Berberine, a plant alkaloid with lipid- and glucose-lowering properties: From in vitro evidence to clinical studies

Pirillo, Angela; Catapano, Alberico L.

doi:10.1016/j.atherosclerosis.2015.09.032

Cited by 265 publications

(171 citation statements)

References 129 publications

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“…It has been well documented that BBR is poorly absorbed via gastrointestinal administration, yet it shows a positive effect on hypolipidemia and hypoglycemia [34] . As the primary metabolite of BBR, few studies have focused on the pharmacological effects of BRB.…”

Section: Discussionmentioning

confidence: 99%

In vitro assessment of the glucose-lowering effects of berberrubine-9-O-β-D-glucuronide, an active metabolite of berberrubine

et al. 2017

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Berberrubine (BRB) is the primary metabolite of berberine (BBR) that has shown a stronger glucose-lowering effect than BBR in vivo. On the other hand, BRB is quickly and extensively metabolized into berberrubine-9-O-β-D-glucuronide (BRBG) in rats after oral administration. In this study we compared the pharmacokinetic properties of BRB and BRBG in rats, and explored the mechanisms underlying their glucose-lowering activities. C57BL/6 mice with HFD-induced hyperglycemia were administered BRB (50 mg· kg -1 ·d -1 , ig) for 6 weeks, which caused greater reduction in the plasma glucose levels than those caused by BBR (120 mg· kg -1 ·d -1 ) or BRB (25 mg· kg -1 ·d -1 ). In addition, BRB dose-dependently decreased the activity of α-glucosidase in gut of the mice. After oral administration of BRB in rats, the exposures of BRBG in plasma at 3 different dosages (10, 40, 80 mg/kg) and in urine at different time intervals (0-4, 4-10, 10-24 h) were dramatically greater than those of BRB. In order to determine the effectiveness of BRBG in reducing glucose levels, we prepared BRBG from the urine pool of rats, and identified and confirmed it through LC-MS-IT-TOF and NMR spectra. In human normal liver cell line L-O2 in vitro, treatment with BRB or BRBG (5, 20, 50 μmol/L) increased glucose consumption, enhanced glycogenesis, stimulated the uptake of the glucose analog 2-NBDG, and modulated the mRNA levels of glucose-6-phosphatase and hexokinase. However, both BBR and BRB improved 2-NBDG uptake in insulin-resistant L-O2 cells, while BRBG has no effect. In conclusion, BRB exerts a stronger glucose-lowering effect than BBR in HFD-induced hyperglycemia mice. Although BRB significantly stimulated the insulin sensitivity and glycolysis in vitro, BRBG may have a greater contribution to the glucose-lowering effect because it has much greater system exposure than BRB after oral administration of BRB. The results suggest that BRBG is a potential agent for reducing glucose levels.

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Section: Discussionmentioning

confidence: 99%

In vitro assessment of the glucose-lowering effects of berberrubine-9-O-β-D-glucuronide, an active metabolite of berberrubine

et al. 2017

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“…Although the low bioavailability [20] limited its wide use in clinical practice, berberine is already studied in a lot of clinical studies due to its various effects including lipid-lowering [21], changing the blood concentration of cyclosporin A in renal transplanted recipients [22], improving insulin resistance in type 2 diabetes mellitus patients [23,24], and ameliorating inflammation in patients with acute coronary syndrome [25]. Several studies have reported that berberine exerts its beneficial effects in diabetic nephropathy (DN) through the suppression of OS and ERS [26,27].…”

Section: Introductionmentioning

confidence: 99%

Berberine Improved Aldo-Induced Podocyte Injury via Inhibiting Oxidative Stress and Endoplasmic Reticulum Stress Pathways both In Vivo and In Vitro

