Alkaline Phosphatase Isoenzymes

Dw, Moss

doi:10.1159/000458916

Cited by 89 publications

(71 citation statements)

References 20 publications

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“…The phosphate esters 4a and 4b must undergo a chemical or enzymatic bioconversion to release the parent drug in order to fulfill the prodrug criteria. In addition to red blood cells 27 alkaline phosphatases have been found in various human tissues; e.g., placenta, intestine, liver, bone, and kidney, 28 and they have been reported to be the responsible enzymes for the hydrolysis of phosphate esters. 16,29 The susceptibility of buparvaquone phosphate esters (4a,b) to enzymatic hydrolysis was studied in alkaline phosphatase enzyme solution (Table 3).…”

Section: Resultsmentioning

confidence: 99%

Synthesis, in Vitro Evaluation, and Antileishmanial Activity of Water-Soluble Prodrugs of Buparvaquone

et al. 2003

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Water-soluble phosphate prodrugs of buparvaquone (1), containing a hydroxynaphthoquinone structure, were synthesized and evaluated in vitro for improved topical and oral drug delivery against cutaneous and visceral leishmaniasis. The successfull prodrug synthesis involved a strong base; e.g., sodium hydride. Buparvaquone-3-phosphate (4a) and 3-phosphonooxymethylbuparvaquone (4b) prodrugs possessed significantly higher aqueous solubilities (>3.5 mg/mL) than the parent drug (e0.03 µg/mL) over a pH range of 3.0-7.4. Moreover, 4a and 4b maintained adequate lipophilicity as indicated by distribution coefficients (log D) between 0.5 and 3.0 over this pH range. Both 4a and 4b were also shown to be substrates for alkaline phosphatase in vitro and thus are promising bioreversible prodrugs for the improved topical and oral bioavailability of 1. Buparvaquone and its prodrugs showed nanomolar or lowmicromolar ED 50 activity values against species that cause cutaneous leishmaniasis, e.g., L. major, L. amazonensis, L. aethiopica, L. mexicana, and L. panamensis and also L. donovani, which is the causative agent of visceral leishmaniasis. From these results, the human skin permeation of the prodrugs 4a and 4b were studied in vitro. While no buparvaquone permeated across post mortem skin in vitro during 72 h of experiments, both prodrugs 4a and 4b permeated readily through the skin. In addition, 4b easily released the parent drug in human skin homogenate and, therefore, is a promising prodrug candidate to deliver buparvaquone through the skin for the treatment of cutaneous leishmaniasis.

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Section: Resultsmentioning

confidence: 99%

Synthesis, in Vitro Evaluation, and Antileishmanial Activity of Water-Soluble Prodrugs of Buparvaquone

et al. 2003

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“…Bone AP is localized in the plasma membrane of osteoblasts and released into the circulation during bone mineralization process. Due to the fact that liver and bone AP isoenzymes are quantitatively the most important in serum, in absence of liver disease, total AP can be considered, in spite of its lack of specificity, an indirect index of osteoblast activity and it is commonly used in diagnosing and monitoring bone formation rate (Moss, 1982).…”

Section: Discussionmentioning

confidence: 99%

Short- and long-term effects of calcium and exercise on bone mineral density in ovariectomized rats

