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CHINESE JOURNAL OF OCEANOLOGY AND LIMNOLOGY · 2016 ·Vol. 34 ·期 6 ·1269-1277 · IF 0.547

Functional characterization of a novel microbial esterase identified from the Indian Ocean and its use in the stereoselective preparation of (R)-methyl mandelate

Liang Jiayuan,Sun Aijun,Zhang Yun,Deng Dun,Wang Yongfei,Ma Sanmei,Hu Yunfeng

Genomic mining has identified a novel microbial alkaline esterase from the Indian Ocean. This esterase was overexpressed in E. coli BL21 (DE3) and further functionally characterized. Under optimal conditions (10 mmol/L substrate, pH 6.0, 2 h at 40 °C), this esterase can hydrolyze racemic methyl mandelate to ( R )-methyl mandelate with very high optical purity ( e.e. >99%) and yield (nearly 90%). Interestingly, the stereoselectivity of this esterase is opposite to that of two previously reported lipases that can generate ( S )-methyl mandelate through the hydrolysis of racemic methyl mandelate. No organic solvents or other additives were required to optimize the optical purity and production of the final chiral product ( R )-methyl mandelate, which can potentially simplify the production procedure of ( R )-methyl mandelate catalyzed by esterase.

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JOURNAL OF BIOTECHNOLOGY · 2016 · IF 2.667

Highly efficient bioreduction of 2-hydroxyacetophenone to (S)- and (R)-1-phenyl-1,2-ethanediol by two substrate tolerance carbonyl reductases with cofactor regeneration

Zhi-Mei Cui,Jian-Dong Zhang,Xiao-Jun Fan,Gao-Wei Zheng,Hong-Hong Chang,Wen-Long Wei

Optically pure 1-phenyl-1,2-ethanediol is a very important chiral building block and intermediate in fine chemical and pharmaceutical industries. Reduction of 2-hydroxyacetophenone provides a straightforward approach to access these important compounds. In this study, two enantiocomplementary carbonyl reductases, BDHA (2,3-butanediol dehydrogenase from Bacillus subtilis ) and GoSCR (polyol dehydrogenase from Gluconobacter oxydans ) were discovered for the first time to convert 2-hydroxyacetophenone (2-HAP) to ( R )-1-phenyl-1,2-ethanediol (( R )-PED) and ( S )-1-phenyl-1,2-ethanediol (( S )-PED) with excellent stereochemical selectivity, respectively. The two enzymes were purified and characterized. In vitro bioreduction of 2-HAP catalyzed by BDHA and GoSCR coupled with glucose dehydrogenase (GDH) from Bacillus subtilis for cofactor regeneration were demonstrated, affording both ( R )-PED and ( S )-PED in   >99% ee and 99% conversion. Recombinant Escherichia coli whole cells co-expressing both GDH and BDHA or GoSCR genes were used to asymmetric reduction of 2-HAP to ( R )-PED or ( S )-PED. Under the optimized conditions, the bioreduction of 400   mM (54   g/L) substrate was proceeded smoothly without the external addition of cofactor, and the product ( R )-PED and ( S )-PED were obtained with 99% yield, >99% ee and 18.0   g/L/h volumetric productivity. These results offer a practical biocatalytic method for the preparation of both ( R )-PED and ( S )-PED with high volumetric productivity.

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INTERNATIONAL IMMUNOPHARMACOLOGY · 2025 · IF 4.7

Distinct roles of A1/A2 astrocytes in blood-brain barrier injury following cerebral I/R via the ROCK/NF-κB and STAT3 pathways

Zhifeng Geng,Guoyi Deng,Ziyu Wang,Xin Xu,Xiaojiao Yin,Sen Zhang,Jiale Shao,Jiyue Wen

