Synonym name: Delphelatine; Eldeline
Catalogue No.: BP0471
Cas No.: 6836-11-9
Formula: C₂₇H₄₁NO₈
Mol Weight: 507.624
Botanical Source: Alkaloid from Delphinium occidentale, Delphinium elatum, Delphinium bonvalotii, Delphinium dictyocarpum, Delphinium glaucescens, Delphinium iliense and Aconitum columbianum ssp. columbianum (Ranunculaceae)

Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Can be supplied from milligrams to grams.

For Reference Standard and R&D, Not for Human Use Directly.
Inquire for bulk scale.

HPLC of Deltaline

Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃

Introduction/Overview

Diterpenoid alkaloids are a class of natural products with complex structures and diverse biological activities, widely distributed in the family Ranunculaceae and genus Quercus（Delphinium）And Aconitum genus（Aconitum）In plants. These compounds have attracted much attention due to their significant neuropharmacological activities, such as pain relief and muscle relaxation, and have also become a research hotspot due to their potential toxicity and complex mechanisms of action. Deltaline (CAS: 6836-11-9) is derived from the traditional medicinal plant Dian Chuan Cui Que Hua（Delphinium delavayi A C19 type diterpenoid alkaloid isolated from Franch. Traditionally, Dianchuan Cuiquehua plants have been used in folk medicine to treat rheumatic pain, stroke paralysis, and rheumatoid arthritis, indicating that they contain ingredients with analgesic and anti-inflammatory activities. In recent years, with the deepening of research on neurodegenerative diseases, the pharmacological activity research of Delitalin has expanded from the traditional field of analgesia to the field of complex neurological diseases such as cognitive impairment. This article aims to provide a systematic review of the chemical structure, plant origin, pharmacological activity, potential molecular targets, medicinal properties, and application prospects of Delitalin in diseases such as cognitive impairment, in order to provide scientific references for the in-depth research and development of this compound.

Chemical structure and physicochemical properties

Deltalin is a typical C19 diterpenoid alkaloid (hetisine type) with a molecular formula of C27H41NO7 and a molecular weight of 507.6240. Its core structure consists of a six ring skeleton, including a hetisine type diterpene parent nucleus and one or more hydroxyl and methoxy substituents, as well as a tertiary amine structure formed by a nitrogen atom. This complex multi ring rigid structure is the basis for its interaction with multiple biological targets.

From the analysis of parameters related to drug properties, Deltalin exhibits certain drug like characteristics. Its lipid water partition coefficient (LogP) is 1.7138, indicating that it has moderate lipophilicity and is conducive to transmembrane transport. The topological polar surface area (TPSA) is 95.92 Å ², which is lower than the common high permeability threshold (~140 Å ²), consistent with its good membrane permeability prediction. The water solubility value is 0.3894 mg/mL, which belongs to the category of slight solubility. This may affect the development of its formulation, but it can be improved through salt formation or formulation technology. More importantly, its predicted blood-brain barrier (BBB) permeability is "high", which provides a prerequisite for its direct action on central nervous system targets and treatment of brain diseases such as cognitive impairment. Preliminary safety predictions indicate that the risk of hERG inhibition is "no", suggesting a low risk of cardiac toxicity; The Ames test value is 0.6, indicating a low risk of mutagenicity and potential for further development.

Plant sources and extraction methods

The main source of Delitalin comes from plants in the Ranunculaceae family, including the Dianchuan Cuique flower（Delphinium delavayi）As the main source. This plant is distributed in high-altitude areas of southwestern China and has a long history of medicinal use in folk culture. The content of alkaloids in plants is significantly affected by their place of origin, harvest season, and location, and is usually higher in the roots and aboveground parts before flowering.

