• MeSH
• bleomycin terapeutické užití   MeSH
• lidé MeSH
• nádory hrtanu farmakoterapie   MeSH
• papilom farmakoterapie   MeSH
• podofylotoxin analogy a deriváty   MeSH
• teniposid terapeutické užití   MeSH
• Check Tag
• lidé MeSH
• mužské pohlaví MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• bleomycin MeSH
• podofylotoxin MeSH
• teniposid MeSH

The direct effect of selected cytostatic drugs on natural killer (NK) cell activity was evaluated. Peripheral blood mononuclear cells from healthy donors were tested for their cytolytic activity in vitro in the presence of adriamycin, methotrexate, leucovorin, vincristin, cytosine arabinoside and teniposide. Most of the tested cytostatic drugs did not show to be active at concentrations comparable to their plasma level. However, diluents of some preparations (cytosine arabinoside, teniposide) containing organic solutions and stabilizing additives (e.g. benzyl alcohol) suppressed the NK activity more than chemotherapeutic agents alone. Thus teniposide, containing such additives, inhibited NK activity already at 5 mg/ml, while its peak plasma concentration was 23.8 mg/ml. The inhibitory concentrations of teniposide did not affect the target binding of effector cells and the expression of 14 tested leukocyte differentiation markers. This implies that a postbinding step of the lytic process was altered by the preparation. Likewise, no inhibition of lectin dependent cellular cytotoxicity by teniposide and its diluent was observed, suggesting that the lectin may substitute the missing lytic signal.

• MeSH
• akutní erytroblastická leukemie farmakoterapie   MeSH
• benzylalkohol MeSH
• benzylalkoholy farmakologie   MeSH
• buňky NK účinky léků   MeSH
• cytarabin farmakologie   MeSH
• cytotoxické testy imunologické MeSH
• diferenciační antigeny biosyntéza   MeSH
• doxorubicin farmakologie   MeSH
• fluorescenční protilátková technika MeSH
• leukovorin farmakologie   MeSH
• lidé MeSH
• methotrexát farmakologie   MeSH
• protinádorové látky farmakologie   MeSH
• techniky in vitro MeSH
• teniposid farmakologie   MeSH
• vinkristin farmakologie   MeSH
• vztah mezi dávkou a účinkem léčiva MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• benzylalkohol MeSH
• benzylalkoholy MeSH
• cytarabin MeSH
• diferenciační antigeny MeSH
• doxorubicin MeSH
• leukovorin MeSH
• methotrexát MeSH
• protinádorové látky MeSH
• teniposid MeSH
• vinkristin MeSH

Lignans and neolignans are plant secondary metabolites derived from the oxidative coupling of phenylpropanoids. Biological activity of these phenolic compounds ranges from antioxidant, antitumor (terminaloside P, IC50 = 10 nM), anti-inflammatory, anti-neurodegenerative (schibitubin B, IC50 = 3.2 nM) and antiviral (patentiflorin A, IC50 = 14-23 nM) to antimicrobial. In addition, it was observed that several members of this group, namely enterolactone and its biochemical precursors also known as phytoestrogens, possess important protective properties. Most of these lignans and neolignans are presented in reasonable amounts in one's diet and thus the protection they provide against the colon and breast cancer, to name a few, is even more important to note. Similarly, neuroprotective properties were observed (schisanwilsonin G, IC50 = 3.2 nM) These structural motives also serve as an important starting point in the development of anticancer drugs. Presumably the most famous members of this family, etoposide and teniposide, synthetic derivatives of podophyllotoxin, are used in the clinical treatment of lymphocytic leukemia, certain brain tumors, and lung tumors already for nearly 20 years. This review describes 413 lignans and neolignans which have been isolated between 2016 and mid-2018 being reported in more than 300 peer-reviewed articles. It covers their source, structure elucidation, and bioactivity. Within the review, the structure-based overview of compounds as well as the bioactivity-based overview of compounds are described.

• Klíčová slova
• Bioactivity, Lignans, Neolignans, Patentiflorin A, Schibitubin B, Schisanwilsonin G, Terminaloside P,
• MeSH
• lidé MeSH
• lignany chemie   farmakologie   MeSH
• rostliny metabolismus   MeSH
• sekundární metabolismus MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• přehledy MeSH
• Názvy látek
• lignany MeSH

Secondary metabolites (SM) from organisms have served medicinal chemists over the past two centuries as an almost inexhaustible pool of new drugs, drug-like skeletons, and chemical probes that have been used in the "hunt" for new biologically active molecules with a "beneficial effect on human mind and body." Several secondary metabolites, or their derivatives, have been found to be the answer in the quest to search for new approaches to treat or even eradicate many types of diseases that oppress humanity. A special place among SM is occupied by lignans and neolignans. These phenolic compounds are generated biosynthetically via radical coupling of two phenylpropanoid monomers, and are known for their multitarget activity and low toxicity. The disadvantage of the relatively low specificity of phenylpropanoid-based SM turns into an advantage when structural modifications of these skeletons are made. Indeed, phenylpropanoid-based SM previously have proven to offer great potential as a starting point in drug development. Compounds such as Warfarin® (a coumarin-based anticoagulant) as well as etoposide and teniposide (podophyllotoxin-based anticancer drugs) are just a few examples. At the beginning of the third decade of the twenty-first century, the call for the treatment of more than a dozen rare or previously "neglected" diseases remains for various reasons unanswered. Leishmaniasis, a neglected disease that desperately needs new ways of treatment, is just one of these. This disease is caused by more than 20 leishmanial parasites that are pathogenic to humans and are spread by as many as 800 sandfly species across subtropical areas of the world. With continuing climate changes, the presence of Leishmania parasites and therefore leishmaniasis, the disease caused by these parasites, is spreading from previous locations to new areas. Thus, leishmaniasis is affecting each year a larger proportion of the world's population. The choice of appropriate leishmaniasis treatment depends on the severity of the disease and its form of manifestation. The success of current drug therapy is often limited, due in most cases to requiring long hospitalization periods (weeks to months) and the toxicity (side effects) of administered drugs, in addition to the increasing resistance of the parasites to treatment. It is thus important to develop new drugs and treatments that are less toxic, can overcome drug resistance, and require shorter periods of treatment. These aspects are especially important for the populations of developing countries. It was reported that several phenylpropanoid-based secondary metabolites manifest interesting antileishmanial activities and are used by various indigenous people to treat leishmaniasis. In this chapter, the authors shed some light on the various biological activities of phenylpropanoid natural products, with the main focus being on their possible applications in the context of antileishmanial treatment.

• Klíčová slova
• Biological activity, Leishmaniasis, Lignans, Neolignans, Phenolic secondary metabolites, Phenylpropanoids,
• MeSH
• antiprotozoální látky * farmakologie   terapeutické užití   MeSH
• fenoly farmakologie   terapeutické užití   MeSH
• léčivé přípravky * MeSH
• leishmanióza * farmakoterapie   MeSH
• lidé MeSH
• lignany * farmakologie   terapeutické užití   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• antiprotozoální látky * MeSH
• fenoly MeSH
• léčivé přípravky * MeSH
• lignany * MeSH