Astrocytes may fail to perform their neuroprotective roles against cerebral ischemia/reperfusion (I/R) injury due to phenotypic transformation. We aimed to demonstrate the distinct roles of A1 astrocytes and A2 astrocytes on the blood-brain barrier (BBB) injury following cerebral I/R, and explore whether H 2 S-mediated A2 astrocytes polarization protects against BBB injury via inhibiting ROCK/NF-κB pathway. The mice cerebral I/R model and the oxygen-glucose deprivation/re‑oxygenation (OGD/R) model of astrocytes were used in present study. Cerebral I/R-induced BBB injury is evidenced by increased EB dye leakage and reduced expressions of ZO-1 and occludin in mice hippocampal tissues. We found that H 2 S-mediated A2 polarization and lipopolysaccharide (LPS)-induced polarization of A1 astrocytes respectively display beneficial and harmful role in BBB injury. Besides, harmful roles of A1 astrocytes in BBB injury can be reduced by H 2 S. Additionally, A1 astrocytes exhibit excessive activation of NF-κB and enhanced expressions of MMP9 and AQP4, which can be inhibited by H 2 S. Moreover, H 2 S-mediated polarization of A2 astrocyte displays enhanced phosphorylation and nuclear translocation of STAT3 and reduced expressions of MMP9 and AQP4. Importantly, ROCK inhibitor Fasudil likewise inhibits the activation of NF-κB and promotes STAT3 activation in OGD/R astrocytes, and NF-κB inhibitor BAY11–7082 reduces the expressions of MMP9 and AQP4 in OGD/R astrocytes. In conclusion, H 2 S-mediated polarization of A2 astrocyte protects against BBB injury following cerebral I/R, the mechanisms may be related to inhibition of ROCK/NF-κB pathway, and activation of STAT3.

CAS / MDL: 103745-39-7
✓ 已验证 产品关联 DOI PubMed 高影响因子
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CERAMICS INTERNATIONAL · 2024 · IF 5.1

High-entropy Mg1.8R0.2Al4Si5O18 (R = Ni, Co, Zn, Cu, Mn) cordierite ceramics: Influence of octahedral distortion and electronegativity mismatch on the microwave dielectric properties

Yang Yao,Lin Cao,Haoyue Yang,Raz Muhammad,Yingjie Ren,Xinjiang Luo,Fayaz Hussain,Bing Liu,Minmin Mao,Hadi Barzegar Bafrooei,Ehsan Taheri-Nassaj,Kaixin Song

In this study, high-entropy Mg 1.8 R 0.2 Al 4 Si 5 O 18 (R Ni, Ni 1/2 Co 1/2 , Ni 1/3 Co 1/3 Zn 1/3 , Ni 1/4 Co 1/4 Zn 1/4 Cu 1/4 , Ni 1/5 Co 1/5 Zn 1/5 Cu 1/5 Mn 1/5 ) cordierite ceramics based on equimolar ratios were designed and synthesized through the solid-state reaction technique at high temperatures. The effect of various R-ionic substitutions at the octahedral site and their relationship with ionic polarization, chemical bonding, and configurational entropy were explored. These factors have greatly affected the microwave dielectric properties of Mg 1.8 R 0.2 Al 4 Si 5 O 18 ceramics. The presence of cation radius mismatch and electronegativity mismatch at [MgO 6 ]-octahedron lattice sites revealed lattice distortion resulting from multiple cation substitutions. As the entropy values increased, the temperature stability of microwave dielectric properties of Mg 1.8 R 0.2 Al 4 Si 5 O 18 ceramics improved. For R Ni 1/2 Co 1/2 , a higher Q×f of approximately 73,658 GHz @ 13 GHz, with ɛ r ∼4.44 and τ f  ∼ −23.9 ppm/°C was obtained. In the case of R Ni 1/5 Co 1/5 Zn 1/5 Cu 1/5 Mn 1/5 , a near zero τ f (−10.7 ppm/°C), ɛ r  = 4.68 and Q×f  = 35,478 GHz @13 GHz were achieved, making it potentially suitable for practical applications.

