Baicalin as an emerging magical nutraceutical molecule: Emphasis on pharmacological properties and advances in pharmaceutical delivery

Ibrahim, Alaa; Nasr, Maha; El‐Sherbiny, Ibrahim M.

doi:10.1016/j.jddst.2022.103269

Cited by 9 publications

(6 citation statements)

References 135 publications

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“…The cellulose‐based dialysis membrane bag used in the drug‐releasing test is known to allow the free passage of test substances with molecular weights 12 to 70 times smaller than MWCO [49] . Previous studies have reported that polymers can be used to modulate the particle size or zeta potential of drugs containing baicalin or berberine, resulting in prolonged effects with delayed release or quick effects with rapid release [50,51] . Chrysin 6A8G and palmatine are suggested to be associated with polymers that are sized to permeate dialysis membranes, thereby enhancing their release.…”

Section: Resultsmentioning

confidence: 99%

“…[49] Previous studies have reported that polymers can be used to modulate the particle size or zeta potential of drugs containing baicalin or berberine, resulting in prolonged effects with delayed release or quick effects with rapid release. [50,51] Chrysin 6A8G and palmatine are suggested to be associated with polymers that are sized to permeate dialysis membranes, thereby enhancing their release. Conversely, baicalin, magnoflorine, columbamine, berberine, and coptisine interacted with the polymer and precipitated to a size that was not permeable to the dialysis membrane.…”

Section: In-vitro Drug Release Studiesmentioning

confidence: 99%

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Chemical Characterization of the Precipitate Found in and Its Effect on Drug Release of the Scutellaria baicalensis‐Coptis chinensis Extract

Kim,

Kim

2023

Chemistry & Biodiversity

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Precipitate generation is a challenging issue during the production of herbal decoction as it affects the stability and bioavailability of active compounds. Here we explored the composition of the natural precipitate formed from and its effect on drug release of Scutellaria baicalensis–Coptis chinensis paired extract (SCPE). Furthermore, the surface morphology of the SCPE precipitate was also investigated. Ultra‐performance liquid chromatography‐mass spectrometry (UPLC‐MS) was used to chemical component analysis and field emission scanning electron microscope (FE‐SEM) was performed to particle observation. Baicalin (BA), berberine (BBR) and starch‐arginine‐rich polymers were abundant in the SCPE precipitate. FE‐SEM micrographs showed spheroidal shaped particles in the SCPE supernatant, while spherical and porous tissue‐shaped particles in the SCPE precipitate. In vitro drug release of baicalin and berberine contained in the precipitate may increase as the polymer is removed. The presence of polymer‐related interactions were confirmed by the greater increase in solubility of baicalin upon addition of arginine and polymer. This was also supported by the solubility decrease of the BA‐BBR complex in polymer solution and the gelation of the BA‐BBR complex in arginine solution. Our results provide a scientific basis for elucidating the pharmaceutical properties of the decoction of S. baicalensis–C. chinensis ‐ based herbal medicine.

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Section: Resultsmentioning

confidence: 99%

Section: In-vitro Drug Release Studiesmentioning

confidence: 99%

Chemical Characterization of the Precipitate Found in and Its Effect on Drug Release of the Scutellaria baicalensis‐Coptis chinensis Extract

Kim,

Kim

2023

Chemistry & Biodiversity

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“…Moreover, baicalin is commonly used as adjuvant therapy for hepatitis. In a clinical study, single dose baicalin (500 mg/kg) in combination with cyclosporin A was found to be safe and well tolerated in adult human subjects without any severe adverse effects[ 125 ]. However, the co-administration of baicalin with other herbal formulations or drugs might impede baicalin’s in vivo actions and consequently its efficacy.…”

Section: Drug Delivery Clinical Trial and Future Prospectsmentioning

confidence: 99%

Role of baicalin as a potential therapeutic agent in hepatobiliary and gastrointestinal disorders: A review

Ganguly¹,

Gupta²,

Pandey³

2022

WJG

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Baicalin is a natural bioactive compound derived from Scutellaria baicalensis , which is extensively used in traditional Chinese medicine. A literature survey demonstrated the broad spectrum of health benefits of baicalin such as antioxidant, anticancer, anti-inflammatory, antimicrobial, cardio-protective, hepatoprotective, renal protective, and neuroprotective properties. Baicalin is hydrolyzed to its metabolite baicalein by the action of gut microbiota, which is further reconverted to baicalin via phase 2 metabolism in the liver. Many studies have suggested that baicalin exhibits therapeutic potential against several types of hepatic disorders including hepatic fibrosis, xenobiotic-induced liver injury, fatty liver disease, viral hepatitis, cholestasis, ulcerative colitis, hepatocellular and colorectal cancer. During in vitro and in vivo examinations, it has been observed that baicalin showed a protective role against liver and gut-associated abnormalities by modifying several signaling pathways such as nuclear factor-kappa B, transforming growth factor beta 1/SMAD3, sirtuin 1, p38/mitogen-activated protein kinase/Janus kinase, and calcium/calmodulin-dependent protein kinase kinaseβ/adenosine monophosphate-activated protein kinase/acetyl-coenzyme A carboxylase pathways. Furthermore, baicalin also regulates the expression of fibrotic genes such as smooth muscle actin, connective tissue growth factor, β-catenin, and inflammatory cytokines such as interferon gamma, interleukin-6 (IL-6), tumor necrosis factor-alpha, and IL-1β, and attenuates the production of apoptotic proteins such as caspase-3, caspase-9 and B-cell lymphoma 2. However, due to its low solubility and poor bioavailability, widespread therapeutic applications of baicalin still remain a challenge. This review summarized the hepatic and gastrointestinal protective attributes of baicalin with an emphasis on the molecular mechanisms that regulate the interaction of baicalin with the gut microbiota.

