Roland Wacker - Academia.edu (original) (raw)
Papers by Roland Wacker
Molecules
β-Caryophyllene (BCP), a common constituent of many spice and food plants, is gaining increased a... more β-Caryophyllene (BCP), a common constituent of many spice and food plants, is gaining increased attention due to recent research identifying numerous potential health benefits. Due to limited oral bioavailability observed in preclinical models, the described benefits of BCP may be maximized by using a suitable delivery system. Additionally, human pharmacokinetics (PK) remain unknown. This study evaluates the relative oral bioavailability of BCP formulated in a self-emulsifying drug delivery system (SEDDS) based on VESIsorb® formulation technology (BCP-SEDDS) compared to BCP neat oil. Hence, a randomized, double-blind, cross-over design, single oral dose study (100 mg BCP) in 24 healthy subjects (12 men/12 women) was performed under fasting conditions. Pharmacokinetic parameters were analyzed from individual concentration-time curves. The data show that BCP-SEDDS resulted in a 2.2/2.0-fold increase in AUC0–12h/AUC0–24h and a 3.6-fold increase in Cmax compared to BCP neat oil. Moreove...
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Cellular Physiology and Biochemistry, 2003
Implants for surgical needs are produced from different materials including metals, alloys, ceram... more Implants for surgical needs are produced from different materials including metals, alloys, ceramics or polymers. Metal implants are preferred in those disciplines where sufficient mechanical strength is needed, including traumatology, orthopedic or dental surgery. Further, modern tissue engineering techniques require scaffold materials to generate shape and stability for in vitro generated transplants. However, the biocompatibility and surface contact of most implants or scaffold materials to vital bone or other tissues are not optimal. Therefore we investigated the biocompatibility of different polymer surfaces to an osteoblastic cell line as a function of wettability or hydrophobicity to describe some of the surface parameters influencing the cell to implant or cell to scaffold contact. Glass slides were coated with different polymers and in some cases physically or chemically modified. SAOS-2 osteosarcoma cells were used for the biocompatibility tests on 16 different polymers and modifications thereof. The viability of the adherent cells was investigated by MTT assay. Commercially available tissue culture vessels served as controls. We report that excellent biocompatibility to SAOS-2 osteoblastic cells can be obtained with hydrophobic surfaces generated for instance by epoxy resins. Chemical modification of epoxy resin surfaces yielded even a further increased viability index surpassing the viability index obtained with cell culture vessels. We conclude that modified hydrophobic surfaces represent an interesting group of compounds for coating endoprosthetic implants or scaffolds for the purposes of tissue engineering.
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Journal of Peptide Science, 2004
The complete primary structure of the A chain of mistletoe lectin III (ML3A), a type II ribosome-... more The complete primary structure of the A chain of mistletoe lectin III (ML3A), a type II ribosome-inactivating protein, was determined using proteolytic digests of ML3A, HPLC separation of the peptides, Edman degration and MALDI-MS. Based on our results, ML3A consists of 254 amino acid residues, showing a high homology to the A chain of isolectin ML1 with only 24 amino acid residue exchanges. A striking important structural difference compared with ML1A is the lack of the single N-glycosylation site in ML3A due to an amino acid exchange at position 112 (ML1A: N112GS↠ML3A: T112GS). The alignment of ML3A with the A chains of ML1, isoabrins, ricin D, Ricinus communis agglutinin and three lectins, identified from the Korean mistletoe Viscum album ssp. coloratum, demonstrates the rigid conservation of all amino acid residues, responsible for the RNA-N-glycosidase activity as reported for ricin D. In addition, the fully determined primary structure of ML3A will give further information about the biological mechanism of mistletoe lectin therapy. Copyright © 2003 European Peptide Society and John Wiley & Sons, Ltd.
