Berberine: a comprehensive Approach to combat human maladies

Figures & data

Figure 1. Chemical structure of berberine.

Table 1. The impact of BBR on the induction of cell cycle arrest in distinct cancer cell types.

Cancer type	Cell line	Effect
Osteosarcoma	Saos-2HOSU2OS	Cell cycle arrest in G1/S phase of P53 presenting cell. Cell cycle arrest in the G2/M phase of P53 deficient cell.
Colorectal adenocarcinoma	LOVOSW620	Cell cycle arrest in G2/M phase by cdc2, cyclin B1, cdc25c, cdc2 inhibition
Leukemia	JurkatL1 210	Cell cycle arrest in G0/G1 phase 101 Cell cycle arrest in G0/G1 phase Increase in G2/M phase, Decrease in S-phase
Glioblastoma	U343U251U87	Cell cycle arrest in the G2 phase Cell cycle arrest in the G1 phase by CDK2, cyclin D, E, and CDK4 inhibition Increase in p27Kip1
Ovarian cancer	OVCAR3	Cell cycle arrest in G0/G1 phase by cyclin D1 inhibition

Figure 2. Anticancer mechanisms associated with berberine.

Figure 3. Synthetic depiction of berberine derivatives.

Table 2. Effect of BBR on blood lipid profiles.

Sr. no.	Test Subjects	BBR Dose, Freq., Time	Results
1.	Hyper-lipidemic subjects	0.2 g/d, once daily, 12 wk	Non-HDL-C (−15%), LDL-C (−19%)
2.	Moderately Hyper-cholesterolemic subjects	500 mg/d, once a day, 12 wk	TC (−5%), LDL-C (−7.8%)
3.	Hyper-cholesterolemic patients	1 g/d, twice daily, 2 months	TC (−21.8%), LDL-C (−23.8%)
4.	Dyslipidemic patients	500 mg/d, once daily, 16 wk	TC (−10%), LDL-C (−13%), HDL-C (+8%)
5.	Elderly (>75 years) hypercholesterolemic patients	500 mg/d, once daily, 12 Months	TC (−20%), LDL-C (−31%)

*TC = total cholesterol, HDL-C = high-density lipoprotein cholesterol, LDL-C = low-density lipoprotein cholesterol

Table 3. The use of BBR to treat systemic inflammation.

Target Subject	Treatment	Effect	Conclusion
Intestinal epithelial barrier dysfunction associated with atherosclerosis	Berberine in water (0.5 g per liter), 14 weeks	Prevention of inflammation in intestines; promoted intestinal epithelial barrier strength. The reinstated thickness of the mucus layer.	Berberine controls gut microbiota, which may add to metabolic protection.
Intestinal glucose and lipid metabolism	Berberine 120 mg and 240 mg/(kg*d), 6 weeks	Reduces FBG and FINS and restored oral glucose tolerance; up-regulated GLP-1 receptor and down-regulated GnRH and GnRH receptor expression in the ileum.	BBR improved GnRH-GLP-1 pathways in the ileum.
Intestinal disaccharide metabolism	In vivo: BBR 100 mg and 200 mg /(kg*d) for 5 weeks; In vitro: BBR 10 μmol/L and 50 μmol/L.	In vivo: restored serum insulin level; decreased sucrase and maltase activity and SI complex expression in the small intestine; In vitro: inhibited sucrase and maltase activity, which was suppressed by H-89 (PKA inhibitor).	BBR suppressed disaccharidase activity and SI complex mRNA expression, which has beneficial metabolic effects.
Intestinal barrier dysfunctions	BBR 100 mg per kg for 2 weeks	Enhanced insulin resistance; restored intestinal mucosa structure; restored glutamine-induced GLP-2 secretion from the ileum	BBR treatment enhances GLP2 secretion and restores intestinal functions in T2DM

*FBG: fasting blood glucose; FINS: fasting insulin; GnRH: gonadotropin-releasing hormone; PKA: protein kinase A; SI complex: sucrase-isomaltase complex; T2DM: type 2 diabetes mellitus; GLP: glucagon-like peptide.