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Berberis vulgaris (B. vulgaris or barberry) is a medicinal plant that has been used for various purposes in traditional medicine. Berberine is one of the main alkaloids isolated from B. vulgaris and other plants. Both B. vulgaris and berberine have shown anti-inflammatory, antioxidant, and immunomodulatory effects in different experimental models and clinical trials. This review aims to summarize the current evidence on the mechanisms and applications of B. vulgaris and berberine in modulating inflammation, oxidative stress, and immune responses. The literature search was performed using PubMed, Scopus, and Google Scholar databases until August 2023. The results indicated that B. vulgaris and berberine could inhibit the production of pro-inflammatory cytokines, such as tumor necrosis factor-alpha (TNF-α), interleukin-1β (IL-1β), interleukin 6 (IL-6), and interleukin-17 (IL-17), and enhance the expression of anti-inflammatory cytokines, such as interleukin 10 (IL-10) and transforming growth factor-β (TGF-β), in various cell types and tissues. B. vulgaris and berberine can also scavenge free radicals, increase antioxidant enzymes, such as superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx), and reduce lipid peroxidation and DNA damage. B. vulgaris and berberine have been reported to exert beneficial effects in several inflammatory, oxidative, and immune-related diseases, such as diabetes, obesity, cardiovascular diseases, neurodegenerative diseases, autoimmune diseases, allergic diseases, and infections. However, more studies are needed to elucidate the optimal doses, safety profiles, and potential interactions of B. vulgaris and berberine with other drugs or natural compounds., (© 2024 John Wiley & Sons Ltd.)

Berberis species have a long history of use in traditional Chinese medicine, Ayurvedic medicine, and Western herbal medicine. The aim of this study was the quantification of the main isoquinoline alkaloids in extracts obtained from various Berberis species by HPLC, in vitro and in silico determination of anti-cholinesterase activity, and in vitro and in vivo investigations of the cytotoxic activity of the investigated plant extracts and alkaloid standards. In particular, Berberis species whose activity had not been previously investigated were selected for the study. In the most investigated Berberis extracts, a high content of berberine and palmatine was determined. Alkaloid standards and most of the investigated plant extracts exhibit significant anti-cholinesterase activity. Molecular docking results confirmed that both alkaloids are more favourable for forming complexes with acetylcholinesterase compared to butyrylcholinesterase. The kinetic results obtained by HPLC-DAD indicated that berberine noncompetitively inhibited acetylcholinesterase, while butyrylcholinesterase was inhibited in a mixed mode. In turn, palmatine exhibited a mixed inhibition of acetylcholinesterase. The cytotoxic activity of berberine and palmatine standards and plant extracts were investigated against the human melanoma cell line (A375). The highest cytotoxicity was determined for extract obtained from Berberis pruinosa cortex. The cytotoxic properties of the extract were also determined in the in vivo investigations using the Danio rerio larvae xenograft model. The obtained results confirmed a significant effect of the Berberis pruinosa cortex extract on the number of cancer cells in a living organism. Our results showed that extracts obtained from Berberis species, especially the Berberis pruinosa cortex extract, can be recommended for further in vivo experiments in order to confirm the possibility of their application in the treatment of neurodegenerative diseases and human melanoma.

Designing biocompatible polymers using plant derivatives can be extremely useful in tissue engineering, nanomedicine, and many other fields of medicine. In this study, it was first looked into how chitosan/alginate scaffolds were made and characterized in the presence of berberine and barberry fruit extract. Second, the process of proliferation and differentiation of ovine fetal BM-MSCs (bone marrow-mesenchymal stem cells) was assessed on these scaffolds after BM-MSCs were extracted and confirmed by developing into osteocyte and adipose cells. To investigate the differentiation, treatment groups include (1) ovine fetal BM-MSCs were plated in Dulbecco's modified eagle medium culture medium with high glucose containing 10% fetal bovine serum and antibiotics (negative control), (2) ovine fetal BM-MSCs were plated in osteogenic differentiation medium (positive control group), (3) positive control group + barberry fruit extract, (4) positive control group + berberine, (5) ovine fetal BM-MSCs were plated in osteogenic differentiation medium on chitosan/alginate scaffold (hydrogel group), (6) ovine fetal BM-MSCs were plated in osteogenic differentiation medium on chitosan/alginate/barberry fruit extract scaffold (hydrogel group containing barberry fruit extract), and (7) ovine fetal BM-MSCs were plated in osteogenic differentiation medium on chitosan/alginate/berberine scaffold (hydrogel group containing berberine). Alkaline phosphatase (ALP) enzyme concentrations, mineralization rate using a calcium kit, and mineralization measurement by alizarin staining quantification were all found after 21 days of culture. In addition, real-time quantitative reverse transcription polymerase chain reaction was used to assess the expression of the ALP, COL1A2, and Runx2 genes. Days 5 and 7 had the lowest water absorption by the hydrogel scaffold containing barberry extract, which was significant in comparison to other groups (p < .05). Among the hydrogel scaffolds under study, the one containing barberry extract exhibited the lowest tensile strength, and this difference was statistically significant (p < .05). The chitosan/alginate hydrogel has the highest tensile strength of all of them. In comparison to the control and other treatment groups, the inclusion of berberine in the chitosan/alginate hydrogel significantly increased the expression of the ALP, Runx2, and COL1A2 genes (p < .05). The osteocyte differentiation of mesenchymal stem cells in in vitro settings appears to have been enhanced by the inclusion of berberine in the chitosan/alginate scaffold., (© 2024 John Wiley & Sons Ltd.)

