Eric Lien - Academia.edu (original) (raw)
Papers by Eric Lien
J
Clinical trials of drugs for Alzheimer’s disease have called into question the role of amyloid in... more Clinical trials of drugs for Alzheimer’s disease have called into question the role of amyloid in the disease. The reasons several drugs recently failed clinical trials for Alzheimer’s disease are presented. An alternative approach with a traditional plant medicine is discussed. The pharmacology of the phytochemicals found in the plant medicine is provided.
Reactions Weekly, 2011
Traditional Chinese medicine , Traditional Chinese medicine , کتابخانه مرکزی دانشگاه علوم پزشکی ت... more Traditional Chinese medicine , Traditional Chinese medicine , کتابخانه مرکزی دانشگاه علوم پزشکی تهران
Journal of Lipid Research, 1977
Lipid accumulation is a hallmark of corpus luteum regression and we characterized lipids stored i... more Lipid accumulation is a hallmark of corpus luteum regression and we characterized lipids stored in rat corpora lutea of pregnancy between days 21 and 24 post coitum, the period of luteolysis. A 10-fold rise in lutein triglyceride concentrations occurred between days 2 1 and 24, which represented the major alteration in luteal lipid metabolism during luteolysis, coinciding with the appearance of numerous lipid droplets in the luteal cells. The fatty acid composition of luteal triglycerides was altered between days 20 and 23 in a pattern consistent with the influx of blood triglyceride fatty acids. No evidence for increased de novo fatty acid synthesis by luteal tissue between days 21 and 24 post coitum was obtained using in vitro methods. [14C]Acetate incorporation into lipids declined between days 16 and 24 and label was preferentially introduced into long chain polyunsaturated fatty acids. Rates of tritium incorporation into fatty acids from tritiated water were relatively low. [14C]Gluc~~e was predominantly incorporated into the glycerol moiety of luteal lipids and incorporation of label into this fraction was augmented between days 21 and 23 post coitum. The incorporation of [ 14C]palmitate into triglycerides of luteal tissue during in vitro incubation also increased between days 2 1 and 23. In vitro lactate production, ['4C]glucose oxidation, and ["C]palmitate oxidation to 14C02 increased significantly during this time. We conclude that specific biochemical alterations occur in regressing corpora facilitating uptake and storage of blood glyceride fatty acids as triglycerides. The physiological significance of this triglyceride accumulation remains to be elucidated.
Virus Research, 1989
Snmmary A series of hydroxyguanidine derivatives, which are substituted salicylaldehyde Schiff-ba... more Snmmary A series of hydroxyguanidine derivatives, which are substituted salicylaldehyde Schiff-bases of 1-amino-3-hydroxyguanidine tosylate, were tested for the inhibition of RNA synthesis of mouse hepatitis virus (MHV). It was shown that these compounds could selectively inhibit virus-specific RNA synthesis. Every aspect of viral RNA synthesis, including synthesis of negative-stranded RNA, subgenomic mRNA transcription and genomic RNA replication, was inhibited to roughly the same extent. These compounds are the first known inhibitors of coronaviral RNA synthesis and should prove useful for understanding the mechanism of viral RNA synthesis. Mouse hepatitis virus; Coronavirus Coronaviruses are enveloped RNA viruses associated with respiratory and gastrointestinal illnesses in humans and many other species of animals (Wege et al., 1982). The prototype coronavirus, mouse hepatitis virus (MHV), causes hepatitis and neurological diseases in mice. These viruses employ a complex mechanism for the synthesis of viral RNA (Lai, 1987). Upon infection of a susceptible cell, the viral genomic RNA, which is a positive-sensed single-stranded RNA of more than 6 x lo6 daltons (Lai and Stoleman, 1978), is released into the cytoplasm and used for the translation of a virus-specific RNA-dependent RNA polymerase (Brayton et al., 1982, 1984). This enzyme, in turn, transcribes the viral RNA into a negative
