- Effects of isocorynoxeine, from Uncaria, on lower urinary tract dysfunction caused by benign prostatic hyperplasia via antagonism of α1A-adrenoceptors. [Journal Article]
- TAToxicol Appl Pharmacol 2019 Aug 01; 376:95-106
- Medical therapy of lower urinary tract symptoms (LUTS) suggestive of benign prostatic hyperplasia (BPH) targets smooth muscle contraction in the prostate, for which α1A-adrenoceptor (α1A-AR) antagoni…
Medical therapy of lower urinary tract symptoms (LUTS) suggestive of benign prostatic hyperplasia (BPH) targets smooth muscle contraction in the prostate, for which α1A-adrenoceptor (α1A-AR) antagonists have been considered to be the primary therapeutic method. We investigated the effects and underlying mechanisms of isocorynoxeine (ICN), one of indole alkaloids from Uncaria, on the treatment of LUTS secondary to BPH via α1A-ARs in mice. The effect of ICN on prostatic contractility was studied via myographic measurements in the prostates of rabbits. The effects of ICN on bladder function, serum-hormone levels, bladder histology, and prostate histology were determined in testosterone propionate-induced prostatic hyperplasic wild-type (WT) and α1A-AR knockout (α1A-KO) mice. The cytotoxicity of ICN in cultured human prostatic stromal cells (WPMY-1) was assessed by the following: a cell-counting kit, measuring the relaxant effect on WPMY-1 by a collagen gel contraction assay, intracellular Ca2+ mobilization indicated by Fluo-4, cytoskeletal organization by phalloidin staining, and expressions of α1A-AR-mediated key messengers by western blot analyses. ICN non-competitively antagonized the contractions of prostates induced by α1A-AR agonists. ICN treatment improved bladder functions in prostatic hyperplasic WT mice, whereas it failed to ameliorate bladder functions in prostatic hyperplasic α1A-KO mice. In WPMY-1, ICN relaxed cell contractions on collagen gels, disrupted F-actin organization, inhibited α1A-AR agonist-stimulated Ca2+ mobilization, and antagonized α1A-ARs via the RhoA/ROCK2/MLC signaling pathway. Our results suggest that ICN may be a promising therapeutic drug for targeting α1A-ARs in the treatment of BPH/LUTS.
- Evaluation of the effects of Uncaria rhynchophylla alkaloid extract on LPS-induced preeclampsia symptoms and inflammation in a pregnant rat model. [Journal Article]
- BJBraz J Med Biol Res 2019; 52(6):e8273
- Excessive pro-inflammatory cytokines result in adverse pregnancy outcomes, including preeclampsia-like phenotypes, and fetal growth restriction. Anti-inflammation might be an effective therapy. The a…
Excessive pro-inflammatory cytokines result in adverse pregnancy outcomes, including preeclampsia-like phenotypes, and fetal growth restriction. Anti-inflammation might be an effective therapy. The aim of this research was to investigate whether Uncaria rhynchophylla alkaloid extract (URE), a highly safe anti-inflammation constituent of the herb, can inhibit inflammation and improve clinical characteristics of preeclampsia in a lipopolysaccharide (LPS)-induced preeclampsia rat model. The rat model was established by daily administration of LPS (1 μg/kg body weight per day) from gestational day (GD) 14 to 19. Different doses of URE (35, 70, and 140 mg/kg body weight per day) were administered from GD 14 to GD 19. The effects of URE on proteinuria, maternal hypertension, pregnancy outcomes, as well as pro-inflammatory cytokines levels in serum and placenta were measured. High-dose URE (HURE) treatment decreased LPS-induced mean 24-h proteinuria and systolic blood pressure, and increased fetal weight, placental weight, and the number of live pups (P<0.05). Moreover, increased serum and placental levels of interleukin (IL)-6, IL-1β, tumor necrosis factor-α, and interferon-γ in the LPS-treated group were obviously inhibited after HURE administration (P<0.01). URE improved preeclampsia symptoms and mitigated inflammatory responses in the LPS-induced preeclampsia rat model, which suggests that the anti-inflammation effect of URE might be an alternative therapy for preeclampsia.