The previous meta-analysis showed an advantageous effect of berberine supplementation on interleukin 6 (IL-6), tumor necrosis factor-α (TNF-α), and serum C-reactive protein (CRP) concentrations; however, it is unknown the dosage that this component influences inflammatory biomarkers. A comprehensive search was done in Scopus, PubMed, and Web of Science until September 2022 to find randomized controlled trials (RCT) that assessed the effects of berberine/barberry on IL-6, TNF-α, and CRP in adults but not trials without a control group. Studies bias was assessed using RoB 2. A random-effects model was performed to calculate the weighted mean difference (WMD). A dose-dependent effect was calculated. Eighteen clinical trials with 1600 participants were included in the current meta-analysis. These interventions significantly mitigate IL-6 levels (-1.18 pg/mL), TNF-α levels (-3.72 pg/mL), and CRP levels (-1.33 mg/L). In addition, the non-linear analysis showed a significant lowering effect of berberine/barberry on IL-6 and TNF-α levels in doses <1000 mg/day and less than 5 weeks of intervention. There are limitations to our findings, including low-quality studies and significant heterogeneity. These interventions might be considered adjunct therapy to managing inflammation status. However, more investigation and high-quality evidence must be conducted to obtain more comprehensive and generalizable results., (© 2023 John Wiley & Sons Ltd.)

Ethnopharmacological Relevance: Aerial parts (leaves and stems) of Berberis ruscifolia Lam. are a usual preparation as an analgesic, anti-inflammatory, antimalarial, antibacterial, and digestive in folk medicine. However, there were no previous studies of its chemical composition and biological activity related to analgesic effects., The Objective of the Study: The evaluation of the anti-nociception of the infusion (I), the decoction (D), and the ethanolic extract (EE) obtained from aerial parts of B. ruscifolia and its main chemical constituent in them, in mouse models., Material and Methods: The chemical constituent of B. ruscifolia extracts was evaluated and quantified by LC-MS and HPLC methodology. The inhibition of nociception in mice was analyzed by formalin and acetic acid-induced contortions tests. Also, when the formalin test was performed to evaluate the antinociceptive activity, the inhibition of edema formation and the antipyretic effect of each extract were simultaneously evaluated in the same experiment. For the oral administration in the in vivo assays, doses ranging from 10 to 1000 mg/kg and 10-30 mg/kg were used for extract and the chemical compound, respectively., Results: The presence of berberine (Berb) was identified in the three evaluated extracts where the EE showed the highest content of this compound getting a yield of 2%, while in the I and D, Berb is present at 0.2%. The three extracts promoted a reduction of the contortions induced by acetic acid, being observed in EE the highest activity with 63 ± 6% of significant inhibition of the nociceptive behavior at a dose of 300 mg/kg, while D significantly inhibited 32 ± 12% at the same dose and for I at a dose of 1000 mg/kg an inhibition of 44 ± 8% was observed. Likewise, in the formalin trial, I and EE reduced nociception at a dose of 1000 (31 ± 5%) and 300 (35 ± 3%) mg/kg, respectively in the neurogenic phase, while in the second phase of the experiment, all the extracts evaluated showed an antinociceptive effect, with significant inhibition of I of 54 ± 6% and D of 44 ± 5% at a dose of 1000 mg/kg and for EE showed a 63 ± 2% inhibition at a dose of 300 mg/kg being the one with the highest antinociceptive activity. These extracts showed no inhibition in temperature and formalin-injected paw edema formation when compared to the control. As for Berb, at a 30 mg/kg dose, it showed significant inhibition of 70 ± 5% in the acetic acid-induced contortion test., Conclusion: Altogether, the present results evidenced the analgesic properties of B. ruscifolia, scientific information presented for the first time, and also provided important knowledge not reported so far about the chemical composition of its extracts, by identifying the presence of Berb in them. Finally, we were able to conclude that the analgesic effect demonstrated by this medicinal plant is partly due to the presence of Berb., Competing Interests: Declaration of competing interest The authors declare no conflicts of interest., (Copyright © 2022 Elsevier B.V. All rights reserved.)