Biochemistry, 1975
A correlative study of the effects of two agents, 2-methyl-2-[p-(1,2,3,4-tetrahydro-1-naphthyl)ph... more A correlative study of the effects of two agents, 2-methyl-2-[p-(1,2,3,4-tetrahydro-1-naphthyl)phenoxy] propionic acid (TPIA) and amiloride, on aldosteroneinduced alterations in Na+ transport, lipid synthesis, and phospholipid fatty acid composition has been carried out in the toad urinary bladder. TPIA, an inhibitor of acetyl-coA carboxylase, inhibits aldosterone-stimulated Na+ transport as well as hormone-induced lipid synthesis and the increase in weight percentage of phospholipid long-chain polyunsaturated fatty acids. Amiloride, a diuretic which blocks so
Biochemical Pharmacology, 1990
A series of ~-hydroxy-~~aminoguanidine (HAG) derivatives were studied and compared for their effe... more A series of ~-hydroxy-~~aminoguanidine (HAG) derivatives were studied and compared for their effects on ribonu~leotide reductase activity in cell-free extracts; on nucleic acid synthesis and the growth of human colon carcinoma HT-29 cells; and on mouse leukemia L1210 cells in culture. The HAG derivatives ~RCH=NNHC(=NH)NHOH-tosy~ate] studied could be grouped as: (1) hydroxybenzylidines; (2) methoxyben~lidines; and (3) nitrobenzylidines substituted at the R position. 2'-Hydroxybenzylidine-HAG, the lead compound, was relatively active in both H'T-29 cells and L1210 cells (20 rt S and 13 f 4 pM for SO% inhibition of HT-29 and L1210 cell growth respectively). The monohydroxybenzylidene compounds were generally more active than the dihydroxy-and trihydroxybenzylidene-HAG derivatives. The methoxybenzylidene-HAGS were as active as the monohydroxybenzylidene-HAGS. 2'-Hydroxy-4'-methoxybenzylidene-HAG was much more active than 2',4'dihydroxybenzylidene-HAG. The mononitrobenzylidene-HAGS were more active than the dinitrobenzylidene-HAG compound. In general, L1210 cells were more sensitive to the effects of the HAG compounds than were HT-29 cells. There was good agreement between the concentration of drng required to inhibit the growth of HT-29 cells and that required to inhibit the growth of L1210 cells. There was also good correlation between the ability of HAG derivatives to inhibit r~bonu~leotide reductase activity and to inhibit tumor cell growth. Some derivatives, such as 2',3',4'-and 3',4',5'trihydroxybenzylidene-HAG inhibited L1210 cell growth by SO% at lower concentrations (7.8 and II .9 PM respectively) than the concentrations needed for SO% inhibition of HT.29 cell growth (1% and 234 HM respectively) and r~bonucleotide reductase activity (122 and 188 PM respectively). The studies of nucleic acid synthesis in Li210 cells using j3H]cytidine as a precursor showed that 2',3',4'-trihydroxybenzylidine-HAG inhibited DNA synthesis at a lower concentration (29 FM for SO% inhibition) than was needed for the inhibition of RNA synthesis and formation of [jH]deoxycytidine nucleotides in the acid-soluble fraction (320 and 820 PM for SO% inhibition respectively). These results indicate that 2',3',4'-trihydroxybenzylidine-HAG inhibits DNA synthesis in L1210 cells through other mechanisms rather than exclusively through the inhibition of ribonucleotide reductase activity.
Drug Discovery, 2013
The species Homo sapiens has existed for 200 000 years or so. Medicinal plants have been importan... more The species Homo sapiens has existed for 200 000 years or so. Medicinal plants have been important to humans as indicated by plants in prehistoric burial sites, mummy wrappings and ancient legends. It is likely that during the entire period of human existence, plants have been used as medicines. Thi...
