In Vitro and In Vivo Anti-Aging Effect of Coffee Berry Nanoliposomes.

Encapsulation of bioactive compounds in the liposome system provides several advantages, such as enhancing the stability and lowering the toxicity of active compounds. Coffee berry extract (CBE) has previously been established to have in vitro anti-aging properties and to retard the aging of human skin. The purposes of this study were to encapsulate CBE in nanoliposomes and to assess its stability and in vitro anti-aging potential in human dermal fibroblasts (HDF), as well as in healthy human skin. In the HDF model, anti-aging potential was determined by nitric oxide (NO) and collagenase inhibition assays and a superoxide dismutase (SOD) activity assay, whereas in healthy human skin (in vivo), the skin elasticity and brightness were examined. First, liposomal CBE (L-CBE) was created with a particle size of 117.33 ± 2.91 nm, a polydispersity index (PDI) of 0.36 ± 0.03, and a zeta potential of -56.13 ± 1.87 mV. The percentages of encapsulation efficacy (%EE) and loading efficacy (%LE) were 71.26 ± 3.12% and 2.18 ± 0.18%, respectively. After undergoing a 12-week stability test, the L-CBE retained more phenolic content than the free CBE when stored at 4 °C, room temperature, and 45 °C. Compared to free CBE, the L-CBE demonstrated a more consistent, elevated, and prolonged release of phenolics from the lipid system. In human dermal fibroblasts, L-CBE showed lower toxicity, and at its maximum nontoxic concentration (10 mg/mL), it exhibited slightly higher anti-aging effects than CBE, including NO inhibition, enhanced SOD activity, and anti-collagenase activities. In clinical trials (30 volunteer subjects), none of the participants' skin was irritated when the L-CBE, the CBE, or base creams were applied. After 2 weeks of application, the L-CBE and CBE creams both demonstrated an improvement in skin elasticity and a reduction in melanin levels, and after 4 weeks, L-CBE cream showed a significantly greater improvement in skin elasticity and lightening. The results demonstrate that the encapsulation of the CBE in liposomal systems could increase its stability and skin penetration, reduce its toxicity, and maintain its anti-aging effect, which is powerful enough to be exploited in anti-aging and whitening agents for application in cosmetics and cosmeceuticals.

Stability and Anti-Aging of Encapsulated Ferulic Acid in Phosphorylated Rice Starch.

Ferulic acid (FA) provides broad biological functions that have been used in cosmetics formulation as a photoprotection, anti-aging, and brightening agent. However, its application is limited by its tendency to deteriorate by exposure to heat, humidity, and light. This study aimed to enhance the stability of FA by encapsulation in phosphorylated rice starch (PRS) and evaluate its effect on improving human skin. First, FA was encapsulated in PRS and characterized by FTIR, SEM, XRD, and DSC. Then, its stability when exposed to a temperature of 45 °C and light and its anti-aging effect on 16 volunteers were investigated. The results indicated that FA was successfully encapsulated in PRS with an encapsulation yield of 77%, EE (73%) and LE (65%). After 1 month at the high temperature/80%RH, the encapsulated FA retained its quantity (70%), whereas free FA was retained at only 50%. Under light exposure conditions, the encapsulated FA was retained at 65%, which was higher than FA (35%). Franz diffusion cell was used and demonstrated that PRS provided the controlled release of FA. Application of encapsulated FA and FA creams showed an absence of skin irritation in all volunteers. After 1 month, the encapsulated FA cream was found to be better than the FA cream on skin lightening, elasticity, smoothness, roughness, scaliness, and wrinkle. The results indicated that PRS is a potential wall material for enhancing the stability of FA, resulting in more efficacious skin lightening and anti-aging properties.

Natural products as photoprotection.