Barberry (Berberis vulgaris L.) is a medicinal plant and its main constituent is an isoquinoline alkaloid named berberine that has multiple pharmacological effects such as antioxidant, anti-microbial, antiinflammatory, anticancer, anti-diabetes, anti-dyslipidemia, and anti-obesity. However, it has restricted clinical uses due to its very poor solubility and bioavailability (less than 1%). It undergoes demethylenation, reduction, and cleavage of the dioxymethylene group in the first phase of metabolism. Its phase two reactions include glucuronidation, sulfation, and methylation. The liver is the main site for berberine distribution. Berberine could excrete in feces, urine, and bile. Fecal excretion of berberine (11-23%) is higher than urinary and biliary excretion routes. However, a major berberine metabolite is excreted in urine greater than in feces. Concomitant administration of berberine with other drugs such as metformin, cyclosporine A, digoxin, etc. may result in important interactions. Thus, in this review, we gathered and dissected any related animal and human research articles regarding the pharmacokinetic parameters of berberine including bioavailability, metabolism, distribution, excretion, and drug-drug interactions. Also, we discussed and gathered various animal and human studies regarding the developed products of berberine with better bioavailability and consequently, better therapeutic effects., (© 2022 John Wiley & Sons Ltd.)

Rheumatoid arthritis (RA), a chronic auto-immune disease, is often result of persistent and misdirectional inflammation and cannot be effectually resolved by single-target selective drugs. Present study attempted to uncover anti-arthritic efficacy and governing molecular mechanism of BLFE and its phytoconstituents berberine and rutin, with focus on dysregulated oxi-inflammation and structural integrity during articular damage using Collagen II-CFA-induced RA mice model. NMR-based phytometabolomic analysis revealed presence of phenolics and alkaloids such as berberine and rutin. BLFE, rutin and berberine remarkably mitigated Collagen II-CFA-induced disease severity index, articular damage, immune cells influx and pannus formation. An effective decrease in levels of TNF-α, IL-6, IL-1β, IFN-γ, IL-13, IL-17, MMPs, RORγt, Ob-cadherin, Cox-2, iNOS and enhancement in IL-10, IL-4 and IL-5, BMP-6/7 was observed in BLFE, rutin and berberine treatments. Molecular mechanistic analysis demonstrated reduction in expression of p-STAT-1/3, p-PI3K, p-Akt, p-JNK, p-p38, p-IκB, p-NF-κB and β-catenin via BLFE, rutin and berberine. Furthermore, reduced activation of p-ERK and p-GSK3β and enhanced splenic Tregs was only noticed in BLFE and berberine. Thus, the signifying presence of these phytoconstituents could contribute to the above-mentioned findings. These findings imply that BLFE could be beneficial for assuaging deleterious aspects of RA mediated via perturbed inflammation., (© 2022. The Author(s), under exclusive licence to Springer Nature Switzerland AG.)

SARS-CoV-2 (or COVID-19) has become a global risk and scientists are attempting to investigate antiviral vaccine. Berberis are important plants due to the presence of bioactive phytochemicals, especially berberine from the protoberberine group of benzylisoquinoline and recent studies have shown its potential in treating COVID-19. B. lycium Royle growing in subtropical regions of Asia had wide applications in Indian system of medicine. Rapid determination and novel optimisation method for berberine extraction has been developed by Soxhlet extraction utilising central composite design-response surface methodology (CCD-RSM). Berberine was detected by high-performance liquid chromatography (HPLC), and the highest yield (13.39%) was obtained by maintaining optimal extraction conditions i.e., extraction time (7.28 hrs), ethyl alcohol (52.21%) and solvent to sample ratio (21.78 v/w). Investigation of two geographic regions (Ramnagar and Srinagar) showed high berberine content in lower altitude. This novel optimisation technique has placed berberine as a potential candidate for developing pharmaceutical products for human health care.

