Release of Soluble Arsenic From Realgar in Simulated Gastric Juice

Kwan, Sik-Yiu; Tsui, Shu-Ki; Man, Tao

doi:10.1081/al-100104917

Cited by 25 publications

(12 citation statements)

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“…In a previous study, only 0.6% of total realgar content taken was finally released into simulated gastric juice (Kwan et al, 2001), that is, the bioaccessibility of realgar into the simulated gastric juice was as low as 0.6%, consistent with another finding (Wu et al, 2002). Niu Huang Jie Du Pian is one of the most commonly used over-the-counter TCM.…”

Section: Low Bioaccessibility and Its Improvementsupporting

confidence: 61%

The medicinal use of realgar (As4S4) and its recent development as an anticancer agent

Shao

et al. 2011

Journal of Ethnopharmacology

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Section: Low Bioaccessibility and Its Improvementsupporting

confidence: 61%

The medicinal use of realgar (As4S4) and its recent development as an anticancer agent

Shao

et al. 2011

Journal of Ethnopharmacology

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“…Analysis of the amount of arsenic available for absorption using three different bioaccessibility methods demonstrated that, although the total arsenic exist as high as 28 mg in a single pill, only 4% of it was available for absorption into the bloodstream (1 mg of arsenic per pill), suggesting that the bioaccessibility of realgar is very poor [50]. In fact, the poor bioaccessibility and/or bioavailability of realgar has also been reported by other researchers [51,52]. Therefore, these observations raise the possibility that mild toxicity of the clinical application of realgar reported might be attributed to poor bioaccessibility and/or bioavailability, rather than its low toxic nature.…”

Section: Pharmacokinetic Studies Of Realgar In Leukemia Patients As Wmentioning

confidence: 86%

Perspective on Therapeutic Strategies of Leukemia Treatment — Focus on Arsenic Compounds

Yuan¹,

Iriyama²,

Hu³

et al. 2015

Leukemias - Updates and New Insights

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Leukemia is a type of cancer of the body's blood-forming tissues, including the bone marrow and the lymphatic system. Treatments for leukemia are complex, depending upon the type of leukemia and other factors. "cute promyelocytic leukemia "PL is a distinct subtype of acute myeloid leukemia "ML and accounts for approximately -% of all cases of "ML in adults. "rsenic and its compounds are widely distributed in the environment and have been used medicinally for over , years. In fact, investigators from China and the US" have demonstrated that treatment with "TO "s O , "s III results in complete remission in % of relapsed "PL patients since mids. Moreover, "s S or "s S , also known as realgar, has been gaining increasing attention and is traditionally used to treat certain types of hematological disorders including chronic myeloid leukemia CML , "ML, myelodysplastic syndrome MDS and MDS/"ML in China. In this chapter, we first highlight the pharmacokinetics of "TO and realgar in leukemia patients and/or healthy volunteer. We will further summarize the detailed mechanisms underlying the cytocidal effects of these arsenic compounds. We also provide detailed insight into potential future clinical application of those promising candidates endowed with potent antitumor activities in view of combination with arsenic compounds.

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“…At the designated time points (5, 10, 20, 30, 45, 60, 90, and 120 min after starting), 2 mL supernatant was taken out for measurement and 2 mL fresh medium was added to replenish the solution. The collected samples were completely digested with nitric acid, and then we used ICP-OES to detect arsenic levels (iCAP6300 ICP-OES, Thermo Scientific, USA) 22 . The dissolution rate ( D ) of each sample was calculated according to the following equation 36 :…”

Section: Methodsmentioning

confidence: 99%

“…Nevertheless, a major drawback of As 4 S 4 is that only 0.6% of the total arsenic content is leachable under simulated alimentary tract conditions 22 because it is poorly soluble in neutral and acidic conditions due to its crystal structure. The bioavailability of As 4 S 4 in the formula of Niu Huang Jie Du Pian was reported to be only 4% 23 .…”

mentioning

confidence: 99%

Fabrication of water-soluble polymer-encapsulated As4S4 to increase oral bioavailability and chemotherapeutic efficacy in AML mice

Guo

et al. 2016

Sci Rep

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Realgar (As4S4) has been demonstrated to be effective for the treatment of acute myeloid leukemia (AML); it has the advantages of no drug resistance and oral administration. Nevertheless, its poor solubility has been an obstacle to its bioavailability, requiring high-dose administration over a long period. We investigated whether crushing realgar crystals to the nanoscale and encapsulating the particles in a water-soluble polymer in one step using hot-melt extrusion would increase the bioavailability of As4S4. Raw As4S4 (r-As4S4) and water-soluble polymer were processed via co-rotating twin screw extrusion. The resulting product (e-As4S4) was characterized by SEM, XRD, and DLS. The cytotoxicity and therapeutic effects of e-As4S4 were evaluated in vivo and in vitro. The results show that e-As4S4 dissolved rapidly in water, forming a stable colloid solution. The average size of e-As4S4 particles was 680 nm, which was reduced by more than 40-fold compared with that of r-As4S4. The bioavailability of e-As4S4 was up to 12.6-fold higher than that of r-As4S4, and it inhibited the proliferation of HL-60 cells much more effectively than did r-As4S4, inducing apoptosis and significantly reducing the infiltration of HL-60 cells into the bone marrow, spleen, and liver. This in turn prolonged the survival of AML mice.

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Release of Soluble Arsenic From Realgar in Simulated Gastric Juice

Cited by 25 publications

References 0 publications

The medicinal use of realgar (As4S4) and its recent development as an anticancer agent

The medicinal use of realgar (As4S4) and its recent development as an anticancer agent

Perspective on Therapeutic Strategies of Leukemia Treatment — Focus on Arsenic Compounds

Fabrication of water-soluble polymer-encapsulated As4S4 to increase oral bioavailability and chemotherapeutic efficacy in AML mice

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