Availability, Pharmaceutics, Security, Pharmacokinetics, and Pharmacological Activities of Patchouli Alcohol

Patchouli alcohol (PA), a tricyclic sesquiterpene, is one of the critical bioactive ingredients and is mainly isolated from aerial part of Pogostemon cablin (known as guanghuoxiang in China) belonging to Labiatae. So far, PA has been widely applied in perfume industries. This review was written with the use of reliable information published between 1974 and 2016 from libraries and electronic researches including NCKI, PubMed, Reaxys, ACS, ScienceDirect, Springer, and Wiley-Blackwell, aiming at presenting comprehensive outline of security, pharmacokinetics, and bioactivities of PA and at further providing a potential guide in exploring the PA and its use in various medical fields. We found that PA maybe was a low toxic drug that was acquired numerously through vegetable oil isolation and chemical synthesis and its stability and low water dissolution were improved in pharmaceutics. It also possessed specific pharmacokinetic characteristics, such as two-compartment open model, first-order kinetic elimination, and certain biometabolism and biotransformation process, and was shown to have multiple biological activities, that is, immunomodulatory, anti-inflammatory, antioxidative, antitumor, antimicrobial, insecticidal, antiatherogenic, antiemetic, whitening, and sedative activity. However, the systematic evaluations of preparation, pharmaceutics, toxicology, pharmacokinetics, and bioactivities underlying molecular mechanisms of action also required further investigation prior to practices of PA in clinic

Enzyme-mediated dual-targeted-assembly realizes a synergistic anticancer effect

We designed and synthesized homochiral-peptide-based boron diketonate complexes. Co-administration of the two stereoisomers in cancer cells led to molecular assembly targeting both the plasma membrane and the lysosomes mediated via membrane-bonded enzymes. The dual-targeted-assembly generates a synergistic anticancer effect with amplified cancer spheroid toxicity and enhanced inhibition efficacy on cancer cell migration

Self-Assembly-Directed Cancer Cell Membrane Insertion of Synthetic Analogues for Permeability Alteration

Inspired by the metamorphosis of pore-forming toxins from soluble inactive monomers to cytolytic trans-membrane assemblies, we developed self-assembly-directed membrane insertion of synthetic analogues for permeability alteration. An expanded pi-conjugation-based molecular precursor with an extremely high rigidity and a long hydrophobic length that is comparable to the hydrophobic width of plasma membrane was synthesized for membrane-inserted self-assembly. Guided by the cancer biomarker expression in vitro, the soluble precursors transform into hydrophobic monomers forming assemblies inserted into the fluid phase of the membrane exclusively. Membrane insertion of rigid synthetic analogues destroys the selective permeability of the plasma membrane gradually. It eventually leads to cancer cell death, including drug resistant cancer cells

Pharmacological Activities of Patchouli Alcohol

Patchouli alcohol (PA), a tricyclic sesquiterpene, is one of the critical bioactive ingredients and is mainly isolated from aerial part of Pogostemon cablin (known as guanghuoxiang in China) belonging to Labiatae. So far, PA has been widely applied in perfume industries. This review was written with the use of reliable information published between 1974 and 2016 from libraries and electronic researches including NCKI, PubMed, Reaxys, ACS, ScienceDirect, Springer, and Wiley-Blackwell, aiming at presenting comprehensive outline of security, pharmacokinetics, and bioactivities of PA and at further providing a potential guide in exploring the PA and its use in various medical fields. We found that PA maybe was a low toxic drug that was acquired numerously through vegetable oil isolation and chemical synthesis and its stability and low water dissolution were improved in pharmaceutics. It also possessed specific pharmacokinetic characteristics, such as two-compartment open model, first-order kinetic elimination, and certain biometabolism and biotransformation process, and was shown to have multiple biological activities, that is, immunomodulatory, anti-inflammatory, antioxidative, antitumor, antimicrobial, insecticidal, antiatherogenic, antiemetic, whitening, and sedative activity. However, the systematic evaluations of preparation, pharmaceutics, toxicology, pharmacokinetics, and bioactivities underlying molecular mechanisms of action also required further investigation prior to practices of PA in clinic

Low-Complexity Power-Balancing-Point Based Optimization for Photovoltaic Differential Power Processing

Differential power processing (DPP) is regarded as a promising architecture in solving mismatching issues among photovoltaic (PV) submodules. Although conventional total-minimum-power-point (TMPP)-based real-time optimization algorithm by using the distributed submodule-level maximum power point tracking and simultaneously the centralized total-minimum-power tracking shows effectiveness in maximizing the power yield. However, uneven power stress among DPP converters, large oscillations, high additional cost for communication among DPP converters, and complicated implementation hinder the practical application. This article proposed a low-complexity power balancing point-based optimization algorithm to reduce the system cost and size, improve the system efficiency, and realize the standardized modular design for DPP converters. Furthermore, simple submodule-level voltage equalization control is implemented to eliminate expensive communication and relieve the control complexity while guaranteeing high maximum-power-point efficiency. The proposed algorithm can reduce the power rating of DPP converters compared with conventional TMPP-based control, which is beneficial to the improvement of system cost, reliability, and lifetime. Both simulation and experimental results under various scenarios are provided to validate the advantages of the proposed algorithm