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“…The main flavonoid of Scutellaria baicalensis is baicalin (its concentration in the roots of the plant reaches from 8.1% to 15.6% [30,31]). Baicalin (7-glucuronic acid, 5,6-dihydroxy-flavone) is a flavonoid compound [36] capable of inhibiting enzymes and regulating the immune response [37,38], exhibiting antitumor, antimicrobial, anti-inflammatory, neuroprotective, antidiabetic, antimutagenic, anticonvulsant, and antioxidant properties [39][40][41]. There are studies in which it has been proven that this flavonoid exhibits antibacterial activity against H. pylori [42]: by Baicalin (7-glucuronic acid, 5,6-dihydroxy-flavone) is a flavonoid compound [36] capable of inhibiting enzymes and regulating the immune response [37,38], exhibiting antitumor, antimicrobial, anti-inflammatory, neuroprotective, antidiabetic, antimutagenic, anticonvulsant, and antioxidant properties [39][40][41].…”

Section: Introductionmentioning

confidence: 99%

“…Baicalin (7-glucuronic acid, 5,6-dihydroxy-flavone) is a flavonoid compound [36] capable of inhibiting enzymes and regulating the immune response [37,38], exhibiting antitumor, antimicrobial, anti-inflammatory, neuroprotective, antidiabetic, antimutagenic, anticonvulsant, and antioxidant properties [39][40][41]. There are studies in which it has been proven that this flavonoid exhibits antibacterial activity against H. pylori [42]: by Baicalin (7-glucuronic acid, 5,6-dihydroxy-flavone) is a flavonoid compound [36] capable of inhibiting enzymes and regulating the immune response [37,38], exhibiting antitumor, antimicrobial, anti-inflammatory, neuroprotective, antidiabetic, antimutagenic, anticonvulsant, and antioxidant properties [39][40][41]. There are studies in which it has been proven that this flavonoid exhibits antibacterial activity against H. pylori [42]: by suppressing the expression of hefA genes (a gene affecting the multidrug resistance of H. pylori) and vacA (a gene that affects the production of exotoxin and promotes bacterial adhesion on stomach cells, leading to vacuolization of the cytoplasm of the target cell, its apoptosis, and death), and by inhibiting the action of urease and increasing the sensitivity of H. pylori strains to the action of amoxicillin and tetracycline [43][44][45].…”

Section: Introductionmentioning

confidence: 99%

Study of the Effect of Baicalin from Scutellaria baicalensis on the Gastrointestinal Tract Normoflora and Helicobacter pylori

Dmitrieva

Kozlova

Atuchin

et al. 2023

IJMS

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The antimicrobial properties of baicalin against H. pylori and several probiotic cultures were evaluated. Baicalin was isolated from a dry plant extract obtained by extraction with water at 70 °C. For isolation, extraction was carried out with n-butanol and purification on a chromatographic column. The antimicrobial potential was assessed by evaluating changes in the optical density of the bacterial suspension during cultivation; additionally, the disk diffusion method was used. During the study, the baicalin concentrations (0.25, 0.5, and 1 mg/mL) and the pH of the medium in the range of 1.5–8.0 were tested. The test objects were: suspensions of H. pylori, Lactobacillus casei, L. brevis, Bifidobacterium longum, and B. teenis. It was found that the greater the concentration of the substance in the solution, the greater the delay in the growth of the strain zone. Thus, the highest antimicrobial activity against H. pylori was observed at pH 1.5–2.0 and a baicalin concentration of 1.00 mg/mL. In relation to probiotic strains, a stimulating effect of baicalin (1.00 mg/mL) on the growth of L. casei biomass at pH 1.5–2.0 was observed. The results open up the prospects for the use of baicalin and probiotics for the treatment of diseases caused by H. pylori.

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Baicalin as an emerging magical nutraceutical molecule: Emphasis on pharmacological properties and advances in pharmaceutical delivery

Cited by 9 publications

References 135 publications

Chemical Characterization of the Precipitate Found in and Its Effect on Drug Release of the Scutellaria baicalensis‐Coptis chinensis Extract

Chemical Characterization of the Precipitate Found in and Its Effect on Drug Release of the Scutellaria baicalensis‐Coptis chinensis Extract

Role of baicalin as a potential therapeutic agent in hepatobiliary and gastrointestinal disorders: A review

Study of the Effect of Baicalin from Scutellaria baicalensis on the Gastrointestinal Tract Normoflora and Helicobacter pylori

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