The Hidden Treasure in Europe?s Garden Plants: Case Examples; Berberis darwinni and Berginia cordifolia

The Quest to Enhance the Efficacy of Berberine for Type-2 Diabetes and Associated Diseases: Physicochemical Modification Approaches

“…They showed that both berberine and nandinine could inhibit serine phosphorylation of insulin receptor substrate-1 induced by IκB kinase β and increased tyrosine phosphorylation of insulin receptor substrate-1 to activate the phosphatidylinositol-3 kinase/protein kinase B (PI3K/Akt) pathway, which finally led to increased insulin-mediated glucose uptake. The compound (22) also increased the AMPK activity and could offer anti-inflammatory effect as it inhibits NF-κB activation. In mice, both berberine and nandinine at the doses of 100 or 200 mg/kg could abolish glucose intolerance and they enhance insulin sensitivity [117].…”

“…In the study by Zhao et al [117], which employed the macrophage-derived conditioned medium in 3T3-L1 adipocytes, dysregulation of adipokine production and activation of the IκB kinase β/NF-κB pathway was induced. Using this model, they performed a comparative analysis of berberine and nandinine (tetrahydroberberrubine) (22) (Figure 5) on the regulation of insulin sensitivity in adipocytes. They showed that both berberine and nandinine could inhibit serine phosphorylation of insulin receptor substrate-1 induced by IκB kinase β and increased tyrosine phosphorylation of insulin receptor substrate-1 to activate the phosphatidylinositol-3 kinase/protein kinase B (PI3K/Akt) pathway, which finally led to increased insulin-mediated glucose uptake.…”

“…For example, it can suppress the expression of hepatocyte nuclear factor-4α (HNF-4α) and the microRNA miR122, which are linked to lipid and glucose metabolism [19]. As a major source of berberine, the stems and roots of Berberis aristata [20,21], B. darwinii [22,23], B. Petiolaris [24] and B. vulgaris [25] have been extensively investigated. Numerous other high berberine-yielding medicinal plants have further been reported with the most famous being Coptis chinensis (Chinese goldthread) and related species and Hydrastis Canadensis or goldenseal.…”

Recent Advances in Berberine Inspired Anticancer Approaches: From Drug Combination to Novel Formulation Technology and Derivatization

“…Berberine (1, Figure 1) is a quaternary isoquinoline alkaloid of natural origin that has been known to show diverse pharmacological effects. As a principal component of plants, berberine has been isolated from the stems and roots of Berberis species including B. aristata [1,2], B. darwinii [3,4], B. petiolaris [5] and B. vulgaris [6]. Two famous plants of medicinal significance and dietary supplements which also attribute their pharmacological effects to berberine and related compounds are Chinese goldthread (Coptis chinensis) [7] and goldenseal (Hydrastis canadensis) [8,9].…”

“…) of which compound 23 (9-(3-bromopropoxy)-10-methoxy-5,6-dihydro-[1,3]dioxolo[4,5-g]isoquino [3,2-a]isoquinolin-7-ylium bromide) was the most active against HeLa and HL-60 cell growth in vitro. With IC 50 values of these compounds range from 0.7 to 16.7 µM for HL-60 cells and 36 to > 200 µM for HeLa cells (48 h), the prototype compound 23 was shown to induce cell cycle arrest at G2/M and S phases with 30-fold superior antiproliferative activity (IC 50 value of 0.7 µM) and 6-fold higher apoptosis-inducing activity in HL-60 leukaemia cells than berberine.…”