partly by caspase-dependent apoptosis (17). Caspase-3, which targeted main regulatory and structural proteins for proteolysis to promote apoptosis, has been identified as a key mediator of apoptosis (28–30). When intracellular caspase-3 is activated, cells enter into the process of irreversible apoptosis (31–33). In order to confirm whether the apoptotic effects induced by irinotecan and OED were mediated by the caspase-3, we evaluated its expression by western-blot assay. The results showed that caspase-3 was activated and turned into cleaved-caspase-3 after treatment with irinotecan or OED. Besides, compared with treatment with irinotecan or OED group, the expression of cleaved-caspase-3 of OCI group was significantly increased. Moreover, the apoptotic effects of OED or/and irinotecan declined after inhibition of caspase-3. Therefore, OED could mostly enhance SW-480 cells apoptosis induced by irinotecan by regulating the activity of caspase-3. However, the detailed mechanism of how the OED regulated the activation of caspase-3 to promote pro-apoptotic effects of irinotecan needs further exploration.
Devil’s Club Falcarinol-Type Polyacetylenes Inhibit Pancreatic Cancer Cell Proliferation
Published in Nutrition and Cancer, 2019
Susan S. C. Cheung, David Hasman, Djamel Khelifi, Joseph Tai, Richard W. Smith, Garth L. Warnock
Natural falcarinol-type (FC-type) polyacetylenes are present in many herbs and root crops, with FC being the most common of the C17 polyacetylenes found in carrot, celery, parsnip, and in several well-known medicinal herbs including ginseng (1). FC’s anticancer activity has been studied in Dendropanax arboreus (2), Saposhnikovae divaricata (3), celery (4), carrot (5), and Panax notoginseng (6). Presence of FC-type polyacetylenes has also been reported in the root bark (7) and inner stem (8) of Devil’s club (DC) Oplopanax horridus. Because of its presence in common vegetable groups, bioactivity studies of FC have largely focused on its antioxidant properties, health benefits, and chemoprevention aspects (9). Recently, it was observed that one of DC’s bioactive polyacetylenes, DCA (9,17-octadecadiene-12,14-diyne-1,11,16-triol,1-acetate), effectively inhibited human pancreatic cancer cell proliferation in monolayer as well as in spheroid culture (10,11). In addition, two other FC-type polyacetylenes, falcarindiol, and oplopantriol A, from DC were also reported to show potent growth inhibition of human breast and colon cancer cells (12–14). With the availability of synthetic protocols for compounds such as FC and 1,2-dihydrofalcarinol (FCH) (15), also known as panaxjapyne, this study investigated the antiproliferation activity of FC-type C17 polyacetylenes on human pancreatic cancer cell lines using synthetic instead of isolated compounds.
Quorum sensing inhibitors: a patent review (2014–2018)
Published in Expert Opinion on Therapeutic Patents, 2018
Xin Chen, Likun Zhang, Mingxiang Zhang, Huayu Liu, Panrui Lu, Kejiang Lin
Falcarindiol is a polyacetylene compound found in Umbelliferae and Araliaceae plants that exhibited a potent inhibitory effect on Gram-positive bacteria, such as S. aureus, and an attenuated effect on Gram-negative strains. Yu et al. disclosed that falcarindiol could inhibit QS under sub-inhibitory concentrations without killing the microorganisms directly. They revealed that 12.5 μM of falcarindiol was sufficient to inhibit the production of the PQS signal in P. aeruginosa which regulates the expression of downstream virulence genes, and 20 μM of falcarindiol inhibited 60% of biofilm formation in P. aeruginosa. It was also reported that the V. harveyi emission behavior was also suppressed with 26 μg/mL falcarindiol [117].