Medicines, 2016
Background: This study examined the chemistry and safety of Heteromeles arbutifolia, also called ... more Background: This study examined the chemistry and safety of Heteromeles arbutifolia, also called toyon or California holly, which is a traditional California Indian food and treatment for Alzheimer's disease. Methods: Plant extracts were examined by HPLC/MS, NMR and other techniques to identify compounds. Volunteers were recruited to examine the acute safety of the plant medicine using a standard short-term memory test. Results: The plant was found to contain icariside E4, dihydroxyoleanenoic acid, maslinic acid, betulin, trihydroxyoxo-seco-ursdienoic acid, catechin, vicenin-2, farrerol, kaempferide and tetrahydroxyoleanenoic acid. These compounds are anti-inflammatory agents that may protect the blood-brain barrier and prevent inflammatory cell infiltration into the brain. The dried berries were ingested by six volunteers to demonstrate the safety of the medicine. Conclusion: The plant medicine was found to contain several compounds that may be of interest in the treatment of Alzheimer's disease. The plant medicine was found to be safe.
RSC Drug Discovery
In traditional Chinese medicine (TCM), usually several different plants are used in the treatment... more In traditional Chinese medicine (TCM), usually several different plants are used in the treatment or prevention of illness, according to the condition and need of the individual patient. The outcome is observed subjectively by the physician so that the prescription can be adjusted according to the e...
Chinese medicine, Jan 23, 2006
Salvia miltiorrhiza (Labiatae, Laminaceae), danshen, is an annual sage mainly found in China and ... more Salvia miltiorrhiza (Labiatae, Laminaceae), danshen, is an annual sage mainly found in China and neighboring countries. The crude drug (dried root) and its preparations are currently used in China to treat patients suffering from heart attack, angina pectoris, stroke and some other conditions. The use of S. miltiorrhiza has been increasing in the management of stroke. Pharmacological examinations showed that the plant and its active ingredients, tanshinones and salvianolic acids, have anticoagulant, vasodilatory, increased blood flow, anti-inflammatory, free radical scavenging, mitochondrial protective and other activities. This review discusses the pharmacology, medicinal chemistry and clinical studies published, especially in China, for danshen and tanshinone preparations. Clinical examinations are evaluated in terms of S. miltiorrhiza preparation, dose, double blinding, control, clinical assessments of outcomes and other parameters. Meta-analyses of S. miltiorrhiza are also discu...
Acta Oncologica, 1994
The 2-hydroxy-1 H-isoindole-l,3-dione (HISD) derivatives are inhibitors of ribonucleotide reducta... more The 2-hydroxy-1 H-isoindole-l,3-dione (HISD) derivatives are inhibitors of ribonucleotide reductase (RR). Among the seven new compounds of the PL series, three were found to be active in cell lines sensitive (CEM/O) or resistant to ara-C (CEM/ara-C/7A; CEM/dCk[-1). The compounds PL4, PL7 and PL8 exhibited ICs0 values in micromolar range against the three CEM cell lines. The 3 compounds showed 100to 1000-fold higher cytotoxicity compared to HU against all three CEM cell lines. Combination of each of the three active PL compounds with ara-C showed high degree of synergism in comparison to the combinations of HU with ara-C against both CEM/O and CEM/ara-C/7A cell lines. The DNA synthetic capacity of CEM/O cells treated with 10 pM PL4 for 24 or 48 h was inhibited 2 99.8% simultaneously the cellular NTP pools were severely depleted. Treatment of CEM/O cells with 10 pM PL4 showed steady depletion in all the dNTP pools at 1 or 2 h and complete depletion by 4 h. The enzyme activity did not recover up to 48 h in presence of the drug suggesting irreversible inhibition of RR. Among the enzymes that show elevated levels of activity in tumor cells, ribonucleotide reductase (R R) (E.C. 1.17.4.1) is one of the most important. It is an allosterically regulated enzyme that converts the nucleoside diphosphates (NDPs) to their corresponding deoxynucleoside diphosphates (dNDPs) through a complex regulatory mechanism involving one or several electron transfer pathways (1-4).