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JOURNAL OF NUTRITIONAL BIOCHEMISTRY · 2026 · IF 5.2

Salvia plebeia R. Br. extract delays cellular senescence and promotes healthy aging via Atg7-dependent autophagy, with rosmarinic acid as a major bioactive constituent

Yan-Ni He,Shi-Ying Li,Pei Xu,Xing-Yue Zhou,Jing Zeng,Da-Lian Qin,Geng Xiong,Lu Yu,Wei Ren,An-Guo Wu,Jian-Ming Wu,Xiao-Gang Zhou

Aging is characterized by progressive cellular dysfunction and increased susceptibility to chronic diseases. Enhancing autophagy, a key cellular clearance process, offers a promising strategy to combat aging. In this study, we investigated the autophagy-inducing and anti-aging properties of Salvia plebeia R. Br. ethanol extract (SPE) using in vitro and in vivo models. Our results showed that SPE enhanced autophagosome and autolysosome formation, elevated LC3-II and Beclin-1 levels, and reduced p62 expression in human foreskin fibroblasts (HFFs), confirming its autophagy-inducing activity. SPE also mitigated D-galactose (D-gal)-induced cellular senescence, reducing SA-β-gal staining, senescence markers (p16, p21), SASP factors, and γ-H2AX foci. These effects were Atg7-dependent, as Atg7 knockout abolished the benefits, highlighting autophagy’s role in SPE’s action. In vivo, SPE improved physical function, reversed cellular senescence, enhanced antioxidant defenses, and restored autophagic activity in D-gal-induced prematurely senescent mice. Furthermore, SPE alleviated age-related cognitive decline, reduced neuronal damage, increased synaptic density, and mitigated Tau accumulation. Notably, SPE demonstrated good tolerability over 12 weeks, with stable body weight, no apparent tissue injury, and unchanged serum ALT, AST, and creatinine. Chemical profiling identified rosmarinic acid (RA) as a major bioactive constituent that recapitulated key autophagy- and senescence-related effects in vitro. These findings suggest that SPE is a promising natural autophagy enhancer with potential to promote healthy aging, combat age-related diseases, and serve as a novel therapeutic strategy for cellular dysfunction in aging.

CAS / MDL: 88899-55-2
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOPROCESS AND BIOSYSTEMS ENGINEERING · 2023 ·Vol. 46 ·期 9 ·1293-1302 · IF 3.8

Efficient asymmetric synthesis of ethyl (R)-3-hydroxybutyrate by recombinant Escherichia coli cells under high substrate loading using eco-friendly ionic liquids as cosolvent

Duan Zhiwen,Wang Yaowu,Ouyang Bin,Wang Pu

Ionic liquids (ILs) which synthesized from bio-renewable materials have recently attracted much attention for their applications in biocatalysis. Ethyl ( R )-3-hydroxybutyrate (( R )-EHB) as a versatile chiral intermediate is of great interest in pharmaceutical synthesis. This study focuses on evaluating the performances of choline chloride (ChCl)-based and tetramethylammonium (TMA)-based neoteric ILs in the efficient synthesis of ( R )-EHB via the bioreduction of ethyl acetoacetate (EAA) at high substrate loading by recombinant Escherichia coli cells. It was found that choline chloride/glutathione (ChCl/GSH, molar ratio 1:1) and tetramethylammonium/cysteine ([TMA][Cys], molar ratio 1:1) as eco-friendly ILs not only enhanced the solubility of water-insoluble EAA in the aqueous buffer system, but also appropriately improved the membrane permeability of recombinant E. coli cells, thus boosting catalytic reduction efficiency of EAA to ( R )-EHB. In the developed ChCl/GSH- or [TMA][Cys]-buffer systems, the space-time yields of ( R )-EHB achieved 754.9 g/L/d and 726.3 g/L/d, respectively, which are much higher than neat aqueous buffer system (537.2 g/L/d space-time yield). Meanwhile, positive results have also been demonstrated in the bioreduction of other prochiral ketones in the established IL-buffer systems. This work exhibits an efficient bioprocess for ( R )-EHB synthesis under 325 g/L (2.5 M) substrate loading, and provides promising ChCl/GSH- and [TMA][Cys]-buffer systems employed in the biocatalysis for hydrophobic substrate.