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Archives of Biochemistry and Biophysics, 2001
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Biochemical and Biophysical Research Communications, 1999
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Journal of Peptide Science, 2005
The primary structure of the B chain of the N-acetyl-D-galactosamine-recognizing mistletoe lectin... more The primary structure of the B chain of the N-acetyl-D-galactosamine-recognizing mistletoe lectin-3 (ML-3B) has been deduced from proteolytic digest peptides of the purified glycoprotein, their HPLC-separation and Edman degradation and confirmation of the peptide sequences by MALDI-MS. ML-3B consists of 262 amino acid residues including 10 cysteine moieties. The structure and linkage of the carbohydrate side chains, connected to two N-glycosylation sites at positions Asn95 and Asn135 of the lectin, were determined by a combination of glycosidase treatment and MALDI-MS of corresponding glycopeptide fragments. The sequence alignment reveals a high homology with other B chains of type-II RIPs, although there are remarkable differences in the D-galactose-specific mistletoe lectin-1B chain. The recently published primary structure of the mistletoe lectin-3A chain1 and the now available primary sequence of the 3B chain allowed the construction of a preliminary homology model of ML-3. The model demonstrates, unequivocally, that ML-3 is a member of the type-II RIP family with rigid conservation of the enzymatic active site of the A chain and an identical overall protein fold. Specific amino acid residue exchanges and the different glycosylation pattern in comparison with ML-1 are discussed and related to the properties of the two glycoproteins. The knowledge of the complete primary structure of mistletoe lectin-3 is a major contribution towards more insight into the mechanism of the biological activity of commercial mistletoe preparations. Copyright © 2004 European Peptide Society and John Wiley & Sons, Ltd.
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Frontiers in Natural Product Chemistry, 2005
ABSTRACT Based on isolation, sequence determination and X-ray studies, the primary and three-dime... more ABSTRACT Based on isolation, sequence determination and X-ray studies, the primary and three-dimensional structure of the glycoprotein mistletoe lectin I (MLI) are determined. ML-I is constituted of two chains (A chain: 254 amino acid residues; B chain: 264 amino acid residues) linked by a disulfide bridge. Three different structurally identified oligosaccharides (I, II, III) are attached to four Ntype glycosylation sites (NA112, NB61, NB96 and NB136). According to these structural characterizations, ML-I is a member of ribosome inactivating proteins (RIP) of type II. The three-dimensional X-ray structure allows a clear-cut picture of the highly toxic effects of ML-I caused by its RNA-N-glycosidase activity, which is in contrast to its immunomodulating activity, applied for the treatment of cancer patients.
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Naturwissenschaften, 1996
ABSTRACT
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Naturwissenschaften, 2000
Metal implants are the preferred materials to generate articular prostheses, plates, or bone peg... more Metal implants are the preferred materials to generate articular prostheses, plates, or bone pegs in orthopedic surgery. Although titanium and titanium alloys show a relatively good biocompatibility, clinical experience revealed that coating of the metallic implant surface may increase the biocompatibility. In a search for optimum bone implant surfaces, we determined polarity and contact angle parameters of a variety of polymers and substances and correlated the findings in a biocompatibility assay using an in vitro bone cell model. We report that an optimum adherence of SAOS-2 cells to such surfaces and a good vitality for polymers are characterized by water-based contact angles of 80° and 20° for advancing and receding probes, respectively.
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Naturwissenschaften, 1996
ABSTRACT
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Cheminform, 2010
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
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Naturwissenschaften, 2000
Metal implants are the preferred materials to generate articular prostheses, plates, or bone pegs... more Metal implants are the preferred materials to generate articular prostheses, plates, or bone pegs in orthopedic surgery. Although titanium and titanium alloys show a relatively good biocompatibility, clinical experience revealed that coating of the metallic implant surface may increase the biocompatibility. In a search for optimum bone implant surfaces, we determined polarity and contact angle parameters of a variety of polymers and substances and correlated the findings in a biocompatibility assay using an in vitro bone cell model. We report that an optimum adherence of SAOS-2 cells to such surfaces and a good vitality for polymers are characterized by water-based contact angles of 80° and 20° for advancing and receding probes, respectively.