Natural products are well known for their high potency with minimum side effects. Plant extracts are the most commonly used natural products because of their ease of availability and relatively low production cost. Berberine (BBR), a phytochemical component of some Chinese medicinal herbs (most commonly Berberis vulgaris), is an isoquinoline alkaloid with several biological and pharmacological effects including antioxidant, anti-inflammatory, antitumour, antimicrobial, antidepressant, hepatoprotective, hypolipidemic, and hypoglycemic actions. Interestingly, multiple studies have shown that BBR is a potential drug candidate with a multi-spectrum therapeutic application. However, the oral delivery of BBR is challenged owing to its poor bioavailability. Therefore, its oral bioavailability needs to be enhanced before it can be used in many clinical applications. This review provides an overview of the various studies that support the broad range of pharmacological activities of BBR. Also, it includes a section to address the issues and challenges related to the drug and methods to improve the properties of BBR, such as solubility, stability and bioavailability that may be explored to help patients reap the maximum benefit from this potentially useful drug., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Background: Hypertension is the highest risk factor for disease globally. When prescription of drug therapy is recommended, patients might decline treatment due to hypertension asymptomatic nature, sometimes turning to alternative therapies. One popular therapy is berberine, a plant alkaloid that has been used in eastern medicine for millennia to treat several ailments, including cardiovascular diseases and their risk factors., Aims: Through a transparent and pragmatic approach towards searching, synthesising, assessing, and reporting the available clinical evidence, the present review aimed to investigate berberine effect on blood pressure and cardiovascular disease risk. It also intended to provide guidance for clinician when advising their patients, and to highlight gaps in the research along offering suggestions to fill them., Methods: The review was conducted following the protocol PRISMA-P, and reported according to the related PRISMA statement. The PICO framework was used to define the scope of the review, and to arrive at a database search strategy. The strategy was run on the databases Medline, CINAHL, AMED, Embase, and Cochrane Library through the platforms EBSCOhost and Ovid. Citations were exported to Mendeley citation manger for screening. Relevant studies were selected based on specified inclusion and exclusion criteria. Data from included studies was extracted in the form of a detailed table of characteristics of studies, and summarised in an evidence table. Quality of studies was assessed using the SIGN methodology checklist for controlled trials. The results from the quality assessment were summarised through an adaptation of the Robvis tool software package output. Effect estimates and their precision were calculated with RevMan 5 computer program from the extracted study outcomes., Results: Five randomised controlled trials and two non-randomised controlled trials were included with 614 participants. All provided data on blood pressure, but none measured cardiovascular events or long-term adverse events. The group of studies was highly heterogeneous in terms of experimental intervention, comparator intervention, length to follow-up, participants' diagnosis, and setting. The heterogeneity prevented a meaningful meta-analysis. Berberine plus amlodipine was not significantly better than amlodipine alone at reducing systolic and diastolic blood pressure. Compared to metformin, berberine provided a statistically significant moderate reduction effect on systolic blood pressure (-11.87 [-16.64, -7.10] mmHg). A proprietary nutraceutical containing berberine as one of its ingredients was in one study significantly effective at reducing blood pressure compared to placebo (-11.80 [-18.73, -4.87] mmHg systolic, and -11.10 [-15.17, -7.43] mmHg diastolic), and also effective in another study compared to dietary advice (-3.40 [-5.48, -1.32] mmHg for systolic 24 h ambulatory blood pressure), although effects could not be reliably attributed to berberine alone. The herbal extract Chunghyul-dan, which contains berberine, showed a significant beneficial moderate effect compared to no treatment on systolic 24 h ambulatory blood pressure (-7.34 [-13.14, -1.54] mmHg) in one study, but in another study employing higher dose and longer treatment duration, no effects were detected. Again, the effects could not be attributed to berberine alone. The quality of the body of evidence was low, especially due to lack of trial design details and presence of outcome reporting bias., Conclusions: The evidence around berberine effect on blood pressure is limited, of low quality, and ultimately inconclusive. Clinicians should be aware that the evidence from randomised trials is not sufficient to establish berberine effectiveness and safety in the treatment of hypertension, and they should balance these findings with the long history of berberine use in the Eastern world. Researchers should aim at improving quality of studies, by raising the standard of designing and reporting them, e.g., by following the CONSORT guidelines, and strive to measure meaningful clinical endpoints, such as cardiovascular events, mortality, and adverse outcomes., (Copyright © 2020 Elsevier Ltd. All rights reserved.)

Berberine, an isoquinoline alkaloid isolated from the Chinese herb Coptis chinensis and other Berberis plants, has a wide range of pharmacological properties. Berberine can be used to treat many diseases, such as cancer and digestive, metabolic, cardiovascular, and neurological diseases. Berberine has protective capacities in digestive diseases. It can inhibit toxins and bacteria, including Helicobacter pylori, protect the intestinal epithelial barrier from injury, and ameliorate liver injury. Berberine also inhibits the proliferation of various types of cancer cells and impedes invasion and metastasis. Recent evidence has confirmed that berberine improves the efficacy and safety of chemoradiotherapies. In addition, berberine regulates glycometabolism and lipid metabolism, improves energy expenditure, reduces body weight, and alleviates nonalcoholic fatty liver disease. Berberine also improves cardiovascular hemodynamics, suppresses ischemic arrhythmias, attenuates the development of atherosclerosis, and reduces hypertension. Berberine shows potent neuroprotective effects, including antioxidative, antiapoptotic, and anti-ischemic. Furthermore, berberine exerts protective effects against other diseases. The mechanisms of its functions have been extensively explored, but much remains to be clarified. This article summarizes the main pharmacological actions of berberine and its mechanisms in cancer and digestive, metabolic, cardiovascular, and neurological diseases.

Objective: Despite controversies, no study has systematically summarized findings from earlier studies on the effect of berberine and barberry on anthropometric measures. Therefore, the current systematic review and meta-analysis was conducted on the effect of berberine and barberry on body mass index (BMI), body weight (BW), waist circumference (WC) and waist-hip ratio (WHR) in adults., Methods: Relevant studies, published up to August 2019, were searched through PubMed/Medline, Scopus, ISI Web of Science, Embase and Google Scholar. All randomized clinical trials investigating the effect of berberine and barberry on the anthropometric measures including BMI, BW, WC or/and WHR were included., Results: Out of 252 citations, 12 trials that enrolled 849 subjects were included. Berberine and barberry resulted in no significant change in BMI (Weighted mean differences (WMD): -0.16 kg/m 2 ; 95 % CI: -0.43 to 0.11, P = 0.247), BW (WMD: -0.11 kg; 95 % CI: -0.13 to 0.91, P = 0.830), and berberine resulted in not significant in WC (WMD: -0.58 cm; 95 % CI: -1.89 to 0.72, P = 0.379) and significant reduction in WHR (WMD: -0.03; 95 % CI: -0.04 to -0.01, P < 0.0001)., Conclusion: We found a significant reduction in WHR following berberine consumption in adults. Further clinical trials with high quality according to challenges mentioned seem to be helpful to use berberine and barberry as a supplement for certain health conditions, efficiently., Competing Interests: Declaration of Competing Interest The authors declared no conflicts of interest., (Copyright © 2020 Elsevier Ltd. All rights reserved.)