- Secondary Metabolites and PI3K Inhibitory Activity of Colletotrichum gloeosporioides, a Fungal Endophyte of Uncaria rhynchophylla. [Journal Article]
- CMCurr Microbiol 2019; 76(7):904-908
- In the present study, nine compounds (1-9) were isolated from Colletotrichum gloeosporioides (an endophytic fungus from Uncaria rhynchophylla) which was cultured in wheat bran medium. Their structure…
In the present study, nine compounds (1-9) were isolated from Colletotrichum gloeosporioides (an endophytic fungus from Uncaria rhynchophylla) which was cultured in wheat bran medium. Their structures were elucidated as 4-Epi-14-hydroxy-10, 23-dihydro-24, 25-dehydroaflavinine (1), 10, 23-Dihydro-24,25 -dehydro-21-oxoaflavinine (2), Ergosterol (3), Ergosterol peroxide (4), Mellein (5), 4, 5-dihydroblumenol A (6), Colletotrichine A (7), Cyclo(L-leucyl-L-leucyl) (8), and Brevianamide F (9) based on NMR spectral data, as well as comparing with previous literature data. This is the first report about the isolation of compounds 1-2, 6, and 8-9 from Colletotrichum genus. All compounds were tested for their phosphoinositide 3-kinase (PI3Kα) inhibitory activity. Compounds 8 and 9 showed potent PI3K α inhibitory activity with IC50 values of 38.1 and 4.8 µM, respectively, while the other compounds showed very weak activity at a concentration of 20 µg/mL.
- The Use of Medicinal Plants in the Riverside Community of the Mazagão River in the Brazilian Amazon, Amapá, Brazil: Ethnobotanical and Ethnopharmacological Studies. [Journal Article]
- EBEvid Based Complement Alternat Med 2019; 2019:6087509
- The inhabitants of the floodplain of the Mazagão River in the State of Amapá in the Brazilian Amazon have inherited from indigenous African and Cabocla cultures indications for the use and forms of p…
The inhabitants of the floodplain of the Mazagão River in the State of Amapá in the Brazilian Amazon have inherited from indigenous African and Cabocla cultures indications for the use and forms of preparation of medicinal plants to cure diseases of the body and spirit. This study aimed to perform an ethnopharmacological survey of medicinal plants used by the riparian community of the floodplains of the Mazagão River, in the State of Amapá. In this study, we chose semistructured interviews with socioeconomic, ethnopharmacological, and ethnobotanical aims. The collection of medicinal plants occurred during guided tours. The Use Value (UV), Informant Consensus Factor (ICF), Correction Factor (CF), and Fidelity level (FL) were calculated. There were 130 species of medicinal plants, distributed in 116 genera and 57 families; Fabaceae (16), Lamiaceae (14), Euphorbiaceae (7), and Arecaceae (6) include 33.33% of the total species sampled. All 95 native species of floodplain forests were previously described, and 35 are exotic species. The species with the highest UV (≥ 0.5) at the mouth of the Mazagão River were Carapa guianensis (0.91), Pentachlethra macroloba (0.83), Dalbergia subcymosa (0.77), Uncaria tomentosa (0.75), Otacanthus azureus (0.62), Virola surinamensis (0.62), Hura crepitans (0.58), Euterpe oleracea (0.56), and Arrabidaea chica (0.51). These species were also the ones that presented the highest ICF among the informants and 100% in FL for a specific therapeutic use. The study is comprised of 16 categories of therapeutic use, of which the majority of the plants used are related to diseases such as microbial infections (20.67%, 73 species), gastrointestinal disorders (13.31%), and inflammation (11.61%). The results showed that knowledge about the use of medicinal plants along the rivers and streams that form the mouth of the Mazagão River is evenly distributed. Most of the interviewees present diversified knowledge about the medicinal resources because they have a close relationship with the floodplain forest. Native species of this forest predominate among the most commonly used medicinal plants as subsidies for future pharmacological studies.
- [Advances in indole alkaloids from traditional Chinese medicine of Uncariae Ramulus Cum Uncis documented in Chinese Pharmacopoeia]. [Journal Article]
- ZZZhongguo Zhong Yao Za Zhi 2019; 44(4):685-695
- Uncaria genus(Rubiaceae) contains 34 species all over the world,of which 11 species and one variant are present in China. Five species,namely U. rhynchophylla,U. macrophylla,U. hirsuta,U. sinensis an…
Uncaria genus(Rubiaceae) contains 34 species all over the world,of which 11 species and one variant are present in China. Five species,namely U. rhynchophylla,U. macrophylla,U. hirsuta,U. sinensis and U. sessilifructus,are documented in Chinese Pharmacopoeia as the raw materials of Uncariae Ramulus Cum Uncis. Indole alkaloids are the characteristic constituents of Uncaria plants,in addition to triterpenes,lignans and flavones. This paper reviews the progress of indole alkaloids and their distribution within the five Uncaria species documented in Chinese Pharmacopoeia for better understanding the active constituents of Uncariae Ramulus Cum Uncis.