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Naturwissenschaften, 1996
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Molecules
β-Caryophyllene (BCP), a common constituent of many spice and food plants, is gaining increased a... more β-Caryophyllene (BCP), a common constituent of many spice and food plants, is gaining increased attention due to recent research identifying numerous potential health benefits. Due to limited oral bioavailability observed in preclinical models, the described benefits of BCP may be maximized by using a suitable delivery system. Additionally, human pharmacokinetics (PK) remain unknown. This study evaluates the relative oral bioavailability of BCP formulated in a self-emulsifying drug delivery system (SEDDS) based on VESIsorb® formulation technology (BCP-SEDDS) compared to BCP neat oil. Hence, a randomized, double-blind, cross-over design, single oral dose study (100 mg BCP) in 24 healthy subjects (12 men/12 women) was performed under fasting conditions. Pharmacokinetic parameters were analyzed from individual concentration-time curves. The data show that BCP-SEDDS resulted in a 2.2/2.0-fold increase in AUC0–12h/AUC0–24h and a 3.6-fold increase in Cmax compared to BCP neat oil. Moreove...
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Cellular Physiology and Biochemistry, 2003
Implants for surgical needs are produced from different materials including metals, alloys, ceram... more Implants for surgical needs are produced from different materials including metals, alloys, ceramics or polymers. Metal implants are preferred in those disciplines where sufficient mechanical strength is needed, including traumatology, orthopedic or dental surgery. Further, modern tissue engineering techniques require scaffold materials to generate shape and stability for in vitro generated transplants. However, the biocompatibility and surface contact of most implants or scaffold materials to vital bone or other tissues are not optimal. Therefore we investigated the biocompatibility of different polymer surfaces to an osteoblastic cell line as a function of wettability or hydrophobicity to describe some of the surface parameters influencing the cell to implant or cell to scaffold contact. Glass slides were coated with different polymers and in some cases physically or chemically modified. SAOS-2 osteosarcoma cells were used for the biocompatibility tests on 16 different polymers and modifications thereof. The viability of the adherent cells was investigated by MTT assay. Commercially available tissue culture vessels served as controls. We report that excellent biocompatibility to SAOS-2 osteoblastic cells can be obtained with hydrophobic surfaces generated for instance by epoxy resins. Chemical modification of epoxy resin surfaces yielded even a further increased viability index surpassing the viability index obtained with cell culture vessels. We conclude that modified hydrophobic surfaces represent an interesting group of compounds for coating endoprosthetic implants or scaffolds for the purposes of tissue engineering.
Bookmarks Related papers MentionsView impact
Journal of Peptide Science, 2004
The complete primary structure of the A chain of mistletoe lectin III (ML3A), a type II ribosome-... more The complete primary structure of the A chain of mistletoe lectin III (ML3A), a type II ribosome-inactivating protein, was determined using proteolytic digests of ML3A, HPLC separation of the peptides, Edman degration and MALDI-MS. Based on our results, ML3A consists of 254 amino acid residues, showing a high homology to the A chain of isolectin ML1 with only 24 amino acid residue exchanges. A striking important structural difference compared with ML1A is the lack of the single N-glycosylation site in ML3A due to an amino acid exchange at position 112 (ML1A: N112GS↠ML3A: T112GS). The alignment of ML3A with the A chains of ML1, isoabrins, ricin D, Ricinus communis agglutinin and three lectins, identified from the Korean mistletoe Viscum album ssp. coloratum, demonstrates the rigid conservation of all amino acid residues, responsible for the RNA-N-glycosidase activity as reported for ricin D. In addition, the fully determined primary structure of ML3A will give further information about the biological mechanism of mistletoe lectin therapy. Copyright © 2003 European Peptide Society and John Wiley & Sons, Ltd.
