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Application of thermochromism in spectrophotometric analysis: selective determination of berberine in pharmaceuticals by solvent extraction.

A solvent extraction and spectrophotometric method for selective determination of berberine in pharmaceuticals is proposed. Berberine forms an ion associate with tetrabromophenolphthalein ethyl ester, which is extracted into ethylene dichloride. Secondary and tertiary amines and alkaloids are coextracted with the berberine and complicate the berberine determination. The absorbance of the secondary and tertiary amines and alkaloids into ethylene dichloride, however, decreases nearly to zero when the temperature is elevated from 25 to 60 degrees. Thus, berberine can be determined successfully in the presence of the secondary and tertiary amines and alkaloids by using thermochromaism.

Berberine

The effect of berberine on bilirubin excretion in the rat.

Berberine-containing herbs have been used in folk medicine to relieve neonatal jaundice. In the present investigation, the acute and chronic effects of berberine on bilirubin excretion were studied in rats. Acute doses of berberine were found to increase the secretion of bilirubin in experimental hyperbilrubinemia without affecting the UDP-glucuronyltransferase activity and BSP clearance. Continuous treatment abolished this effect. This apparent tolerance could be attributed to the inhibitory action of chronic berberine treatment on UDP-glucuronyltransferase activity, but the mechanism of this inhibition was not elucidated. Liver microsomal protein concentration, ethylmorphine N-demethylation, and BSP clearance were unchanged.

Animals

Berberine shows potential in mitigating PM2.5-induced breast cancer progression by inducing DNA damage and inhibiting error-prone DNA repair pathways.

Breast cancer remains the most common cancer among women, with 2.3 million new cases reported globally in 2022. Alongside established risk factors such as age, family history, genetics, obesity, smoking, and alcohol, exposure to fine particulate matter (PM2.5) has recently emerged as an environmental contributor. This risk is especially concerning for low- and middle-income countries (LMICs), where both PM2.5 exposure and cancer burden are disproportionately high; however, mechanistic studies from these regions remain limited. To address this gap and develop mitigation strategies, we investigated the oncogenic potential of water-soluble PM2.5 collected from ambient air on breast cancer and evaluated the potential role of nutraceuticals in mitigating these effects. PM2.5 exposure increased proliferation, migration, and ROS generation, while promoting the formation of multinucleated giant cells, leading to genomic instability. Berberine, a natural alkaloid, countered these effects by increasing DNA damage and exploiting tumor-specific genomic vulnerabilities through disruption of DNA damage response and repair networks, thereby promoting programmed cell death. Transcriptomic profiling of Delhi PM2.5-treated MCF7 cells revealed a Delhi PM2.5-associated carcinogenic gene signature enriched in MAPK signalling, reactive oxygen species, metabolic, lysosomal, and ribosomal pathways. We also found that several genes, including BIRC5, WSB1, and RCC1, within this PM2.5-induced gene signature were dysregulated in breast cancer patients and were inversely regulated by berberine treatment, suggesting that berberine counteracts the transcriptional effects of PM2.5. Our findings highlight ambient PM2.5 exposure as a driver of breast cancer progression and identify berberine as a promising candidate in mitigating PM2.5 effects; however, thorough preclinical and clinical validations are warranted.

Berberine

[The action of Berberin-drops on the intraocular pressure (IOP) (author's transl)].

A double-blind trial was performed on 12 patients with chronic open angle glaucoma with Berberin and Placebo drops. There was no evidence for the hypothesis that Berberin or Placebo cause changes in the bio-regulation of the IOP. The statistical analysis was done by a new procedure (Kannemann 1976). The authors tried to propose generally valid rules for the planning of trials which are supposed to prove or disaprove the connection between various eye-drops and IOP-changes.

Aged

[Fluorescence microscopy demonstration of mitochondria in tissue culture cells using berberine].

The possibility of fluorescence microscopical examination of mitochondria in living animal cells using fluorochrome berberine sulphate is shown. At concentrations of 30--50 g per ml the chemical is accumulated selectively in mitochondria of living cells. The specificity of berberine sulphate accumulation in mitochondria was shown by comparative phase contrast and fluorescence microscopy. The advantages of the method is its high sensitivity and simplicity, especially when mitochondria can not be examined by the phase contrast microscopy.

Animals

[2 new fluorochromation methods for blood smears and chromosomes using berberine sulfate following deoxyribonucleoprotein denaturation].

The authors reported a Berberine sulfate technique based on DNP-denaturation with modifications for the purposes of fluorescent cytochemistry in cytology of blood and vaginal smears. A similar fluorochromation technique for staining of metaphase chromosomes and chromosomes in meiotic division has been applied. The fluorescent specificities, probably due to the differences in the denaturation properties of the hetero- and euchromatin desoxyribonucleoprotein-complexes, are discussed in comparison with other fluorochrome techniques and in relation with differences in distribution of hetero- and euchromatin and amounts of proteins in DNP, as far as DNA denaturation and tinction properties are concerned. The weaker fluorescence of immature (or leucemic) nuclei in blood smears and certain chromosomal regions would be due to the greater amount of active euchromatin (DNA which is slow reassociating or unstable to denaturation), which obviously does not bind to a sufficient degree the fluorochrome applied. The differences established in the fluorescence of active euchromatin and inactive heterochromatin zones by post-denaturing fluorochromation with Berberine sulfate gave grounds to recommend the application of these techniques in haematological and cytological (normal and abnormal) practice and for the cytogenetical and microfluorimetrical analyses.

