Author
Hengyuan Zhang
Bio: Hengyuan Zhang is an academic researcher from China Pharmaceutical University. The author has contributed to research in topics: Antibacterial activity & HeLa. The author has an hindex of 10, co-authored 15 publications receiving 245 citations.
Papers
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TL;DR: Biological evaluation in vivo suggested that 14f is obviously superior to that of reference drug losartan in RHRs, and meanwhile, 14f has no significant impact on heart rate.
54 citations
TL;DR: It is concluded that ORA reverseABCB1-mediated MDR by competitively inhibiting the ABCB1 drug efflux function by reverse the resistance to paclitaxel and vincristine in ABCB 1-overexpressing SW620/Ad300 and HEK/ABCB 1 cells.
Abstract: Overexpression of ATP-Binding Cassette transporters leads to multidrug resistance in cancer cells and results in the failure of chemotherapy. In this in-vitro study, we investigated whether or not (20S, 24R/S)-epoxy-12β, 25-dihydroxy-dommarane-3β-amine (ORA and OSA), a pair of semi-synthetic ocotillol analogue epimers, could inhibit the ABCB1 transporter. ORA (1 μM and 3 μM) significantly reversed the resistance to paclitaxel and vincristine in ABCB1-overexpressing SW620/Ad300 and HEK/ABCB1 cells, whereas OSA had no significant effects. In addition, ORA (3 μM) significantly increased the intracellular accumulation of [3H]-paclitaxel by suppressing the efflux function of ABCB1. Meanwhile, both ORA (3 μM) and OSA (3 μM) did not significantly alter the expression level or the subcellular location of ABCB1 protein. Moreover, the ABCB1 ATPase study suggested that ORA had a stronger stimulatory effect on the ATPase activity than OSA. ORA also exhibited a higher docking score as compared with OSA inside transmembrane domain of ABCB1. Overall, we concluded that ORA reverse ABCB1-mediated MDR by competitively inhibiting the ABCB1 drug efflux function.
39 citations
TL;DR: A novel class of ocotillol-type triterpenoid derivatives have been synthesized and evaluated for their in-vitro antibacterial activity against several representative pathogenic bacterial strains.
36 citations
TL;DR: Mechanistic investigation showed that the representative compound 17 affected cell cycle and induced apoptosis at low micro-molar level in human hepatoma Bel-7402 cells, via an oxidative stress triggered mitochondria-related caspase-dependent pathway.
34 citations
TL;DR: The biological screening results showed that all of the derivatives exhibited more significant antiproliferative activity than the parent compound and pyrazine-fused 23-hydroxybetulinic acid exhibited the most potent activity.
26 citations
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TL;DR: Owing to the development of novel and new pyrazole based therapeutic agents at a faster pace, there is a need to couple the latest information with previously available information to understand status of this moiety in medicinal chemistry research.
286 citations
TL;DR: It is revealed that modification of NPs is a versatile approach to explore their mode of actions, which may lead to the discovery of novel drugs.
Abstract: Introduction: Throughout history, natural products (NPs) have provided a rich source of compounds that have wide applications in the fields of medicine, health sciences, pharmacy and biology. Although naturally active substances are good lead compounds for the discovery of new drugs, most of them suffer from various deficiencies or shortcomings, such as complex structures, poor stability and solubility. Therefore, structural modification of NPs is needed to develop novel compounds with specific properties.Areas covered: This article presents an overview on the structural modifications of NPs in drug development. The application of multiple classes of NPs to the treatment of conditions such as cancers, infection, Alzheimer’s and diabetes are discussed. This article also reveals that modification of NPs is a versatile approach to explore their mode of actions, which may lead to the discovery of novel drugs.Expert opinion: NPs are usually described by structural diversity and complexity. The use of i...
140 citations
TL;DR: This review summarizes the recent advances in medicinal chemistry on the explorations of novel oridonin analogues as potential anticancer therapeutics, and provides a detailed discussion of future directions for the development and progression of this class of molecules into the clinic.
117 citations
TL;DR: A brief summary on oridonin and its analogs in cancer drug discovery and antiinflammation is provided and its emerging therapeutic potential in neuroprotection applications is highlighted.
Abstract: Oridonin, a diterpenoid natural product commonly used in East Asian herbal medicine, is garnering increased attention in the biomedical community due to its extensive biological activities that include antitumor, anti-inflammatory, antimicrobial, hepatic fibrosis prevention, and neurological effects. Over the past decade, significant progress has been made in structure activity relationship and mechanism of action studies of oridonin for the treatment of cancer and other diseases. This review provides a brief summary on oridonin and its analogs in cancer drug discovery and antiinflammation and highlights its emerging therapeutic potential in neuroprotection applications.
86 citations
TL;DR: This review covers the isolation and chemistry of diterpenoids from terrestrial as opposed to marine sources and includes labdanes, clerodanes, abietanes, pimaranes, kauranes, cembranes and their cyclization products.
78 citations