5 Reasons Why Your Business Needs Berberine Hydrochloride Exporter？

In China, the expansion of the berberine supplement market is significantly influenced by its longstanding usage in herbal and traditional Chinese medicine. Berberine has been utilized for decades in the treatment of diabetes, with a recorded increase of 10.5% year-over-year in diabetes cases among the populace in .

• A clinical trial involving 409 participants by Premote revealed that when combining berberine and probiotic powder, patients experienced lowered blood sugar levels.

In the United States, retail sales of vitamin and mineral products reported a modest annual growth rate of approximately 1% during the period from to .

• A survey conducted by the Council for Responsible Nutrition (CRN) found that 69% of adults in the U.S. consume dietary supplements to remedy nutritional deficiencies.

As berberine is classified as a dietary supplement, the rise in demand for nutritional products is poised to substantially foster market growth. Being an alkaloid compound found across multiple herbs, berberine is benefitting from an overall trend focused on natural alternatives due to increasing concerns over the side effects of pharmaceutical drugs.

Typically priced between US$ 15 and US$ 40 for a month's supply, berberine supplements are easily accessible online. Despite certain countries, including the United States, lacking locally grown plants containing berberine, these supplements remain widely accessible through online channels. The increasing inclination toward natural alternatives and higher health consciousness among netizens further drives the demand for berberine supplements.

The demand for berberine supplements in tablet form is witnessing a pronounced uptick due to their quick absorption characteristics, making them the favored choice among numerous consumers. Tablets facilitate consistent dosing, ensuring that users effectively gain the desired benefits.

The ongoing trend of consumers shifting toward plant-based and vegan products also enhances the popularity of berberine capsules, which align with these preferences.

Traditional Chinese medicine has become increasingly relevant in treating various ailments, drawing considerable interest for clinical applications. Vascular illnesses impacting the heart, cerebrovascular diseases, atherosclerosis, and complications arising from diabetes compromise the quality of life for many and elevate healthcare burdens. Berberine, an isoquinoline alkaloid sourced from Rhizoma coptidis, is extensively utilized in China as folk medicine due to its antibacterial and anti-inflammatory properties. Encouragingly, a growing body of research has indicated several cellular and molecular targets associated with berberine, substantiating its role as an alternative therapeutic option for vascular disorders and providing evidence of its efficacy against these conditions. This review aims to present a thorough systematic assessment of the evidence supporting berberine as a therapeutic agent for vascular diseases, which will encompass its pharmacological effects, mechanism of action, and pharmacokinetic profiles. Existing research illustrates that berberine possesses significant anti-inflammatory, antioxidant, anti-apoptotic, and anti-autophagic activity through the modulation of multiple signaling pathways, including AMP-activated protein kinase (AMPK), nuclear factor κB (NF-κB), SIRT-1, hypoxia-inducible factor 1α (HIF-1α), PI3K, Akt, JAK-2, Ca 2+ channels, and endoplasmic reticulum stress. Additionally, we tackle the inherent limitations posed by berberine in treating vascular diseases and offer potential solutions. We also outline research perspectives and prevailing challenges while providing a robust foundation from which future studies can draw on to discover novel effective medications derived from components of traditional Chinese medicine.

In recent times, unique molecular entities isolated from herbal medications containing berberine have sparked growing attention regarding the compound's potential in addressing vascular disease (Lee et al.,; Ren et al.,; Rajabi et al.,). Alongside advancements in pharmaceutical research, berberine is deemed a highly promising natural compound aimed at treating numerous human vascular diseases by modulating several signaling pathways. However, there lacks a comprehensive review delineating the pharmacological and pharmacokinetic properties of berberine within the framework of vascular disease. Consequently, we filtered through relevant studies on berberine's influence on vascular diseases published from years using databases such as Web of Science, ScienceDirect, PubMed, Google Scholar, and China National Knowledge Infrastructure to consolidate our findings, thereby providing insights into berberine’s application for treating vascular diseases.