The rise in solar ultraviolet radiation on the earth's surface has led to a depletion of stratospheric ozone over recent decades, thus accelerating the need to protect human skin against the harmful effects of UV radiation such as erythema, edema, hyperpigmentation, photoaging, and skin cancer. There are many different ways to protect skin against UV radiation's harmful effects. The most popular way to reduce the amount of UV radiation penetrating the skin is topical application of sunscreen products that contain UV absorbing or reflecting active molecules. Based on their protection mechanism, the active molecules in sunscreens are broadly divided into inorganic and organic agents. Inorganic sunscreens reflect and scatter UV and visible radiation, while organic sunscreens absorb UV radiation and then re-emit energy as heat or light. These synthetic molecules have limited concentration according to regulation concern. Several natural compounds with UV absorption property have been used to substitute for or to reduce the quantity of synthetic sunscreen agents. In addition to UV absorption property, most natural compounds were found to act as antioxidants, anti-inflammatory, and immunomodulatory agents, which provide further protection against the damaging effects of UV radiation exposure. Compounds derived from natural sources have gained considerable attention for use in sunscreen products and have bolstered the market trend toward natural cosmetics. This adds to the importance of there being a wide selection of active molecules in sunscreen formulations. This paper summarizes a number of natural products derived from propolis, plants, algae, and lichens that have shown potential photoprotection properties against UV radiation exposure-induced skin damage.

(E)-1-(4-Amino-phen-yl)-3-(naphthalen-2-yl)prop-2-en-1-one.

The mol-ecule of the title chalcone derivative, C(19)H(15)NO, exists in a trans configuration with respect to the C=C double bond. The mol-ecule is slightly twisted with a dihedral angle of 6.12 (12)° between the benzene ring and the naphthalene ring system. The prop-2-en-1-one bridge is nearly planar, with an r.m.s. deviation of 0.0194 (2), and makes dihedral angles of 8.05 (19) and 11.47 (18)° with the benzene ring and the naphthalene ring system, respectively. In the crystal, mol-ecules are linked by N-H⋯O hydrogen bonds into chains along the b axis. Weak N-H⋯π and C-H⋯π inter-actions and a short N⋯O contact [2.974 (4) Å] are also observed.

(E)-3-(4-Eth-oxy-phen-yl)-1-(2-hy-droxy-phen-yl)prop-2-en-1-one.

In the title compound, C(17)H(16)O(3), the carbonyl group is in an s-cis configuration with respect to the olefinic double bond. The dihedral angle between the two benzene rings is 2.85 (3)°. The prop-2-en-1-one bridge makes dihedral angles of 4.77 (4) and 4.15 (4)°, respectively, with the 2-hy-droxy-phenyl and 4-eth-oxy-phenyl rings. The eth-oxy group is coplanar with the attached phenyl ring [C(ar)-O-C-C = 179.72 (5)°]. An intra-molecular O-H⋯O hydrogen bond generates an S(6) ring motif. In the crystal structure, mol-ecules are stacked in an anti-parallel manner to form columns along the b axis. The columnar structure is stabilized by C-H⋯π inter-actions involving the 2-hy-droxy-phenyl ring.

Antimalarial tetranortriterpenoids from the seeds of Lansium domesticum Corr.

Five tetranortriterpenoids, domesticulide A-E (1-5), were isolated from seeds of Lansium domesticum Corr. together with 11 known triterpenoids (6-16). Their structures were elucidated by analysis of their spectroscopic data. Compounds 2, 3, 4, 7, 8, 10, 11, and 15 showed antimalarial activity against Plasmodium falciparum with IC(50)'s of 2.4-9.7 microg/ml.

Exploratory studies to investigate a linked prebiotic origin of RNA and coded peptides. 4th Communication. Further observations concerning pyrimidine nucleoside synthesis by stepwise nucleobase assembly.

As part of an ongoing investigation into a possible linked origin of RNA and coded peptides, we have (further) investigated the potentially prebiotic synthesis of pyrimidine ribonucleosides (ribonucleotides), by stepwise nucleobase assembly on sugar (sugar phosphate) scaffolds. In this paper, we complete our description of this assembly process on aldopentose scaffolds. Treatment of D-ribose (14) and D-xylose (20) with cyanamide smoothly produces the furanosylamino-oxazolines 15 and 21, respectively (Schemes 1 and 3). Similar treatment of D-lyxose (26) also produces the furanosylamino-oxazoline 29, but as a minor component of an equilibrating mixture in which the pyranosylamino-oxazoline 28 predominates (Scheme 4). Treatment of the various amino-oxazolines with cyanoacetylene gives furanosylcytidines 16, 25, and 31, and the lyxopyranosylcytidine 30 (Schemes 1-4). Minor by-products of the cyanoacetylene reaction include imino lactone 17, acetals 19, 22, and 24, and cyanovinyl adducts 22 and 23 resulting from initial addition of nucleoside OH groups to the terminal acetylenic C-atom of cyanoacetylene (Schemes 2-4).