Chinese Medicine, 2007
A literature survey was conducted on herbs, their preparations and ingredients with reported live... more A literature survey was conducted on herbs, their preparations and ingredients with reported liver protection activities, in which a total of 274 different species and hundreds of active ingredients have been examined. These ingredients can be roughly classified into two categories according to their activities: (1) the main ingredients, such as silybin, osthole, coumarin, glycyrrhizin, saikosaponin A, schisandrin A, flavonoids; and (2) supporting substances, such as sugars, amino acids, resins, tannins and volatile oil. Among them, some active ingredients have hepatoprotective activities (e.g. anti-inflammatory, anticancer, antioxidant, immunomodulating and liver cirrhosis-regulating effects). Calculation of physicochemical parameters indicates that the main ingredients with negative and positive Elumo values possibly display their hepatoprotective effects through different mechanisms, such as antioxidative, anti-inflammatory and immunomodulating effects. As the combination of herb...
Current medicinal chemistry, Jan 18, 2018
Inflammatory states are among the most common and most treated medical conditions. Inflammation c... more Inflammatory states are among the most common and most treated medical conditions. Inflammation comes along with swelling, pain and uneasiness in using the affected area. Inflammation is not always a simple symptom; more often is part of a defensive response of the body to an external threat or is a sign that the damaged tissue has not healed yet and needs to rest. The management of the pain associated with an inflammatory state could be a tricky task. In fact, most remedies simply quench the pain, leaving the inflammatory state unaltered. This review focuses on sesquiterpene lactones, a class of natural compounds, that represents a future promise in the treatment of inflammation. Sesquiterpene lactones are efficient inhibitors of multiple targets of the inflammatory process. Their natural sources are often ancient remedies with relevant traditional uses in folk medicines. This work also aims to elucidate how these compounds may represent the starting material for the development of...
J
Clinical trials of drugs for Alzheimer’s disease have called into question the role of amyloid in... more Clinical trials of drugs for Alzheimer’s disease have called into question the role of amyloid in the disease. The reasons several drugs recently failed clinical trials for Alzheimer’s disease are presented. An alternative approach with a traditional plant medicine is discussed. The pharmacology of the phytochemicals found in the plant medicine is provided.
J
Clinical trials of drugs for Alzheimer’s disease have called into question the role of amyloid in... more Clinical trials of drugs for Alzheimer’s disease have called into question the role of amyloid in the disease. The reasons several drugs recently failed clinical trials for Alzheimer’s disease are presented. An alternative approach with a traditional plant medicine is discussed. The pharmacology of the phytochemicals found in the plant medicine is provided.
Evidence-Based Complementary and Alternative Medicine, 2010
Chinese and Chumash traditional medical approaches are similar in terms of disease causation, use... more Chinese and Chumash traditional medical approaches are similar in terms of disease causation, use of acupuncture or healing touch, plants, spiritual and philosophical approaches. This article provides a brief comparison and discussion of Chinese and Chumash traditional medical practices. A table of 66 plants is presented along with Chinese and Chumash uses of each plant. These uses are compared and contrasted.
Evidence-Based Complementary and Alternative Medicine, 2010
Chinese and Chumash traditional medical approaches are similar in terms of disease causation, use... more Chinese and Chumash traditional medical approaches are similar in terms of disease causation, use of acupuncture or healing touch, plants, spiritual and philosophical approaches. This article provides a brief comparison and discussion of Chinese and Chumash traditional medical practices. A table of 66 plants is presented along with Chinese and Chumash uses of each plant. These uses are compared and contrasted.
Chinese medicine, 2006
Salvia miltiorrhiza (Labiatae, Laminaceae), danshen, is an annual sage mainly found in China and ... more Salvia miltiorrhiza (Labiatae, Laminaceae), danshen, is an annual sage mainly found in China and neighboring countries. The crude drug (dried root) and its preparations are currently used in China to treat patients suffering from heart attack, angina pectoris, stroke and some other conditions. The use of S. miltiorrhiza has been increasing in the management of stroke. Pharmacological examinations showed that the plant and its active ingredients, tanshinones and salvianolic acids, have anticoagulant, vasodilatory, increased blood flow, anti-inflammatory, free radical scavenging, mitochondrial protective and other activities. This review discusses the pharmacology, medicinal chemistry and clinical studies published, especially in China, for danshen and tanshinone preparations. Clinical examinations are evaluated in terms of S. miltiorrhiza preparation, dose, double blinding, control, clinical assessments of outcomes and other parameters. Meta-analyses of S. miltiorrhiza are also discu...