✓ 已验证 DOI PubMed 高影响因子
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RSC Advances · 2021 ·Vol. 11 ·期 32 ·19450-19460 · IF 3.361

Natural steroid-based cationic copolymers cholesterol/diosgenin-r-PDMAEMAs and their pDNA nanoplexes: impact of steroid structures and hydrophobic/hydrophilic ratios on pDNA delivery

Zhao Wang,Jingjing Sun,Mingrui Li,Ting Luo,Yulin Shen,Amin Cao,Ruilong Sheng

Using natural-based lipids to construct biocompatible, controllable and efficient nanocarriers and elucidating their structure–function relationships, was regarded as an important area for creating sustainable biomaterials. Herein, we utilized two natural steroids: cholesterol and diosgenin (bearing different hydrophobic tails) as the building blocks, to synthesize a series of natural steroid-based cationic random copolymers PMA6Chol-r-PDMAEMA and PMA6Dios-r-PDMAEMA via RAFT polymerization. The results demonstrated that the steroid-r-PDMAEMA copolymers could efficiently bind pDNA (N/P < 3.0) and then form near-spherical shape (142–449 nm) and positively-charged (+11.5 to +19.6 mV) nanoparticles. The in vitro cytotoxicity and gene transfection efficiency greatly depend on the steroid hydrophobic tail structures and steroid/PDMAEMA block ratios. Optimum transfection efficiency of the (Chol-P1/pDNA and Dios-P3/pDNA) nanoplexes could reach to 18.1–31.2% of the PEI-25K/pDNA complex. Moreover, all of the steroid-r-PDMAEMA/Cy3-pDNA nanoplexes have an obvious “lysosome localization” effect, indicating the steroid structures do not remarkably influence the intracellular localization behaviors of these nanoplexes.

CAS / MDL: 78-67-1 25154-86-3
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JOURNAL OF LUMINESCENCE · 2025 · IF 3.6

Machine learning analysis and discovery of novel blue-cyan-emitting Na18Ca13Mg5(PO4)18:Eu2+ phosphor

Zhichao Zhang,Jun Zhou,Jintai Wen,Fangnan Liang,Fang Zhang,Qianxiu Liu,Jifan Hu

Currently, data-driven methodologies for discovering advanced luminescent materials are receiving considerable focus, driven by the potential to expedite material development timelines and provide multi-faceted insights into material properties. This study implements machine learning to develop a predictive model for emission wavelengths in Eu 2+ -activated A I B II PO 4 -type phosphors, thereby advancing rational design strategies. Furthermore, the model's performance is rigorously evaluated by synthesizing a novel Na 18 Ca 13 Mg 5 (PO 4 ) 18 :Eu 2+ phosphor and comparing its emitting wavelength with the value predicted by the model, showing satisfactory agreement. The compound Na 18 Ca 13 Mg 5 (PO 4 ) 18 exhibits a glaserite-type crystal structure and belongs to the R-3m space group of the Trigonal crystal system. The Eu 2+ -activated Na 18 Ca 13 Mg 5 (PO 4 ) 18 phosphor demonstrates intense broadband absorption spanning 250–400 nm in the near-ultraviolet region, emitting bright blue-cyan luminescence under 365 nm excitation. The high Ra (93.3) and low correlated color temperature (CCT: 5096 K) values of the as-fabricated w-LED lamp indicate that Na 18 Ca 13 Mg 5 (PO 4 ) 18 :Eu 2+ can act as a promising blue-cyan-emitting phosphor for full-spectrum healthy lighting applications.

CAS / MDL: 1308-96-9
研究领域: 材料科学 · 机器学习 · 光电子学 · 固态照明 · 晶体学 · 发光材料 · 数据驱动发现
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ACS Applied Nano Materials · 2024 · IF 5.3

Dual Targeted Nanoparticles Encapsulating Cantharidin for Treatment of Hepatocellular Carcinoma and Lymphatic Metastasis

Wenwen Jiao,Hao Li,Yingjie Wu,Qing Wen,Wenzhen Wang,Jia Tian,Yulong Ren,Jinyuan Ma,Danxiang Zhao,Junli Zhao,Yu Zhang,Guang Han

