Lysophosphatidylcholine (Lysolecithin) and its Synthetic Analogues. Immunomodulating and Other Biologic Effects

Munder, P. G.; Modolell, Manuel; Andreesen, Reinhard; Weltzien, Hans Ulrich; Westphal, Otto

doi:10.1007/978-3-642-67809-7_12

Cited by 21 publications

(20 citation statements)

References 48 publications

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“…Edelfosine was initially considered a very promising molecule owing to its immunomodulatory properties and inhibitory activity over tumor cell proliferation (3,4). However, cytotoxicity assays carried out on a large variety of tumors (solid and hemathological, such as leukemia) and normal cell lines, showed that edelfosine is not highly selective for tumor cells (5,6,7,8).…”

Section: Introductionmentioning

confidence: 99%

“…________________________________________ This chemical modification, however, did not alter significantly its metabolic stability or cytotoxic effect, preventing the clinical use of ilmofosine. Nonetheless, preliminary studies showed that this molecule is as an effective inhibitor of tumor cell proliferation (3,4), encouraging the search for more stable analogs.…”

Section: Introductionmentioning

confidence: 99%

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Alkylphospholipids – A Promising Class of Chemotherapeutic Agents with a Broad Pharmacological Spectrum

et al. 2013

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-PURPOSE:Since when alkylphospholipds (ALPs) were discovered and, even further after miltefosine's approval for the treatment of cutaneous metastasis of breast cancer and leishmaniasis, their activity against many other diseases have been extensively studied. This review aims to provide a summary of the alkylphospholipids' applications investigated so far. RESULTS: The mechanism of action of ALPs is not fully understood, however it is believed that they interfere with lipid homeostasis leading to cell apoptosis. Due to ALPs cytotoxic activity, this class of molecules has shown to be effective against many diseases and conditions. Besides the approval of miltefosine for application in cutaneous metastasis of breast cancer and visceral and cutaneous leishmaniasis, several other analogs have proved efficacy and are promising as less toxic alternatives. ALPs have also shown in vitro and in vivo activity against Trypanosoma spp., amoebae, Tricomonas vaginalis, Schistosoma mansoni, HIV, and some fungi and bacteria species. The use of ALPs for intraocular lens coating is also under investigation. In addition, a clinical trial comparing miltefosine with usual treatments to spontaneous urticaria is also being conducted. CONCLUSIONS: Alkylphospholipids present such a broad pharmacological spectrum that justifies the need for further investigations of the drug class mechanisms of action, as well as the search for new analogs with improved activity and toxicological profiles.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Alkylphospholipids – A Promising Class of Chemotherapeutic Agents with a Broad Pharmacological Spectrum

et al. 2013

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“…The purity of these lysophospholipids was greater than or equal to 99% pure, 0.5% precursor of lysophospholipids and no other compounds such as lipopolysaccaride (LPS) were detectable. Rac-1 -octadecyl-2-methyl-glycero-3-phosphocholine (ET-18-OCH3-choline) [17] and ET-18-OCH3-ethanolamine were kindly synthesized by Kureha Chemical Company, Tokyo, Japan. Ether analogues of monoglycerides, rac-SN-l-(3)-dodecylglycerol (DDG) and tridecylglycerol (TDG) were synthesized by the method of Baumann and Mangold [3] by Evan Gustow, Temple University.…”

Section: Ether Phospholipidsmentioning

confidence: 99%

“…On this basis, we hypothesize that macrophages within the host recognize a stimulatory signal radiating out from the inflammatory region. Inflammation and accompanying cellular damage result in activation of membrane enzymes, phospholipases, for accelerated degradation of phospholipids [8,17,18,21]. Some of the metabolic products, lysophospholipids, are soluble and cytotoxic.…”

Section: Introductionmentioning

confidence: 99%

Activation of macrophages by ether analogues of lysophospholipids

Yamamoto

Ngwenya

Sery

et al. 1987

Cancer Immunol Immunother

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Inflammation processes cause activation of phospholipase A in plasma membranes resulting in the production of various lysophospholipids. Treatment of mice with L-alpha-lysophosphatidyl-DL-glycerol (lyso-Pg) resulted in an enhanced ingestion activity of peritoneal macrophages as did other lysophospholipids. However, lyso-Pg is rather toxic as indicated by a rapid decrease in macrophage activity 3 days after treatment while macrophage activity of lysophosphatidylcholine-treated mice continued to increase at least up to the 6th day after treatment. Alkyl-lysophospholipid derivatives, racemic 1-0-octadecyl-2-methylglycero-3-phosphocholine and -phosphoethanolamine stimulated mouse macrophages for Fc-mediated ingestion. Decomposed products of alkyl-lysophospholipids, alkyl-glycerols, were also found to be excellent activators of macrophages not only for ingestion of IgG-coated target cells but also antibody-mediated tumoricidal activity. Macrophages from mice treated with alkylglycerols developed superoxide generating capacity. Furthermore, alkyl-glycerols were found to be tumoricidal by direct contact with retinoblastoma cells. Therefore, the advantage of the potential application of alkylglycerols as chemotherapeutic agents is that they have dual beneficial effects: potentiation of macrophage activity and cytotoxicity to malignant cells.

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“…Esta proteína está localizada predominantemente na membrana plasmática de células. Atualmente, várias outras proteínas relacionadas à MRP1, incluindo nove humanas, foram descobertas em eucariotos (LITMAN et al, 2001;HIPFNER et al, 1999 (MUNDER et al,1979;ANDREESEN et al, 1978, EIBL et al, 1967.…”

Section: Mecanismos De Resistência a Antineoplásicosunclassified

Síntese e estudo da atividade antitumoral de análogos alcóxicicloalquílicos da miltefosina

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Lysophosphatidylcholine (Lysolecithin) and its Synthetic Analogues. Immunomodulating and Other Biologic Effects

Cited by 21 publications

References 48 publications

Alkylphospholipids – A Promising Class of Chemotherapeutic Agents with a Broad Pharmacological Spectrum

Alkylphospholipids – A Promising Class of Chemotherapeutic Agents with a Broad Pharmacological Spectrum

Activation of macrophages by ether analogues of lysophospholipids

Síntese e estudo da atividade antitumoral de análogos alcóxicicloalquílicos da miltefosina

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