J
Clinical trials of drugs for Alzheimer’s disease have called into question the role of amyloid in... more Clinical trials of drugs for Alzheimer’s disease have called into question the role of amyloid in the disease. The reasons several drugs recently failed clinical trials for Alzheimer’s disease are presented. An alternative approach with a traditional plant medicine is discussed. The pharmacology of the phytochemicals found in the plant medicine is provided.
Reactions Weekly, 2011
Traditional Chinese medicine , Traditional Chinese medicine , کتابخانه مرکزی دانشگاه علوم پزشکی ت... more Traditional Chinese medicine , Traditional Chinese medicine , کتابخانه مرکزی دانشگاه علوم پزشکی تهران
Journal of Lipid Research, 1977
Lipid accumulation is a hallmark of corpus luteum regression and we characterized lipids stored i... more Lipid accumulation is a hallmark of corpus luteum regression and we characterized lipids stored in rat corpora lutea of pregnancy between days 21 and 24 post coitum, the period of luteolysis. A 10-fold rise in lutein triglyceride concentrations occurred between days 2 1 and 24, which represented the major alteration in luteal lipid metabolism during luteolysis, coinciding with the appearance of numerous lipid droplets in the luteal cells. The fatty acid composition of luteal triglycerides was altered between days 20 and 23 in a pattern consistent with the influx of blood triglyceride fatty acids. No evidence for increased de novo fatty acid synthesis by luteal tissue between days 21 and 24 post coitum was obtained using in vitro methods. [14C]Acetate incorporation into lipids declined between days 16 and 24 and label was preferentially introduced into long chain polyunsaturated fatty acids. Rates of tritium incorporation into fatty acids from tritiated water were relatively low. [14C]Gluc~~e was predominantly incorporated into the glycerol moiety of luteal lipids and incorporation of label into this fraction was augmented between days 21 and 23 post coitum. The incorporation of [ 14C]palmitate into triglycerides of luteal tissue during in vitro incubation also increased between days 2 1 and 23. In vitro lactate production, ['4C]glucose oxidation, and ["C]palmitate oxidation to 14C02 increased significantly during this time. We conclude that specific biochemical alterations occur in regressing corpora facilitating uptake and storage of blood glyceride fatty acids as triglycerides. The physiological significance of this triglyceride accumulation remains to be elucidated.
Virus Research, 1989
Snmmary A series of hydroxyguanidine derivatives, which are substituted salicylaldehyde Schiff-ba... more Snmmary A series of hydroxyguanidine derivatives, which are substituted salicylaldehyde Schiff-bases of 1-amino-3-hydroxyguanidine tosylate, were tested for the inhibition of RNA synthesis of mouse hepatitis virus (MHV). It was shown that these compounds could selectively inhibit virus-specific RNA synthesis. Every aspect of viral RNA synthesis, including synthesis of negative-stranded RNA, subgenomic mRNA transcription and genomic RNA replication, was inhibited to roughly the same extent. These compounds are the first known inhibitors of coronaviral RNA synthesis and should prove useful for understanding the mechanism of viral RNA synthesis. Mouse hepatitis virus; Coronavirus Coronaviruses are enveloped RNA viruses associated with respiratory and gastrointestinal illnesses in humans and many other species of animals (Wege et al., 1982). The prototype coronavirus, mouse hepatitis virus (MHV), causes hepatitis and neurological diseases in mice. These viruses employ a complex mechanism for the synthesis of viral RNA (Lai, 1987). Upon infection of a susceptible cell, the viral genomic RNA, which is a positive-sensed single-stranded RNA of more than 6 x lo6 daltons (Lai and Stoleman, 1978), is released into the cytoplasm and used for the translation of a virus-specific RNA-dependent RNA polymerase (Brayton et al., 1982, 1984). This enzyme, in turn, transcribes the viral RNA into a negative
