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Dear Colleague, This Newsletter highlights a joint Planta Medica issue combining issues 2 and 3. I would like to focus on a review, a pharmacological study, and a natural product chemistry paper. In their review Wölfe et al. cover the topical applications of St. John's wort (Hypericum perforatum). This herb is one of the most prominent and best investigated medicinal plants of the last decades, mainly because of its antidepressant activity. From the beginning, however, traditional use was also characterized by external applications, mainly in the form of oils and tinctures, e.g. as a treatment for burns. |
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In Mexico, the combination of medicinal herbs and pharmaceutical drugs is a common practice; unfortunately, there is little scientific evidence for the pharmacological interactions between natural products and drugs. Déciga-Campos et al. have combined ursolic acid, a pentacyclic triterpene isolated from various plant species used for their analgesic properties, with diclofenac (a non-steroidal anti-inflammatory drug) and tramadol (an agonist opioid drug), in order to evaluate their antinociceptive synergistic interactions. Pancreatic cancer is one of the most deadly forms of cancer associated with the lowest 5-year survival rates known for cancers. Pancreatic cancers are hypovascular in nature resulting in an inadequate supply of nutrition and oxygen to aggressively proliferating cells. However, pancreatic cancer cells show an extraordinary tolerance to starvation enabling them to survive in hypovascular (austerity) conditions. Development of drugs aimed at countering this tolerance to nutrient starvation is a novel antiausterity approach in anticancer drug discovery. Mai Thanh Thi Nguyen et al. have screened a series of medicinal plants for antiausterity activity, using the PANC-1 human pancreatic cancer cell line. Some geranyl dihydrochalcones from Artocarpus altilis were identified as potent antitumoural candidates. It is my pleasure to offer you free access to these publications! Sincerely yours,  Luc Pieters Planta Medica, Editor-in-Chief |
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CONTENTS
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Topical Application of St.
John's Wort (Hypericum perforatum) (FREE ACCESS)
Ute Wölfle, Günter Seelinger, Christoph M. Schempp |
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St.
John's wort (Hypericum
perforatum) has been intensively investigated for its
antidepressive activity, but dermatological applications also have a long
tradition. Topical St. John's wort preparations such as oils or tinctures are
used for the treatment of minor wounds and burns, sunburns, abrasions,
bruises, contusions, ulcers, myalgia, and many others. Pharmacological
research supports the use in these fields. Of the constituents,
naphthodianthrones (e.g., hypericin) and phloroglucinols (e.g., hyperforin)
have interesting pharmacological profiles, including antioxidant,
anti-inflammatory, anticancer, and antimicrobial activities.
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In
addition, hyperforin stimulates growth and differentiation of keratinocytes,
and hypericin is a photosensitizer which can be used for selective treatment
of non-melanoma skin cancer. However, clinical research in this field is
still scarce. Recently, sporadic trials have been conducted in wound healing,
atopic dermatitis, psoriasis, and herpes simplex infections, partly with
purified single constituents and modern dermatological formulations. St.
John's wort also has a potential for use in medical skin care. Composition
and stability of pharmaceutical formulations vary greatly depending on origin
of the plant material, production method, lipophilicity of solvents, and
storage conditions, and this must be regarded with respect to practical as
well as scientific purposes. Read more
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Isobolographic Analysis of
the Antinociceptive Interaction between Ursolic Acid and Diclofenac or
Tramadol in Mice (FREE ACCESS)
Myrna Déciga-Campos, Alejandra Cortés, Francisco Pellicer, Irene Díaz-Reval, María Eva González-Trujano |
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It
is considered that natural products used in folk medicine can potentiate the
effect of drugs. The aim of this study was to evaluate the pharmacological
interaction between ursolic acid, a triterpene isolated from herbal medicines
to treat pain, and the analgesics diclofenac or tramadol. Individual
dose-response curves of the antinociceptive effect of these compounds were
built to calculate the ED50, as well as the pharmacological
interaction, by using isobolographic analysis. All treatments decreased
significantly and in a dose-dependent manner the writhing behavior with ED50
values of 103.50 ± 19.66, 20.54 ± 6.05, and 9.60 ± 1.69mg/kg, for ursolic
acid, diclofenac, and tramadol, respectively.
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An
isobolographic analysis allowed the characterization of the pharmacological
interaction produced by a fixed ratio combination of 1:1 and 1:3 of
equi-effective doses of these compounds. Theoretical antinociceptive ED50
values of ursolic acid–diclofenac were 62.12 ± 10.28 and 41.43 ± 6.69 mg/kg,
respectively, not statistically different from those obtained experimentally
(44.52 ± 5.25 and 44.89 ± 49.05 mg/kg, respectively), reporting an additive
interaction. Theoretical antinociceptive ED50 values of ursolic
acid-tramadol (56.56 ± 9.87 and 33.08 ± 5.07 mg/kg, respectively) were
significantly lower than those observed experimentally (138.36 ± 49.05 and
67.34 ± 18.98 mg/kg, respectively) reporting antagonism in this interaction.