Civilization diseases associated with memory disorders are important health problems occurring due to a prolonged life span. The manuscript shows the results of an in vivo study targeting the emergence of two drug candidates with anti-amnestic properties. The preceding quantitative structure-activity relationship (QSAR) studies provided information on the ability of berberine and magnoflorine to cross the blood-brain barrier (BBB). In the light of these findings, both compounds were purified from crude plant extracts of barberries: berberine-from Berberis siberica using a method published earlier, and magnoflorine-from Berberis cretica by centrifugal partition chromatography (solvent system: ethyl acetate:butanol:water-0.6:1.5:3 v / v / v ). Both the compounds were evaluated for their memory enhancing and scopolamine inhibitory properties in an in vivo passive avoidance (PA) test on mice towards short-term and long-term memory. Cognition enhancing properties were observed at the following doses: 5 mg/kg (i.p.) for berberine and 20 mg/kg (i.p.) for magnoflorine. In addition, both the tested isoquinolines with the co-administered scopolamine were found to block long-term but not short-term memory impairment. No influence on the locomotor activity was observed for the tested doses. The results confirmed a marked central activity of magnoflorine and showed the necessity to lower the dosage of berberine. Optimized purification conditions have been elaborated for magnoflorine., Competing Interests: The authors declare no conflict of interest. The founding sponsors had no role in the design of the study; in the collection, analyses, or interpretation of data; in the writing of the manuscript, and in the decision to publish the results.

The excessive production of reactive oxygen species in nervous tissues is considered one of the major risk factors of neurodegenerative diseases. During the last two decades, much attention has been paid to the antioxidant and anti-inflammatory activity of natural products and compounds isolated from natural products which are often characterized by high efficacy and low adverse effects. Berberine is an isoquinoline alkaloid, widely present in different medicinal herbs, especially in the genus Berberis. It is mainly used as antidiarrhoeal, antibacterial, antifungal, and antiprotozoal agent. However, current research has focused on its beneficial role in neurodegenerative diseases, mainly due to its powerful antioxidant effect. The therapeutic potential of Berberine in different neurodegenerative diseases such as Alzheimer, Parkinson and Huntington disease has been brought to evidence by numerous studies. However, a limited number of reviews focus on the beneficial role of Berberine against neurodegeneration. The main objective of this review is to discuss the role of oxidative stress in neurodegeneration and the potential role of antioxidant compounds, in particular Berberine which is analyzed in its chemical structure, source, bioavailability, therapeutic potential, with special attention to its mechanism of action at a molecular level., (Copyright © 2015 Institute of Pharmacology, Polish Academy of Sciences. Published by Elsevier Urban & Partner Sp. z o.o. All rights reserved.)

Berberine is an isoquinoline alkaloid present in several plant species, including Coptis sp. and Berberis sp. In traditional medicine, extracts of berberine are used in the treatment of diarrhea of different origins. Recent studies have shown that berberine and its derivatives have significant biological effects on gastrointestinal (GI) and other functions and may become therapeutics for the treatment of diarrhea, gastroenteritis, diabetes, hyperlipidemia, cardiovascular diseases and inflammatory conditions. This paper summarizes the current knowledge on the actions of berberine in the GI tract. Binding and target sites, activated intracellular pathways, as well as the absorption and metabolism of berberine are discussed. Effects that may be useful in future clinical treatment, like antidiarrheal, anti-inflammatory and antitumor effects are critically reviewed and potential clinical applications are presented in detail.

The compounds 8-ethyl- (2), 8-butyl- (3), 8-hexyl- (4), 8-octyl- (5), 8-decyl- (6) and 8-dodecylberberine chloride (7) were synthesized and tested for their antimicrobial activity in vitro to evaluate structure-activity relationships. Substitution of the alkyl groups at C-8 led to significant changes in the antimicrobial activity. All compounds were more potent against the tested microorganisms than berberine (1), especially against Gram-positive bacteria. The antimicrobial activity increased as the length of aliphatic chain was elongated and then decreased gradually when the alkyl chain exceeded eight carbon atoms. 8-octylberberine (5) displayed the highest antimicrobial activity of all compounds. The toxicity of compounds 2 - 7 was stronger than that of 1. However, upon elongating the aliphatic chain, the toxicity decreased gradually.