Pharmacokinetics of Berberine

Distribution

Research demonstrates that berberine distributes rapidly across various tissues, including the liver, kidneys, muscle, lungs, brain, heart, pancreas, and adipose tissue, with the concentration in most tissues exceeding that found in plasma four hours after administering an oral dose of 200 mg/kg in rats. Additionally, berberine concentrations remain relatively stable in liver, heart, brain, muscle, and pancreatic tissues in rats (Tan et al.,). However, recent investigations focused on the in vivo distribution of berberine remain scarce, often attributed to its broad tissue distribution post-oral administration. The availability of novel methodologies, such as high-performance liquid chromatography combined with electrospray ionization mass spectrometry (HPLC-ESI/MS) and mass spectrometry imaging, could facilitate improved exploration of the tissue distribution of berberine (Jove et al.,). The extensive distribution of berberine across tissues presents an opportunity for its use in treating various ailments while broadening the scope of its clinical applications. For example, oral administration of 100 mg/kg berberine can encourage the excretion of cholesterol from liver to bile (Li et al., b). Accordingly, berberine's tissue distribution embodies a crucial pharmacokinetic characteristic that warrants additional research in the future.

Metabolism

One investigation utilized a sensitive HPLC-ESI/MS method to track the metabolites of berberine in human plasma, revealing that berberrubine was the most prevalent, displaying high lipid solubility in individuals who ingested an oral dose of 15 mg/kg of berberine chloride daily for three months (Spinozzi et al.,). Evidence suggests a similar metabolic profile for berberine exists in both rats (100 mg/kg administered orally) and humans (300 mg taken orally three times a day over two days) via urine (Qiu et al.,). Utilizing liquid chromatography in conjunction with ion trap time-of-flight mass spectrometry, Ma et al. () identified 16 distinct metabolites present in rat bile, urine, and fecal samples derived from oral berberine (200 mg/kg). Subsequent oral administrations of varying doses (48.2, 120, or 240 mg/kg) indicated that the levels of phase II metabolites surpassed those of phase I metabolites for the AUC0-48h values. Simultaneously, nine principal metabolites of berberine (including demethyleneberberine and jatrorrhizine-3-O-β-D-glucuronide) were detected within rat serum via an LC-MS/MS approach (Feng et al.,). Furthermore, the metabolism of berberine via oral ingestion is closely intricately linked to liver function and gut microbiota. Following the oral administration of 300 mg/kg berberine to mice, levels of cytochrome P3A11 (CYP3A11), CYP3A25 mRNA, and CYP3A11 and CYP2D22 enzyme activity were found to have decreased, while the CYP1A2 mRNA levels were heightened (Guo et al.,). Similarly, oral consumption of 200 mg/kg berberine results in metabolism by the liver through CYP450 isoenzymes involving oxidative demethylation at C2, C3, C9, and C10, which is succeeded by the conjugation of hydroxyl groups with glucuronic acid (Singh et al.,). Moreover, gut microbiota significantly affects berberine's metabolism post-oral ingestion, as indicated by studies where 200 mg/kg berberine administered orally was transformed into absorbable dihydroberberine by nitroreductases produced by gut microbiota, exhibiting nearly five times higher intestinal absorption rates than berberine in rats; subsequently, dihydroberberine converts back to berberine upon absorption into intestinal tissue before entering the bloodstream (Feng et al.,; Han et al., a). Additionally, in vitro and in vivo observations indicate that gut microbiota can oxidize berberine to form oxyberberine, which has a notably stronger binding affinity to hemoglobin compared to plasma (Li et al., a; Chen et al.,).

In summary, the liver and intestines serve as the primary metabolic organs for berberine administered orally. Inhibiting first-pass metabolism may enhance its bioavailability. Notably, thorough investigations regarding berberine's metabolism in vivo reveal that phase II metabolites predominate as the primary metabolic products (Feng et al.,), contradicting previous studies (Ma et al.,). Future research must give due attention to the role of nitroreductases from gut microbiota and the overall metabolism of berberine to thoroughly establish its pharmacodynamic foundation as a component of traditional Chinese medicine.

Excretion

To ascertain the poor absorption characteristics of berberine in vivo, researchers have focused on its excretion in relation to digestive health. Following a single oral dose (200 mg/kg), subsequent studies found that berberine was present in fecal matter with a recovery rate of 22.74% recorded within 48 hours, with thalifendine being the most prevalent metabolite excreted in bile, urine, and feces in rats (Ma et al.,). A separate investigation indicated that 18.6% of berberine was excreted through feces as berberrubine following an intragastric administration at a dose of 48.2 mg/kg. Notably, the cumulative recovery of berberine along with its metabolites from urine, bile, and feces reached 41.2% in rats (Feng et al.,). To condense, berberine and its metabolites are predominantly excreted by the kidneys (urine and feces) and bile in rodents.

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