́az-curiel

Piedra

et al. 2001

Br J Nutr

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At the level of prevention of bone mineral loss produced by ovariectomy, the aim of the present study was to determine the effect produced by supplementation of Ca in the diet and a moderate exercise programme (treadmill), simultaneously or separately, in ovariectomized rats, an experimental model of postmenopausal bone loss. Female Wistar rats (n 110, 15 weeks old) were divided into five groups: (1) OVX, rats ovariectomized at 15 weeks of age, fed a standard diet; (2) SHAM, rats sham operated at 15 weeks of age, fed a standard diet; (3) OVX -EX, ovariectomized rats, fed a standard diet and performing the established exercise programme; (4) OVX -Ca, ovariectomized rats fed a diet supplemented with Ca; (5) OVX -EXCa, ovariectomized rats with the exercise programme and diet supplemented with Ca. The different treatments were initiated 1 week after ovariectomy and were continued for 13 weeks for subgroup 1 and 28 weeks for subgroup 2, to look at the interaction of age and time passed from ovariectomy on the treatments. Bone mineral density (BMD) was determined, at the end of the study, in the lumbar spine (L2, L3 and L4) and in the left femur using a densitometer. Bone turnover was also estimated at the end of the study, measuring the serum formation marker total alkaline phosphatase (AP) and the resorption marker serum tartrate-resistant acid phosphatase (TRAP). As expected, OVX rats showed a significant decrease (P,0 : 05) in BMD, more pronounced in subgroup 2, and a significant increase in AP and TRAP with regard to their respective SHAM group. The simultaneous treatment with Ca and exercise produced the best effects on lumbar and femoral BMD of ovariectomized rats, partially avoiding bone loss produced by ovariectomy, although it was not able to fully maintain BMD levels of intact animals. This combined treatment produced a significant increase in AP, both in subgroups 1 and 2, and a decrease in TRAP in subgroup 1, with regard to OVX group. The exercise treatment alone was able to produce an increase in BMD with regard to OVX group only in subgroup 1 of rats (younger animals and less time from ovariectomy), but not in subgroup 2. In agreement with this, there was an increase of AP in both subgroups, lower than that observed in animals submitted to exercise plus Ca supplement, and a decrease of TRAP in subgroup 1, without significant changes in this marker in the older rats. Ca treatment did not produce any significant effect on BMD in OVX rats in both subgroups of animals, showing a decrease of AP and TRAP levels in the younger animals with no significant variations in markers of bone remodelling in the older female rats compared with their respective OVX group. Bone is a dynamic tissue in a continuous process of formation and resorption, activities performed by the osteoblasts and the osteoclasts respectively. The increase in bone mass or, on the contrary, bone loss, depends on the balance between these two processes (Canalis, 1996). Bone turnover is regulated by systemic hormones and by local factors. Oestrog...

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“…The estimation of SPO 4 was done by direct method [18]. Serum ALP was done by means of kinetic enzymatic method [19]. Serum creatinine estimation was done by Jaffe's method [20].…”

Section: Methodsmentioning

confidence: 99%

Biochemical Alterations in Postmenopausal Women Having Osteoporic Risk

Sharma

2017

Asian J Pharm Clin Res

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Objective: Osteoporosis is the most common disease worldwide; nutritional factors may play a significant role in the progression of the disease. The aim of this study was to assess the various biochemical parameters in the postmenopausal women with osteoporosis or osteopenia. Methods:In this hospital-based study, total 70 postmenopausal women, 45-80 years of age group, were studied. They were categorized into two groups as Case I and Case II on the basis of diagnosis of osteoporosis and osteopenia, respectively. The bone mineral density using T-score was estimated for diagnosis of osteoporosis or osteopenia. Bone mineral markers, i.e., total calcium and ionized calcium (CAI) were estimated by colorimetric method. Serum phosphate was estimated by direct method, and alkaline phosphatase (ALP) was measured by kinetic method. Biochemical parameters, i.e., urea, were estimated by diacetyl monoxime method. Serum albumin and serum creatinine were measured by bromocresol green method and Jaffe's method, respectively. Serum uric acid and magnesium were estimated by colorimetric method. Results:Total calcium and CAI were significant (<0.05) between the groups. The levels of serum phosphate and ALP were higher in osteoporotic group, but the results were not significant between the groups. Serum urea and serum albumin were comparatively higher and lower in osteoporotic group, respectively, but the findings were not significant between the groups. The significant results of serum creatinine, serum uric acid, and serum magnesium were obtained while comparing between osteoporotic patients and osteopenia patients. The levels were higher in osteoporosis group. There was a negative association of ALP with serum calcium and negative association with serum phosphate and uric acid. Conclusion:Biochemical alterations are characterized in osteoporotic as well as osteopenic patients. Monitoring of these parameters may be beneficial while giving the treatment to these patients for the prevention of other life-threatening risks.

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Alkaline Phosphatase Isoenzymes

Cited by 89 publications

References 20 publications

Synthesis, in Vitro Evaluation, and Antileishmanial Activity of Water-Soluble Prodrugs of Buparvaquone

Synthesis, in Vitro Evaluation, and Antileishmanial Activity of Water-Soluble Prodrugs of Buparvaquone

Short- and long-term effects of calcium and exercise on bone mineral density in ovariectomized rats

Biochemical Alterations in Postmenopausal Women Having Osteoporic Risk

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