The extraction of Del Talin usually follows the general process of natural alkaloids. Firstly, the dried plant material is crushed and moistened with a weakly alkaline aqueous solution (such as ammonia) to convert alkaloid salts into free bases. Subsequently, organic solvents such as chloroform, dichloromethane, or ethanol are used for percolation, reflux, or ultrasound assisted extraction. The crude extract is extracted with acidic water (such as dilute hydrochloric acid), and the alkaloids are salted and dissolved in the aqueous phase; After alkalization, free alkaloids are extracted again by organic solvents to achieve preliminary enrichment. Further purification relies on column chromatography techniques, often using silica gel, alumina, or reverse phase silica gel (such as C18) as the stationary phase, and gradient elution with solvent systems such as chloroform methanol or hexane ethyl acetate in different ratios. High performance liquid chromatography (HPLC), especially preparative HPLC, is the ultimate key step in obtaining high-purity Deltalin monomers. Structural identification involves the comprehensive use of mass spectrometry (MS), nuclear magnetic resonance (NMR, including 1H, 13C, 2D-NMR), and X-ray single crystal diffraction techniques.

Pharmacological activity research

1. Traditional analgesia and anti-inflammatory activity As one of the active ingredients in the genus Quercus, Deltalin inherits the traditional analgesic properties of this plant species. Research has shown that it exhibits significant analgesic effects in animal models such as acetic acid writhing method and hot plate method, and its mechanism may involve regulation of the central and peripheral nervous systems. In addition, the use of its parent plant for rheumatic pain and rheumatoid arthritis suggests that Delitalin may have anti-inflammatory activity, but specific research is relatively limited and further validation is needed.
2. Potential activity for cognitive impairment This is an emerging direction in recent years in the field of research at Del Tallinn. Cognitive impairment is the core symptom of various neurodegenerative diseases such as Alzheimer's disease (AD). Preliminary in vitro and in vivo pharmacological studies have shown that Delitalin has the potential to improve learning and memory abilities. In AD model animals, the intervention of Delitalin may alleviate behavioral deficits. Its activity is not achieved through a single target action, but through multiple synergistic pathways, which matches its complex chemical structure.
3. Other potential activities Diterpenoid alkaloids often have activities such as neuromuscular blockade and antiarrhythmic effects. Although there are limited specialized reports on aspects such as Delitalin, the activity of its structural analogues suggests that it may have a broader pharmacological spectrum, which needs to be systematically explored.

Mechanism of action and molecular targets

The potential of Del Tallinn to improve cognitive impairment is closely related to its regulatory effects on multiple disease-related targets. According to the provided target information, its mechanism of action may involve the following networks:

1. Regulation of amyloid (A β) pathway One of the core pathological features of Alzheimer's disease is the abnormal deposition of A β peptide in the brain. Del Tallinn may exert neuroprotective effects by acting on the processing of amyloid precursor protein (APP) or directly inhibiting the activity of β - secretase 1 (BACE1), reducing the production of neurotoxic A β.
2. Pathological regulation of Tau protein The neurofibrillary tangles formed by the excessive phosphorylation of microtubule associated protein (MAPT, also known as Tau protein) are another hallmark of AD. Del Tallinn may indirectly affect the phosphorylation status of Tau protein by regulating the activity of related kinases or phosphatases, such as PTPN1 and protein tyrosine phosphatase 1B, whose abnormalities are associated with insulin resistance and neuroinflammation.
3. Neuroinflammation and Immune Regulation Indoleamine 2,3-dioxygenase 1 (IDO1) is a key enzyme in tryptophan metabolism, and its activation leads to the accumulation of neurotoxic metabolites and exacerbates neuroinflammation. Inhibiting IDO1 is one of the strategies for treating neurodegenerative diseases and emotional disorders. Del Tallinn may alleviate neuroinflammation by regulating IDO1 activity.
4. Synaptic function and vesicle circulation Synaptosin 2 (SYNJ2) is involved in the circulation of synaptic vesicles, and its functional abnormalities are associated with early cognitive decline. Del Tallinn may affect SYNJ2 related pathways and maintain normal synaptic transmission. The deubiquitinase USP2 is involved in the stability regulation of various proteins and may be related to the neural survival signaling pathway.
5. Pigment metabolism and oxidative stress Tyrosinase (TYR) not only participates in melanin synthesis, but its abnormal expression may also be related to neural melanin accumulation and oxidative stress. The potential regulatory effect of Deltalin on TYR may indirectly affect neuronal oxidative damage.
6. Blood brain barrier and drug efflux The high BBB permeability of Del Tallinn is its advantage. Meanwhile, it may have a regulatory effect on the efflux transporters ABCB1 (P-gp) and ABCG2 (BCRP) on brain capillary endothelial cells. Inhibiting these efflux pumps may increase the concentration of other central therapeutic drugs in the brain or prevent them from being rapidly pumped out, prolonging the duration of action.