Biochemistry, 1975
A correlative study of the effects of two agents, 2-methyl-2-[p-(1,2,3,4-tetrahydro-1-naphthyl)ph... more A correlative study of the effects of two agents, 2-methyl-2-[p-(1,2,3,4-tetrahydro-1-naphthyl)phenoxy] propionic acid (TPIA) and amiloride, on aldosteroneinduced alterations in Na+ transport, lipid synthesis, and phospholipid fatty acid composition has been carried out in the toad urinary bladder. TPIA, an inhibitor of acetyl-coA carboxylase, inhibits aldosterone-stimulated Na+ transport as well as hormone-induced lipid synthesis and the increase in weight percentage of phospholipid long-chain polyunsaturated fatty acids. Amiloride, a diuretic which blocks so
Biochemical Pharmacology, 1990
A series of ~-hydroxy-~~aminoguanidine (HAG) derivatives were studied and compared for their effe... more A series of ~-hydroxy-~~aminoguanidine (HAG) derivatives were studied and compared for their effects on ribonu~leotide reductase activity in cell-free extracts; on nucleic acid synthesis and the growth of human colon carcinoma HT-29 cells; and on mouse leukemia L1210 cells in culture. The HAG derivatives ~RCH=NNHC(=NH)NHOH-tosy~ate] studied could be grouped as: (1) hydroxybenzylidines; (2) methoxyben~lidines; and (3) nitrobenzylidines substituted at the R position. 2'-Hydroxybenzylidine-HAG, the lead compound, was relatively active in both H'T-29 cells and L1210 cells (20 rt S and 13 f 4 pM for SO% inhibition of HT-29 and L1210 cell growth respectively). The monohydroxybenzylidene compounds were generally more active than the dihydroxy-and trihydroxybenzylidene-HAG derivatives. The methoxybenzylidene-HAGS were as active as the monohydroxybenzylidene-HAGS. 2'-Hydroxy-4'-methoxybenzylidene-HAG was much more active than 2',4'dihydroxybenzylidene-HAG. The mononitrobenzylidene-HAGS were more active than the dinitrobenzylidene-HAG compound. In general, L1210 cells were more sensitive to the effects of the HAG compounds than were HT-29 cells. There was good agreement between the concentration of drng required to inhibit the growth of HT-29 cells and that required to inhibit the growth of L1210 cells. There was also good correlation between the ability of HAG derivatives to inhibit r~bonu~leotide reductase activity and to inhibit tumor cell growth. Some derivatives, such as 2',3',4'-and 3',4',5'trihydroxybenzylidene-HAG inhibited L1210 cell growth by SO% at lower concentrations (7.8 and II .9 PM respectively) than the concentrations needed for SO% inhibition of HT.29 cell growth (1% and 234 HM respectively) and r~bonucleotide reductase activity (122 and 188 PM respectively). The studies of nucleic acid synthesis in Li210 cells using j3H]cytidine as a precursor showed that 2',3',4'-trihydroxybenzylidine-HAG inhibited DNA synthesis at a lower concentration (29 FM for SO% inhibition) than was needed for the inhibition of RNA synthesis and formation of [jH]deoxycytidine nucleotides in the acid-soluble fraction (320 and 820 PM for SO% inhibition respectively). These results indicate that 2',3',4'-trihydroxybenzylidine-HAG inhibits DNA synthesis in L1210 cells through other mechanisms rather than exclusively through the inhibition of ribonucleotide reductase activity.
Drug Discovery, 2013
The species Homo sapiens has existed for 200 000 years or so. Medicinal plants have been importan... more The species Homo sapiens has existed for 200 000 years or so. Medicinal plants have been important to humans as indicated by plants in prehistoric burial sites, mummy wrappings and ancient legends. It is likely that during the entire period of human existence, plants have been used as medicines. Thi...
