A bird's eye view on a therapeutically ‘wonder molecule’: Berberine

Patel, P. R.

doi:10.1016/j.phyplu.2021.100070

Cited by 21 publications

(34 citation statements)

References 124 publications

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“…Besides, BBR and erythrocytes tended to assemble rapidly in vitro , which might be due to the electrostatic attraction. From the structure of BBR, BBR has both hydrophobic and hydrophilic groups with a positive charge (Wang et al., 2016 ; Kostjukova and Kostjukov, 2021 ;; Patel, 2021 ), while the surface of erythrocytes has negative electrical potential (Fontes et al., 2008 ; Fernandes et al., 2011 ). Hence, the accumulation of BBR in erythrocytes might be intimately associated with electrostatic force, the potential primary step to form the BBR-erythrocyte system.…”

Section: Discussionmentioning

confidence: 99%

The discovery of berberine erythrocyte-hemoglobin self-assembly delivery system: a neglected carrier underlying its pharmacokinetics

Chen

et al. 2022

Drug Delivery

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Berberine (BBR) has extremely low concentration and high tissue distribution. However, current pharmacokinetic studies predominantly focus on its concentration in plasma, which could hardly make a comprehensive understanding of its pharmacokinetic process. This study made a pioneering endeavor to explore the erythrocyte-hemoglobin (Hb) self-assembly system of BBR by exploring the interaction of BBR with erythrocyte and the combination of BBR with Hb. Results showed that BBR had a low bioavailability ( C 0 = 2.833 μg/mL via intravenous administration of 2.5 mg/kg BBR and C max = 0.260 μg/mL via oral administration of 400 mg/kg BBR). Besides, BBR achieved higher concentrations in erythrocytes than plasma, and the erythrocytes count and Hb content were significantly decreased after intravenous administration. Hemolysis rate indicated the BBR-erythrocyte system (with 2% erythrocytes) was relatively stable without hemolysis at the concentration of 1.00 mg/mL. And the maximum percentage of drug loading was 100% when the BBR-erythrocyte concentration was 0.185 μg/mL. Furthermore, incubation of BBR and erythrocytes resulted in internalization of the erythrocyte membrane and the formation of intracellular vacuoles. The thermodynamic parameters indicated that the binding process of bovine hemoglobin (BHB) and BBR was spontaneous. UV-vis absorption spectra, synchronous fluorescence, circular dichroism and Raman spectra collectively indicated that BBR showed strong binding affinity toward BHB and affected the molecular environment of residues like tryptophan and tyrosine in BHB, resulting in the conformational changes of its secondary and tertiary structure. Molecular docking indicated BBR interacted with Arg-141 residue of BHB via hydrogen bond with the bond length of 2.55 Å. The ΔG value of the BHB-BBR system was −31.79 kJ/mol. Molecular dynamics simulation indicated the root mean square derivation of BBR-BHB was <0.025 nm, suggestive of stable conformation. Cumulatively, there was an erythrocyte-Hb self-assembled drug delivery system after oral or intravenous administration of BBR, which conceivably gained novel insight into the discrepancy between the extremely low plasma concentration and relatively high tissue concentration of BBR.

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Section: Discussionmentioning

confidence: 99%

The discovery of berberine erythrocyte-hemoglobin self-assembly delivery system: a neglected carrier underlying its pharmacokinetics

Chen

et al. 2022

Drug Delivery

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“…In these conventional methods, exposure to light and heat results in the degradation of berberine, thereby reducing berberine recovery from plant matrices [ 21 ]. Currently, research is focused on employing novel and innovative extraction techniques (supercritical fluid or pressurized liquid extractions, ultrasonication, microwave-assisted extraction, and ultrahigh pressure extraction) due to their enhanced extraction efficiency, reduced extraction time, and minimal detrimental effects [ 22 ]. Choices of the solvent and the type of extraction technique are considered critical steps in both the extraction and the isolation of berberine.…”