Rare-earth-doped fluoride nanoparticles with engineered long luminescence lifetime for time-gated: In vivo optical imaging in the second biological window

Biomedicine is continuously demanding new luminescent materials to be used as optical probes for the acquisition of high resolution, high contrast and high penetration in vivo images. These materials, in combination with advanced techniques, could constitute the first step towards new diagnosis and therapy tools. In this work, we report on the synthesis of long lifetime rare-earth-doped fluoride nanoparticles by adopting different strategies: core/shell and dopant engineering. The here developed nanoparticles show intense infrared emission in the second biological window with a long luminescence lifetime close to 1 millisecond. These two properties make the here presented nanoparticles excellent candidates for time-gated infrared optical bioimaging. Indeed, their potential application as optical imaging contrast agents for autofluorescence-free in vivo small animal imaging has been demonstrated, allowing high contrast real-time tracking of gastrointestinal absorption of nanoparticles and transcranial imaging of intracerebrally injected nanoparticles in the murine brainThis work was supported in part by the grants from the Fundamental Research Funds for the Central Universities, China (HIT. BRETIV.201503 and AUGA5710052614) and the National Natural Science Foundation of China (51672061). We thank Dr Lina Wu at the Fourth Hospital of Harbin Medical University for her kind help with the MTT assay, and Dr Tymish Y. Ohulchanskyy at Shenzhen University for his kind help with the fluorescence lifetime measurement. The work was also supported by the Ministerio de Economia y Competitividad of Spain (grant MAT2016-75362-C3-1-R). Jie Hu acknowledges the scholarship from the China Scholarship Council (No. 201506650003). Dirk H. Ortgies is grateful to the Spanish Ministry of Economy and Competitiveness for a Juan de la Cierva scholarship (No. FJCI-2014-21101) and the Spanish Institute of Health (ISCIII) for a Sara Borell Fellowship (No. CD17/00210

The complex hexaploid oil‐Camellia genome traces back its phylogenomic history and multi‐omics analysis of Camellia oil biosynthesis

Summary: Oil‐Camellia (Camellia oleifera), belonging to the Theaceae family Camellia, is an important woody edible oil tree species. The Camellia oil in its mature seed kernels, mainly consists of more than 90% unsaturated fatty acids, tea polyphenols, flavonoids, squalene and other active substances, which is one of the best quality edible vegetable oils in the world. However, genetic research and molecular breeding on oil‐Camellia are challenging due to its complex genetic background. Here, we successfully report a chromosome‐scale genome assembly for a hexaploid oil‐Camellia cultivar Changlin40. This assembly contains 8.80 Gb genomic sequences with scaffold N50 of 180.0 Mb and 45 pseudochromosomes comprising 15 homologous groups with three members each, which contain 135 868 genes with an average length of 3936 bp. Referring to the diploid genome, intragenomic and intergenomic comparisons of synteny indicate homologous chromosomal similarity and changes. Moreover, comparative and evolutionary analyses reveal three rounds of whole‐genome duplication (WGD) events, as well as the possible diversification of hexaploid Changlin40 with diploid occurred approximately 9.06 million years ago (MYA). Furthermore, through the combination of genomics, transcriptomics and metabolomics approaches, a complex regulatory network was constructed and allows to identify potential key structural genes (SAD, FAD2 and FAD3) and transcription factors (AP2 and C2H2) that regulate the metabolism of Camellia oil, especially for unsaturated fatty acids biosynthesis. Overall, the genomic resource generated from this study has great potential to accelerate the research for the molecular biology and genetic improvement of hexaploid oil‐Camellia, as well as to understand polyploid genome evolution

Novel Fast-Speed Partial-Shading-Tolerant Flexible Power Point Tracking for Photovoltaic Systems with Explicit Key Points Estimation

Recent power curtailment-based photovoltaic (PV) flexible power point tracking (FPPT) algorithms mainly adopted intricate curve fitting or sophisticated curve-scanning mecha-nisms to ensure the grid supportive functionalities under partial shading conditions (PSCs), showing the limitations of mathe-matical solidity or system dynamics improvement. Accordingly, a novel fast-speed partial-shading-tolerant FPPT (PST-FPPT) algorithm is proposed in this paper. Regarding the proposed scheme, a modified explicit PV model is developed to express the key operation points with the assistance of several representative current-voltage samples from the initialization process, which is beneficial to computational burden reduction and irradiance sensors removal. Additionally, to guarantee the tracking speed to system dynamics, a set point estimation-based direct voltage regulation strategy is proposed in this paper, eliminating the redundant searching in approaching the predefined power com-mand. Simulation and experimental evaluations under various PSCs and operational circumstances validated the effectiveness of the proposed control