Antinociceptive response obtained from isobolograms in the writhing test was
corroborated by using formalin test in mice. Adverse effects such as gastric
damage in the ursolic acid-diclofenac combination did not increase in an
additive form similarly as with antinociception. Conversely, sedative
response was significantly increased in the ursolic acid-tramadol
combination. As observed in the formalin test, the antagonism on the
antinociceptive response between ursolic acid and tramadol (1:1) was not reverted
in the presence of the opioid antagonist naltrexone (1mg/kg, i. p.). These
results provide evidence for a differential pharmacological interaction, in
which ursolic acid does not interfere with the antinociceptive effect of
diclofenac but antagonizes that obtained with tramadol in an independent
opioid mechanism. Therefore, medicinal plants containing abundant presence of
ursolic acid may also modify efficacy in the alternative combinations for
pain therapy. Read more
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Geranyl Dihydrochalcones
from Artocarpus altilis and Their Antiausteric Activity (FREE ACCESS)
Mai Thanh Thi Nguyen, Nhan Trung Nguyen, Khang Duy Huu Nguyen, Hien Thu Thi Dau, Hai Xuan Nguyen, Phu Hoang Dang, Tam Minh Le, Trong Huu Nguyen Phan, Anh Hai Tran, Bac Duy Nguyen, Jun-ya Ueda, Suresh Awale |
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Human
pancreatic cancer cell lines have remarkable tolerance to nutrition
starvation, which enables them to survive under a tumor microenvironment. The
search for agents that preferentially inhibit the survival of cancer cells
under low nutrient conditions is a novel antiausterity strategy in anticancer
drug discovery.
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In
this study, the methanolic extract of the leaves of Artocarpus altilis showed
100% preferential cytotoxicity against PANC-1 human pancreatic cancer cells
under nutrient-deprived conditions at a concentration of 50 μg/mL. Further
investigation of this extract led to the isolation of eight new geranylated
dihydrochalcones named sakenins A-H together with four known compounds. Among
them, sakenins F and H were identified as potent preferentially cytotoxic
candidates with PC50 values of 8.0 μM and 11.1 μM, respectively. Read more
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Table of Contents: Issues 2 and 3,
February 2014
Reviews Topical Application of St. Johnʼs Wort (Hypericum perforatum) Ute Wölfle, Günter Seelinger, Christoph M. Schempp Abstract | HTML | PDF Biological and Pharmacological Activity Original Papers The Ethanol Extract of Lonicera japonica (Japanese Honeysuckle) Attenuates Diabetic Nephropathy by Inhibiting p-38 MAPK Activity in Streptozotocin-Induced Diabetic Rats Thing-Fong Tzeng, Shorong-Shii Liou, Chia Ju Chang, I-Min Liu Abstract | HTML | PDF The Effect of 2,3,4′,5-Tetrahydroxystilbene-2-O-ß-D-Glucoside on Pressure Overload-Induced Cardiac Remodeling in Rats and Its Possible Mechanism Xiao Le Xu, Qiu Yan Zhu, Cheng Zhao, Fei Wang, Zhong Yin Zhou, Ya E Hu, Wei Zhang Abstract | HTML | PDF Isobolographic Analysis of the Antinociceptive Interaction between Ursolic Acid and Diclofenac or Tramadol in Mice Myrna Déciga-Campos, Alejandra Cortés, Francisco Pellicer, Irene Díaz-Reval, María Eva González-Trujano Abstract | HTML | PDF The Total Phenolic Fraction of Anemarrhena asphodeloides Inhibits Inflammation and Reduces Insulin Resistance in Adipocytes via Regulation of AMP-Kinase Activity Wenjun Zhao, Meng Wang, Lu Shao, Min Liao, Kang Liu, Fang Huang, Baolin Liu Abstract | HTML | PDF The Inhibitory Effect of Scutellaria baicalensis Extract and Its Active Compound, Baicalin, on the Translocation of the Androgen Receptor with Implications for Preventing