Hepatocellular carcinoma (HCC) is a challenging cancer to treat due to its high malignancy, strong invasiveness, and high risk of metastasis. Inhibiting lymphatic metastasis in the early stages is crucial for HCC therapy. Active targeted drug delivery systems, imbued with tumor and lymphatic targeting capability via ligand–receptor mediation, represent a promising therapeutic strategy. Cantharidin (CTD), the primary effective component of poisonous traditional Chinese medicine (PTCM) Mylabris, has unique therapeutic effects on HCC. However, its high toxicity limits its clinical application. In this study, based on the high expression of lymphatic vessel endothelial hyaluronan receptor-1 (LYVE-1) in the peritumoral lymphatic vessels and glycyrrhetinic acid receptor (GA-R) in hepatocellular carcinoma cells, we developed CTD-loaded poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles modified with glycyrrhetinic acid (GA)–hyaluronic acid (HA) copolymers (GA-HA-PLGA/CTD NPs) through electrostatic interactions. This nanoparticle platform could preferentially accumulate cargo into the tumors and peritumoral lymphatic vessels, increasing drug accumulation in tumors and lymph nodes while decreasing drug accumulation in other organs, particularly the heart and kidney. As a result, it could enhance antitumor efficacy and inhibit lymphatic metastasis better than PLGA/CTD NPs while also reducing systemic toxicity. Furthermore, the variation of HA molecular weights and degrees of GA substitution could regulate the distribution of nanoparticles within tumors and lymph nodes. Overall, GA-HA-PLGA/CTD NPs exhibit promising potential as a therapeutic approach for HCC treatment and lymphatic metastasis inhibition, providing a potential strategy for the application of PTCMs in HCC treatment.

研究领域: 肿瘤学 · 药学 · 纳米技术 · 分子生物学
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JOURNAL OF COLLOID AND INTERFACE SCIENCE · 2025 · IF 9.7

Zirconium‑tin oxide interlayer modification enhances the performance and stability of the titanium-based lead dioxide electrode for efficient electrocatalytic degradation of alizarin yellow R

Asha Ergu,Jingang Yu,Xinyu Jiang

In this study, a novel titanium/zirconium‑tin oxide/alpha‑lead dioxide/beta‑lead dioxide (Ti/Zr-SnO 2 /α-PbO 2 /β-PbO 2 ) electrode was prepared and utilized for degrading alizarin yellow R (AYR) dye. The Integration of impregnation drying, drop coating with a solvent, and high-temperature pyrolysis significantly diminished the characteristic fissure morphology of conventional pyrolytic metal oxide interlayers, thereby modulating the electrodeposition process of alpha‑lead dioxide (α-PbO 2 ) and enhancing electrode stability and electrochemical performance. Electrode characterization revealed that the charge transfer resistance ( R ct ) was 88.0 Ω/cm 2 , and the oxygen evolution potential (OEP, vs. Ag/AgCl) was 2.02 V. The electrochemically active surface area was the largest, with an accelerated lifetime of up to 82.37 h. That was 13.18 times longer than that of the Ti/α-PbO 2 /β-PbO 2 electrode (6.25 h) and 8.83 times longer than that of the Ti/Zr-SnO 2 /β-PbO 2 electrode (9.33 h). Under optimal experimental conditions (400 A/m 2 , 50 mg/L, 20 °C, pH = 8.00), the removal rate of AYR by this electrode was 99.90 %, the chemical oxygen demand (COD) removal rate was 74.64 %, the average current efficiency (ACE) was 50.94 %, and the electric energy per order ( E EO ) was 41.17 kWh/m 3 . The AYR degradation process followed to a quasi-zero-order kinetic model ( k  = 0.2745 min −1 ). In the real water treatment, AYR and COD removal rates remained above 90.13 % and 62.57 %, respectively. This study demonstrated that the Ti/Zr-SnO 2 /α-PbO 2 /β-PbO 2 electrode significantly improved electrocatalytic performance and stability through the unique preparation of its interlayer, exhibiting great potential for efficient dye wastewater treatment.