Medicines, 2016
Background: This study examined the chemistry and safety of Heteromeles arbutifolia, also called ... more Background: This study examined the chemistry and safety of Heteromeles arbutifolia, also called toyon or California holly, which is a traditional California Indian food and treatment for Alzheimer's disease. Methods: Plant extracts were examined by HPLC/MS, NMR and other techniques to identify compounds. Volunteers were recruited to examine the acute safety of the plant medicine using a standard short-term memory test. Results: The plant was found to contain icariside E4, dihydroxyoleanenoic acid, maslinic acid, betulin, trihydroxyoxo-seco-ursdienoic acid, catechin, vicenin-2, farrerol, kaempferide and tetrahydroxyoleanenoic acid. These compounds are anti-inflammatory agents that may protect the blood-brain barrier and prevent inflammatory cell infiltration into the brain. The dried berries were ingested by six volunteers to demonstrate the safety of the medicine. Conclusion: The plant medicine was found to contain several compounds that may be of interest in the treatment of Alzheimer's disease. The plant medicine was found to be safe.
RSC Drug Discovery
In traditional Chinese medicine (TCM), usually several different plants are used in the treatment... more In traditional Chinese medicine (TCM), usually several different plants are used in the treatment or prevention of illness, according to the condition and need of the individual patient. The outcome is observed subjectively by the physician so that the prescription can be adjusted according to the e...
Chinese medicine, Jan 23, 2006
Salvia miltiorrhiza (Labiatae, Laminaceae), danshen, is an annual sage mainly found in China and ... more Salvia miltiorrhiza (Labiatae, Laminaceae), danshen, is an annual sage mainly found in China and neighboring countries. The crude drug (dried root) and its preparations are currently used in China to treat patients suffering from heart attack, angina pectoris, stroke and some other conditions. The use of S. miltiorrhiza has been increasing in the management of stroke. Pharmacological examinations showed that the plant and its active ingredients, tanshinones and salvianolic acids, have anticoagulant, vasodilatory, increased blood flow, anti-inflammatory, free radical scavenging, mitochondrial protective and other activities. This review discusses the pharmacology, medicinal chemistry and clinical studies published, especially in China, for danshen and tanshinone preparations. Clinical examinations are evaluated in terms of S. miltiorrhiza preparation, dose, double blinding, control, clinical assessments of outcomes and other parameters. Meta-analyses of S. miltiorrhiza are also discu...
Acta Oncologica, 1994
The 2-hydroxy-1 H-isoindole-l,3-dione (HISD) derivatives are inhibitors of ribonucleotide reducta... more The 2-hydroxy-1 H-isoindole-l,3-dione (HISD) derivatives are inhibitors of ribonucleotide reductase (RR). Among the seven new compounds of the PL series, three were found to be active in cell lines sensitive (CEM/O) or resistant to ara-C (CEM/ara-C/7A; CEM/dCk[-1). The compounds PL4, PL7 and PL8 exhibited ICs0 values in micromolar range against the three CEM cell lines. The 3 compounds showed 100to 1000-fold higher cytotoxicity compared to HU against all three CEM cell lines. Combination of each of the three active PL compounds with ara-C showed high degree of synergism in comparison to the combinations of HU with ara-C against both CEM/O and CEM/ara-C/7A cell lines. The DNA synthetic capacity of CEM/O cells treated with 10 pM PL4 for 24 or 48 h was inhibited 2 99.8% simultaneously the cellular NTP pools were severely depleted. Treatment of CEM/O cells with 10 pM PL4 showed steady depletion in all the dNTP pools at 1 or 2 h and complete depletion by 4 h. The enzyme activity did not recover up to 48 h in presence of the drug suggesting irreversible inhibition of RR. Among the enzymes that show elevated levels of activity in tumor cells, ribonucleotide reductase (R R) (E.C. 1.17.4.1) is one of the most important. It is an allosterically regulated enzyme that converts the nucleoside diphosphates (NDPs) to their corresponding deoxynucleoside diphosphates (dNDPs) through a complex regulatory mechanism involving one or several electron transfer pathways (1-4).
Chinese Medicine, 2007
A literature survey was conducted on herbs, their preparations and ingredients with reported live... more A literature survey was conducted on herbs, their preparations and ingredients with reported liver protection activities, in which a total of 274 different species and hundreds of active ingredients have been examined. These ingredients can be roughly classified into two categories according to their activities: (1) the main ingredients, such as silybin, osthole, coumarin, glycyrrhizin, saikosaponin A, schisandrin A, flavonoids; and (2) supporting substances, such as sugars, amino acids, resins, tannins and volatile oil. Among them, some active ingredients have hepatoprotective activities (e.g. anti-inflammatory, anticancer, antioxidant, immunomodulating and liver cirrhosis-regulating effects). Calculation of physicochemical parameters indicates that the main ingredients with negative and positive Elumo values possibly display their hepatoprotective effects through different mechanisms, such as antioxidative, anti-inflammatory and immunomodulating effects. As the combination of herb...