Androgenetic Alopecia Ah-Reum Kim, Su-Na Kim, In-Keun Jung, Hyun-Hee Kim, Young-Ho Park, Won-Seok Park Abstract | HTML | PDF Ferulic Acid Enhances the Chemical and Biological Properties of Astragali Radix: A Stimulator for Danggui Buxue Tang, An Ancient Chinese Herbal Decoction Ken Y. Z. Zheng, Zhen X. Zhang, Crystal Y. Q. Du, Wendy L. Zhang, Cathy W. C. Bi, Roy C. Y. Choi, Tina T. X. Dong, Karl W. K. Tsim Abstract | HTML | PDF Acaricidal Activities against House Dust Mites of Spearmint Oil and Its Constituents Ji-Yeon Yang, Min-Gi Kim, Sung-Eun Lee, Hoi-Seon Lee Abstract | HTML | PDF Inhibition of Hepatitis C Virus Replication In Vitro by Xanthohumol, A Natural Product Present in Hops Sai Lou, Yi-Min Zheng, Shan-Lu Liu, Jianming Qiu, Qunying Han, Na Li, Qianqian Zhu, Pingping Zhang, Cuiling Yang, Zhengwen Liu Abstract | HTML | PDF Kaempferol Derivatives as Antiviral Drugs against the 3a Channel Protein of Coronavirus Silvia Schwarz, Daniel Sauter, Kai Wang, Ronghua Zhang, Bing Sun, Anastasia Karioti, Anna Rita Bilia, Thomas Efferth, Wolfgang Schwarz Abstract | HTML | PDF Letters In Vitro and In Vivo Studies of Trypanocidal Activity of Dietary Isothiocyanates Dietmar Steverding, Sarah Michaels, Kevin D. Read Abstract | HTML | PDF Pharmacokinetic Investigations Original Papers Pharmacokinetic Interaction of Astragaloside IV with Atractylenolide I and Prim-O-Glucosylcimifugin in Male Sprague Dawley Rats Jue Song, Shi-rui Zheng, Yong Jin, Jun Li Abstract | HTML | PDF Natural Product Chemistry Original Papers Geranyl Dihydrochalcones from Artocarpus altilis and Their Antiausteric Activity Mai Thanh Thi Nguyen, Nhan Trung Nguyen, Khang Duy Huu Nguyen, Hien Thu Thi Dau, Hai Xuan Nguyen, Phu Hoang Dang, Tam Minh Le, Trong Huu Nguyen Phan, Anh Hai Tran, Bac Duy Nguyen, Jun-ya Ueda, Suresh Awale Abstract | HTML | PDF Xanthones from Swertia mussotii and Their α-Glycosidase Inhibitory Activities Cui-Ting Luo, Huan-huan Zheng, Shuang-Shuang Mao, Mao-xun Yang, Cheng Luo, Heru Chen Abstract | HTML | PDF Sphaeralcic Acid and Tomentin, Anti-inflammatory Compounds Produced in Cell Suspension Cultures of Sphaeralcea angustifolia Juanita Pérez-Hernández, Manasés González-Cortazar, Silvia Marquina, Maribel Herrera-Ruiz, Mariana Meckes-Fischer, Jaime Tortoriello, Francisco Cruz-Sosa, María del Pilar Nicasio-Torres Abstract | HTML | PDF Hepatoprotective Triterpenoids and Saponins of Schefflera kwangsiensis Yan Wang, Chun-Lei Zhang, Yan-Fei Liu, Dong Liang, Huan Luo, Zhi-You Hao, Ruo-Yun Chen, De-Quan Yu Abstract | HTML | PDF Cinchona Alkaloids from Cinchona succirubra and Cinchona ledgeriana Gui-Guang Cheng, Xiang-Hai Cai, Bao-Hong Zhang, Yan Li, Ji Gu, Mei-Fen Bao, Ya-Ping Liu, Xiao-Dong Luo Abstract | HTML | PDF Letters Diterpene Alkaloids from the Roots of Aconitum moldavicum and Assessment of Nav 1.2 Sodium Channel Activity of Aconitum Alkaloids Botond Borcsa, László Fodor, Dezsõ Csupor, Peter Forgo, Attila Molnár V., Judit Hohmann Abstract | HTML | PDF Analytical Studies Original Papers Simultaneous Determination of Five Minor Coumarins and Flavonoids in Glycyrrhiza uralensis by Solid-Phase Extraction and High-Performance Liquid Chromatography/Electrospray Ionization Tandem Mass Spectrometry Xue Qiao, Chun-Fang Liu, Shuai Ji, Xiong-Hao Lin, De-An Guo, Min Ye Abstract | HTML | PDF Fast Quantification of S-adenosyl-L-methionine in Dietary Health Products Utilizing Reversed-Phase High-performance Liquid Chromatography: Teaching an Old Method New Tricks Jing-Ru Liou, Li-Yeh Chuang, Yuan-Han Yang, Tung-Ying Wu, Mohamed El-Shazly, Shyh-Jong Wu, Tusty-Jiuan Hsieh, Yang-Chang Wu, Jiumn-Yih Wu, Fang-Rong Chang Abstract | HTML | PDF Click here to see the full table of contents for this issue.
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