研究领域: 环境工程 · 电化学 · 材料科学 · 水处理技术
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DRUG DELIVERY · 2020 · IF 4.902

A polyoxyethylene sorbitan oleate modified hollow gold nanoparticle system to escape macrophage phagocytosis designed for triple combination lung cancer therapy via LDL-R mediated endocytosis

Yan Shen,Yun Xia,Ershuang Yang,Zixuan Ye,Yuan Ding,Jiasheng Tu,Yong Zhang,Pengcheng Xu

Presently, a combination of chemotherapy, radiotherapy, thermotherapy, and other treatments has become a hot topic of research for the treatment of cancer, especially lung cancer. In this study, novel hollow gold nanoparticles (HGNPs) were used as drug carriers, and in order to improve the targeting ability of HGNPs to a lung tumor site, polyoxyethylene sorbitol oleate (PSO) was chosen here as a target ligand since it can be specifically recognized by the low-density lipoprotein (LDL) receptor which is usually over expressed on A549 lung cancer cells. In this way, a PSO-modified doxorubicin-loaded HGNP drug delivery system (PSO-HGNPs-DOX) was constructed and its physicochemical properties, photothermal conversion ability, and drug release of PSO-HGNPs-DOX was investigated. Further, the effects of triple combination therapy, the intracellular uptake, and the ability to escape macrophage phagocytosis of PSO-HGNPs-DOX were also studied using A549 cells in vitro. In addition, an in vivo mouse model was also used to study the targeting of PSO-HGNPs-DOX to lung cancer. PSO-HGNPs-DOX demonstrated a good triple therapeutic effect for lung cancer (A549 cell viability was only 10% at 500 μM) by LDL receptor mediated endocytosis and was able to escape macrophage phagocytosis to enhance its accumulation at the target site. Therefore, PSO-HGNPs-DOX is a novel, safe, promising, and targeted drug carrier designed for triple combination lung cancer therapy which should be further studied for such applications.

✓ 已验证 DOI PubMed 高影响因子
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NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY · 2019 ·Vol. 393 ·期 6 ·967-978 · IF 2.058

Synthesis, pharmacological evaluation and molecular docking of novel R-/S-2-(2-hydroxypropanamido)-5-trifluoromethyl benzoic acid as dual anti-inflammatory anti-platelet aggregation agents

Rong Rong,Zhang Rui-zhen,Wang Xin,Dan Yu-han,Zhao Yun-li,Yu Zhi-guo

R -/ S -2-(2-hydroxypropanamido) benzoic acid ( R -/ S -HPABA), marine-derived anti-inflammatory antiplatelet drugs, were initially synthesised in our group. However, preliminary research showed that R -/ S -HPABA were eliminated rapidly because of extensive hydroxylation metabolism of phenyl ring in vivo. In order to reduce significant hydroxylation metabolism to improve pharmacological activity and bioavailability, trifluoromethyl group was incorporated into R -/ S -HPABA to synthesise R -/ S -2-(2-hydroxypropanamido)-5-trifluoromethyl benzoic acid ( R -/ S -HFBA), respectively. The purposes of this study were to report the synthesis of R -/ S -HFBA and compare the anti-inflammatory antiplatelet effect and pharmacokinetic properties of R -/ S -HFBA with those of R -/ S -HPABA. Carrageenan-induced rat paw edema assay was used for the evaluation of the anti-inflammatory activity. R -/ S -HFBA showed better results in inhibiting edema and were able to prolong the anti-inflammatory effect after carrageenan injection. The antiplatelet aggregation activity of R -/ S -HFBA and R -/ S -HPABA was studied on arachidonic acid-induced platelet aggregation of rabbit platelet-rich plasma. The aggregation inhibition rate of R- / S -HFBA was significantly ( p < 0.05) higher than that of R- / S -HPABA, respectively. Molecular docking study revealed that R -/ S -HFBA possess more potent binding affinity with COX-1/COX-2 than R -/ S -HPABA, respectively, and that the presence of trifluoromethyl group leads to increase in activity of R -/ S -HFBA. R -/ S -HFBA also afford more favorable pharmacokinetic properties than R- / S -HPABA, respectively, such as higher C max , larger AUC 0-∞ , and longer t 1/2 , which, as expected, are more metabolically stable.

CAS / MDL: 50-78-2
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