Current medicinal chemistry, Jan 18, 2018
Inflammatory states are among the most common and most treated medical conditions. Inflammation c... more Inflammatory states are among the most common and most treated medical conditions. Inflammation comes along with swelling, pain and uneasiness in using the affected area. Inflammation is not always a simple symptom; more often is part of a defensive response of the body to an external threat or is a sign that the damaged tissue has not healed yet and needs to rest. The management of the pain associated with an inflammatory state could be a tricky task. In fact, most remedies simply quench the pain, leaving the inflammatory state unaltered. This review focuses on sesquiterpene lactones, a class of natural compounds, that represents a future promise in the treatment of inflammation. Sesquiterpene lactones are efficient inhibitors of multiple targets of the inflammatory process. Their natural sources are often ancient remedies with relevant traditional uses in folk medicines. This work also aims to elucidate how these compounds may represent the starting material for the development of...
J
Clinical trials of drugs for Alzheimer’s disease have called into question the role of amyloid in... more Clinical trials of drugs for Alzheimer’s disease have called into question the role of amyloid in the disease. The reasons several drugs recently failed clinical trials for Alzheimer’s disease are presented. An alternative approach with a traditional plant medicine is discussed. The pharmacology of the phytochemicals found in the plant medicine is provided.
J
Clinical trials of drugs for Alzheimer’s disease have called into question the role of amyloid in... more Clinical trials of drugs for Alzheimer’s disease have called into question the role of amyloid in the disease. The reasons several drugs recently failed clinical trials for Alzheimer’s disease are presented. An alternative approach with a traditional plant medicine is discussed. The pharmacology of the phytochemicals found in the plant medicine is provided.
Evidence-Based Complementary and Alternative Medicine, 2010
Chinese and Chumash traditional medical approaches are similar in terms of disease causation, use... more Chinese and Chumash traditional medical approaches are similar in terms of disease causation, use of acupuncture or healing touch, plants, spiritual and philosophical approaches. This article provides a brief comparison and discussion of Chinese and Chumash traditional medical practices. A table of 66 plants is presented along with Chinese and Chumash uses of each plant. These uses are compared and contrasted.
Evidence-Based Complementary and Alternative Medicine, 2010
Chinese and Chumash traditional medical approaches are similar in terms of disease causation, use... more Chinese and Chumash traditional medical approaches are similar in terms of disease causation, use of acupuncture or healing touch, plants, spiritual and philosophical approaches. This article provides a brief comparison and discussion of Chinese and Chumash traditional medical practices. A table of 66 plants is presented along with Chinese and Chumash uses of each plant. These uses are compared and contrasted.
Chinese medicine, 2006
Salvia miltiorrhiza (Labiatae, Laminaceae), danshen, is an annual sage mainly found in China and ... more Salvia miltiorrhiza (Labiatae, Laminaceae), danshen, is an annual sage mainly found in China and neighboring countries. The crude drug (dried root) and its preparations are currently used in China to treat patients suffering from heart attack, angina pectoris, stroke and some other conditions. The use of S. miltiorrhiza has been increasing in the management of stroke. Pharmacological examinations showed that the plant and its active ingredients, tanshinones and salvianolic acids, have anticoagulant, vasodilatory, increased blood flow, anti-inflammatory, free radical scavenging, mitochondrial protective and other activities. This review discusses the pharmacology, medicinal chemistry and clinical studies published, especially in China, for danshen and tanshinone preparations. Clinical examinations are evaluated in terms of S. miltiorrhiza preparation, dose, double blinding, control, clinical assessments of outcomes and other parameters. Meta-analyses of S. miltiorrhiza are also discu...