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Archives of Biochemistry and Biophysics, 2001
Bookmarks Related papers MentionsView impact
Biochemical and Biophysical Research Communications, 1999
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Journal of Peptide Science, 2005
The primary structure of the B chain of the N-acetyl-D-galactosamine-recognizing mistletoe lectin... more The primary structure of the B chain of the N-acetyl-D-galactosamine-recognizing mistletoe lectin-3 (ML-3B) has been deduced from proteolytic digest peptides of the purified glycoprotein, their HPLC-separation and Edman degradation and confirmation of the peptide sequences by MALDI-MS. ML-3B consists of 262 amino acid residues including 10 cysteine moieties. The structure and linkage of the carbohydrate side chains, connected to two N-glycosylation sites at positions Asn95 and Asn135 of the lectin, were determined by a combination of glycosidase treatment and MALDI-MS of corresponding glycopeptide fragments. The sequence alignment reveals a high homology with other B chains of type-II RIPs, although there are remarkable differences in the D-galactose-specific mistletoe lectin-1B chain. The recently published primary structure of the mistletoe lectin-3A chain1 and the now available primary sequence of the 3B chain allowed the construction of a preliminary homology model of ML-3. The model demonstrates, unequivocally, that ML-3 is a member of the type-II RIP family with rigid conservation of the enzymatic active site of the A chain and an identical overall protein fold. Specific amino acid residue exchanges and the different glycosylation pattern in comparison with ML-1 are discussed and related to the properties of the two glycoproteins. The knowledge of the complete primary structure of mistletoe lectin-3 is a major contribution towards more insight into the mechanism of the biological activity of commercial mistletoe preparations. Copyright © 2004 European Peptide Society and John Wiley & Sons, Ltd.
Bookmarks Related papers MentionsView impact
Frontiers in Natural Product Chemistry, 2005
ABSTRACT Based on isolation, sequence determination and X-ray studies, the primary and three-dime... more ABSTRACT Based on isolation, sequence determination and X-ray studies, the primary and three-dimensional structure of the glycoprotein mistletoe lectin I (MLI) are determined. ML-I is constituted of two chains (A chain: 254 amino acid residues; B chain: 264 amino acid residues) linked by a disulfide bridge. Three different structurally identified oligosaccharides (I, II, III) are attached to four Ntype glycosylation sites (NA112, NB61, NB96 and NB136). According to these structural characterizations, ML-I is a member of ribosome inactivating proteins (RIP) of type II. The three-dimensional X-ray structure allows a clear-cut picture of the highly toxic effects of ML-I caused by its RNA-N-glycosidase activity, which is in contrast to its immunomodulating activity, applied for the treatment of cancer patients.
Bookmarks Related papers MentionsView impact
Naturwissenschaften, 1996
ABSTRACT
Bookmarks Related papers MentionsView impact
Naturwissenschaften, 2000
Metal implants are the preferred materials to generate articular prostheses, plates, or bone peg... more Metal implants are the preferred materials to generate articular prostheses, plates, or bone pegs in orthopedic surgery. Although titanium and titanium alloys show a relatively good biocompatibility, clinical experience revealed that coating of the metallic implant surface may increase the biocompatibility. In a search for optimum bone implant surfaces, we determined polarity and contact angle parameters of a variety of polymers and substances and correlated the findings in a biocompatibility assay using an in vitro bone cell model. We report that an optimum adherence of SAOS-2 cells to such surfaces and a good vitality for polymers are characterized by water-based contact angles of 80° and 20° for advancing and receding probes, respectively.
Bookmarks Related papers MentionsView impact
Naturwissenschaften, 1996
ABSTRACT
Bookmarks Related papers MentionsView impact
Cheminform, 2010
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Bookmarks Related papers MentionsView impact
Naturwissenschaften, 2000
Metal implants are the preferred materials to generate articular prostheses, plates, or bone pegs... more Metal implants are the preferred materials to generate articular prostheses, plates, or bone pegs in orthopedic surgery. Although titanium and titanium alloys show a relatively good biocompatibility, clinical experience revealed that coating of the metallic implant surface may increase the biocompatibility. In a search for optimum bone implant surfaces, we determined polarity and contact angle parameters of a variety of polymers and substances and correlated the findings in a biocompatibility assay using an in vitro bone cell model. We report that an optimum adherence of SAOS-2 cells to such surfaces and a good vitality for polymers are characterized by water-based contact angles of 80° and 20° for advancing and receding probes, respectively.
Bookmarks Related papers MentionsView impact
Naturwissenschaften, 1996
Bookmarks Related papers MentionsView impact