The effects of berberine on growth, arylamine N-acetyltransferase (NAT) activity, and gene expression in Salmonella Typhi (Typhi) were described. The growth inhibition of Typhi was determined by measuring absorbance by optical density (OD at 650 nm). The NAT activity was determined by measuring the levels of 2-aminofluorene (AF) and N-acetyl-2-aminofluorene (AAF) by high-performance liquid chromatography. The results demonstrated that 24-h berberine treatment decreased bacteria growth and amounts of AAF in Typhi. Western blotting and flow cytometry were used for examining the levels of NAT after bacteria were cotreated with or without various concentrations of berberine, and results indicated that berberine decreased the levels of NAT in Typhi. Polymerase chain reaction was used for examining the gene expression of NAT (mRNA NAT), and results indicated that berberine affects mRNA NAT1 expression in Typhi.

N-acetyltransferases (NATs) are recognized to play a key role in the primary step of arylamine compounds metabolism. Polymorphic NAT is coded for rapid or slow acetylators, which are being thought to involve cancer risk related to environmental exposure. Berberine has been shown to induce apoptosis and affect NAT activity in human leukemia cells. The purpose of this study is to examine whether or not berberine could affect arylamine NAT activity and gene expression (NAT mRNA) and the levels of NAT protein in mouse leukemia cells (L 1210). N-acetylated and non-N-acetylated AF were determined and quantited by using high performance liquid chromatography. NAT mRNA was determined and quantited by using RT-PCR. The levels of NAT protein were examined by western blotting and determined by using flow cytometry. Berberine displayed a dose-dependent inhibition to cytosolic NAT activity and intact mice leukemia cells. Time-course experiments indicated that N-acetylation of AF measured from intact mice leukemia cells were inhibited by berberine for up to 24 h. The NAT1 mRNA and NAT proteins in mouse leukemia cells were also inhibited by berberine. This report is the first demonstration, which showed berberine affect mice leukemia cells NAT activity, gene expression (NAT1 mRNA) and levels of NAT protein.

The antimicrobial activity of Berberis heterophylla leaves, stems and root aqueous extracts was studied in vitro on Gram-positive and Gram-negative bacteria and fungi. The in vitro antifungal activity of berberine isolated from the same source against different Candida species was also investigated.

Dyslipidemia is a chronic disease characterized by elevated blood lipid levels treatable with statins. However, long-term statin use may have adverse effects, such as liver damage and memory loss. Nevertheless, plants and their active compounds effectively and safely improve lipid profiles. This review aims to update information on the genus Berberis as a hypolipidemic agent, assess the effects of these extracts on organisms and provide evidence supporting the use of these natural products in pharmaceutical drugs. Berberis species with therapeutic potential include B. vulgaris, B. integerrima, B. aristata, B. lycium, B. orthobotrys, and B. calliobotrys, which have shown promising results in reducing lipid levels in humans and other animals. In addition, combining berberine with nutraceuticals may improve its intestinal absorption, enhancing its lipid-lowering effect. Herbal medicine studies suggest that Berberis has a high potential for the management of hyperlipidemia. [ABSTRACT FROM AUTHOR]

[Objectives] To establish the quality standard of barberry branches. [Methods] Microscopic identification and thin layer identification were used to qualitatively identify barberry branches. Berberine content was determined by HPLC method, and the content of water, total ash, acid insoluble ash and extract was detected according to the method of the Chinese Pharmacopoeia (2020 edition). [Results] The microscopic identification showed that the features were obvious, and stone cells, cork cells, epidermal cells, stomata, fibers and catheter with reticulated pores could be found. Berberine was detected in barberry branches by thin layer chromatography, and the characteristic spots were separated clearly. Moisture, total ash, and acid insoluble ash content shall not exceed 13%, 6%, and 3%, respectively, and extract content shall not be less than 10%. Berberine hydrochloride (Cx, H]s C1NO4) should be calculated in the branches of Berberis wilsonae Hemsley and Berberis aggregaia C. K. Schneid., and berberine (C20H1N04) content should not be less than 0.05%. The linear relationship was good in the range of 0.002 - 0.240 mg/mL (R2 =0.999 5). The average recovery was 89.63%, and BSD vias 5.28%. [ Conclusions] The method was simple, accurate and reproducible, and can be used for the quality control of barberry branches. [ABSTRACT FROM AUTHOR]

Berberine and berbamine are bioactive compounds of benzylisoquinoline alkaloids (BIAs) present in Berberis species. The contents of berbamine are 20 times higher than berberine in leaf tissues in three closely related species: Berberis koreana, B. thunbergii and B. amurensis. This is the first report on the quantification of berberine compared to the berbamine in the Berberis species. Comparative transcriptome analyses were carried out with mRNAs from the leaf tissues of the three-species. The comparison of the transcriptomes of B. thunbergii and B. amurensis to those of B. koreana, B. thunbergii showed a consistently higher number of differentially expressed genes than B. amurensis in KEGG and DEG analyses. All genes encoding enzymes involved in berberine synthesis were identified and their expressions were variable among the three species. There was a single copy of CYP80A/berbamunine synthase in B. koreana. Methyltransferases and cytochrome P450 mono-oxidases (CYPs) are key enzymes for BIA biosynthesis. The current report contains the copy numbers and other genomic characteristics of the methyltransferases and CYPs in Berberis species. Thus, the contents of the current research are valuable for molecular characterization for the medicinal utilization of the Berberis species. [ABSTRACT FROM AUTHOR]

