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関連する概念動画

ATP Driven Pumps I: An Overview01:27

ATP Driven Pumps I: An Overview

9.9K
ATP-driven pumps, also known as transport ATPases, are integral membrane proteins. They have binding sites for ATP located on the membrane's cytosolic side and the ion-conducting domain in the transmembrane region. These pumps use the free energy released from ATP hydrolysis to move the solutes across cell membranes against an electrochemical gradient.
There are four main types of ATP-driven pumps - P-type, V-type, F-type, and ABC transporter. All these pumps are of varying complexities and...
9.9K
Xylem and Transpiration-driven Transport of Resources02:03

Xylem and Transpiration-driven Transport of Resources

26.9K
The xylem of vascular plants distributes water and dissolved minerals that are taken up by the roots to the rest of the plant. The cells that transport xylem sap are dead upon maturity, and the movement of xylem sap is a passive process.
26.9K
ATP Driven Pumps II: P-type Pumps01:34

ATP Driven Pumps II: P-type Pumps

6.5K
The P-type pumps are a large family of integral membrane transporter ATPases. They are divided into five major types based on substrate specificity, from I to V.
A typical P-type pump has three cytosolic domains: nucleotide-binding (N), phosphorylation (P), and activator (A) domains. These domains are connected to the membrane-spanning helices by short amino acid segments. ATP hydrolysis and covalent phosphoenzyme intermediate formation are crucial parts of the catalytic cycle. At the highly...
6.5K
ATP Driven Pumps III: V-type Pumps01:30

ATP Driven Pumps III: V-type Pumps

4.9K
V-type pumps are ATP-driven pumps found in the vacuolar membranes of plants, yeast, endosomal and lysosomal membranes of animal cells, plasma membranes of a few specialized eukaryotic cells, and some prokaryotes. They are also known as the V1Vo-ATPase, that couple ATP hydrolysis to transport protons against a concentration gradient.
The peripheral or cytosolic V1 domain with eight subunits is involved in ATP hydrolysis. The integral or transmembrane V0 domain containing at least five subunits...
4.9K
Secondary Active Transport01:55

Secondary Active Transport

138.2K
One example of how cells use the energy contained in electrochemical gradients is demonstrated by glucose transport into cells. The ion vital to this process is sodium (Na+), which is typically present in higher concentrations extracellularly than in the cytosol. Such a concentration difference is due, in part, to the action of an enzyme “pump” embedded in the cellular membrane that actively expels Na+ from a cell. Importantly, as this pump contributes to the high concentration of...
138.2K
Primary Active Transport01:47

Primary Active Transport

200.7K
In contrast to passive transport, active transport involves a substance being moved through membranes in a direction against its concentration or electrochemical gradient. There are two types of active transport: primary active transport and secondary active transport. Primary active transport utilizes chemical energy from ATP to drive protein pumps that are embedded in the cell membrane. With energy from ATP, the pumps transport ions against their electrochemical gradients—a direction...
200.7K

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Updated: Feb 12, 2026

Synthesis, Cellular Delivery and In vivo Application of Dendrimer-based pH Sensors
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PEG化ヘテロ機能性デンドリマーによるROS駆動型抗がん活性のための多価ジクロフェナク送達の実現

Arunika Singh1, Natalia Sanz Del Olmo1,2,3, Michael Malkoch1

  • 1Department of Fibre and Polymer Technology, KTH Royal Institute of Technology, Stockholm 100 44, Sweden.

ACS applied materials & interfaces
|February 10, 2026
PubMed
まとめ

エンジニアリングされたデンドリマーは、抗炎症薬であるジクロフェナクをがん治療として効果的に送達します。ナノキャリアは、健康な細胞に対する毒性を低下させ、がん細胞の殺傷能力を向上させ、有望な薬物再利用戦略を提供します。

キーワード:
PEG化ROS活性抗がん治療薬共有結合細胞毒性ジクロフェナク再利用ヘテロ機能性ポリエステルデンドリマー

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Preparation and In Vitro Characterization of Dendrimer-based Contrast Agents for Magnetic Resonance Imaging
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Dendrimer-based Uneven Nanopatterns to Locally Control Surface Adhesiveness: A Method to Direct Chondrogenic Differentiation
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Synthesis, Cellular Delivery and In vivo Application of Dendrimer-based pH Sensors
16:19

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Preparation and In Vitro Characterization of Dendrimer-based Contrast Agents for Magnetic Resonance Imaging
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Dendrimer-based Uneven Nanopatterns to Locally Control Surface Adhesiveness: A Method to Direct Chondrogenic Differentiation
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科学分野:

  • ナノメディシン
  • ドラッグデリバリー
  • がん治療学

背景:

  • がん治療薬の開発は、高コストと成功率の低さに直面しており、薬物の再利用が必要とされています。
  • NSAIDであるジクロフェナクは、抗がん作用の可能性を示していますが、溶解性が低く、急速なクリアランスを示します。
  • ジクロフェナクの化学療法の適合性を向上させるためには、新しいナノキャリアが必要です。

研究 の 目的:

  • PEG化されたヘテロ機能性ポリエステルデンドリマー（HFD）を設計し、制御されたジクロフェナク送達を可能にすること。
  • ジクロフェナク負荷HFDの抗がん効果と選択性を評価すること。
  • 活性酸素種（ROS）生成を含む作用機序を調査すること。

主な方法:

  • 銅(I)触媒アジド-アルキン環化付加（CuAAC）を介したジクロフェナクの結合。
  • 無水エステル化による末端PEG化。
  • G1およびG2デンドリマー構築物（G1-(Dicl)3-(mPEG)6およびG2-(Dicl)9-(mPEG)12）の特性評価。
  • がんおよび線維芽細胞株における細胞毒性のinvitro評価。
  • ROSレベルの評価およびメカニズム研究。

主要な成果:

  • 加水分解直径170〜330 nmの、両親媒性コアシェルナノ構造が形成されました。
  • G1-(Dicl)3-(mPEG)6は、1〜10μMで有意ながん細胞生存率の低下（50〜70％）を示し、線維芽細胞に対する選択性が高い（治療指数が20倍以上改善）ことが示されました。
  • 両方のデンドリマーは、遊離ジクロフェナクよりも有意に低い濃度でROSを誘導し、これは細胞毒性と相関していました。
  • G2-(Dicl)9-(mPEG)12は、強力ですが細胞株依存的な活性を示しました。

結論:

  • HFDは、ジクロフェナクのような薬物を再利用するための多用途なナノメディシンプラットフォームです。
  • G1デンドリマーは、がん治療のための有効性、選択性、および臨床応用の可能性の最適なバランスを提供します。
  • ROSを介した細胞毒性は、ジクロフェナク負荷デンドリマーの重要な作用機序です。