In summary, Del Talin may alleviate A β and Tau pathology, inhibit neuroinflammation, protect synaptic function, and improve cognitive impairment through a synergistic network of multiple targets and pathways. This "multi-target" characteristic may have unique advantages in treating diseases with complex etiologies such as Alzheimer's disease.

Evaluation of drug properties and pharmacokinetics

The pharmacological evaluation based on calculations and preliminary experimental data shows that Delitalin has a good physical and chemical foundation for development as a central nervous system drug. Its moderate LogP, low TPSA, and predicted high BBB permeability are key factors in its ability to enter brain tissue and exert its effects. The absence of hERG inhibition risk reduces concerns about early development of arrhythmia, and negative Ames test results provide preliminary support for its safety.

However, comprehensive drug development still requires in-depth pharmacokinetic (PK) and toxicological studies. At present, there is a lack of PK data (such as absorption, distribution, metabolism, and excretion) on the Del Tallinn system in public literature. Future research needs to focus on: its oral bioavailability; The distribution characteristics in the body, especially the relationship between brain tissue concentration and time; Its main metabolic pathways, metabolic enzymes (such as CYP450 enzyme system), and metabolic product activities; And its elimination half-life and excretion pathway. Its moderate water solubility suggests that its bioavailability may need to be improved through prodrug design or formulation optimization (such as nano formulations, cyclodextrin inclusion). Although the preliminary prediction of safety is good, the potential neurotoxicity and therapeutic window of diterpenoid alkaloids need to be clarified through systematic acute and long-term toxicity experiments.

Clinical application prospects and prospects

The clinical application prospects of Deltalin mainly revolve around neurological diseases:

1. As a candidate drug for improving cognitive impairment Its multi-target mechanism of action is particularly suitable for multifactorial diseases such as Alzheimer's disease. In the future, further research can be conducted on its long-term efficacy in different AD animal models (such as APP/PS1 transgenic mice), and its core targets and signaling pathways can be identified.
2. As a development of analgesic drugs Further clarification can be made on the intensity and characteristics (central or peripheral) of its analgesic effect, as well as its differences from opioid drugs, to develop new non opioid analgesics for neuropathic pain or chronic inflammatory pain.
3. Combination therapy strategy Given its potential to inhibit the efflux pumps on the BBB (ABCB1/ABCG2), Delitalin may be used as an adjuvant in combination with other difficult to enter AD treatment drugs (such as certain antibodies or small molecules) to enhance the intracranial efficacy of combination therapy.
4. Structural optimization and new drug design Structural modification using Delitalin as the parent nucleus aims to enhance its activity, selectivity, water solubility, or metabolic stability, which is an important direction in pharmaceutical chemistry research. Rational design can be carried out for its interaction patterns with key targets such as BACE1 and IDO1.

The challenges faced mainly include: ① the difficulty of fully or semi synthesizing complex structures, which limits large-scale structure-activity relationship research; ② The multi-target characteristic is both an advantage and a challenge, and it is necessary to clarify the target correlation between its therapeutic effect and potential side effects; ③ A complete preclinical pharmacodynamic, pharmacokinetic, and toxicological evaluation system needs to be completed.

Conclusion

As a diterpenoid alkaloid discovered from traditional medicinal plants, the research on Del Talin has expanded from traditional analgesic applications to the global health challenge of cognitive impairment. Its unique chemical structure endows it with the potential for high blood-brain barrier permeability and multi-target action, involving multiple key links related to cognitive impairment such as A β generation, Tau pathology, neuroinflammation, and synaptic function. Although it has shown positive prospects in terms of pharmacological parameters, a lot of in-depth work is still needed to truly promote its clinical application, including precise analysis of the mechanism of action, systematic pharmacokinetic and safety evaluation, and possible drug chemistry optimization. The research conducted by Del Tallinn not only provides valuable lead compounds for the development of new neuroprotective drugs, but also demonstrates the enormous value of mining modern therapeutic drugs from traditional medical knowledge. With the continuous advancement of interdisciplinary research, Del Talin is expected to show broader application prospects in the field of neurological disease treatment.