Abstract Objectives The aim of this in‐vitro study was to determine the antimicrobial capacity of a Berberis vulgaris plant extract on the bacteria being associated with caries including, Streptococcus mutans, S. sobrinus, S. sanguinis, S. salivaris and Lactobacillus rhamnosus. Material and methods Chlorhexidine 2% (CHX) mouthwash and ampicillin (10 μg/disk) were applied as positive control groups. Inhibition zone, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) related to stem, leaf and fruit of B. vulgaris plant were recorded for every five bacteria. Data were analyzed using SPSS ver. 22, one‐way ANOVA repeated measure and post hoc Tukey statistical test. The significance level was set at p 0.05). The MIC values of the extract from the stem were significantly lower against S. sobrinus (64 μg/ml) and L. rhamnosus (128 μg/ml). The MIC value of the extract against S. mutans was significantly lower in the fruit group (64 μg/mL). The MBC value of the extract against S. sobrinus and L. rhamnosus was significantly lower in the stem group (128 μg/ml). The MBC value against S. mutans was significantly lower in the fruit group (128 μg/ml). Conclusions The results showed that CHX and B. vulgaris plant extract have similar antimicrobial activity against bacteria being associated with caries. Therefore, B. vulgaris, which shows antibacterial capacity, could be considered for further investigation as a safe, phytotherapeutic mouthwash to prevent dental caries.

An in vitro propagation protocol has been developed for Berberis asiatica, an important Himalayan medicinal shrub. Significantly higher in vitro seed germination (50%) was obtained in Murashige and Skoog (MS) medium with 1.0 µM 6-benzyladenine (BA). MS medium containing 1.0 µM BA and 0.1 µM 2,4-dichlorophenoxyacetic acid (2,4-D) yielded maximum callus induction percentage (100%) from in-vitro grown leaf explants. Maximum shoot proliferation (100%) was obtained when callus was transferred to MS medium containing 2.0 µM BA plus 0.5 µM IAA or 6.0 µM BA plus 0.5 µM NAA. The maximum rooting percentage (70%) and root number per shoot (2.36) were recorded in ½ MS containing 0.05 µM IAA. Rooted shoots when transferred to potting medium containing vermiculite, soil, and sand (1:1:1) resulted in 65% survival. The phytochemical analysis of leaf samples of tissue culture-raised plants showed significantly higher alkaloids (berberine and palmatine) content than the leaf samples collected from the wild (mother plant). A similar trend was also observed in studied antioxidant and antimutagenic activities. Therefore, micropropagation of B. asiatica can be promoted for harnessing its potential as a source of berberine and natural antioxidants. This may help to reduce the pressure on the natural populations of the species. [ABSTRACT FROM AUTHOR]

Background: Methanolic extracts of the stems of six species of Berberis e.g., Berberis umbellata, B. vulgaris (Syn: B. nepalensis), B. insignis, B. asiatica, and B. aristata were studied for their antioxidant properties and acetylcholinesterase inhibitory properties. Materials and Methods : Antioxidant property was studied in different systems of assay e.g., DPPH radical scavenging assay, superoxide radical scavenging assay, nitric oxide scavenging assay, assay to chelate metal. Acetylcholinesterase (AChE) inhibitory property was measured using AChE from electric eel. Results: It was observed that all the extracts scavenged DPPH, superoxide and nitric oxide radical and chelated metal ion in a dose dependent manner. The antioxidant properties were correlated with total phenol content, total flavonoid content, berberine and palmatine content. The AChE inhibitory activities of the extracts were also correlated well with berberine, palmatine, total phenol and total flavonoid content. A few phenolic compounds were detected by GC-MS. Highest activity in all respect was observed in B. aristata. Conclusion: Methanolic extracts of the stems of B. aristata exhibited the highest antioxidant activity. [ABSTRACT FROM AUTHOR]

Objectives: The aim of this in‐vitro study was to determine the antimicrobial capacity of a Berberis vulgaris plant extract on the bacteria being associated with caries including, Streptococcus mutans, S. sobrinus, S. sanguinis, S. salivaris and Lactobacillus rhamnosus. Material and methods: Chlorhexidine 2% (CHX) mouthwash and ampicillin (10 μg/disk) were applied as positive control groups. Inhibition zone, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) related to stem, leaf and fruit of B. vulgaris plant were recorded for every five bacteria. Data were analyzed using SPSS ver. 22, one‐way ANOVA repeated measure and post hoc Tukey statistical test. The significance level was set at p < 0.05. Results: There were no significant differences between the antimicrobial capacity of the positive controls and the extract from the stem and fruit of B. vulgaris (p > 0.05). The MIC values of the extract from the stem were significantly lower against S. sobrinus (64 μg/ml) and L. rhamnosus (128 μg/ml). The MIC value of the extract against S. mutans was significantly lower in the fruit group (64 μg/mL). The MBC value of the extract against S. sobrinus and L. rhamnosus was significantly lower in the stem group (128 μg/ml). The MBC value against S. mutans was significantly lower in the fruit group (128 μg/ml). Conclusions: The results showed that CHX and B. vulgaris plant extract have similar antimicrobial activity against bacteria being associated with caries. Therefore, B. vulgaris, which shows antibacterial capacity, could be considered for further investigation as a safe, phytotherapeutic mouthwash to prevent dental caries. [ABSTRACT FROM AUTHOR]

