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Botanical Sources, Chemistry Aspects and Biological Functions of Berberine: An Updated Critical Review

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Botanical Leads for Drug Discovery

Abstract

Alkaloid berberine is chemically represented as quaternary nitrogen structure, first isolated from Xanthoxylon cava Wall. long ago in the eighteenth century. Currently, this alkaloid is regarded as the most bioactive compound used by pharma industries for research and development of drugs and herbal formulations, and it is extensively employed for hundreds of years in curing numerous infectious diseases and in traditional Ayurvedic and Chinese medicine for curing diarrhoea as a detoxifying agent. Since long time, this compound is detected, isolated, and quantified from different families of plants such as Annonaceae (e.g. Xylopia L.), Berberidaceae (e.g. Berberis L.), Menispermaceae (e.g. Tinospora Miers), Papaveraceae (e.g. Argemone L.), Ranunculaceae (e.g. Coptis Salisb.) and Rutaceae (e.g. Zanthoxylum L.); most of these plants are growing in high-altitude regions of the Himalaya. Reported studies indicate that berberine possesses several pharmacological activities and cure inflammation, diabetes, cancer etc., thereby multiple of mechanisms, as the case may be halting cycle of the cell progression or triggers apoptosis. This chemical constituent shows significant activities such as antimicrobial (bacterial, fungal, protozoans, viral, helminthes), antidiarrhoeal, antitumor and apoptosis, anticarcinogenic, immunomodulatory, antihyperglycaemic, antioxidant, hepatoprotective, cardiovascular and several miscellaneous biological functions associated with human healthcare. This communication reviews and provided various undated information on the botanical sources, berberine extraction techniques and quantification methods, chemistry and several biological functions coupled with different clinical studies undertaken associated with berberine and allied research. This one place data will serve as future baseline data for researchers interested to work more on berberine and pharma industry for drug discovery and medicine development.

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Abbreviations

MAP:

Medicinal and aromatic plants (MAPs)

QPA:

Quaternary protoberberine alkaloid

R&D:

Research and development

TM:

Traditional medicinal

WHO:

World Health Organization

w/w:

Weight/weight

mL:

Millilitre

USE:

Ultrasound-assisted solvent extraction

MAE:

Microwave-assisted solvent extraction

SFE:

Supercritical fluid extractions

PLE:

Pressurized liquid extraction

v/v:

Volume/volume

rpm:

Rotation per minute

ES:

Extraction solvents

h:

Hour

0C:

Degree Celsius

g:

Gram

%:

Percent

MPa:

Mega Pascal

m/z:

Mega Hertz

LC-MS:

Liquid chromatography-mass spectrophotometer

Mg:

Milligram

NYHA:

New York Heart Association

LVEF:

Left ventricular ejection fraction

ACEI:

Angiotensin-converting enzyme inhibitors

AMPK:

AMP-activated kinase

AKT:

Protein kinase

JAK/STAT:

Janus kinase/signal transducers and activators of transcription

GSK3β:

Glycogen synthase kinase 3β

TLR4:

Toll-like receptor 4

CCl4:

Carbon tetrachloride

iNOS:

Inducible nitric oxide synthase

Th1:

T helper type 1

Th2:

T helper type 2

CD4:

Cluster of differentiation 4

IL-6:

Interleukin 6

TNF α:

Tumour necrosis factor-alpha

MMP:

Matrix metalloproteinase

MMP2:

Matrix metalloproteinase-2

MMP9:

Matrix metalloproteinase-9

BBB:

Blood-brain barrier

5-ASA:

5-Aminosalicylic acid

DSS:

Dextran sulphate sodium

COX2:

Cyclooxygenase-2

IL6:

Interleukin 6

IL23:

Interleukin 23

mRNA:

Messenger Ribonucleic acid

NF-kB:

Nuclear factor kappa-light-chain-enhancer of activated B cells

JAK2:

Janus Kinase 2 gene

PGPSN:

Postganglionic parasympathetic nerve

GBS:

Guillain-Barre syndrome

AIEPM:

Autoimmune encephalomyelitis

CCSM:

Corpus cavernosum smooth muscle

H2O2:

Hydrogen peroxide

NO:

Nitric oxide

SOD:

Superoxide dismutase

LDH:

Lactate dehydrogenase

CV:

Cell viability

iNOS:

Inducible nitric oxide synthase

HPW:

Hydraulic permeability of water

TCM:

Transport cell model

CMS:

Cell membrane stabilizing

SCC:

Squamous cell carcinoma

HCT:

Human colon tumour

VT:

Ventricular tachyarrhythmias

CLQR:

Chloroquine-resistant

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Acknowledgement

We would like to thanks all the authors whose publications have been cited in this review communication. We would also like to thank Director CSIR-IIIM Jammu for the facilities.

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The authors declare no conflict of interest for this publication.

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Authors and Affiliations

  1. Plant Sciences (Biodiversity and Applied Botany Division), CSIR-Indian Institute of Integrative Medicine, Jammu, Jammu and Kashmir, India

    Bikarma Singh

  2. Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, Uttar Pradesh, India

    Bikarma Singh

  3. cGMP/Chemical Engineering Division, CSIR-Indian Institute of Integrative Medicine, Jammu, Jammu and Kashmir, India

    Anil Kumar Katare

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  1. Bikarma Singh
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  2. Anil Kumar Katare
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Correspondence to Bikarma Singh or Anil Kumar Katare .

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  1. Plant Sciences (Biodiversity and Applied Botany Division), CSIR-Indian Institute of Integrative Medicine, Academy of Scientific and Innovative Research (AcSIR) Ghaziabad, Uttar Pradesh, India, Jammu, Jammu and Kashmir, India

    Bikarma Singh

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Singh, B., Katare, A.K. (2020). Botanical Sources, Chemistry Aspects and Biological Functions of Berberine: An Updated Critical Review. In: Singh, B. (eds) Botanical Leads for Drug Discovery. Springer, Singapore. https://doi.org/10.1007/978-981-15-5917-4_20

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