Wang¹,

Xu²,

He³

et al. 2016

Cell Physiol Biochem

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Background/Aims: Berberine, a naturally occurring isoquinoline alkaloid, acts against oxidative stress (OS) and endoplasmic reticulum stress (ERS), both of which are responsible for Aldosterone (Aldo) -induced podocyte injury. However, the direct effects of berberine on Aldo-induced OS, ERS, and podocyte injury are not well defined. Methods: Uninephrectomized Sprague-Dawley rats were given 1% NaCl (salt) in their water and an Aldo infusion (0.75 µg/h) for 28 days to induce podocyte injury in the Aldo group. In the Aldo/berberine group, in addition to Aldo infusion, rats were administered 150 mg/kg berberine per day by gastric gavage for 4 weeks. Podocytes were incubated in media containing either buffer or Aldo in the presence or absence of berberine for variable time periods. The kidney tissues and podocytes were then investigated using morphological analysis, immunohistochemistry, transmission electron microscopy, western blot, DHE staining, DCFDA fluorescence, and Annexin V staining. Results: Here, we have reported that berberine attenuated Aldo-induced OS, ERS, and podocyte injury both in vivo and in vitro. Additionally, berberine treatment improved the extensive fusion of foot processes in electron micrographs resulting from Aldo/salt infusion in rats. Conclusion: Berberine may be examined as an effective agent against Aldo-induced podocyte injury.

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“…This effect is similar to that of statins currently used in the market without any major adverse effects. [23] Another study in rabbits on aerial part of Anethum graveolens L. presented the same results that alkaloids can prevent a rise in serum total cholesterol, triglycerides, LDLcholesterol, very LDL (VLDL)-cholesterol, atherogenic index and significantly increase total antioxidant capacity and HDL-cholesterol. [24] Tannins are heterogeneous high molecular weight polyphenolic compounds with the capability of forming complexes with proteins, polysaccharides, alkaloids, nucleic acids, and minerals.…”

Section: Discussionmentioning

confidence: 74%

Antidiabetic effects of Cycas riuminiana leaf extracts on alloxan-induced diabetic ICR mice (Mus musculus L.)

Barroso¹,

Lacanilao²,

Sac³

et al. 2017

Natl J Physiol Pharm Pharmacol

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Background:The Philippines is one of the countries with high prevalence of diabetes mellitus. Although there are several drugs marketed to control it, there are unwanted side effects. Knowing this, alternative options have been sought for to control the disease. Aims and Objectives: To evaluate the effects of aqueous extracts of Cycas riuminiana on the blood glucose and cholesterol levels of alloxan-induced diabetic mice. Materials and Methods: Aqueous crude leaf extract from C. riuminiana was administered to 6 and 30 ICR mice (Mus musculus) to determine whether there are toxic effects and effects on the blood glucose and cholesterol levels, respectively. The 30 mice were divided into six groups and were either treated with double distilled water, glimepiride, or the C. riuminiana aqueous extract. Results: After performing the acute oral toxicity, there were no deaths signifying that the extracts may be safe to administer in mice. After 28 days of treatment, statistical analyses indicated that the treatment groups had anti-hyperglycemic effects on the diabetic mice. The high-dose group had the lowest mean blood glucose values, which surpassed the hypoglycemic effects of the positive control group, which was treated with glimepiride. Furthermore, there was no difference between the control and the treatment groups. On the other hand, blood cholesterol values of the treatment and control groups were within the normal range after the 28 days study. Conclusion: The results of the study shows that C. riuminiana leaves have antidiabetic properties by lowering glucose and cholesterol levels at doses between 250 and 1000 mg/kg body weight.

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Berberine, a plant alkaloid with lipid- and glucose-lowering properties: From in vitro evidence to clinical studies

Cited by 265 publications

References 129 publications

In vitro assessment of the glucose-lowering effects of berberrubine-9-O-β-D-glucuronide, an active metabolite of berberrubine

In vitro assessment of the glucose-lowering effects of berberrubine-9-O-β-D-glucuronide, an active metabolite of berberrubine

Berberine Improved Aldo-Induced Podocyte Injury via Inhibiting Oxidative Stress and Endoplasmic Reticulum Stress Pathways both In Vivo and In Vitro

Antidiabetic effects of Cycas riuminiana leaf extracts on alloxan-induced diabetic ICR mice (Mus musculus L.)

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