Berberine and berbamine are bioactive compounds of benzylisoquinoline alkaloids (BIAs) present in Berberis species. The contents of berbamine are 20 times higher than berberine in leaf tissues in three closely related species: Berberis koreana, B. thunbergii and B. amurensis. This is the first report on the quantification of berberine compared to the berbamine in the Berberis species. Comparative transcriptome analyses were carried out with mRNAs from the leaf tissues of the three-species. The comparison of the transcriptomes of B. thunbergii and B. amurensis to those of B. koreana, B. thunbergii showed a consistently higher number of differentially expressed genes than B. amurensis in KEGG and DEG analyses. All genes encoding enzymes involved in berberine synthesis were identified and their expressions were variable among the three species. There was a single copy of CYP80A/berbamunine synthase in B. koreana. Methyltransferases and cytochrome P450 mono-oxidases (CYPs) are key enzymes for BIA biosynthesis. The current report contains the copy numbers and other genomic characteristics of the methyltransferases and CYPs in Berberis species. Thus, the contents of the current research are valuable for molecular characterization for the medicinal utilization of the Berberis species.

The incidences of diabetic mellitus and other metabolic diseases such as hypertension and hyperlipidemia are increasing worldwide; however, the current treatment is not able to control the rapidly increasing trend in diabetes mortality and morbidity. Studies related to the effectiveness of extracts and pure compounds obtained from plants have shown promising responses in preclinical and clinical studies related to these metabolic diseases. Plants belonging to the genus Berberis (Family: Berberidaceae) are widely distributed with nearly 550 species worldwide. Extracts and compounds obtained from Berberis species, especially Berberine alkaloid, showed effectiveness in the management of diabetes and other metabolic diseases. Various pharmacological experiments have been performed to evaluate the effects of Berberis extracts, berberine, and its natural and chemically synthesized derivatives against various cell and animal disease models with promising results. Various clinical trials conducted so far also showed preventive effects of Berberis extracts and berberine against metabolic diseases. The present review focuses on i) research updates on traditional uses, ii) phytopharmacology and clinical studies on Berberis species, and iii) active metabolites in the prevention and treatment of diabetes and other metabolic diseases with a detailed mechanism of action. Furthermore, the review critically analyzes current research gaps in the therapeutic use of Berberis species and berberine and provides future recommendations.

The incidences of diabetic mellitus and other metabolic diseases such as hypertension and hyperlipidemia are increasing worldwide; however, the current treatment is not able to control the rapidly increasing trend in diabetes mortality and morbidity. Studies related to the effectiveness of extracts and pure compounds obtained from plants have shown promising responses in preclinical and clinical studies related to these metabolic diseases. Plants belonging to the genus Berberis (Family: Berberidaceae) are widely distributed with nearly 550 species worldwide. Extracts and compounds obtained from Berberis species, especially Berberine alkaloid, showed effectiveness in the management of diabetes and other metabolic diseases. Various pharmacological experiments have been performed to evaluate the effects of Berberis extracts, berberine, and its natural and chemically synthesized derivatives against various cell and animal disease models with promising results. Various clinical trials conducted so far also showed preventive effects of Berberis extracts and berberine against metabolic diseases. The present review focuses on i) research updates on traditional uses, ii) phytopharmacology and clinical studies on Berberis species, and iii) active metabolites in the prevention and treatment of diabetes and other metabolic diseases with a detailed mechanism of action. Furthermore, the review critically analyzes current research gaps in the therapeutic use of Berberis species and berberine and provides future recommendations. [ABSTRACT FROM AUTHOR]

Plants belonging to Berberis are reported in several folklore medicinal pharmacopeias and are used in traditional medicines in Asia and European countries. The plants have been used in the preparation of various traditional and synthetic medicines since pre-historic times for wound healing, fever, eye disease, jaundice, vomiting during pregnancy, rheumatism, kidney and gall balder stones, and several other illnesses. Their healing properties are appear to be due to the presence of secondary metabolites and important alkaloids with different pharmacological activities. Their antibacterial, antifungal, antiviral, anti-diabetic, and anti-tumor activities as well as positive effects on the cardiovascular and body immune systems have been reported. Root extracts of some species of the plant genus contain quinine which acts as a powerful anti-malarial agent. The main chemical constituents of Berberis plants are alkaloids, steroids, glycosides, flavonoids, saponins, terpenoids and reducing sugars. Of these alkaloids, berberine is the most important. The present review focuses on recent advances in phytopharmacological and ethnomedicinal uses of plants belonging to Berberis genus. [ABSTRACT FROM AUTHOR]

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