Section: Sources and Extraction Techniquesmentioning

confidence: 99%

Berberine as a Potential Anticancer Agent: A Comprehensive Review

et al. 2021

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Berberine (BBR), a potential bioactive agent, has remarkable health benefits. A substantial amount of research has been conducted to date to establish the anticancer potential of BBR. The present review consolidates salient information concerning the promising anticancer activity of this compound. The therapeutic efficacy of BBR has been reported in several studies regarding colon, breast, pancreatic, liver, oral, bone, cutaneous, prostate, intestine, and thyroid cancers. BBR prevents cancer cell proliferation by inducing apoptosis and controlling the cell cycle as well as autophagy. BBR also hinders tumor cell invasion and metastasis by down-regulating metastasis-related proteins. Moreover, BBR is also beneficial in the early stages of cancer development by lowering epithelial–mesenchymal transition protein expression. Despite its significance as a potentially promising drug candidate, there are currently no pure berberine preparations approved to treat specific ailments. Hence, this review highlights our current comprehensive knowledge of sources, extraction methods, pharmacokinetic, and pharmacodynamic profiles of berberine, as well as the proposed mechanisms of action associated with its anticancer potential. The information presented here will help provide a baseline for researchers, scientists, and drug developers regarding the use of berberine as a promising candidate in treating different types of cancers.

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“…Nó chứa nhiều đặc tính dược lý như chống oxy hóa, kháng vi rút, chống đái tháo đường, chống trầm cảm, chống tiêu chảy, kháng khuẩn. Bên cạnh những tác dụng có lợi của Berberine, một số hạn chế như khả năng hòa tan trong nước kém và sinh khả dụng đường uống thấp đã cản trở các ứng dụng của nó [4]. -Động vật thí nghiệm: Nghiên cứu tiến hành đánh giá trên thỏ.…”

Section: đặT Vấn đềunclassified

“…-Thời gian tiếp xúc: theo quy định [4][5][6]; vào cuối thời gian tiếp xúc, thường là 4 giờ, chất thử còn lại sẽ là loại bỏ, nếu có thể, sử dụng nước hoặc dung môi thích hợp mà không làm thay đổi phản ứng hiện có hoặc sự toàn vẹn của lớp biểu bì. Chúng tôi duy trì tiếp xúc trong 4h, sau đó sử dụng nước cất nhẹ nhàng rửa sạch vùng da, đảm bảo không gây tổn thương, không làm thay đổi tình trạng hiện có vùng da tiếp xúc.…”

Section: Mô Hình Thử Nghiệmunclassified

Nghiên cứu tính kích ứng da của gel nano Berberin trên da lành của động vật thực nghiệm

Nguyễn¹,

Lê²,

Nguyễn³

2022

yhthvb

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Berberin được phân lập từ cây Coscinium fenestratum và một số cây trong họ Ranunculaceae có tác dụng chữa vết thương, vết bỏng. Nghiên cứu xác tính kích ứng da lành thỏ của gel nano Berberine do Bệnh viện Bỏng quốc Lê Hữu Trác gia sản xuất. Phương pháp nghiên cứu được thực hiện theo hướng dẫn của Bộ Y tế, OECD. Tiến hành trên 3 thỏ, đắp gạc tẩm gel nano Berberin 0,5g lên vùng da lành 2,5 x 2,5cm; sau 4 giờ bóc bỏ gạc, làm sạch. Đánh giá chỉ số kích ứng sau 24, 48 và 72 giờ sau bóc bỏ gạc.Kết quả: Chỉ số kích ứng bằng 0 (không xuất hiện ban đỏ và tạo vảy, không phù nề ở da lành thỏ). Không có thỏ chết, thỏ vẫn khỏe mạnh, sinh hoạt bình thường.Kết luận: Gel nano Berberin an toàn, không gây kích ứng trên da lành thỏ.

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A bird's eye view on a therapeutically ‘wonder molecule’: Berberine

Cited by 21 publications

References 124 publications

The discovery of berberine erythrocyte-hemoglobin self-assembly delivery system: a neglected carrier underlying its pharmacokinetics

The discovery of berberine erythrocyte-hemoglobin self-assembly delivery system: a neglected carrier underlying its pharmacokinetics

Berberine as a Potential Anticancer Agent: A Comprehensive Review

Nghiên cứu tính kích ứng da của gel nano Berberin trên da lành của động vật thực nghiệm

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