Animals

Network pharmacology approach to unveiling the mechanism of berberine in the amelioration of morphine tolerance.

OBJECTIVE: To investigate the mechanism underlying the effect of the Huanglian decoction (, HLD) on morphine tolerance (MT), using network pharmacology, and to verify these mechanisms in vitro and in vivo. METHODS: Available biological data on each drug in the HLD were retrieved from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform. The target proteins of MT were retrieved from the GeneCards, PharmGkb, Therapeutic Target Database, DrugBank, and Online Mendelian Inheritance in Man databases. Information regarding MT and the drug targets was compared to obtain overlapping elements. This information was imported into the Search Tool for the Retrieval of Interacting Genes/Proteins platform to obtain a protein-protein interaction network diagram. Then, a "component-target" network diagram was constructed using screened drug components and target information, viaCytoscape (Institute for Systems Biology, Seattle, WA, USA). The database for annotation, visualization, and integrated discovery was used for Gene Ontology enrichment and Kyoto Encyclopedia of Genes and Genomes pathways analyses. Pathway information predicted by network pharmacology was verified using animal studies and cell experiments. RESULTS: Network pharmacology analysis identified 22 active compounds of HLD and revealed that HLD partially ameliorated MT by modulating inflammatory, apoptosis, and nuclear factor kappa B (NF-κB) signaling pathways. Berberine (BBR), one of the main components of HLD, inhibited the development of MT in mice. BBR reduced cell viability while increasing B-cell lymphoma 2 (Bcl-2) protein expression and decreasing CD86, NF-κB, Bax, and Caspase-3 protein expression in brain vascular 2 (BV2) mcroglia cells treated with morphine. Additionally, BBR contributed to a reduction in pro-inflammatory cytokine release and apoptotic cell number. CONCLUSIONS: BBR, a key component of HLD, effectively suppressed microglial activation and neuro-inflammation by regulating the NF-κB and apoptosis signaling pathways, thereby delaying MT. This study offers a novel approach to enhance the clinical analgesic efficacy of morphine.

Berberine

[Inhibition of the respiratory chain by the alkaloids berberine sulfate, alpinigenine, and tetrahydropalmatine].

The three alcaloids inhibited the NADH oxidase system of electron transfer particles from beef heart up to 90--100 percent. The concentrations of half-inhibition amounted to 50 muM for berberine sulphate and tetrahydropalmatine and 0.55 mM for alpinigenine. All three compounds showed comparable inhibitions on the succinate-cytochrome c oxidoreductase system only at concentrations 20--25 times as high. The site of action may be the iron sulphur region of the complex I of the electron transfer system. The biological importance of this respiratory inhibitions should be taken into account.

Alkaloids

DNM1L depletion leads to accelerated heteroplasmy shifting of m.10191C allele through ATG7-dependent pathways.

Nucleotide composition bias in mitochondrial DNA (mtDNA) makes the heavy strand prone to form a DNA secondary structure called a guanine quadruplex (G4). This secondary structure has been shown to inhibit polymerase processivity in vitro. We previously identified pathogenic mtDNA variants that lead to increased G4-forming propensity, including a T to C mutation at m.10191 (m.10191 T > C) that causes Leigh syndrome. Cells treated with G4 binding agent (G4BA) berberine show a reduction in m.10191C pathogenic heteroplasmy levels. To help better understand the underlying mechanism behind berberine-induced heteroplasmy shift, we examined the relationship between mitochondrial fission and berberine-mediated shift. Here we show that knockdown of the fission factor DNM1L leads to an accelerated heteroplasmy shift towards the healthy mtDNA allele, lowering m.10191C by 10% in 3 weeks, compared to the 5 weeks required for berberine alone. The specific mechanism involves ATG7, as knockdown of ATG7 is able to partially delay this accelerated heteroplasmy shift. Taken together, we show that DNM1L knockdown is able to accelerate berberine-induced m.10191C heteroplasmy shifting through an autophagy-related mechanism.

Humans

Identification and validation of natural dengue virus NS1 inhibitors with promising antiviral potential.

Dengue infection remains a major global public health challenge, with no specific antiviral therapy currently available. The dengue virus non-structural protein 1 (NS1) exists in both intracellular and secreted forms playing a pivotal role in viral replication, immune evasion, and pathogenesis, particularly by contributing to endothelial disruption and vascular leakage during severe disease, thereby making it a promising therapeutic target. In silico screening identified berberine, betulinic acid, and ursolic acid as top candidates, exhibiting high binding affinities and stable interactions within the NS1 binding pocket. These computational predictions were further validated by biophysical assays, which demonstrated strong and specific binding interactions between the purified NS1 protein and the selected compounds. All three compounds significantly reduced viral genome levels, with the highest inhibition observed for berberine (60%), and followed by betulinic acid (40%) and ursolic acid (28%). Consistently, berberine showed the most potent inhibition of both intracellular and extracellular NS1. Overall, these findings highlight the inhibitory potential of natural compounds against DENV NS1 and provide a strong foundation for the development of NS1-targeted antivirals as a novel therapeutic strategy against dengue infection.

Antiviral Agents