- Yokukansan-induced reduction of ethanol preference is associated with antagonism of 5-HT3 receptors. [Journal Article]
- PPhytomedicine 2019; 59:152897
- CONCLUSIONS: Yokukansan contributes to reduced ethanol preference and antagonism of 5-HT3 receptors is associated with the effect.
- Isorhynchophylline exerts anti-inflammatory and anti-oxidative activities in LPS-stimulated murine alveolar macrophages. [Journal Article]
- LSLife Sci 2019 Apr 15; 223:137-145
- CONCLUSIONS: IRN exerted anti-inflammatory and anti-oxidant effects on LPS-stimulated murine alveolar macrophages via inhibition of the TLR4/NF-κB/NLRP3 inflammasome pathway.
- Evidence on Integrating Pharmacokinetics to Find Truly Therapeutic Agent for Alzheimer's Disease: Comparative Pharmacokinetics and Disposition Kinetics Profiles of Stereoisomers Isorhynchophylline and Rhynchophylline in Rats. [Journal Article]
- EBEvid Based Complement Alternat Med 2019; 2019:4016323
- Isorhynchophylline (IRN) and rhynchophylline (RN), a pair of stereoisomers, are tetracyclic oxindole alkaloids isolated from Uncaria rhynchophylla, a commonly used Chinese medicinal herb. These two c…
Isorhynchophylline (IRN) and rhynchophylline (RN), a pair of stereoisomers, are tetracyclic oxindole alkaloids isolated from Uncaria rhynchophylla, a commonly used Chinese medicinal herb. These two compounds have drawn extensive attention due to their potent neuroprotective effects with promising therapeutic potential for the treatment of Alzheimer's disease (AD). However, IRN and RN can interconvert into each other in vivo after oral administration. The present study aimed to elucidate the pharmacokinetic profiles and disposition kinetics of the administered and generated stereoisomers in the brain and cerebrospinal fluid (CSF) after oral administration of equal dose of IRN or RN to rats. Our study demonstrated that after oral administration, RN showed significantly higher systemic exposure (6.5 folds of IRN, p < 0.001) and disposition in the brain (2.5 folds of IRN, p < 0.01) and CSF (3 folds of IRN, p < 0.001) than IRN. The results indicated that interconversion between IRN and RN occurred. Notably, regardless of the orally administered IRN or RN, RN would always be one of the major or predominant forms present in the body. Our results provided sound evidence supporting further development of RN as a potential therapeutic agent for the treatment of AD. Moreover, the present study sets a solid example that integrating pharmacokinetics is crucial to identify the truly therapeutic agent.
- In silico Inhibition of BACE-1 by Selective Phytochemicals as Novel Potential Inhibitors: Molecular Docking and DFT Studies. [Journal Article]
- CDCurr Drug Discov Technol 2019 Feb 14
- CONCLUSIONS: Out of seven phytochemicals, four are from plant Glycyrrhiza glabra i.e. Shinflavanone, Glabrolide, Glabrol and PrenyllicoflavoneA, one from Huperzia serrate i.e. Macleanine, one from Uncaria rhynchophylla i.e. 3a-dihydro-cadambine and another one is VolvalerelactoneB from plant Valeriana-officinalis. It is concluded that these phytochemicals are candidate for drug/inhibitor against BACE-1, and can be administered to humans after experimental validation through in vitro and in vivo trials.
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- Phenolic plant extracts are additive in their effects against in vitro ruminal methane and ammonia formation. [Journal Article]
- AJAsian-Australas J Anim Sci 2019 Jan 02
- CONCLUSIONS: The study identified methane and ammonia mitigating potential of various phenolic plant extracts and showed a number of additive and some non-linear effects of combinations of extracts. Further studies, especially in live animals, should concentrate on combinations of extracts from grape seed, green tea leaves and acacia bark and determine the ideal dosages of such combinations for purpose of methane mitigation.